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Phytochemical screening
Phytochemicals are chemical compounds formed during the plants normal
metabolic processes. These chemicals are often referred to as Secondary
metabolites of which there are several classes including alkaloids, flavonoids,
coumarins, glycosides, polysaccharides, phenols, tannins, terpenes and terpenoids
(Okwu, 2004). In addition to these substances, plants contain other chemical
compounds. These can act as agents to prevent unconsiderable side effects of the main
active substances or to assist in the assimilation of the main substances. Plants have
an almost limitless ability to synthesize aromatic substances, mainly secondary
metabolites of which 12,000 have been isolated, a number estimated to be less than
10% of the total (Mallikharjuna et al., 2007).
Faraz et al. (2003) carried out phytochemical screening in fifty five Iranian
plants belonging to 21 families. Wang et al. (2003) isolated the active principles from
selected Chinese herbs and used Gas Chromatography-Mass Spectrometric analysis
for structure elucidation. Theeshan et al. (2005) studied the phytochemical
constituents of Cassia fistula. Falodun et al. (2006) reported the occurrence of
flavonoids, saponins, diterpenes and phorbol estersin in the aqueous and methanol
extracts of Euphorbia heterophylla. Two new homoisoflavonoids were isolated from
Caesalpinia pulcherrima by Maheswara et al. (2006). Raghavendra et al. (2006)
examined different solvent extracts of the powdered leaf of Oxalis corniculata and
reported the presence of phenols, glycosides, carbohydrates, phytosterols and tannins.
Rahaman et al. (2006) reported 3, 5, 7, 4-tetrahydroxy flavone from the leaves of
Cassia alata.
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Awoyinka et al. (2007) isolated eight bioactive compounds from the water and
ethanol extracts of dried leaf of Cnidoscolus aconitifolius. Sixty two compounds were
identified by Chowdhury et al. (2007), from the leaves of Lantana camara using
GC-MS technique. Different extracts of Semecarpus anacardium were analysed by
Mohanta et al. (2007) for their phytochemical properties. Onwukaeme et al. (2007)
detected reducing sugars, phenols, tannins and flavonoids in Pycanthus angolensis.
Uma Devi et al. (2007) carried out the phytochemical analysis in Achyranthes
bidentata. The methanol and acetone extracts of 14 plants belonging to different
families were evaluated to detect the presence of various phytochemicals by
Vaghasiya and Chanda (2007) and this study revealed the presence of tannins, cardiac
glycosides, steroids and saponins.
Arokiyaraj et al. (2008), by HPTLC finger print technique, evaluated
methanol extract of Pterocarpus santalinus leaf to detect the presence of various
phytochemicals. Ayoola et al. (2008) investigated the phytochemical components of
four medicinal plants used in the treatment of malaria in Southwestern Nigeria.
Ivana et al. (2008) used GC-MS technique to analyze the chemical composition of the
leaf extracts of Stevia rebaudiana. The extracts of two varieties of Aloe greatheadii
were examined, quantified and compared for the phytochemical contents using
GC-MS technique (Lisa et al., 2008). Suhad and Viorica (2008) conducted
quantitative analysis of the bioactive compounds (flavonoids) in Hibiscus sabdariffa.
Sathishkumar et al., (2008) screened the in vitro antioxidant properties of ethanol
extract of Canthium parviflorum leaves.
Mature and immature leaves and stems of eight plant species belonging
to 7 families were screened for alkaloids, saponins, tannins and total phenolics
contents by Abdulkabirkhan et al. (2009). Aiyelaagbe and Osamudiamen (2009)
11
screened Mangifera indica for its bioactive active compounds. Aurapa and Wandee
(2009) estimated total anthraquinone glycosides from the fresh and cooked leaves of
Senna siamea. Ayo et al. (2009) studied the phytochemicals present in the methanol
leaf extract of Cassia nigricans by GC-MS technique. Bhise and Salunkhe (2009), by
using TLC and HPTLC techniques, screened the phytochemical components from
Ashwagandha, Tulsi, Mulethi, Awala, Shatavari, Gokharu, Arjun, Giloy, Safed musli,
Kalimirchi, Haldi and Jaiphal. Qualitative analyses were carried out for detecting the
bioactive compounds present in Acalypha indica, Cassia auriculata, Eclipta alba and
Phyllanthus niruri (Chitravadivu et al., 2009).
