Food Chemistry 165 (2014) 424–443

Contents lists available at ScienceDirect

Food Chemistry
j o u r n a l h o m e p a g e : w w w. e l s e v i e r. c o m / l o c a t e / f o o d c h e m

Review

Hibiscus sabdariffa L. – A phytochemical and pharmacological review

⇑
Inês Da-Costa-Rocha a, Bernd Bonnlaender b, Hartwig Sievers c, Ivo Pischel a,c, Michael Heinrich a,
a
Centre for Pharmacognosy and Phytotherapy, UCL School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK
b
Plantextrakt GmbH & Co. KG, Dutendorfer Str. 5–7, D-91487 Vestenbergsgreuth, Germany
c
Phytolab GmbH & Co. KG, Dutendorfer Str. 5–7, D-91487 Vestenbergsgreuth, Germany

a r t i c l e
Article history:
Received 24 November 2013
Received in revised form 26 March 2014
Accepted 1 May 2014
Available online 27 May 2014
Keywords:
Roselle
Malvaceae
Lipid metabolism (anti-cholesterol)
Nephro- and hepato-protective
Renal/diuretic effect
Anti-diabetic Anti-
oxidant
Hydroxycitric acid
Hibiscus acid
Protocatechuic acid
Anthocyanins
i n f o a b s t r a c t
Hibiscus sabdariffa L. (Hs, roselle; Malvaceae) has been used traditionally as a food, in herbal drinks, in hot
and cold beverages, as a flavouring agent in the food industry and as a herbal medicine. In vitro and in
vivo studies as well as some clinical trials provide some evidence mostly for phytochemically
poorly characterised Hs extracts. Extracts showed antibacterial, anti-oxidant, nephro- and hepato-
protective, renal/diuretic effect, effects on lipid metabolism (anti-cholesterol), anti-diabetic and anti-
hypertensive
effects among others. This might be linked to strong antioxidant activities, inhibition of a-glucosidase
and a-amylase, inhibition of angiotensin-converting enzymes (ACE), and direct vaso-relaxant effect or
calcium channel modulation. Phenolic acids (esp. protocatechuic acid), organic acid (hydroxycitric acid
and hibiscus acid) and anthocyanins (delphinidin-3-sambubioside and cyanidin-3-sambubioside) are
likely to contribute to the reported effects.
More well designed controlled clinical trials are needed which use phytochemically characterised
preparations. Hs has an excellent safety and tolerability record.
2014 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license
(http://
creativecommons.org/licenses/by/3.0/).

Contents

1. Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 425
2. Botanical description . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 425
2.1. Morphology . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 425
2.2. Ecology/cultivation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
2.3. Karyotype. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
3. Uses – economic botany . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
3.1. Traditional culinary use . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
3.2. Use in local and traditional food and medicine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
4. Other uses . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
4.1. Source of fibre . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
4.2. Animal feed . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 426
4.3. Cosmetic . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
4.4. The current importance of H. sabdariffa . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
4.5. Economical–botanical aspects . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
4.6. FairTrade certified and organic certified . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
5. Phytochemistry. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
5.1. Nutritional value . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
5.2. Bioactive constituents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
5.3. Organic acids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
5.3.1. Hydroxycitric acid . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427

⇑ Corresponding author. Tel.: +44 20 7753 5844.

E-mail address: m.heinrich@ucl.ac.uk (M. Heinrich).

http://dx.doi.org/10.1016/j.foodchem.2014.05.002
0308-8146/ 2014 The Authors. Published by Elsevier Ltd.
This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/3.0/).
 I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443 169

5.3.2. Hibiscus acid . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427

5.3.3. Anthocyanins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
5.3.4. Flavonoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 428
5.3.5. Mucilage, pectin and carbohydrates (polysaccharides) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 429
5.3.6. Volatile compounds . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 429
6. Biological and pharmacological activities . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 430
6.1. Effects on smooth muscles . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 430
6.2. Antibacterial, antifungal and antiparasitic activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 430
6.3. Antipyretic, antinociceptic and anti-inflammatory activities . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 430
6.4. Clinical studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 430
6.5. Antioxidant activity. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 430
6.6. Clinical studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 431
6.7. Hepatoprotective activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 431
6.8. Nephroprotective activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 431
6.9. Renal effects/diuretic effect (incl. clinical studies) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 431
6.10. Cancer-preventive activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 432
6.11. Lipid metabolism – anticholesterol effects/effects on lipid metabolism . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 432
6.12. Clinical studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 432
6.13. Anti-obesity activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 432
6.14. Lactating activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 433
6.15. Anti-diabetic activity. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 433
6.16. Clinical studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 433
6.17. Delayed puberty activity. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 433
6.18. Anti-hypertensive activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 433
6.19. Clinical studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 434
6.20. Anti-anaemic activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 434
6.21. Others . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 434
7. Safety . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 434
7.1. Toxicology . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 435
7.2. Interactions . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 436
8. Scientific applications and translational research . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 436
8.1. Future research . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 436
Appendix A. Supplementary data . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 439
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 439
1701. Introduction I. Da-Costa-Rocha
India or Saudi Arabia et al. / Food Chemistry
(Ismail, 165 (2014)while
2008), 424–443 Murdock petioles. The leaves of young
Ikram, & Nazri, (Murdock, 1959) showed seedlings and upper leaves of
Hibiscus sabdariffa L. (Hs), evidence that Hs was older plants are simple; lower
also known as roselle, is an domesticated by the black leaves are deeply 3 to 5 or
ideal crop for developing populations of western even 7 lobed; the margins are
countries as it is relatively Sudan (Africa) sometime toothed. Flowers, borne
easy to grow, can be grown before 4000 BC. singly in the leaf axils, are up
as part of multi-cropping Nowadays, it is widely to 5 in (12.5 cm) wide, yellow
systems and can be used as cultivated in both tropical or buff with a rose or mar- oon
food and fibre. In China the and subtropical regions eye, and turn pink as they
seeds are used for their oil (Morton, wither at the end of the day.
and the plant is used for its 1987; USDA, 2007) including At this time, the typically red
medicinal properties, while in India, Saudi Arabia, China, calyx, consisting of 5 large
West Africa the leaves and Malaysia, Indonesia, The sepals with a collar (epicalyx)
powdered seeds are used in Philippines, Vietnam, Sudan, of 8 to 12 slim, pointed bracts
meals. Additionally, it is used Egypt, Nigeria and México (or bracteoles) around the
in the pharmaceutical and (Chewonarin et al., 1999; base, begins to enlarge,
food industries. Dung et al., 1999; becomes fleshy, crisp but juicy,
A limited number of Eslaminejad 1 1/4 to 2 1/4
reviews on Hs have been & Zakaria, 2011; Ismail,
conducted. Only one detailed Ikram, & Nazri, 2008;
review on the Mahran, El-Hossary, & El-
phytochemical, Labban, 1979; Rao, 1996;
pharmacological and Sharaf, 1962; Yagoub Ael,
toxicological properties of Hs Mohamed, Ahmed, & El Tinay,
(Ali, Al Wabel, & Blunden, 2004).
2005) and two more There are two main
focused, later reviews are varieties of Hs, the first
available: One on the being Hs var. altissima
effectiveness of Hs in the Wester, cultivated for its
treatment of hypertension jute-like fibre and the
(Wahabi, Alansary, Al- second is Hs var. sabdariffa.
Sabban, & Glasziuo, 2010) The second variety includes
and another on the shorter bushy forms, which
treatment of hypertension have been described as races:
and hyperlipidemia bhagalpuriensi, interme- dius,
(Hopkins, Lamm, Funk, & albus and ruber. The first
Ritenbaugh, 2013). This variety has green, red-
review will focus not only on streaked, ined- ible calyces,
the phytochemistry and while the second and third
pharmacological properties race have yellow-green
of Hs in more detail, but edible calyces (var. ruber) and
also on economic-botanical also yield fibre (Morton,
aspects of Hs, its scientific 1987).
applications and translational
research. 2
.
2. Botanical description 1
.
The genus Hibiscus
(Malvaceae) includes more M
than 300 species of annual or o
r
perennial herbs, shrubs or
p
trees (Wang, Morris, Tonnis, h
Davis, & Pederson, 2012). Hs o
(syn.: Abelmoschus cruentus l
(Bertol.) Walp., Furcaria o
sabdariffa Ulbr., Hibiscus g
cruentus Bertol., Hibiscus y
fraternus L., Hibiscus
palmatilobus Baill. and Hs var. sabdariffa ruber is
Sabdariffa rubra Kostel (The an annual, erect, bushy,
Plant list, 2010) is herbaceous subshrub that can
commonly known as roselle, grow up to 8 ft (2.4 m) tall,
hibiscus, Jamaica sorrel or red with smooth or nearly
sorrel (English) and in Arabic, smooth, cylindrical, typically
karkadeh (Ali et al., 2005; red stems. The leaves are
Ross, 2003). Its native alternate, 3 to 5 in (7.5–12.5
distribution is uncertain, cm) long, green with reddish
some believe that is from veins and long or short
I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443 171
172
in (3.2–5.7 cm) long and fully of leavesI. Da-Costa-Rocha
may be about et al. / Food
10 Chemistry 165 (2014) 424–443 with onions and groundnuts,
encloses the velvety capsule, t/ha (EcoCrop., 2007; Plotto, 3 while in Malaysia the cooked
1/2 to 3/ 2004). . leaves are eaten as vegetables
4 in (1.25–2 cm) long, which 1 (Ismail, Ikram,
is green when immature, 5- . & Nazri, 2008). In Africa, the
2
valved, with each valve seeds are roasted or ground
.
containing 3 to 4 kidney- 3 T into pow- der and used in
shaped, light-brown seeds, . r meals, suh as oily soups and
1/8 to 3/16 in (3–5 mm) long a sauces. In China and West
d
and minutely downy. The K Africa, the seeds are also
i
capsule turns brown and a used for their oil (Atta &
t
splits open when mature and r i Imaizumi, 2002). Another use
dry. The calyx, stems and y o for the seed is as a substitute
leaves are acid and closely o n for cof- fee (Morton, 1987).
resemble the cranberry t a
(Vaccinium spp.) in flavour y l
p
(Morton, 1987; Ross, 2003).
e
c
u
2 2n = 36 (Huang, Zhao, l
. Chen, Chen, & Huang, 1989; i
2
Menzel & Wilson, 1961) and n
.
72 (Chennaveeraiah & a
Subbarao, 1965; Rao, r
E 1935; Wilson & Menzel, y
c
1964) were observed.
o
l Somatic tissue showing u
o diploid and tetraploid s
g segments were also e
y occasionally noticed (Tjio,
/ 1948). In a Fresh or dried calyces of H.
c karyomorphological study sabdariffa (cHs) are used in the
u conducted in India, both root prep- aration of herbal drinks,
l hot and cold beverages,
and flower segments showed
t fermented drinks, wine, jam,
i great similarity in the types
of chromosomes in the jellied confectionaries, ice
v
a complement. This indicates cream, chocolates, flavouring
t that the tetraploid tissue must agents, puddings and cakes
i have arisen in an (Bako, Mabrouk, &
o autotetraploid manner (Bhatt Abubakar, 2009; Bolade,
n & Dasgupta, 1976). Later, this Oluwalana, & Ojo, 2009;
species was reported to be Esselen & Sammy, 1975;
Hs is easy to grow in most tet- raploid (2n = 72) (Hiron, Ismail, Ikram, & Nazri, 2008;
well drained soils but can Alam, Ahmed, Begum, & Alam, Okoro, 2007; Plotto, 2004;
tolerate poor soils. It requires 2006). Rao, 1996; Tsai, McIntosh,
4-8 months growth with Pearce, Camden, & Jordan,
night-time temper- atures 2002; Wilson & Menzel,
with a minimum of 20 C, as 3 1964). In Egypt, the fleshy
well as 13 h of sunlight and a . calyces are used in making
monthly rainfall ranging ‘‘cacody tea’’ and fermented
from 5–1000 (130–250 mm) U drinks (Kochhar, 1986), while
during the first few months s in Sudan and Nigeria, the
e
to prevent premature calyces are boiled with sugar
s
flowering. Rain or high to produce a drink known as
humidity during the harvest ‘‘Karkade’’ or ‘‘Zoborodo’’
time and drying process can – (Gibbon & Pain, 1985). In
down- grade the quality of Mexico this drink is called
the calyces and reduce the e Jamaica or ‘‘agua de Jamaica’’’
yield. The quality of Hs is c or ‘‘té de Jamaica’’. In the West
determined by seed stock, o Indies the calyces can also be
n
local growing conditions, used as colouring and fla-
o
time of harvest, post-harvest m vouring ingredient in rum
handling and mainly the i (Ismail, Ikram, & Nazri, 2008).
drying step. Most of the time c The seeds are eaten
it grows as a supplement roasted or ground in meals,
crop and it is susceptible to b while the leaves and shoots
fungi, viral and bacterial o are eaten raw or cooked, or as
attack and also to insects. A t a sour-flavoured vegeta- ble or
single plant produces about a condiment (Wilson & Menzel,
1.5 kg of fruit, n 1964). In Sudan, the leaves are
approximately 8 t/ha. Yields y eaten green or dried, cooked
3.2. Use in h I. Da-Costa-Rocha et al. / Food production of Kenaf
Chemistry 165 (2014) fibres
(H.
424–443 173
local and e cannabinus) has reached
traditional r 272,000 tons in 2008, Hs
food and fibres have not gained the
medicine
u same economic importance
s (http://www.naturalfibersinfo
Hs has been widely used in e .org/natural- fibers/kenaf/,
local medicines. In India, s accessed 09/11/13).
Africa and Mexico, infusions
However, Hs fibres are
of the leaves or calyces are 4 subject to ongoing research
traditionally used for their .
showing promising technical
diuretic, cholerectic, 1
. properties when used as a
febrifugal and hypotensive
substitute for syn- thetic or
effects, decreasing the
mineral fibres in composite
viscosity of the blood and S
materials, as well as a source
stimulating intestinal o
u material for high quality
peristalsis. It is also
r paper production (Dutt,
recommended as a
c Upadhyaya, & Tyagi, 2010;
hypotensive in Senegal e Kumar, Dutt, & Bharti, 2013;
(Morton, 1987). In Egypt,
Singha & Kumar, 2008).
preparations from the calyces
o
have been used to treat
f
cardiac and nerve diseases 4
and also to increase the .
production of urine (diuresis). fi 2
b .
In Egypt and Sudan, an
r
infusion of e
‘‘Karkade’’ calyces is also A
n
used to help lower body Hs is one of the most i
temperature (Leung, 1996). In important species grown m
Guatemala it is used for commercially as a fibre plant a
treating drunkenness and became increasingly l
(Morton, 1987). In North important in India after inde-
Africa, calyces preparations pendence and partition with f
are used to treat sore throats Pakistan, where the most e
and coughs, as well as important jute (Corchorus e
genital problems, while the capsularis L. or Corchorus d
emollient leaf pulp is used olitorius L.) growing areas are.
for treating external wounds It is used as a jute substitute The leaves are used for
and abscesses (Neuwinger, in making clothing, linen, animal fodder and fibre
2000). In India, a decoction fishing nets, ropes and similar (Plotto, 2004). The seeds can
from the seeds is used to items (Clydesdale, Main, & be used to feed poultry as well
relieve pain in urination and Francis, 1979). Despite the as sheep and the res- idue
indigestion. In Brazil, the fact that this species is slow from the seeds oil extraction
roots are believed to have growing, as it requires about can also be used to feed
stomachic and emollient 180 days to produce a cattle and chicks (Al-
properties. In Chinese folk satisfactory yield of fibre, Wandawi, Al-Shaikhly, &
medicine, it is used to treat there is still interest in the Abdul-Rahman, 1984;
liver disorders and high plant as some varieties of Hs
blood pressure (Morton, (not edible but fibre type)
1987). In Iran, sour hibiscus have a high degree of genetic
tea is reportedly a resistance to root-knot nema-
traditional treatment for todes. The main
hypertension (Burnham, disadvantages of growing Hs
Wickersham, & Novak, in comparison with other
2002), while in Nigeria the Hibiscus species is:
decoction of the seeds is
traditionally used to enhance (1) The slow growth rate
or induce lactation in cases of which increases costs in
poor milk production, poor weed control and land
letdown and maternal mortal- occupation by the crop.
ity (Gaya, Mohammad, (2) The difficulty of
Suleiman, Maje, & Adekunle, separating the
2009). ribboning stalks from
the bark when
4 compared to, for
. example, H.
cannabinus (Wilson &
O Menzel, 1964).
t
While the world’s
174 I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443
Elamin, Hassan, Abdalla, (Cooper,I. Da-Costa-Rocha
1993; et al. / Food
McCaleb, Chemistry
(1329165± (2014)
1.47 424–443
mg/100 g), including citric 175
acid,
Arabi, & Tameem Eldar, 2000; Mohamed, Sulaiman, & followed by sodium (659 hydroxycitric acid, hibiscus
2012; Morton, Dahab, 2012; Plotto, 2004). ± 1.58 mg/ acid, malic and tartaric acids
1987; Mukhtar, 2007). 100 g), calcium (647 ± 1.21 as major compounds, and
mg/100 g), phosphorus (510 oxalic and ascorbic acid as
4.6. FairTrade certified and
4.3. Cosmetic organic certified ± 1.58 mg/100 g) and minor compounds. Based on
magnesium (442.8 ± 1.80 previous studies, the
In Malaysia the oil is used Until very recently, the mg/100 g). The major sat- percentage of organic acids in
to produce scrubs and soaps Arab Republic of Egypt was urated fatty acids identified ‘‘hibisci flos’’ varies; hibiscus
(Ismail, Ikram, & Nazri, 2008). the only source country for in the seed oil are palmitic acid accounts for 13–24%,
certified and organic certified (20.84%) and stearic (5.88%) citric acid 12–20%, malic acid
hibiscus flower. In 2011 a acids and the main 2–9%, tartaric acid 8% and
4.4. The current importance of
H. sabdariffa number of producers and unsaturated fatty acids are 0.02–
traders from Burkina Faso linoleic (39.31%) and oleic acid 0.05% of ascorbic acid
Besides its importance as a achieved certification (32.06%) (Nzikou et al., 2011). (vitamin C) (Eggensperger &
food or traditional medicine through the FairTrade Wilker, 1996; Schilcher,
in the countries of its Labelling Organisa- tions 5 1976).
. In the late 1930s, citric
geographic origin, hibiscus International FLO-CERT GmbH
2
flower is traded and used (http://www.flo-cert.net) and malic acids were first
.
worldwide today as an (Brinckmann, 2011). reported in aqueous extracts
important ingredient in of the calyx (Buogo &
B Picchinenna, 1937; Indovina
industrially produced teas 5. Phytochemistry i
and beverages. The United & Capotummino, 1938;
o
States and Germany are the a Reaubourg & Monceaux,
5.1. Nutritional value
primary markets for dried c 1940) and also in five different
cHs. England satisfies most of t strains (from Egypt, Senegal,
The nutritional
its consumers demands by i India, Thailand and Central
composition of fresh cHs
importing herbal teas form v America) of Hs var. sabdariffa
varies between studies, e
Germany (Plotto, 2004). (Khafaga, Koch, El Afry, & Prinz,
probably due to different
Statistics for the volume and 1980). Ascorbic acid is also
varieties, genetic,
value of dried hibiscus c present in cHs but its content
environmental, ecology and o
imported into these markets varies dramatically between
harvest conditions of the n
were not available, but the fresh (6.7–14 mg/100 g
plant. Early studies reported s
major cli- ents for hibiscus (Ismail, Ikram, & Nazri, 2008;
that cHs contains protein t
importers are herbal teas Morton, 1987)) and dried
(1.9 g/100 g), fat (0.1 g/100 i
manufactures, as this plant is t calyces (260–280 mg/100 g
g), carbohydrates (12.3 g/100
used as base in many u (Ismail, Ikram, & Nazri,
g) and fibre (2.3 g/100 g).
herbal/fruit teas, along with e 2008)). The amount of
They are rich in vitamin C
apple peel, orange peel and n ascorbic acid in the latter
(14 mg/100 g), b-carotene t
lemon twist. (McCaleb, 2000; report being much higher
(300 lg/100 g), calcium s
Plotto, 2004). (1.72 mg/ than the ones previously
100 g) and iron (57 mg/100 g) reported in the literature. The
The main constituents of differences observed might be
4.5. Economical–botanical (Ismail, Ikram, & Nazri, 2008).
H. sabdariffa relevant in the due to different varieties,
aspects The leaves contain protein
context of its pharmacological genetics, environment,
(3.3 g/100 g), fat (0.3 g/100 g),
carbo- hydrate (9.2 g/100 g), are organic acids, ecology and harvest
Hibiscus is available from
minerals (phosphorus (214 anthocyanins, polysaccha- conditions.
China, Thailand, Sudan,
mg/100 g), iron (4.8 mg/100 g) rides and flavonoids
Mexico and some other
thiamine (0.45 mg/100 g), b- (Eggensperger & Wilker, 5
countries with smaller
carotene (4135 lg/ 1996; Müller & Franz, 1990). .
suppliers like Egypt, Senegal,
Tanzania, Mali and Jamaica. 100 g), riboflavin (0.45 3
mg/100 g) and ascorbic acid 5 .
Hibiscus quality strongly
. 1
depends on geographic origin. (54 mg/100 g) (Ismail, Ikram,
3 .
The most desirable product is & Nazri, 2008).
.
from Thailand and Sudan; The seeds contained
crude fatty oil (21.85%), H
however the main world y
crude protein (27.78%), O
suppliers are China and r d
Thailand. The best Hs grows in carbohydrate (21.25%), crude r
g
Sudan, however its quality is fibre (16.44%) and ash a o
subsequently often impaired (6.2%). In terms of minerals, n x
due to poor pro- cessing. the most prevalent is i y
Thailand has invested greatly potassium c c
i
in Hibiscus production con-
t
trary to China, where the a
r
product is less reliable and c
i
reputable due to less i
c
stringent quality control d
s
practices. However, China is a
the dominant supplier of the c
Hs extracts contain a high
United States market i
percentage of organic acids,
 d
176 Rodrigues,
I. Da-Costa-Rocha Balaban,
et al. / Food Chemistry 165 (2014) 424–443
(Fig. 1) has an additional Marshall, & Rouseff,
hydroxyl group at the second 2011
carbon of citric acid. This acid a,b;
has four stereoisomers, (2S, Rodr
3S), (2R, 3R), (2S, igue
z-
3R) and (2R, 3S), and their
Med
lactone forms. The principal ina
organic acid found in the cHs et
is the (2S, 3R)-hydroxycitric al.,
acid (Hida, Yamada, & 2009
Yamada, 2007). It is the ).
principal organic acid found
in the calyces of Hs. It is 5
worth noting that, (2S, 3R)- .
hydroxycitric acid from 3
.
Hibiscus is different from
3
the more commonly known .
(2S,3S)- hydroxycitric acid
(HCA) extracted from, e.g.,
A
Garcinia sp., thus raising the
n
question as to whether both t
diastereomers have identi- cal h
or partially different o
pharmacological profiles. c
y
5 a
. n
3 i
. n
2 s
. The anthocyanins are a
group of flavonoid derivatives
H and nat- ural pigments
i present in the dried flowers
b of Hs and their colour varies
i with pH.
s
c
u
s

a
c
i
d
(Fig. 1) is the lactone form
of (+)-allo-hydroxycitric acid.
It com- promises a citric acid
moiety with an additional
hydroxyl group at the second
carbon and has two
diastereomers due to the
existence of two chiral
centers in the molecule
(Boll, Sørensen, & Balieu,
1969; Eggensperger &
Wilker, 1996; Griebel &
Lebensm, 1939,
1
9
4
2
)
.
Hydroxycitric acid,
hibiscus acid and it
derivatives as the major
organic acids in the leaves
and calyces extracts of Hs
(Beltran-Debon et al., 2010;
Herranz-Lopez et al., 2012;
Peng et al., 2011; Ramirez-
I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443 177

Fig. 1. Citric acid and its derivatives.