The aerial parts of Hypericum perforatum were analysed to find out the
bioactive compounds (Gioti et al., 2009). Krishna et al. (2009) conducted preliminary
phytochemical studies and also estimated the total phenolics and flavonoid contents in
the methanol extract of Justicia gendarussa. A comparative phytochemical study
between six Malaysian medicinal plants, belonging to different families, was
carried out by Krishnaiah et al. (2009). Methanol extract of Ocimum basilicum
was analysed by TLC/HPTLC techniques to detect the phytochemicals by
Maria et al. (2009). The leaf, stem and root of Ichnocarpus frutescens were
investigated for their phytochemical properties by Mishra et al. (2009) Nadjet et al.
(2009) isolated and identified flavonoids from Chrysanthemum myconis. GC-MS
analysis of leaf extract of Cleistanthus collinus revealed the presence of a number of
phytochemicals (Parasuraman et al., 2009). Quantitative estimation of phytochemical
constituents from the wood of Caesalpinia pulcherrima was carried out using Camag
HPTLC system (Pawar et al., 2009).
Using HPTLC, Preeti et al. (2009) made qualitative and quantitative analyses
of phytochemical components in Leidium sativum. Ravirajsinh et al. (2009) conducted
12
both qualitative and quantitative studies for detecting the phytochemical constituents
found in methanol extract of Clerodendron glandulosum. Sazada et al. (2009) studied
preliminary phytochemicals found in some important medicinal and aromatic plants.
Senthil Kumar and Venkatesalu (2009), using GC-MS technique, analysed the
phytochemical contents found in the leaf of Clausena anisata. Shafaghat et al. (2009)
extracted the essential oils found in the leaf, stem and root of Chrysanthemum
parthenium by distillation technique and studied phytochemicals by GC and GC-MS
methods. The results of GC-MS analyses of Mentha arvensis from three different
locations were compared by Sharma et al. (2009). Sirohi et al. (2009) evaluated
twenty one different herbal plants and their parts for total sugar, protein, tannin and
saponin contents using aqueous, methanol and acetone extracts. Tannins, saponins,
phlobatannins,
flavonoids,
anthraquinones,
terpenoids,
steroids,
alkaloids,
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14
arboretum Sm. spp. nilagiricum. Laitonjam et al. (2011) isolated and compared the
chemical constituents present in the leaves of Cissus adnata and roots of Smilax
lanceiefolia.
15
16
constituents by Shruthi et al. (2012). Agnel Ruba et al. (2013) carried out preliminary
phytochemical analysis of Arthocnemum fruticosum leaf using five different solvents.
Packia Lincy et al. (2013) conducted the preliminary phytochemical study of
Ventilago maderaspatana whole plant, using different solvents.
Antioxidant activity
Antioxidant activities of 23 Iranian Ocimum accessions were studied by
Javanmardi et al. (2003). Chen et al. (2004) used microplated ABTS (2,2-azino-bis[3-ethylbenzothiazoline- 6-sulphonic acid]), H2O2 and HRP (Horseradish peroxide)
system for evaluating total antioxidant activity of several popular vegetables and
traditional Chinese herbals. An in vitro survey for the antioxidant potentials of three
local Mediterranean food plant extracts (Cichorium intybus, Sonchus oleraceus and
Papaver rhoeas) was made by Schaffer et al. (2005). Pourmorad et al. (2006) carried
out a comparative study on the antioxidant potentials of some selected Iranian
medicinal plant extracts. The antioxidant properties of 25 edible tropical plants were
studied by Wong et al. (2006). Badami and Channabasavaraj (2007) studied the
in vitro antioxidant activities of thirteen medicinal plants collected from Western
Ghats of India.
Ademiluyi and Oboh (2008) studied the antioxidant activity of methanol leaf
extract of Viscum album. By using linolenic acid peroxidation and DPPH methods,
Effat et al. (2008) screened thirteen medicinal plant extracts for antioxidant activity.