178 Delphinidin and cyanidin- I. Da-Costa-Rocha
glucopyranoside) as theetmajor
al. / Food Chemistry
from 165
cHs(2014) 424–443
(Alarcon-Aguilar
et quercetin, luteolin and the
based anthocynins, include anthocyanins present in al., 2007; Alarcon-Alonso et sterols b-sitosterol and
delphini- din-3-sambubioside extracts al., 2012; Beltran-Debon et ergosterol (McKay, 2009;
(hibiscin), cyanidin-3- al., 2010; Degenhardt, Williamson et al., 2009).
sambubioside (gossypi- Knapp, & Winterhalter, Earlier the flowers of Hs
cyanin), cyanidin-3,5- 2000; Herranz-Lopez et al., were recorded to contain 3-
diglucoside, delphinidin 2012; Peng et al., 2011) and monog- lucoside of
(anthocyanidin) and others leaves hibiscetin (hibiscitrin) (Rao
(Williamson, Driver, & Baxter, ( & Seshadri, 1942a,b,
2009). R 1948), 7-glucoside of
o
The first anthocyanin from gossypetin (gossypitrin) and
d
the calyx of Hs to be sabdaritrin, which on acid
r
isolated was hydrolysis yielded an
i
‘‘hiviscin’’, also known as g hydroxyflavone named sab-
‘‘hibiscin’’, later named u daretin (Rao & Seshadri,
delphinidin-3- sambubioside e 1942a,b). The presence of
and assigned the structure of z these flavonol glycosides was
cyanidin-3-glucoside - low, with hibiscitrin being the
(Yamamoto & Osima, 1932), M
major compound fol- lowed
which was later renamed as e
d by gossypitrin and sabdaritrin
delphini- din-pentoside- (Rao & Seshadri, 1942a,b). In
i
glucoside (Yamamoto & n 1961, gossypetin-3-glucoside
Osima, 1936). From the pig- Fig. 2. Chemical
a (gossytrin) was isolated
structures of main
ments of cHs, three different anthocyanins. (Seshadri & Thakur, 1961). The
anthocyanins were isolated: petals of Hs var. altissima also
e
delphinidin-3-sambubioside t contain gossype- tin-8-
(hibiscin), delphinidin-3- glucoside (0.4%) and
glucoside and cyanidin-3- gossypetin-7-glucoside
a
glucoside (chrysanthenin) l (Subramanian & Nair, 1972).
(Fig. 2) using material from . From the leaves of Hs,
Taiwan and Trinidad (Du & , b-sitosteryl-b-D-galactoside
Francis, 1973; Shibata & (Osman, El-Garby-Younes, &
Furukawa, 1969). The last 2 Mokhtar, 1975) and from the
study also identified cyanidin- 0 seeds ergosterol (Salama &
3-sambu- bioside 0 Ibrahim, 1979) were reported.
(gossypicyanin) (Fig. 2). Later, 9 b-sitosterol and ergos- terol
the presence of cyanidin-3, ) were also reported in Hs
5-diglucoside and cyanidin-3- .
extracts (McKay, 2009;
(2G-glucosylrutinoside) in the Williamson et al., 2009).
flower pigments of Hs var. The methanolic extract of
5
altissima (Subramanian & . the flowers also contains
Nair, 1972) was reported. A 3 quercetin, luteolin and its
study conducted with 5 . glycoside (Salah, Gathumbi,
different strains of Hs var. 4 & Vierling, 2002). Quercetin
sabdariffa reported cyanidin- . had already been identified
3-sambubioside and in Hs (Takeda & Yasui,
cyanidin-3-glu- coside as the F 1985). One study reported
major compounds present in l that the amount of quercetin
this plant (Khafaga, Koch, El a present in cHs WE was 3.2
Afry, & Prinz, 1980). In one v
mg/g while rutin was 2.1
of the strains (Senegalese o
n mg/g (Alarcon- Alonso et al.,
strain), delphinidin glycosides 2012). Quercetin and its
o
were absent. In this study, the i conjugated glycosides (quer-
antho- cyanin content d cetin-3-glucoside), as well as,
reached 1.7% to 2.5% of the dry s rutin (quercetin-3-rutinoside;
weight in all strains. A similar Hs contain polyphenols of Fig. 3) were frequently
anthocyanin content was the flavonol and flavanol identified in cHs WE,
observed in another study type in simple or polymerised alongside with kaempferol
where their amount was form. The following (Beltran-Debon et al., 2010;
about 1.5 g per 100 g of dry flavonoids have been Herranz-Lopez et al., 2012;
weight of cHs, in terms of described in Hs extracts: Peng et al., 2011; Ramirez-
delphinidin-3-sambubioside hibiscitrin (hibiscetin-3- Rodrigues, Balaban, Marshall,
(Du & Francis, 1973). glucoside), sabdaritrin, & Rouseff,
Several studies have gossypitrin, gossytrin and 2
identified delphinidin-3- other gossypetin glucosides, 0
sambubioside (delphinidin-3- quercetin and luteolin (McKay, 1
O-(2-O-b-D-xylopyranosyl)-b- 2009; Williamson et al., 1
D-glucopyranoise) and 2009); as well as chlorogenic a
cyanidin-3-sambubioside ,
acid, protocatechuic acid,
b
(cyanidin-3-O-(2-O-b-D- pelargonidic acid, eugenol, )
xylopyranosyl)- b-D-
. I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443 179
The water extract of the
dried leaves showed the
presence of catechin (4.25%)
and ellagic acid (28.20%) (Lin
et al., 2012), while cHs WE
showed the presence of
protocatechuic acid (24.24%),
catechin (2.67%), gallocatechin
(2.44%), caffeic acid (19.85%),
gallocatechin gallate (27.98%)
(Yang et al., 2010). Similar
results were reported by
Huang and co-workers
(Huang et al., 2009).
Phenolic acid:
Protocatechuic acid (PCA) is an
important pheno- lic acid
present in Hs extract (Fig. 4)
(Lee et al., 2002; 2003;
McKay,
180 I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443
 I. Da-Costa-Rocha et al. / Food Chemistry
Fig. 3. Quercetin-3-rutinoside.
2009; Williamson et al., 2009). It was isolated from the dried
flowers of Hs and assigned the structure of 3,4-dihydrobenzoic
acid) (Osman, El-Garby-Younes, & Mokhtar, 1975; Tseng, Wang,
Kao, & Chu, 1996).
Chlorogenic acid is another phenolic acid present in both leaf
and cHs extracts and belongs to a family of esters formed between
certain trans-cinnamic acids (caffeic acid, ferulic acid and
p-coumaric acid) and quinic acid (Clifford, Johnston, Knight, &
Kuhnert, 2003). Several studies reported the presence of this acid
and its derivatives in extracts of cHs (Beltran-Debon et al., 2010;
Herranz-Lopez et al., 2012; Peng et al., 2011; Ramirez-Rodrigues,
Balaban, Marshall, & Rouseff, 2011a,b; Salah et al., 2002) and
leaves (Rodriguez-Medina et al., 2009). In one study, the
amount of chlorogenic acid in the extract was reported to
be 2.7 mg/g (Alarcon-Alonso et al., 2012).
181
were 165 (2014) 424–443
reported in seed
oil of Hs. They were mainly unsaturated
hydrocarbons, alcohols and aldehydes from C8 to C13. (Jirovetz
et al., 1992) Subsequently, thirty-seven volatile compounds from
five different groups from the cHs WE were characterised. These
compounds included fatty acid derivatives (such as 2-ethylfuran
and hexanal), sugar derivatives (furfural and 5-methyl-2-furalde-
hyde), phenolic derivatives (eugenol), terpenes (such as 1,4-cine-
ole, limonene) and miscellaneous compounds (e.g. acetic acid)
(Chen, Huang, Ho, & Tsai, 1998). In another study, the volatile pro-
file was examined in four aqueous extracts from fresh and dried
calyx using two different, time–temperature extraction conditions
by GC–MS. A total of thirty-two compounds were identified and
could be divided into five chemical groups: aldehydes (fourteen
compounds), alcohols (ten compounds), ketones (five compounds),
terpenes (two compounds) and acids (one compound) (Ramirez-
Rodrigues, Balaban, Marshall, & Rouseff, 2011a,b). A total of seven
aromatic volatiles were common to all four samples tested (hex-
anal, 3-octanone, octanal, 1-octen-3-one, nonanal, 2,4-nonadienal
(E,E), and geranylacetone).
The following table (Table 1) shows an overview on the constit-
uents present in H. sabdariffa water extract (cHs WE), which are rel-
evant for use in herbal teas, detected on RP HPLC coupled with the
photodiode array detection (DAD) and ESI-TOF-MS in positive and
negative mode.
Table 1
Overview on constituents in H. sabadriffa calyces water extract.
Class Compound References

5.3.5. Mucilage, pectin and carbohydrates (polysaccharides) Organic acid

Hydroxycitric acid 1, 4
Polysaccharides are another key group of compounds present
Hibiscus acid 1, 2, 3, 4
in large quantities in the cHs WE. In one study, the ethanol- Hibiscus acid glucoside 3
precipitated water extract yielded 10% of reddish polysaccharides. Hibiscus acid 6-methyl ester 2, 3, 4
The following compounds were identified in two different Anthocyanins
fractions, arabinose, galactose, glucose, rhamnose and smaller Delphinidin-3-sambubioside 1, 2, 4
amounts of galacturonic acid, glucuronic acid, manose and xylose Cyanidin-3-sambubioside 1, 2, 4
(Müller, Kraus, & Franz, 1989). Similar results were obtained in Flavonoids and phenolic acid
two other studies (Brunold et al., 2004; Müller & Franz, 1992). Gallic acid 2, 3
Chlorogenic acid isomer I 1
The mucilage content was determined in the calyces of five
Chlorogenic acid 1, 2, 4
strains of Hs var. sabdariffa, reaching 24–28% in strains from
Chlorogenic acid isomer II 1
Central America and Egypt but only 15% in an Indian strain. This 5-Hydroxymethylfurfural 2
amount was only reached at a later stage of development in the Methyl gallate 4
strains from Senegal and Thailand. The pectin content only 2-O-trans-Caffeoyl-hydroxicitric acid 4
5-Caffeoylquinic acid 2, 3
accounted for 2–4% while the sugars reached a maximum of
Myricetin-3-arabinogalactoside 1, 4
3–5% in these five strains. Mucilage and pectin consisted of 3-Caffeoylquinic acid 3
60–80% anhydrouronic acid (Afry, Khafaga, Koch, & Prinz, 1980). Protocatechuic acid 2
The petals of Hs yielded 65% of dry weight of mucilage, which Protocatechuic acid glucoside 3
Coumaroylquinic acid 4
on hydrolysis produced galactose, galacturonic acid and rhamnose,
Quercetin-3-sambioside 1, 4
while the leaves only yield 10% (El-Hamidi, Saleh, & Ahmed, 1967;
Quercetin-3-rutinoside 1, 3, 4
Sengupta & Banik, 2011). 5-O-Caffeoylshikimic acid 1, 4
Leucoside(kaempferol-3-O-sambubioside) 4
5.3.6. Volatile compounds Quercetin-3-glucoside 1, 4
Kaempferol-3-O-rutinoside 1, 4
Volatile compounds are responsible for the aroma of Hs. In a
Feruloyl derivative 2
study conducted in 1992, more then twenty-five volatile com- Methyl(AS in Methylepigallocatechin) 4
pounds (accounting for less than 8% of total Hs seeds composition) Myricetin 4
N-Feruloyltyramide 1, 4
4-Caffeoylquinic acid 2, 3
Caffeoylquinic acid isomer 3
Kaempferol-3-p-coumarylglucoside 1
Quercetin 1, 4
Caffeic acid 2
Galloyl ester 2
Feruloyl quinic acid derivative
Kaempferol-3-glucoside 2
Quercetin derivative 2
Tiliroside 2