Janat et al. (2008) prepared the crude extracts of stem and leaves of Adenia lobata and
Desmodium ascendens, root and leaves of Glyphea brevis and Palisota hirsuta and
analyzed antioxidant potentials using DPPH assay. Moni Rani et al. (2008) evaluated
antioxidant activities of methanol extract of Ixora coccinea by DPPH free radical
scavenging activity, reducing power and total antioxidant activity assays.
17
Rahman et al. (2008) using DPPH assay, confirmed free radical scavenging activity of
methanol leaf extract of Cassia sophera. Suresh Kumar et al. (2008) surveyed
antioxidant activities of Albizzia amara, Achyranthes aspera, Cassia fistula,
C. auriculata and Datura stramonium.
Aliyu et al. (2009) evaluated antioxidant potentials of Bauhinia rufescens leaf
extract by DPPH and reducing power assays. Amal Kumar et al. (2009) evaluated the
antioxidant potentials of leaf and bark of Azadirachta indica. Bushra et al. (2009)
prepared four solvent extracts of the leaves of Terminalia arjuna and Aloe
barbadensis by adopting two extraction techniques and observed their antioxidant
activities. Devi et al. (2009) evaluated the antioxidant activity of Nephellium
lappaccum. Demiray et al. (2009) screened the leaves of Tilia argentea and Crataegi
folium and roots of Polygonum bistorta for their antioxidant properties. Jaleel (2009)
evaluated the antioxidant potentials of leaf and root tissues of Withania somnifera.
Laetitia and Christian (2009) studied antioxidant activity of Crithmum maritimum.
The methanol leaf extracts of Aegle marmelos, Abroma augusta, Lagersroemia
speciosa, Cassia fistula, Anthocephalus chinensis and Syzygium cumini were
evaluated for their antioxidant potentialities by Laizuman et al. (2009).
Ljiljana et al. (2009) studied the antioxidant activity of Hieracium pilosella extracts.
Methanol and aqueous leaf extracts of Martynia annua were evaluated by
Nagda et al. (2009), for their antioxidant abilities, using various in vitro systems like
reducing power assay, DPPH radical scavenging activity, nitric oxide scavenging
activity, H2O2 radical scavenging activity, superoxide radical scavenging assay and
hydroxyl radical scavenging activity. Nazin and Hasan Nur (2009) used the methanol
leaf and flower extracts of Lippia alba to determine antioxidant activities by DPPH
and reducing power assay. A comparative study on the antioxidant potentials of four
18
19
evaluated for their antioxidant activities by Imaga et al. (2010). Patel et al. (2010)
studied the total phenols, flavonoids and radical scavenging activities of certain
medicinal plants in Gujarat region. Paula et al. (2010) evaluated antioxidant
properties of Jacaranda puberula leaf extract. Pavithra et al. (2010) estimated
antioxidant activity of methanol extract of Evolvulus nummularius. The crude
methanol extracts of four Philippine medicinal plants viz., Brucea amarissima, Intsia
bijuga, Laportea meyeniana and Pipturus arborescens were examined by Peteros and
Uy (2010), for their antioxidant activities. Praveen Kumar et al. (2010) screened the
leaf extract of Vitex negundo for its antioxidant activity. Rekha et al. (2010) screened
the antioxidant activity of dry soup mix extracts containing Anethum sowa leaves.
The antioxidant activities of aqueous and methanol extracts of Erythrina
indica leaves were tested by DPPH, nitric oxide radical scavenging activity under in
vitro condition by Sakat and Juvekar (2010). Shajiselvin and Kottai Muthu (2010)
examined in vitro antioxidant potentials of various extracts of whole plant of Borreria
hispida by DPPH radical scavenging activity, Superoxide anion scavenging activity
and Iron chelating activity. The antioxidant capacity and total phenolic contents
present in the acetone and methanol extracts of different parts of Melothria
maderaspatana were evaluated by Sowndharajan et al. (2010).
Antioxidant potentials of methanol leaf extracts of Caesalpinia coriaria,
Flacourtia cataphracta, Hiptage benghalensis, Sesbania sesban, Persea macrophylla
and tubers of Gloriosa superba were analysed by Amutha and Shanthi (2011).
Gokhan et al. (2011) examined in vitro antioxidant activity and fatty acid composition
of Centaurea urvillei. Mishra et al. (2011) screened the extracts of ten Indian
medicinal plant species for their antioxidant activities. Antioxidant potentials of
Gynura procumbens, Achyranthes aspera and Polygonum tomentosum were studied
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by Mon et al. (2011). The chloroform and methanol leaf extracts of 124 Egyptian
plant species belonging to 56 families were investigated and compared by
Moussa et al. (2011), for their antioxidant potentials.
Naveen Prasad et al. (2011) screened antioxidant potentials of some common
plants. Nithya and Balakrishnan (2011) screened 13 important medicinal plants for
their antioxidant properties. Panda et al. (2011) screened the in vitro antioxidant
activity of aerial parts of Cocculus hirsutus. Patil and Patil (2011) studied the in vitro
antioxidant activity of seeds of blue and white flowered varieties of Clitoria ternatea.
Using some in vitro antioxidant models like DPPH radical scavenging activity,
superoxide radical scavenging activity, ferric reducing power and hydrogen peroxide
scavenging activity, Priya et al. (2011) studied the antioxidant activity of aqueous,
ethyl acetate, ethanol and methanol extracts of Caralluma fimbriata. Sathisha et al.
(2011) determined antioxidant potentials of Curcuma longa, Coffea arabica, Tribulus
terrestris, Moniera cuneleolia and Trigonella foenumgraecum using various in vitro
assays. Antioxidant potentials of root, stem, leaf and tuber of Coleus forskohlii was
analysed by Selima et al. (2011). Sengul et al. (2011) analysed the antioxidant
activities of Artemisia santonicum and Saponaria officinalis, the native Turkish
medicinal and aromatic plants. Stankovic et al. (2011) derived twenty different
extracts from stem, leaf and flower of Teucrium montanum and determined their
antioxidant activities. . Sudha et al. (2011) screened the in vitro antioxidant activity of
fresh fruit of Solanum muricatum. Venkateshwarlu et al. (2011) studied the in vitro
and in vivo antioxidant activity of methanol extract of Solena amplexicaulis
Alsabri et al. (2012) reported the in vitro antioxidant activities of aerial parts
of Cistus incanus, C. parviflorus, Helianthemum lippii, Arbutus pavarii, Capparis
spinosa,
Rhamnus
alaternus,
Quercus
21
coccifera
and
Globularia
arabica.
22
scavenging activity. Balamurugan et al. (2013) studied the in vitro antioxidant activity
of Melastoma malabathricum.
Anticancer activity
Cancer, the second leading cause of death worldwide next to cardiovascular
diseases, is a group of more than 100 different diseases, characterized by uncontrolled
cellular growth, local tissue invasion and distant metastases (Dashroa et al., 2010).
Cancer is the cause of more than six million deaths each year in the world. In 2001,
about 1,268,000 new cancer cases and 553,400 deaths were reported in the United
States (Izevbigie, 2003). It can be treated with surgery, radiation, chemotherapy,
hormone therapy and biological therapy. Chemotherapy is still a major challenge to
the cancer patients because such highly potent drug can be toxic and less than 1% of
injected drug molecules can reach their target cells whereas the rest may damage
healthy cells and tissue especially bone marrow, epithelial tissues, reticulo-endothelial
system and gonads (Kathiriya et al., 2010). Since medieval times, plants have been
the source of medicines for the treatment of diseases. Regardless of the availability of
a wealth of synthetic drugs, plants remain-even in the 21st century-an integral part of
the health care in different countries, especially the developing ones. In the late 90s,
the WHO stated that a big percentage of the worlds population depends on plant
based therapies to cover the needs of the primary health care (WHO, 1999; Dikshit
et al., 2004). The areas of cancer and infectious diseases have a leading position in
utilization of medicinal plants as a source of drug discovery. Among FDA approved
anticancer and antiinfectious preparations drugs of natural origin have a share of 60%
and 75% respectively (Newman et al., 2003). It is worthy to mention the vivid current
interest in discovery of natural drugs for cancer treatment and chemoprevention
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(Kucuk, 2002; Balunas and Kinghorn, 2005). Huge number of plant species is
screened and bioassayed for this purpose worldwide (Richardson, 2001).