Legend: 1 – Beltran-Debon et al. (2010); 2 – Peng et al. (2011); 3 – Ramirez-

Fig. 4. Protocatechuic acid. Rodrigues, Balaban, Marshall, & Rouseff, (2011a,b); 4 – Herranz-Lopez et al. (2012).
 It is important to keep in smooth muscle (Obiefuna, antibacterial effect against E. coli O157:H7, Listeria
mind that while researching Owolabi, Adegunloye, Streptococcus mutans, monocytogenes, S. aureus and
the phar- macological actions Obiefuna, & Sofola, 1994). cariogenic bacteria from the B. cereus. Again the
of Hs extract (next section), Interestingly, from various oral cavity, with a minimum antibacterial effect was not
the polyphenol content of isolated muscle prepara- inhibi- tory concentration of affected by heat treatment
the extract was, for some tions, the extract of Hs 2.5 mg/ml (Afolabi, and the ethanolic extract
activities, reported as the one inhibited the tone of rabbit Ogunsola, & Coker, showed greater
responsible for the effect. aortic strip, rhythmically 2008) and Campylobacter antimicrobial effect than the
Nevertheless, the polyphenol contracting rat uterus, species (Campylobacter jejuni, aqueous extract. The study
con- tent is a very general guinea-pig tracheal chain Campylo- bacter coli and further suggests that both,
and often poorly defined and rat diaphragms, but it Campylobacter fetus) that ethanolic extract and
term, as it includes a complex stimulated the tone of solated contaminates meat like protocatechuic acid, might be
poultry, beef and pork at a
mixture of anthocyanins, quiescent rat uterus and frog potent agents for use as food
concentration range of 96–
organic acids, phenolic acids rectus abdominis (Ali, Salih, additives to prevent
and flavonoid compounds. Mohamed, & Homeida, 1991). 152 lg/ml (Yin & Chao, contamination from these
More recently, the Hs WE 2008). This time, the bacteria (Chao & Yin, 2009;
aqueous-methanol extract of
(1–100 mg/kg) was found to Yin & Chao, 2008).
6. dried cHs also showed an in
Biologica inhibit rat bladder and uterine A methanol-water extract
vitro inhibitory effect against
l and contractibility in a dose of Hs was effective against
several
pharmac dependent manner, but via a E. coli O157:H7 isolates from
bacterial strains, such as S.
ological mechanism unrelated to food, veterinary and clinical
aureus, Bacillus
activities local or remote autonomic samples (Fullerton,
stearothermophilus,
receptors or calcium channels Khatiwada, Johnson, Davis,
Micrococcus luteus, Serratia
A detailed review of the (Fouda, Daba, & Dahab, 2007) & Williams, 2011), with the
mascences, Clostridium
pharmacological effects of Hs as pre- viously suggested by highest concentration (10%)
sporogenes, Escherichia coli, K.
extracts is presented in this Salah (Salah et al., 2002). being the most effective.
pneumonia, Bacillus cereus and
section with additional Later, it was shown that The crude extracts of Hs
Pseudomonas fluo- rescence,
information on the studies Hs crude extracts mainly seeds (200 mg/l) also showed
but did not effect the growth
reviewed in the induced the endothelium- antimi- crobial effect against
of fungus Candida albicans
supplementary data dependent relaxant effect in three types of Gram-negative
(Olaleye, 2007). The fresh
(Supplementary Tables 1–15) the isolated thoracic aorta of bacteria. The extract
cHs WE, ethanol extract and
section. rats, via stimulation of NOS exhibited higher activity
proto- catechuic acid (20
enzyme by the Pi3-K/Akt against Salmonella followed
mg/ml) was effective in
6 path- way. It was suggested by Shigella and Enterobacter
inhibiting the growth of food
. that this was due to (Nwaiwu, Mshelia, & Raufu,
spoilage bacteria such as
1 polyphenols. The non- 2012).
Salmonella typhimurium
. endothelium dependent
DT104,
relaxation is a direct smooth 6.3. Antipyretic,
E muscle acti- vation and antinociceptic and anti-
f results in the activation of inflammatory activities
f smooth muscle potassium
e channels (Sarr et al., 2009). Despite the claims that Hs
c is effective in the relief of
t pyrexia in popular medicines,
s 6.2.
Antibacterial, limited studies are available.
antifungal and The antipyretic and anti-
o antiparasitic inflammatory potential of the
n activity cHs extract were studied in
vivo. The ethanol (more
s The cHs WE and potent) and aqueous extracts
m protocatechuic acid (5 showed antipyretic effects by
o significantly reversing yeast-
mg/ml) inhibited the growth
o
of methicillin-resistant induced fever in rats. The
t
h Staphylococcus aureus, mechanism is different from
Klebsiella pneumoniae, the one of aspirin, a pros-
Pseudomonas aeruginosa and taglandin inhibitor.
m
Acinetobacter baumannii (Liu, Nevertheless, fever entails
u
s Tsao, & Yin, 2005). Moreover, enhanced formation of
c protocatechuic acid (in a cytokines such as
l dose dependent manner) interleukins (IL), interferons
e showed greater antimicrobial and tumour
s activity against these necrosis factor-a (TNF-a). The
pathogens in broth than in cHs extract may be involved
Early studies showed that human plasma. The study in the
the alcoholic extract of Hs also revealed that the inhibition of some of these
flowers had an antispasmodic antibacterial effect was substances, resulting also in
effect by relaxing the uterus independent from an anti- inflammatory effect
and intestine stips in vitro temperature, as shown by a (Reanmongkol & Itharat,
(Sharaf, 1962). This was also heat treatment. Hibiscus 2007). Similar results were
observed in rabbit aortic extract also demonstrated obtained by Dafallah (Dafallah
& al-Mustafa, 1996), suggest- n
ing that the flavonoids, t
polysaccharides and organic i
acids might be the o
x
compounds responsible for
i
the pharmacological activity. d
In a more recent study the a
ethanolic extract from the n
calyces also showed t
antinociceptive effect in a rat
model (Ali, Ashraf, Biswas, a
Karmakar, & Afroz, 2011). c
Another in vivo study t
showed that the two fractions i
of the crude aqueous- v
ethanolic extract of the dried i
t
cHs exhibited impressive
y
immunostimulatory activity
by increasing the
Several studies both in
production of
vitro (Duh & Yen, 1997;
IL-10 and decreasing the
Farombi & Fakoya, 2005;
production of TNF-a
Hirunpanich et al., 2005;
(Fakeye, 2008).
Mohd-Esa, Hern, Ismail,
Another mechanism in
& Yee, 2010; Sayago-Ayerdi,
which the polyphenol extract
Arranz, Serrano, & Goni,
exhibit its anti-inflammatory
2007; Steenkamp, Fernandes,
activity is by impairing
& van Rensburg, 2004; Tseng
cyclooxygenase-2 induc- tion
et al., 1997) and in vivo
by down-regulating JNK and
(Farombi & Fakoya, 2005;
p38 MAPK (Kao et al., 2009).
Mossalam, Aty, Morgan,
Youssaf, & Mackawy, 2011;
6
. Olalye & Rocha, 2007; Usoh,
4 Akpan, Etim, & Farombi,
. 2005) have shown that
extracts of Hs have a potent
C antioxidant effect.
l The antioxidant activity of
i the extract is due to its strong
n scav- enging effect on
i reactive oxygen and free
c radicals (Farombi & Fakoya,
a 2005; Mohd-Esa, Hern,
l
Ismail, & Yee, 2010; Olalye
& Rocha, 2007; Sayago-Ayerdi,
s Arranz, Serrano, & Goni, 2007;
t
Tseng et al., 1997; Usoh,
u
Akpan, Etim, & Farombi,
d
i 2005), inhibition of
e
s

A study conducted with 10

healthy volunteers also
supports the claim for its
anti-inflammatory activity.
The ingestion of cHs WE
(dried) decreased plasma
monocyte chemoattractant
protein 1 (MCP-1)
concentration, a biomarker in
the evaluation of
inflammatory diseases
(Beltran-Debon et al., 2010).

6
.
5
.