Another important addition to the anticancer drug armamentarium is the class
of clinically-active agents derived from camptothecin, which is isolated from the
Chinese ornamental tree Camptotheca acuminata Decne (Nyssaceae), known in China
as the tree of joy. The derivatives of Camptothecin, Topotecin and Irinotecan, were
originally developed by Japanese company, YAKUH Honsha, are now in clinical use.
These are used for the treatment of ovarian lung cancer and colorectal cancers (Cragg
and Newman, 2004/Rev.2006).
Other plant derived agents in clinical use are homoharringtonine, isolated
from the Chinese tree Cephalotaxus harringtonia var. drupacea and elliptinium a
derivative of the ellipticine, isolated from species of several genera of the family
Apocynaceae, including Bleekeria vitensis have reputed anticancer properties (Cragg
and Newman, 2004/Rev.2006).
Some medicinal plants have been found effective in various types of
malignant (cancer) and benign tumors of humans and experimental animals. These
include: Agrimonia pilosa in sarcoma-180; Ailanthus altissima in intestinal cancer,
sarcoma-180, sarcoma-37 and leukaemia-16; Akebia quinata in sarcoma-180 and
sarcoma-37; Chelidonium jajus var. asiaticum in stomach cancer; Chimaphila
umbellata in breast tumor; Coix lachrymahjobi
sarcoma; Fritillaria thunbergii in tumors of the throat, chest, neck and breast; Larrea
tridentata in various cancers, especially leukaemia; Lonicera japonica in ascites
carcinoma and sarcoma-180; Nidus vespae in gastric and liver cancer; Oldenlandia
diffusa in leukaemia, Yoshidas sarcoma, sarcoma-180 and Ehrlichs ascites sarcoma
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antitumor activity against B16F10 melanoma cell line by trypan blue exclusion assay
for cell viability and found out that 70% methanolic extract of Foeniculum vulgare
showed good antitumor activity and 50% methanolic extract of Helicteres isora
exhibited good antitumor activity. They concluded that Foeniculum vulgare and
Helicetres isora could be considered as normal resource of antitumor agents.
The methanol extract of Zingiber officinalis was evaluated for anticancer activity
against Ehrlich ascites carcinoma (Hanafy, 2009). Some Egyptian medicinal plants
such as leaves of Luffa aegyptiaca, Solenostemma argha, Cassia italica, Ocimum
basillicum, Colocasia antiguorum, Beta vulgaris and fruits of Capsicum frutescens
were evaluated for in vitro anticancer activity against Acute Myeloid Leukemia
(AML) and Acute Lymphocyte Leukemia (ALL) and in vivo anticancer activity
against Ehrlich ascites carcinoma (Nasar-Allah et al., 2009). The anticancer activity
of hydro-distilled essential oils obtained from flowers of Matricaria chamomilla and
the dried leaves of Marjorana hortensis against leukaemia HL-60 and NB 4 cells
were tested in vitro by Romeilah (2009), and the results obtained by him proved that
the essential oils of above plants could be used as a potential natural antioxidant and
anticancer agents.
. Bala et al. (2010) reported the anticancer activity of Cleome gynandra in
Swiss albino mice against Ehrlich ascites carcinoma cell line. Forty four extracts from
sixteen plants, used traditionally as anticancer agents, were evaluated in vitro for their
antiproliferative activity against Hep-2, MCF-7 and Vero cell lines. Twenty of these
extracts demonstrated significant antiproliferative activity against one or more of the
cell lines. Among the tested extracts, methanol fractions of Ononis hirta aerial parts
and Irula viscosa flowers were the most active fractions against MCF-7 cells, (Talib
and Mahasneh, 2010).
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Anbu et al. (2011) studied the anticancer activity of petroleum ether extract of
Abrus precatorius seed against Ehrlich ascites carcinoma in mice. Jeevanantham et al.