A
xanthine oxidase activity, antiox- idant potential in 2003; Amin & Hamza, 2005; Wang et al., 2000). Another
protective action against tert- plasma and urine, increasing Asagba, Adaikpoh, Kadiri, & compound that has been
Obi,
butyl hydroperoxide (t-BHP)- the hippuric acid excretion identified to have this effect
2007; Essa et al., 2006; Lin et
induced oxidative damage with decreased was protocatechuic acid, a
al., 2003; Liu, Wang, Chu,
(Tseng et al., malondialdehyde phenolic compound present in
Cheng, & Tseng, 2002, 2010;
1997), protection of cell from concentration in urine the Hs extract (Lin et al.,
damage by lipid peroxidation Liu et al., 2006; Olaleye &
(biomarker for oxidative 2003; Liu, Wang, Chu, Cheng,
(Duh Rocha, 2008; Tseng, Wang,
stress) (Frank et al., 2012). & Tseng,
& Yen, 1997; Farombi & Kao, & Chu, 1996; Wang et 2002; Tseng,
Polyphenols in particular
Fakoya, 2005; Olalye & Rocha, al., 2000) and in vitro Wang, Kao,
the anthocyanins (eg.
2007), inhi- bition in Cu2+- (Ajiboye et al., 2011; Lee et & Chu,
delphinidin-3- glucoside) and
mediated oxidation of LDL and al., 2012; Yin, Cao, Xu, Jeney, 1996).
protocatechuic acid
the formation of thio- & Nakao, 2011).
(Degenhardt et al., 2000;
barbituric acid reactive This effect is due to a 6
Mohd-Esa, Hern, Ismail, &
substances (TBARs) strong antioxidant activity, .
Yee, 2010; Sayago-Ayerdi, 8
(Hirunpanich et al., which reduces cellular
Arranz, Serrano, & Goni, 2007; .
2005; Ochani & D’Mello, damage by reducing
Tseng et al., 1997) are key
2009; Olalye & Rocha, 2007), oxidative stress and by
classes of com- pounds linked
inhibition of the formation attenuating mitochondrial N
to the antioxidant activity. e
of malondialdehyde content dysfunction through
This activity is also the basis p
(100–300 mg/kg) (Farombi & decreasing Bax and tBid
of many other activities h
Fakoya, 2005; Usoh, Akpan, expression in the liver (Lee et
including hepatoprotective r
Etim, & Farombi, 2005), al., 2012). The extract also o
and nephroprotective
reduction of glutathione increased the activity of p
activities from the extract.
depletion, increase of the superoxide dismutase (SOD), r
liver and decrease blood catalase (CAT), glutha- thione o
6
activity of superoxide peroxidase (GPx), and d- t
.
dismutase and catalase aminolevulinate dehydratase e
7
(d-ALA-D) enzymes while c
(Usoh, Akpan, Etim, & .
t
Farombi, 2005) while in the decreasing lipid peroxidation
i
liver it increased superoxide H in induced models of liver v
dismutase, catalase and e damage (Adaramoye, e
glutathione and decreased p Ogungbenro, Anyaegbu, &
mal- ondialdehyde a Fafunso, 2008; Ajiboye et al.,
a
(Mossalam, Aty, Morgan, t 2011; Olaleye & Rocha, c
Youssaf, & Mackawy, 2011). o 2008), and decreased liver t
p marker enzymes such as
The effects were observed for i
r
both water and ethanolic aspartate transaminase (AST), v
o
extracts from flowers of Hs, as alanine transaminase (ALT) i
t
and alkaline phosphatase t
well as from the seeds or e
(ALP) in experimental y
leaves (Mohd-Esa, Hern, c
Ismail, & Yee, 2010). t hyperammonemia (Essa et al.,
i 2006). An Hibiscus Two studies were reported
v anthocyanin extract also on the nephroprotective
6
e induced phase II drug- activity of Hs extracts on
.
6 detoxifying enzymes, such as diabetic nephropathy in
. a glutathione S-transferase, streptozotocin-induced type 1
c NAD(H):quinone oxi- diabetic rats (Lee et al., 2009;
t doreductase, and uridyl Wang et al., 2011). Nephrop-
C
i diphosphoglucuronosyl athy may progress to end-
l
v stage renal disease. A study
i transferase in an induced
i was con- ducted to
n liver damage model (CCl4-
t
i investigate the effect of the
y mediated toxicity model)
c polyphenol extract of Hs (100
a (Ajiboye et al., 2011).
The anthocyanins present and 200 mg/kg/day) in
l cHs WE (100–800 mg/kg)
in the extract seem to be the streptozotocin-induced
showed hepatoprotective
ones responsible for this diabetic nephropathy in rats.
s effects in a range of models
effect (Ajiboye et al., 2011; The extract revealed
t based on toxin-induced
Ali et al., 2003; beneficial effects as the
u hepatitis including, tert-
kidney mass was reduced and
d butylhydroperoxide,
i the hydropic change of renal
lipopolysaccharides,
e proxi- mal convoluted tubules
azathioprine, carbon tet-
s was improved, it reduced
rachloride, cadmium,
serum triglycer- ide, total
ammonium chloride,
One single randomised, cholesterol and LDL as well
acetaminophen and
open-label, two-way cross- as increased the activity of
irradiation in vivo
over study was conducted catalase and glutathione and
(Adaramoye, Ogungbenro,
with 8 healthy volunteers. reduced lipid peroxidation in
Anyaegbu, & Fafunso, 2008;
One single dose (0.05 g/ml) the kid- ney (Lee et al., 2009).
Ajiboye et al., 2011; Ali,
of a Hs WE significantly It was found that the extracts
Mousa, & El-Mougy,
increased the systemic reduced kidney mass and
improved hydropic change of evidence for antilithiatic or
renal proximal convoluted diuretic effects. No significant
tubules in this rat model. The difference in serum sodium
positive effect shown by the and urinary vol- ume were
extracts might be via observed during this study.
improving oxidative status However, Hs tea consump-
and regulating Akt/Bad/ tion produced a uricosuric
14-3-3c signalling (anti- effect (Prasongwatana,
apoptotic mechanisms). Woottisin, Sriboonlue, &
Another in vivo Kukongviriyapan, 2008).
study also revealed that its Similar results were
nephroprotective effect is a observed in albino rats when
result of the protection of given a decoction of dried
the kidney from the calyces at an oral dose of 1
oxidative stressed g/kg (Caceres, Giron, &
(Mossalam, Aty, Morgan, Martinez, 1987).
Youssaf, & Mackawy, 2011). However, in vivo an
antilithiatic effect was
6.9. Renal observed. In Wistar rats,
effects/diuretic which were given extract of
effect (incl. Hs orally at a dose of 3.5 mg
clinical
daily, the oxalate retention
studies)
in the kidney decreased
with increased excretion into
The renal effect of Hs has
urine and decreased calcium
been characterised
crystal deposition in the
pharmacologically both in
kidneys (Woottisin et al.,
clinical trials (Herrera-
2011). The cHs WE (250, 500
Arellano, Flores-Romero,
and
Chávez-Soto, & Tortoriello,
750 mg/kg body weight) also
2004; Kirdpon, Nakorn, &
effectively prevented the
Kirdpon,
develop- ment of urolithiasis
1994; Prasongwatana,
(stone-disorder) in male
Woottisin, Sriboonlue, &
Kukongviriyapan, albino rats (Laikangbam &
2008) and in pre-clinical Damayanti Devi, 2012). A
experiments in rats decrease in renal Ca2+ and
2+
(Aguwa, Ndu, Nwanma, Mg -ATPase activity and
Udeogaranya, & Akwara, unaltered renal calcium
2004; Laikangbam & handling in rats after
Damayanti Devi, 2012). administration of cHs WE at
A two-phase study in 25 and 50 mg/kg was shown.
Thailand with thirty-six Renal function was also
healthy men was conducted enhanced by reduction of
to evaluate the changes in serum
urine after consumption of Hs
juice (16 g/day and 24 g/day)
to determine its effect on the
treat- ment and prevention of
renal stones. Despite the fact
that the con- sumption of Hs
caused a decrease in
creatinine, uric acid, citrate,
tartrate, calcium, sodium,
potassium and phosphate it
did not affect the
concentration of oxalate in
urinary excretion. The
authors suggested that there
was no beneficial effect in
preventing renal stone
formation and that long term
and higher doses should be
investigated (Kirdpon et al.,
1994). Another intervention
study carried out in Thailand
with eighteen subjects with or
without his- tory of renal
stones revealed that Hs tea
drinking, at a dose of 3 g/ day
for 15 days, did not show
urea and creatinine compound demonstrated in athymic nude mice. The reduce very-low density
concentrations (Olatunji, vitro protective effects extract from leaves instead of lipoprotein cholesterol
Usman, Adebayo, & Olatunji, against cytotoxicity and calyces rep- resented a (VLDL-c)
2012). In another pre-clinical genotoxicity of hepatocytes possible source of greater
study in rats, cHs WE pro- induced by tert-butyl- polyphenolic compounds.
duced diuretic and natriuretic hydroperoxide (t-BHP),
effects at the dose range of through inhibiting action on 6.11. Lipid metabolism –
500 to DNA repair synthesis caused anticholesterol
2500 mg/kg b.w. with a by t-BHP and by showing effects/effects on lipid
potassium-sparing effect radical quenching effect metabolism
(Alarcon-Alonso et al., 2012). (Tseng, Wang, Kao, & Chu,
This diuretic effect is in 1996). It also inhibited 12-O- Several studies have
accordance with previous tetradecan- olyphorbol-13- showed that extracts of Hs
studies in experimental acetate (TPA)-induced skin have a lipid lowering
animals (Aguwa, Ndu, tumour formation in CD1- activity, which could prevent
Nwanma, Udeogaranya, & mice (Tseng et al., 1998) and diseases like hyperlipid- emia
Akwara, 2004; Caceres et al., inhibited the survival of and cardiovascular diseases
1987; Onyenekwe, Ajani, human promyelocytic (atherosclerosis and coronary
Ameh, & Gamaniel, 1999; leukaemia HL-60 cells heart disease) (Carvajal-
Ribeiro Rde et al., 1988) and (Tseng et al., 2000). The Zarrabal et al., 2005;
one clinical trial (Herrera- mechanism by which it Chang, Huang, Huang, Ho, &
Arellano, Flores-Romero, exerted anticancer properties Wang, 2006; Chen et al.,
Chávez-Soto, & Tortoriello, might be through antitumour 2003, 2004; el-Saadany et al.,
2004). In this single clinical promotion by reducing 1991; Gosain et al., 2010;
trial, assessing a chemically reactive oxygen spe- cies Hirunpanich et al., 2006;
characterised extract of Hs (ROS), DNA fragmentation, G1 Ochani
(9.6 mg of total arrest and apoptosis. The &
anthocyanins) in patients apop- tosis-inducing activity
with mild to moderate was associated with the D
hypertension, the treatment phosphorylation and ’
dem- onstrated a natriuretic degradation of RB and the M
effect with no effects on suppression of Bcl-2 protein. e
Similar effects were observed l
chloride, potassium and pH
l
(Herrera-Arellano, Flores- in human gastric carcinoma
o
Romero, Chávez-Soto, & (AGS) cells in which the ,
Tortoriello, 2004). apoptotic effect may be
mediated via p53 signaling
2
6 and p38 MAPK/FasL cascade
0
. pathway (Lin, Huang, 0
1 Huang, Chen, & Wang, 2005). 9
0 Another group of compounds ;
. present in cHs extracts are
anthocyanins such as Y
C delphinidin-3-sambubioside. a
a They induced apoptosis n
n against human leukaemia cells g
c
(Chang, Huang, Hsu, Yang, &
e
r Wang, 2005; Hou, Tong, e
- Terahara, Luo, & Fujii, 2005) t
p via the p38-FasL and Bid
r pathway and ROS-mediated a
e mitochondrial dysfunction l
v pathway and against smooth .
e muscle cells (SMC) via p38 ,
n
and p53 pathway (Lo, Huang,
t
i Lin, Chien, & Wang, 2007). 2
v Recently, the anti-cancer 0
e activity of Hs leaf extracts 1
were assessed against human 0
prostate cancer cells in vitro )
a .
c and in vivo (Lin et al., 2012).
The extracts (water and
t The study showed the anti-
ethanolic extracts of dried
i apoptotic effect to be
v calyces or leaves) were able
mediated via both intrinsic
i to decrease low-density
(Bax/cytochrome c-mediated
t lipoprotein cholesterol (LDL-
cas- pase 9) and extrinsic
y c), triglycerides (TAG), total
(Fas-mediated caspase 8/t-
cholesterol (TC) and lipid
Bid) pathways, as well as by
Hs is rich in phenolic peroxi- daxion in vivo. A few of
inhibiting the growth of
compounds, such as them even reported that the
prostate tumour xenograft in
protocatechuic acid. This extract was also able to
(Farombi & Ige, 2007; with this study, another effect of standardised cHs
Ochani & D’Mello, 2009) randomised clinical trial with extract on the lipid profile.
along with an increase in 53 patients with type II Consumption of 100 mg/kg for
serum level of high density diabetes also showed that a 6 weeks was able to decrease
lipoprotein cholesterol (HDL- tea of Hs had a significant the total cholesterol and
c) levels (Ochani & D’Mello, effect on the blood lipid triglycerides level in rats in a
2009; Yang et al., 2010). profile. Patients were given high fat diet, while similar
Addition- ally, it also reduced Hs (one tea sachet (2 g) in results were observed in
foam cell formation and water) twice a day for a humans taking 100 mg of an
inhibited smooth mus- cle cell month (Mozaffari- Khosravi, extract (1.4 mg/kg) orally for
migration and calcification in Jalali-Khanabadi, Afkhami- 30 days. Additionally, the
blood vessels of treated Ardekani, & Fatehi, 2009a). basal HDL-c levels after treat-
rabbits. A possible Despite this, in one ment also increased in human
explanation for the decrease in randomised clinical trial, subjects. This increase in HDL-
LDL-c could be related to the ninety hypertensive patients c lev- els after treatment was
inhibition of the triacylglycerol were given Hs tea or black tea also observed in a clinical trial
synthesis or other for 15 days, with the results with type II diabetic patients
hypolipidemic effects, through showing no hyperlipidemic (Mozaffari-Khosravi, Jalali-
the antioxidant activity against effect as previously reported Khanabadi, Afkhami-
LDL-c oxidation and hepatic in vivo. In addition, no Ardekani, & Fatehi, 2009a).
liver clearance. Several groups differences in creatinine level, The anthocyanin content of
of compounds in the extract, Na and K electrolytes were the extract has been
such as anthocyanins and observed after implicated as responsible for
protocatechuic acid, have administration of the tea. its effects, but an extended
been implicated as However, the short-term chemical profile
responsible for these effects administration did not show characterisation is needed.
(Chang, Huang, Huang, Ho, & any harmful effect
Wang, (Mohagheghi, Maghsoud, 6
200 Khashayar, & Ghazi-Khansari, .
6; 2011). Similar results were 1
Lee found in a double-blind 3
et .
placebo controlled
al.,
randomised trial with a dose
201 A
2; of 1 g/day for 90 days, in
which the leaf ethanol-water n
Tsen t
g et extract of Hs did not appear
i
al., to have a blood lipid -
199 lowering effect over and o
7). above the effect of standard b
dietary and lifestyle advice e
6 (Kuriyan, Kumar, Rajedran, & s
. Kurpad, 2010). The difference i
1 t
between this clinical trial
2 y
. and the one conducted in
2007 is that in the second, the
flower water extract a
C c
administered at a dose of two
l t
i capsules (1 g) three times a
i
n day (total of 3 g/day) for 30 v
i days significantly lowered i
c serum cholesterol levels. t
a Differ- ences might be due to y
l different dosage being
administered, the size of the Pre-clinical data from
s test group and duration of the Brazil indicates a potential
t study. role in the control of certain
u The use of the Hs extract conditions associated with
d was also assessed in a rat obesity, such as
i
model (Oppliger et al., 2012) hyperlipidemia. However,
e
s and in patients (Gurrola-Diaz further studies were
et al., 2010) with metabolic suggested (Dickel, Rates, &
In one clinical trial using syndrome. Metabolic Ritter, 2007).
an oral preparation of Hs syndrome has been charac-
flower extract capsules (with terised as a combination of
a defined composition) serum several metabolic risk factors
cholesterol level was reduced such as hypertension, insulin
after 4 weeks. The best results resistance, dyslipidemia,
were obtained with the excess adipose tis- sue and
dosage of two capsules per cardiovascular disease. Both
meal (Lin et al., 2007). Along studies showed a beneficial
 A report showed that a well as reduced the plasma diabetic rats showed that
standardised (33.64 mg of advanced glycation end an ethanolic extract of Hs
a
total anthocy- anins per each c products (AGE) forma- tion flowers (200 mg/kg) had a
120 mg) water extract of cHs t and lipid peroxidation (Peng strong hypolipidemic as well
was able to reduce weight i et al., 2011). as antioxidant effect. Thus, Hs
gain in obese mice while at v The currently accepted extract showed therapeutic
the same time it increase the i therapeutic strategy for the promise in decreasing and
liquid intake in healthy and t control of postprandial preventing the development
y hyperglycaemia is based on
obese mice (Alarcon-Aguilar of atherosclerosis and
et al., the inhibition of a-gluco- possible related
The ethanolic seed extract sidase and a-amylase. This
2007). This effect is probably cardiovascular pathologies
of Hs (200–1600 mg/kg) results in an aggressive delay
achieved through the linked with diabetes. The
increased the serum prolactin of carbo- hydrate digestion to
modulation of PI3-K/Akt and authors suggest that this
level (p < 0.01) when absorbable monosaccharide.
ERK pathway, which play activity might be linked to
compared to the control in a With this in mind, a study
pivotal roles during adipo- polyphenolic compounds and
dose-dependent manner in was conducted to determine
genesis (Kim et al., 2007). the effect of Hs extract dihydrobenzoic acids, like
lactating Albino Wistar rats
In vitro and in vivo studies on intestinal a-glucosidase protocatechuic acids, but
(Gaya, Mohammad, Suleiman,
showed that Hibiscus extract and pancreatic a-amylase further identification of the
(or tea) inhibited the activity Maje, & Adekunle, 2009).
activity active compounds is
of a-amylase, blocking in vitro. As a result, Hs extract warranted (Farombi & Ige,
6
sugars and starch absorption, was shown to be a potent 2007). A similar effect was
.
which may assist in reported (Huang et al., 2009)
1 pancreatic a-amylase
weight loss (Hansawasdi, with the extract suppressing
5 inhibitor (Adisakwattana,
Kawabata, & Kasai, 2000, . the high-glucose-induced
Ruengsamran, Kampa, &
2001; Preuss, Echard, Bagchi, migration in a vascular
Sompong, 2012). Similar
& Stohs, results were found for hibiscus smooth muscle cell model.
2007). A study conducted in A
n acid (hibis- cus-type (2S,3R)-
Mexico using an ethanol hydroxycitric acid lactone) 6
t
extract of Hs concluded the i (Yamada, Hida, & Yamada, .
extract could be considered - 2007), which inhibited 1
as a possible anti- obesity d pancreatic a-amylase and 6
agent due to its effects on fat i intesti- .
absorption-excretion and a nal a-glucosidase
body weight of rats (Carvajal- b enzyme (Hansawasdi C
Zarrabal et al., 2009). e et al., 2000, 2001). l
t i
The therapeutic use of the Diabetes mellitus is a risk
i n
extract, possibly due to c factor for coronary heart
polyphenols, was also diseases as well as i
c
evaluated in patients with atherosclerosis. An
a a
metabolic syndrome, an obes- ethnobotanical study l
c
ity-associated collection of t conducted in the Caribbean for
disorders (Perez-Torres, Ruiz- i urinary problems and diabetes
s
Ramirez, Banos, & El-Hafidi, v mellitus revealed that Hs is
t
2012). Meanwhile a study i traditionally used to ‘clean’ u
showed that the aqueous t the liver and blood within a d
extract was more efficient in y group of plants used for i
inhibiting triglyceride accu- ‘‘cooling’’, high cholesterol and e
mulation when devoid of Diabetes mellitus can be urinary problems. When the s
fibre and polysaccharides, defined as an endocrine and respondents were asked
but when polyphenols were metabolic disorder which medicinal plants were Recently a double-blind,
fractionated and isolated, the characterised by chronic used for high blood randomised, controlled trial
benefits of the whole extract hyperglycaemia, dyslipidemia, pressure, diabetes and was car- ried out to compare
was greater than the sum of and protein metabolism that jaundice, Hs was referred to the anti-hypertensive
its parts (Herranz- Lopez et results from defects in both hypertension (Lans, 2006). A efficacy of Hs (tea) in
al., 2012). regula- tions of insulin study in alloxan-induced diabetic patients. The results
secretion and/or insulin demonstrated that the
6 action. consumption of the sour tea
. The protective effect of a had positive effects on blood
1 polyphenol extract of Hs was pressure in type II dia- betic
4 studied in a type II diabetic patients with mild
. rat model (high fat diet hypertension (Mozaffari-
model). At a dose of Khosravi, Jalali- Khanabadi,
L 200 mg/kg, the extract Afkhami-Ardekani, Fatehi, &
a demonstrated anti-insulin Noori-Shadkam, 2009b).
c resistance prop- erties as it Following this study another
t reduced hyperglycaemia and randomised clinical trial (no
a
hyperinsulinemia. It decreased control group or double-
t
i serum triacylglycerol, blinding) in identical patients
n cholesterol and the ratio of (100 individuals) showed that
g low- density lipoprotein/high- consuming three glasses of
density protein (LDL/HDL), as
green or hibiscus (sour) tea delayed onset of puberty (ranging from 125 to 500
daily for a period of 4 weeks and elevated body mass mg/kg) indeed reduce both
significantly decreased index at onset of puberty the systolic and diastolic
systolic and diastolic blood in the female offsprings pressures, lowering heart rate
pressures in those patients (Iyare & Adegoke, 2008a,b,c; and work- ing as a
(Mozaffari- Khosravi, Ahadi, Iyare & Nwagha, 2009). The vasodilator (Adegunloye et
& Barzegar, 2013). However, consumption of the extract al., 1996; Ajay, Chai, Mustafa,
sodium, potassium or during pregnancy and Gilani, & Mustafa, 2007;
calcium concentrations were lactation caused decrease of Inuwa et al., 2012;
neither qualified nor maternal fluid and food intake Mojiminiyi et al.,
specific amounts of the other with increased plasma Na+ 2007; Onyenekwe, Ajani,
active constituents of tea, and cor- ticosterone Ameh, & Gamaniel, 1999;
such as caffeine, were taken concentration, while the Shehata & El
into consideration. Other accelerated growth and
clinical trial was conducted to delayed puberty observed in
investigate the hypolipidemic the offspring could be due
effects of sour tea in patients to increased corticosterone
with diabetes. Again, the and decreased leptin
beneficial effect of the sour delivery through breast milk
tea in diabetic patients was (Iyare & Adegoke, 2008b;
found. The sour tea was able Iyare, Adegoke, & Nwagha,
to significantly effect the 2010). These studies however
blood lipid profile by require confirmation as no
increasing high-density observa- tions have been
lipoprotein-cho- lesterol, reported in the literature up
decreasing total cholesterol, to-date pointing to the
low density lipoprotein-cho- presence of respective effects
lesterol, triglycerides and in humans.
Apo-B100, with no effect
on apolipoprotein-A1 and 6
lipoprotein a (Mozaffari- .
Khosravi, Jalali- Khanabadi, 1
Afkhami-Ardekani, & Fatehi, 8
.
2009a).

6 A
. n
1 t
7 i
. -
h
y
D p
e e
l r
a t
y e
e n
d s
i
p v
u e
b
e a
r c
t t
y i
v
a i
c t
t y
i
v Decoctions of Hs have
i been used traditionally in
t West Africa and Mexico as
y
an anti-hypertensive
remedy. Several in vitro
A few studies with rats
(Jonadet et al., 1990;
have shown that
Obiefuna, Owolabi,
consumption of Hs WE during
Adegunloye, Obiefuna, &
pregnancy and lactation
Sofola, 1994) and in vivo
resulted in increased
studies have shown that the
postnatal weight gain,
extract of the calyces
Menoufy, 2008). The anti- t (Hopkins, Lamm, Funk, & The effect of cHs extract
hypertensive activity might u Ritenbaugh, 2013). (200 to 1000 mg/kg body
be through: d Anthocyanins, including weight) on some
inhibition of angiotensin- i delphinidin-3-O- haematological parameters in
converting enzymes (ACE) e sambubioside (hibi- scin) rats was studied to determine
(Jonadet et al., s and cyanidin-3-O- its medicinal usefulness in
1990; Ojeda et al., 2010), sambubioside the treatment of anaemia.
acetylcholine-like and Several clinical trials were (gossypicyanin), have been The study suggested that at
histamine-like mechanisms carried out to determine the identified as being a comparatively high dose
(Adegunloye et al., 1996), anti- hypertensive effect of responsible for ACE range of 200 to
diuretic effect (Mojiminiyi, Hs (Haji Faraji & Haji inhibition (Herrera- Arellano 400 mg/kg, the extract had a
Adegunloye, Egbeniyi, & Tarkhani, 1999; Herrera- et al., 2007; Ojeda et al., beneficial effect on the red
Okolo, 2000), reduction in Arellano, Flores-Romero, 2010). cells, but this was not
the diffusion distance Chávez-Soto, & Tortoriello,
sustained at even higher
between capillaries and 2004; Herrera-Arellano et 6 doses (Adigun, Ogundipe,
myocytes, as well as new al., 2007; Mozaffari- . Anetor, & Odetunde, 2006).
vessel formation (Inuwa et al., Khosravi, Jalali- Khanabadi, 2
Another study using a rat
2012) and direct vaso-relax- Afkhami-Ardekani, Fatehi, & 0
model of infection with
ant effects (Adegunloye et al., Noori-Shadkam, 2009b). Both .
Trypanosoma congolense
1996; Ajay, Chai, Mustafa, a Cochrane review and a
showed that the use of Hs WE
Gilani, & Mustafa, 2007; systematic review carried out A
(equivalent to 9.61 mg/100
Obiefuna, Owolabi, in n
t g/day of ascorbic acid for 3
Adegunloye, Obiefuna, & 2010 concluded that the
i weeks) prevented the
Sofola, 1994; Adegunloye et studies did not provided
- disease-induced anomalies
al., 1994). The relaxant effect reliable evidence to support
a with increase of serum
might be partially recommendation of this plant
n creatinine and urea levels. It
endothelium independent to control or lower blood a was concluded that
and possibly mediated by pressure in hypertensive e consumption of the extract
endothelium-derived nitric patients, when compared to m
ameliorated the pathological
oxide (EDNO)-dependent placebo or no treatment i
c changes in blood as well as
action. Endo- thelium- (Ngamjarus, Pattanittum, &
hepatic and renal structures
dependent vasodilator Somboonporn, 2010; Wahabi,
of T. congolense-infected rats.
component results through Alansary, Al-Sabban, & a
The observed effects might be
activa- tion of the Glasziuo, 2010). However, a c
t due to the ascorbic acid
endothelium-derived nitric recent randomised, double-
i component or other
oxide/cGMP-relaxant blind, placebo-controlled
v antioxidants present, which
pathway, whereas the clinical trial showed that Hs
i presumably kept the free
endothelium-independent tea (1.25 g of H. sabdariffa per
t radical load in infected rats
component could be due to 240 mL boiled water; 3 serv- y low as well as preventing the
inhibition of Ca2+ influx (Ajay, ings a day for 6 weeks)
disease-associ- ated
Chai, Mustafa, Gilani, & effectively reduced blood A preliminary study on the depletion in systemic
Mustafa, 2007). pressure in pre- and mildly- use of Hs decoctions as an antioxidants. Nevertheless,
Additionally, Hs showed hypertensive adults (McKay, alterna- tive source of iron for further studies are needed to
antiplatelet but no Chen, Saltzman, & Blumberg, the treatment of anaemia and determine the long-term
thrombolytic activ- ity in 2010). Similar effects on some other mineral effects and the mechanism
vitro (Yamamoto, Yamada, decreasing systolic and dia- deficiency diseases was of action before
Naemura, Yamashita, & Arai, stolic blood pressures were conducted and showed that recommendations could be
2005). One in vivo study observed in mildly dry fermented calyces of made (Umar et al., 2009).
reported that despite the hypertensive type II diabetic hibiscus exhibited a very low
beneficial effect as an anti- individuals when taking pH value which enhanced
hypertensive, Hs might green or hibiscus (sour) tea mineral availability. Another 6
produce undesirable effects for 4 weeks (three times a .
reason for enhancing min-
on gonadal activity (Shehata day, 2 h after each meal) 2
eral (iron, zinc, calcium and 1
& El Menoufy, 2008). (Mozaffari- Khosravi et al., magnesium) bioavailability is .
2013). The authors also the high concentration of
6 concluded that this might be ascorbic acid (Falade et al.,
. useful in preventing the O
2005). t
1 progression to moderate or
9 h
more severe hypertension, e
. potentially decreasing cases r
of cardiovascular dis- ease. s
C Furthermore, a recent
l comprehensive review on The clinical use of Hs
i
animal and human studies on was reported for
n
the effect of Hs in the conjunctivitis
i
c treatment of hypertension (
a and hyperlipidemia concluded F
l that Hs has great potential to r
reduce risk factors associated a
u
s with cardiovascular diseases
n
and warrants further studies
f Genome shuffling of
e Streptomyces sp. U121 was
l used to achieve improvements
d on the production of
e
hydroxycitric acid, an organic
r
, acid present in Hs (Hida et
al., 2007). This technique is
of great interest to the
2
biotechnological production
0
0 of this compound in the food
4 industry as a safe food
) additive. As previously
. reported, hibiscus acid, the
A Hs flower tea was shown (+)-allo-hydroxycitric acid
to be a very efficient oral lactone, has been
negative contrast agent for demonstrated to have an
magnetic resonance inhibitory effect on pancreatic
cholangiopancreaticogra- phy a-amylase
(MRCP) study in reduction of and intestinal a-glucosidase
high intensity fluid in the (Hansawasdi et al., 2000,
stom- ach and duodenum. 2001), resulting in reduction
The authors suggested that of carbohydrate metabolism
this was natural, safe, and blood insu-
inexpensive and palatable l
for oral administration i
(Varavithya et al., 2005). n
The effect of WE of dried
cHs was also assessed on l
intestinal transit in e
experimental rats providing a v
e
potential use in the control of
l
diarrhoea, as there was a s
reduction in percentage .
transit point indicating a
reduction in intestinal
motility and increased 7
transit time. At an appropriate .
dose it could therefore
become a constipat- ing agent S
(Owulade, Eghianruwa, & a
Daramola, 2004). f
e
A study reported that
t
crude polysaccharides from y
Hs flowers had a potent
stimulator effect on H. sabdariffa
keratinocytes proliferation preparations, predominantly
with an influence on the the infusion and aqueous
early differentiation extracts, have a long standing
behaviours of the cells. Thus, traditional use both in food
polysaccharide-containing and in medicine, and in
extracts from Hs could be general are considered to be
used for dermatological or safe. The
cosmetic applications
(Brunold et al., 2004).
Another unorthodox use
proposed for Hs flowers is as a
pH indi- cator for
environmental protection. The
flowers of this plant con- tain
anthocyanine pigments. As
these pigments change
colour depending on pH, they
could work as a
environmental indicator
replacing synthetic indicators,
therefore being safer for the
user’s health, minimising
chemical pollution and
become more cost effective
(Soltan & Sirry, 2002).
available toxicological data, LD50 of cHs aqueous extract 9 authors regarding a putative
however limited, are in ) cardio- or liver toxicity of the
was >5000 mg/kg b.w. The
.
support of this assessment. same authors assessed the tested extract have to be read
Administration of the
The literature search for this effect of the extract on blood with caution.
water-soluble fraction of a
review did not reveal any case pressure in spontaneously In recent years the effect
concentrated cHs extract
reports of adverse reactions hypertensive and of Hibiscus extracts on
(extraction solvent: MeOH
following oral consumption of normotensive Wistar-Kyoto reproduction and
80%) given orally at up to
H. sabdariffa preparations. rats. As part of this study it development in rats has been
15 successive doses of 250
was observed that between subject to in vivo studies by
mg/kg/d to Wistar albino rats
7 the seventh and the twenty- sev- eral authors. In female
showed no pathological
. first day after extract rats, addition of hibiscus
1 features in both liver and
administration, the highest extracts to drink- ing water
. heart after 24 h
dose of 1000 mg/kg resulted resulted in a dose-dependent
(Akindahunsi & Olaleye,
in spontaneous deaths in reduction of fluid and feed
2003). The authors observed
T hyperten- sive but not in intake. The effects observed in
o a dose- related increase in
normotensive rats. With the pups included increased
x the levels of serum aspartate
reference to the well known weight gain and delayed
i aminotransferase (AST) and
increased risk of sudden onset of puberty. As the
c alanine aminotransferase
cardiac death in patients authors rightly state, these
o (ALT) when compared to the
l receiving non-potassium effects have likely been
control group. However,
o sparing diuretics, the caused by the reduced fluid
levels of the same enzymes
g authors speculate that the and feed intake in accordance
death of the animals may decreased slightly in the
y with earlier publications.
have been due to a diuretic liver. In view of the
Rather than repre- senting
effect of the extract extraordinarily high serum
In a bioassay for specific toxicologic properties
screening plant extracts for (Onyenekwe, Ajani, Ameh, & AST value in the control
of hibiscus, the decreased
their biological activity, the Gamaniel, 1999), however, the group as compared to fluid and feed intake and
lethal dose (LD50) of three dose found to be active is reference values from the
subsequent adverse effects
different types of Hs extract excessively high. Although literature (Boehm et al., observed in this study may be
was assessed in the brine Kirdpon and co-authors 2007), the conclusions of the
the result of the animals
shrimp toxicity assay. report a decrease of dislike for the flavour of
Aqueous Hs extract (i.e., potassium and sodium in 36 hibiscus (Iyare & Adegoke,
infusion) produced an LD50 of healthy young men after 2008a,b; Iyare et al., 2010).
9.59 lg/ml, while for the successive administration of Despite the fact that earlier
dichlo- 16 g/d Hibis- cus ‘‘Juice’’ studies showed the LD50 to
romethane extract it was (while surprisingly no such be above
24.51 lg/ml and 4.75 lg/ml effect was seen in the high 5000 mg/kg and doses as
for the eth- high as 4600 mg/kg were
dose group with 24 g/d), this
anolic extract (Serrano, administered
interpretation remains
Ortega, & Villar, 1996). Given to rats in drinking water for
questionable in view of a
the very limited value of the 12 weeks with no increase in
much larger and well-
brine shrimp assay for mortal- ity, the extract
documented controlled
complex mixtures like plant induced testicular toxicity
clinical study in which
extracts (Manilal, Sujith, Hibiscus extract showed a (reduced sperm counts and
Kiran, Selvin, & Shakir, 2009) natriuretic effect with no spermatogenesis with
and the incomplete effects on chloride, potassium evidence of marked
information on the mode of and pH in 171 men with degenerative histo- logical
preparation of the extracts, mild to moderate changes) at all
this work is mentioned here hypertension (Herrera- concentrations tested (1150–
for completeness only. Arellano, Flores-Romero, 4600 mg/kg) (Orisakwe,
The LD50 in mice (b.w. 30 Chávez-Soto, & Tortoriello, Husaini, & Afonne, 2004).
g) was reported to be 2004). Lack of acute toxicity Additionally, deleterious
about 0.4– effects on the testis and
with calcu- lated LD50 values
0.6 ml on intraperitoneal spermatozoa and an adverse
administration of a 30% >5000 mg/kg b.w. was
reported for a methanolic influence in the male
aqueous Hs decoction (20 reproductive fertility of
min in distilled water) dried flower extract in adult
albino mice on a herb-drug albino mice were also
(Sharaf, 1962). The same reported after a cHs WE was
interaction study after 24 h
authors observed a lowered administered daily for 4
administration (i.p.) (Ndu,
blood pressure in dogs (b.w.: weeks in a dose of
Nworu, Ehiemere, Ndukwe, &
7 kg) with no side effects 200 mg/kg (Y. I. Mahmoud,
Ochiogu, 2011) and for an
after administering (i.p.) 10 2012). In contrast to these
ethanolic extract of Hs seed in
ml of a 10% solu- tion of the studies, long term
albino Wistar rats while
Hs decotion. administration of Hs WE for
studying the effect of the
According to a study of 10 weeks and hibiscus
extract on lac- togenic activity
Onyenekwe and coauthors, no anthocy- anins (50–200 mg/kg
(Gaya, Mohammad, Suleiman,
deaths were observed in b.w.) for 5 days did not affect
Maje, & Adekunle,
Albino mice after fourteen the male repro- ductive
2
day’s administration (i.p.) at system in rats (Ali et al.,
0
doses of 1000–5000 mg/kg 0 2012).
b.w./d., thus the calculated
 Fakeye and co-authors ethanolic Hs extracts (200
assessed toxicological effects mg/kg and 300 mg/kg, orally)
of a 90- day oral in rabbits over a period of
administration of aqueous, eight weeks did not show any
ethanol or 50% ethanol toxic effect when
extracts of dried cHs at doses dyslipidemia and oxi- dant
of 300 and 2000 mg/kg b.w., stress associated with
respec- tively, in male Charles prolonged excessive intake of
Foster rats. Strikingly choles- terol was studied in
contrasting with pre- vious these animals (Ekor et al.,
studies by various other 2010).
authors, they observed a Based on the data
strong toxicity with total presented above, dosages up
mortality in all 2000 mg to 200 mg/kg should be safe
groups until day 28, and in and not show signs of
the aqueous and 50% toxicity, but further studies,
ethanol groups at 300 mg, most importantly with
until day 60 and 40, chemically well
respectively. (Fakeye, Pal, characterised extracts, are
Bawankule, Yadav, & warranted.
Khanuja, 2009). At a dose of
300 mg/kg (b.w.) all extract
types produced a significant
increase of plasma creatinine
after 30 days administration
of the extracts. High
creatinine blood levels may
be associated with muscular
dystrophy, loss of kidney
function or even mortality.
However, since the ethanol
extract produced the
strongest increase in
creatinine but no mortality
at the
300 mg dose level, it is
unlikely that the elevated
creatinine levels have been
the cause of death in the
other groups (Fakeye, Pal,
Bawankule, Yadav, &
Khanuja, 2009). Overall, the
results of this study remain
highly questionable. The
possible reasons consid- ered
by the authors, including
differences in anthocyanin
content, are not convincing
in view of the still
moderate anthocyanin doses
provided with the extracts.
A similar effect was
observed on rat testis in a
cisplatin (CIS)- induced
rodent model of
reproductive toxicity when
ethanol extracts of Hs was
administered for 26 days (1
g/kg per day) (Amin &
Hamza, 2006). The extract
also revealed anti-mutagenic
activity in vitro against 1-
nitropyrene, a potent
mutagen (Olvera- Garcia et
al., 2008) and reduction of
micronuclei in polychromatic
erythrocytes (PCEs)
(Adetutu, Odunola, Owoade,
Adeleke, & Amuda, 2004).
The administration of
7 the type of preparation comple- ments the evidence (305 hits), like roselle (753
. (methanol extract) and mode based on the complete hits), karkade (22 hits), which
2 of administration absence of drug inter- action delivered a remarkable
. (intraperitoneal), the case reports involving number of relevant hits,
relevance of these findings hibiscus in the scientific whereas results for the
I for the use of traditional literature. terms rosemallow, flor de
n hibiscus preparations remains Jamaica, Abelmoschus
t highly questionable. cruneatus, sorrel (not Rumex
e 8. Scientific
The pharmacokinetics of acetosa) or bissap were not
r applications and
a chloroquine (600 mg) and a found or lead to non-rele-
freshly prepared Hs beverage, translational vant patents.
c research
t similar in taste and Based on the research
i concentration to the one outcome, further queries were
o In order to assess the level
usually consumed by performed with AND
n of translational research on Hs
Sudanese people, were (Boolean operator) search
s prod- ucts, a patent research
studied in healthy males. The options Tea, Extract, Food,
at the Espacenet patent
study showed a statistically Health, Medic⁄ (for
While there is no database of the European
significant reduction in the Medical, medicine/s,
particular ground for Patent Office
area under the plasma medicinal, medication/s etc.).
suspicion of a relevant (http://worldwide.espacenet.c
concentration versus time Table 2 shows a survey of the
interaction potential of om) incorpo- rating 90+
curve and the peak plasma results/hits and representative
Hibiscus, several preclinical national patent databases was
concentration of examples as selected patent
and one clini- cal study have performed in March 2013
chloroquine (Mahmoud, titles, the nations of their
addressed this issue. The (Worldwide – collection of
Ali, Homeida, & Bennett, application (e.g. CN-China,
sub-acute effect of an published applications from
1994). In view of the very JP-Japan, MX-Mexico etc.)
aqueous cHs extract on 90+ coun- tries). The result of
small group size (N = 6) and and the year of their
CYP450 activity, clinical this research on intellectual
the poor information on the publication.
blood chemistry and property rights regarding Hs
mode of preparation and Also recent clinical
haematology was shows an increasing interest
dosage of the hibiscus research topics are already
investigated in male Wistar in novel technological
beverage, the results of this reflected in newer patents.
rats at 250 and 1000 applications of potential
study need to be interpreted For instance, the
mg/kg/day for 30 days. The future products derived from
with caution. hypertensive effect of
authors found no effect on Hs.
The effect of so-called hibiscus preparations, like the
hepatic phase I enzymes Research queries used
Zobo Drink (sweetened tea or extract can be found.
(CYP 1A1, 1A2, 2B1/2, 2E1 were: hibiscus (1450 hits)
aqueous extract prepared The term ‘‘Hibis- cus Tea’’
and 3A) and the extract did AND sabda- riffa (51 hits)
from 30 g dried hibiscus yielded in 305 hits and the
not significantly affect and common names for
calyces/l) on acetaminophen query ‘‘Hibiscus Tea Hyperten-
blood chemistry and hibiscus or hibiscus tea
pharmacokinetics was studied sion’’, as well as, ‘‘Hibiscus
haematology. (Prommetta, in healthy young men (N = 6, AND Hypertension’’ yielded
Phivthong-ngam, cross- over design). No two relevant patents. The
Chaichantipyuth, significant kinetic changes same patents are found
Niwattisaiwong, & were observed when the starting from ‘‘hibis- cus
Lawanpraset, 2006). More extract was administered extract’’ with 793 hits; those
recently, the interac- tion of a concomitantly with connected with AND
methanolic Hs flower extract acetaminophen, except for a hyperten- sion showed two
and hydrochlorothiazide (a slight elevation of the hits (see Table 3 for more
diuretic drug) was examined clearance by ca. 11%. Given details), whereas AND ‘‘blood
in adult albino mice, albino the poorly described study pressure’’ gave no hits.
rats and healthy adult protocol and the small sample Regarding bioactive principles,
rabbits. Co-administration of size of N = 6, the conclusions one of the main
the extract (20– of the authors on a possible phytochemicals found in Hs
40 mg/kg b.w.) with interaction potential of calyxes, besides the more
hydrochlorothiazide (10 hibiscus should be read known anthocyanins, is
mg/kg) caused a significant with caution (Kolawole & hibiscus acid, a (2S,3R)-
increase in the volume of Maduenyi, hibiscus type enantiomer.
urine excreted, as well as a 2 Patent search for ‘‘hibiscus
significant decrease in the pH 0 acid’’ revealed 9 patents. The
of urine and the 0 query ‘‘hydroxycitric acid
concentrations of sodium, 4
AND hibiscus’’ yielded 2
bicarbonate and chloride ions. )
results, but only five of those
It also increased and pro- .
results are relevant (see Table
longed the plasma Taken together, the data
3 for more details).
concentration, the mean area available today from
under the concen- tration– preclinical and clinical
studies does not provide 8
time curve and the volume of .
distribution of the diuretic substantiated evidence of
1
drug over a 24 h sampling any therapeutically relevant .
period (Ndu, Nworu, interaction potential of
Ehiemere, Ndukwe, & commonplace teas or
F
Ochiogu, 2011). Regarding beverages containing hibiscus u
and its preparations. This
t options available (Hritcu et
u al., 2011).
r Hibiscus rosa sinensis L.
e roots have been used in
fertility regula- tion, showing
r strong anti-implantation and
e uterotropic activity (Kholkute
s & Udupa, 1976; Vasudeva &
e
Sharma, 2008). This plant
a
r forms an important
c constituent of several
h Ayurvedic contraceptive
preparations (Kamboj &
The available information Dhawan, 1982). Further
on H. sabdariffa shows a wide research with Hibiscus
range of traditional as well species including Hs may be
as potentially new health warranting with regard to
applications and therapeutic gynaecologic applications.
targets associated with such Limited data is available
uses. More robust, that correlates the therapeutic
randomised, controlled uses of Hs and the chemical
clinical trials would be profile of the extracts being
desirable with well- used. Most of the studies
characterised Hs reported in this review only
preparations to corroborate identify the type of extract
its beneficial effects in pre- and part of plant used, but do
and mildly-hypertensive not quantify the compounds
patients. The same applies for present in the extract.
its diuretic effects.
Obesity is a growing
problem affecting not only
adults but also children. The
effectiveness of Hs extract for
metabolic disorders like type
II diabetes should be
investigated further, as
previous clinical studies have
shown promising effects on
hyperlipidemia and
hypertension, conditions
strongly correlated with type
II dia- betes or metabolic
syndrome (Hernandez-Perez
& Herrera- Arellano, 2011;
Hopkins, Lamm, Funk, &
Ritenbaugh, 2013). Given the
longstanding safe use of
hibiscus preparations as food,
it could be of great help in
the supportive treatment of
these pathologies.
Other therapeutic uses
could also be pursued. In a
study with Hibiscus asper
Hook.f., a closely related
species, the methanolic
extract of leaves showed
neuroprotective activity
against 6- OHDA-induced
toxicity, through its
antioxidant and anti-apoptotic
activities in a Parkinson’s
disease model. Further
studies will be needed to
determine if an extract of Hs
would have similar effects.
Parkinson’s disease is a
progressive
neurodegenerative disorder
with limited therapeutic
Table 2
Results/hits and representative examples as selected patent titles of Hibiscus sabdariffa L.
 Hits Hibiscus sabdariffa (total of 51 hits
(Hibiscus 1459 hits))
AND tea 3 hits: relevant only JPS6212767 (B) of
Mutsuo (see Table 3)
AND extract 31 hits: EU, US, mainly Asian: CN, KR, TW;
published 1981–2013. Selected patent
titles: Patents on extract use in for
hepatic, inflammatory, metabolic
disorders,
related to lipase activity inhibitor, fat
metabolism improving composition, anti-
allergic effect, anti-aging, cosmetic use as
activators of aconitase and their use in
anti-ageing skin care, skin protecting
agent, hair care, active oxygen scavenger
cosmetic, as meat quality preservative
due to its antioxidant effect
AND food 8 hits: JP, RU, TW, MX; published 2003–
2012. Composition of Hibiscus sabdariffa L.
calyces for the manufacture of drugs, food
supplements, functional food and
sweeteners for beverage, cosmetic use,
and in atherosclerosis prevention
AND health 2 hits: (1) JP2005333942; published 2005.
Fermented herb vinegar and method for
producing the same. (2) CN1404740,
published 2003. Eight-ingredients slim tea
and its making method
⁄
AND medic 13 hits: mainly of Asian origin; published
2003 and thereafter. Use of the Hibiscus
sabdariffa extract in the preparation of a
medicament; mainly in atherosclerosis
prevention or inhibition; mainly within
mixtures of 1–8 herbals
Abbreviations: CN-China, JP-Japan, RU-Russia, TW-Taiwan, MX-Mexico, KR-Korea, GE-Georgia, EP-Europe, WO-World.
Preliminary studies also demonstrated very interesting phar-
macologic effects for Hs in obesity and diabetic conditions. In rela-
tion to type II diabetes, the combined presence of
nephroprotective and a-amylase inhibiting properties deserves
further attention.
Overall, Hs preparations, particularly Hs tea and aqueous
extracts can be considered to be safe.
Roselle (746 hits) Karkade (22 hits)
46 hits: 39xCN,3xJP,2xRU,2xTW; published 2000– 19 hits: 14 RU patents all of inventors: Butina, et
2012. Selected patent titles: Flower/fruit/natural al. published 2010–2012. Functional food
tea drink and preparation method, blood product with antitoxic radioprotective,
nourishing and facial beautifying composition, immunomodulating, hypoglycaemic, ergogenic,
refreshing composition with low glycaemic index, hepato-protective, hypocholesteremic,
weight reducing tea, health protection herbal tea, interseptum protective, hypolipidemic,
radiation-resistant functional tea beverage, liver- antioxidant, herophophylactic, hypotensive
nourishing tea, natural colourful total nutrient, tea properties, anti-inflammatory properties against
drink capable of removing toxin and beautifying, digestive tract diseases, others: sweet liqueur or
wisdom brain enlightening drink, tea for benefiting alcoholic beverage 2xRU//2xJP Dough improving
wisdom and awakening brain, natural tea for agent,//1xEP drink//1986–2011 RU, JP, GE
nourishing entrails and reducing blood fat, blood
sugar and blood pressure, tea drink for promoting
mentality and building body, health-care tea and
its making method, quick dissolving roselle tea
bag, Roselle tea and method for producing the
same, etc 15 hits: 14 RU patents of Inventor: Butina E.A.
19 hits: 10xCN, 4xJP, 2xMX, 1xTW, 1xRU, 1xUS, et al.; published 2010-2012. On functional food
published 1987–2012. Method for extracting product, 1xJP external use
roselle calyx red pigment, refreshing composition
with low glycaemic index, nutritional healthy
beverage, fabric refreshing cabinet device, the
improvement of anthocyanin content from
extraction of the roselle calyx infusion, preparation
capable of defaecating, adjusting qi and blood,
improving internal secretion and preventing
senescence, method for producting roselle chewing
gum and the resultant product, production of
concentrated drink from Hibiscus and Roselle, etc 15 hits: 14 RU patents of Inventor: Butina E.A.
53 hits: 25xCN, 5US, 2xMX etc.; published 1997– et al.; published 2010–2012. On functional food
2012. Selected patent titles: Nutrient health care product. 1xJP dough improving agent.
product for reducing trioxypurine, rose oral liquid,
rose jam, composition and food for improving
metabolic syndrome, health protection herbal tea,
method of preparing healthy food, roselle red
pigment, baked food, multicolored hypoglycaemic
tea drink, roselle fast food, drink and food
obtained by using leaf of roselle, food biologically
active addition, microorganism reduction methods
and compositions for food cleaning,
cleaning/sanitising methods, compositions, and/or
articles for fabric, articles, methods for cleaning
produce and edible and edible animal protein, etc 0 hit
51 hits: 47xCN, 2xTW, 2xJP; published 1995-2012.
Selected patent titles: many of the roselle tea
patents; health protection herbal tea, method of
preparing healthy food, natural tea drink capable
of clearing away heat, roselle mooncake, roselle
eight- flavour rice dumpling, method for
cultivating roselle, application of roselle for
preparing health product for promoting lead-
eliminating effect, process of making preserved
vanilla-roselle calyx, roselle notoginseng beverage,
roselle calyx jam, roselle series product, etc 8 hits: 8 RU patents of Inventor: Butina, et al.,
24 hits: 15xCN, 3xRU etc.; published 1998–2012; published 2010–2012. On functional food product
Roselle solid beverage, species ‘‘Dirosavit’’ eliciting
general tonic effect, roselle calyx beverage, elixir
for gastroenteric tract disease treatment
normalizing metabolism and eliciting sedative
effect, arrangement for delivering liquid to medical
treatment point, nitric oxide donor compounds
and pharmaceutical compositions for pulmonary
hypertension and other indications, etc
An increasing body of pharmacologic and clinical studies is pro-
viding promising perspectives for an interesting range of therapeu-
tic applications as well as potential health claims. However, this
review has also identified a wide range of problems associated
with the quality of many aspects of these studies, but most impor-
tantly the pharmacological or clinical approaches (or models) used
Table 3
Patents list that include Hibiscus sabdariffa L., Hibiscus acid and Hs Tea and hypertention
 438
Patent or Issue date Title Summary Inventor(s) Applicant/assignee
application
number