(2011) studied the anticancer activity of methanolic extract of aerial part of
Momordica cymbalaria against Ehrlich ascites carcinoma in mice. The ethanol
extracts of Eugenia flocossa and Eugenia singampattiana leaves were evaluated for
anticancer activity against Dalton Ascites Lymphoma in Swiss albino mice (Kala et
al., 2011). Mahadik (2011) studied the antitumor and antioxidant activity of ethanolic
extract of Vitis vinifera leaves against Ehrlich ascites carcinoma induced Swiss albino
mice on dose dependent manner. The ethanolic extract of leaves of Butea
monosperma was evaluated for its anticancer activity against Ehrlich ascites
carcinoma in Swiss albino mice (Rekha and Jayakar, 2011). The methanol extract of
Cucurbita maxima aerial parts was evaluated for its antitumor activity against Ehrlich
ascites carcinoma model in mice (Saha et al., 2011).
Islam et al. (2012) studied the anticancer activity of petroleum ether extracts
of Eucalyptus camaldulensis against Ehrlich ascites carcinoma. Anticancer activity of
methanolic flower extract of Tecamo stans was evaluated using both in vivo and in
vitro methods (Kameshwaran et al., 2012). Kota et al. (2012) reported the anticancer
activity of various concentrations of ethanolic extract of the leaves of Achyranthes
bidentata against DAL and EAL cell lines. Lalee et al. (2012) reported the anticancer
activity of ethanolic and aqueous extracts of Aerva sanguinolenta against Ehrlich
ascites carcinoma cells induced Swiss mice. Marappan and Subramaniyan (2012)
reported the antitumor activity of methanolic extract of Cynodon dactylon leaves
against Ehrlich ascites carcinoma in mice. The ethanol extract of Madhuca longifolia
leaves were evaluated for its anticancer activity Ehrlich ascites carcinoma in mice
(Sangameswaran et al., 2012). The acetone and ethanol extracts from the leaves of
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Adina cordifolia were evaluated for anticancer activity against Ehrlich ascites
carcinoma bearing Swiss albino mice (Sangameswaran and Saluja, 2012).
The ethanol extracts of P. chinensis, P. rosmarinifolia and Polygala javana whole
plants were evaluated for anticancer activity against DAL bearing mice (Alagammal
et al., 2012 a, b; 2013).
Antidiabetic activity
Diabetes mellitus is a clinical syndrome characterized by inappropriate
hyperglycemia caused by a relative or absolute deficiency of insulin or by a resistance
to the action of insulin at cellular level. It is the most common endocrine disorder,
affecting 16 million individuals in the United States and more than 150 million
worldwide. Diabetes mellitus (DM) is the condition arising due to abnormal
metabolism of carbohydrate, proteins and fats. It is caused by insulin deficiency, often
combined with insulin resistance. This disorder occurs worldwide and its occurrence
is increasing quickly in most of the countries. Various complications develop as a
consequence of the metabolic derangement in diabetes type-2. The treatment of DM is
based on parental insulin and oral anti-diabetic drugs. Oral hypoglycemic agents,
currently used, have serious side effects; hence there is a need to search for newer
anti-diabetic agents having high therapeutic efficacy with minimum side effects. This
may be fulfiled by treating DM with plant derived anti-diabetic agents.
Diabetes mellitus has been known since ages and the sweetness of diabetic
urine has been mentioned in Ayurveda by Sushruta. Its pharmacotherapy however is
over 80 years old. Diabetes is a chronic disease affecting around 2-3% of the
population worldwide. Unfortunately, after the introduction of sulfonylurea and
metformin about 50 years back, no major lead has been obtained in this direction of
finding a proper drug for diabetes. Plant materials which are being used as traditional
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medicine to treat diabetes are considered to be one of the best sources for new drugs
or a lead to make new drugs. Plant extracts or different folk plant preparations are
being prescribed by the traditional practitioners and are accepted by the users for
diabetes, like for any other disease, in many countries especially in third world
countries. Now-a-days, more than 400 plants are being used in different forms for
hypoglycemic effects. Therefore, a proper scientific evaluation and screening of
plants by pharmacological tests followed by chemical investigations is necessary.