US 6127553 (A) Oct 3, 2000 Convenient method for large-scale
isolation of hibiscus acid
US 6849278 (B) Feb 1, 2005 Method to counter oxidation of LDL,
decrease triglyceride or cholesterol
and inhibit atherosclerosis using
Hibiscus sabdariffa extract
US 2008/ April Hydroxycitric acid compositions from
0095867 A1 24, 2008 garcinia cambogia and hibiscus sp.,
methods of making, and therapeutic
uses of same
The invention relates to a process for the isolation of Hibiscus acid or (+)hydroxycitric Ibrahim Ibnusaud, Rani Department of
acid lactone (2S,3R-dihydroxy-1,2,3-propanetricarboxylic acid lactone) from the leaves of Rajasekharan, Teena Science
Hibiscus furcatus, Hibiscus sabdariffa and Hibiscus cannabinus. Garcinia acid, one of the Philip, Salini Thomas and Technology,
optical isomers of hydroxycitric acid is a potentially interesting molecule and found Government of
extensive application in the pharmacological as well as synthetic fronts. India
A method for countering oxidization of low density lipoproteins, reducing cholesterol or Chau-Jong Wang Universal Biotech
triglyceride in plasma or inhibiting atherosclerosis comprising administering an effective Co., Ltd.
amount of a Hibiscus sabdariffa extract
Herbal compositions that comprise one or more of extracts of hydroxycitric acid, Scott Alexander Renaissance Herbs,
( ) HCA and (+) HCA, from Garcinia cambogia and Hibiscus sabdariffa, and anthocyanins Moffett Inc.
from Hibiscus sabdariffa; all constituent extracts at independently controlled
concentrations which optionally include second therapeutic agents and pharmaceutically
acceptable additives. Processes for the preparation of these herbal compositions, such
processes including steps of extracting hydroxycitric acids and anthocyanins from

I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443

Garcinia and Hibiscus species, reacting the hydroxycitric acid with IA and IIA group
metals of periodic table, isolating the metal salt of hydroxycitric acid and drying and
optionally mixing anthocyanins. Uses of the compositions that comprise extracts
containing hydroxycitric acids (positive and negative isomers) and anthocyanins
from Garcinia and Hibiscus species optionally along with secondary agents and
pharmaceutically acceptable additives to manufacture a medicament for multiple
therapeutic uses, as well as beverages and powdered beverage premixes, all of which
provide healthful benefits, are also provided
Hs Tea
JPS6212767 (B) March Tea bag of Hibiscus sabdariffa L. and Purpose: To obtain the titled tea bag useful for a fancy drink, having effect of herb Satou Mutsuo Hounan Shiyokuhin
20, 1987 its preparation medicine on diabetes, hypertension, malum cordis, etc., by adhering uniformly and firmly Kogyo KK
a specific amount of stevia extract powder as a sweetener to dried ground pieces of
Hibiscus sabdariffa L., followed by packing. Constitution: Dried ground pieces of Hibiscus
sabdariffa L. is sprayed with 1–3 wt% aqueous solution or alcoholic solution of stevia
extract powder so that the powder is adhered to Hibiscus sabdariffa L. uniformly and
firmly. Water or alcohol is evaporated by a dryer, etc. to make water content of the
prepared product 10 wt% and it is packed in tea bags.; Hibiscus sabdariffa L. contains no
caffeine, has effect of herb medicine on diabets, hypertension, malum cordis, renopathy,
respiratory diseases, diuresis, reduction of cholesterol in the blood, etc. and exhibits
bright ruby and proper acidity. While stevia extract powder has sweetness about 100
times as much as that of sugar. An amount of the latter per bag is preferably 0.02–0.04 g.
EFFECT: Even excess drinking is harmless
Hibiscus acid
US6703515 (B2) March Novel chiral derivatives of hibiscus (see title) Saud Ibrahim Ibnu [IN] Dept Science and
09, 2004 acid bearing lactone ring moiety, Gopinath Chitra [IN] Technology,
process for preparing the same and a Technology Bhavan
convenient method for the large-
scale isolation of hibiscus acid
US6489493 (B2) December Novel acyclic chiral derivatives of (see title) Saud Ibrahim Ibnu Saud Ibrahim Ibnu,
03, 2002 hibiscus acid and the process of [IN], Nair Rani Nair Rani
preparing the same Rajasekharan Rajasekharan
US6127553 (A) October 03, Convenient method for large-scale Dept Science & Tech
2000 isolation of hibiscus acid (see above) Ibnusaud Ibrahim [IN], [IN]
Rajasekharan Rani [IN]
JP2000239164 September Glycosidase Inhibitor – Kasai Takanori Kawabata Kikkoman Corp
(A) 05, 2000 Jun
US 2008/ April 24, Hydroxycitric acid compositions from Herbal compositions that comprise one or more of extracts of hydroxycitric acid, ( ) Scott Alexander Moffett Renaissance Herbs,
0095867 A1 2008 garcinia cambogia and Hibiscus sp., HCA and (+) HCA, from Garcinia cambogia and Hibiscus sabdariffa, and anthocyanins Inc.
methods of making, and therapeutic from Hibiscus sabdariffa;
uses of same
 I. Da-Costa-Rocha et al. / Food Chemistry 165 (2014) 424–443 183

and a lack of linking these to a careful profiling of the extracts.

Therefore, a better chemical profiling of the extracts, as well as

Hounan Shiyokuhin
Rajendran Kamala
Ramaswamy [IN]

its standardisation and the correlation between the chemical com-

ponents and the pharmacologic/therapeutic action will be essential
Rajendran

in future studies with this very promising traditional plant.

Kogyo KK
[IN]

Appendix A. Supplementary data

Rajendran Ramaswamy

Supplementary data associated with this article can be found,

[IN] Rajendran Kamala

in the online version, at

http://dx.doi.org/10.1016/j.foodchem.2014.
05.002.
Combinations thereof with the extracts of Hibiscus sabdariffa, and 20 other extracts or Satou Mutsuo

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