Diabetes is a disorder of metabolism, the way our body uses digested food for
growth and energy. Most of the food we eat is broken down into glucose, the form of
sugar in the blood. Glucose is the main source of fuel for the body. After digestion,
glucose passes into the bloodstream, where it is used by the cells for growth and
energy. For glucose to get into cells, insulin is essential. Insulin is a hormone
produced by pancreas, the large gland behind the stomach. When we eat, the pancreas
automatically produces the right amount of insulin to move glucose from blood into
our cells. In people with diabetes, however, the pancreas either produces little or no
insulin, or the cells do not respond appropriately to the insulin that is produced.
Glucose built up in the blood, overflows into the urine, and passes out of the body in
the urine. Thus, the body loses its main source of fuel even though the blood contains
a large amount of glucose.
The first stage in type-2 diabetes is the condition called insulin resistance;
although insulin can attach normally to receptors on liver and muscle cells, certain
mechanisms prevent insulin from moving glucose into these cells where it can be
used. Most type-2 diabetics produce variable, even normal or high amounts of insulin,
and in the beginning, this amount is usually sufficient to overcome such resistance.
Over time, the pancreas becomes unable to produce enough insulin to overcome
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resistance. In type-2 diabetes, the initial effect of this stage is usually an abnormal rise
in blood sugar right after a meal (called postprandial hyperglycemia). This effect is
now believed to be particularly damaging to the body. Eventually, the cycle of
elevated glucose further impairs and possibly destroys beta cells, thereby stopping
insulin production completely and causing full-down diabetes. This is made evident
by fasting hyperglycemia, in which elevated glucose levels are present most of the
time.
Several medicinal plants have been used as dietary adjunct and in the
treatment of numerous diseases without proper knowledge of their function. Although
phytotherapy is continued to be used in several countries, a few plants have received
scientific or medical scrutiny. Moreover, a large number of medicinal plants possess
some degree of toxicity. For example, Marles and Farnsworth (1994) reported that
about one third of medicinal plants used in the treatment of diabetes are considered to
be toxic. Numerous animal studies have shown that the ethanol leaf and flower
extracts of Vinca rosea and Ficus racemosa lower the blood glucose levels (Ghosh
and Gupta, 1980).
The extract of Achyranthes aspera produced a significant dose-related
hypoglycemic effect in normoglycemic and alloxan induced diabetic rabbits.
The water and methanol extracts of this plant also decreased blood sugar levels in
these animals. This plant might be providing certain necessary elements like calcium,
zinc, magnesium, manganese and copper to the beta-cells (Akhtar and Iqbal, 1991).
Oral administration of Asteracantha longifolia extract significantly improved glucose
tolerance in healthy human and diabetic patients (Fernando et al., 1991).
S-allyl cysteine sulphoxide (SACS), a sulphur-containing amino acid of Allium
sativum, is the precursor of allicin and garlic oil. SACS had been found to show a
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extracts of Beta vulgaris var. cicla inhibited the increase in the non-enzymatic
glycosylation of skin proteins and blood glucose. These results demonstrated the
ability of this plant in preventing or at least retarding the development of some
diabetic complications (Tunali et al., 1998). Oral administration of with aqueous
extract of Tinospora cordifolia roots produced a significant decrease in glycemia and
brain lipids in alloxan induced diabetic rats (Stanley et al., 1999). The ethanol bark
and leaf extracts of Thespesia populnea were investigated for hypoglycemic effects in
streptozotocin induced diabetic rats and this was compared with glibenclamide,
a standard hypoglycemic agent; also measured the lipid peroxide, superoxide
dismutase and catalase enzymes level in the kidney of the animal. The root and aerial
parts extracts of Sida cordifolia showed hypoglycemic activity. Moreover, the
methanol root extract was found to possess significant hypoglycemic activity.
Several plant species such as Opuntia streptacantha, Trigonella foenum-graecum,
Memordica charantia, Ficus benghalensis, Polygala senega, Gymnema sylvestre,
Allium sativum, Citrullus colocynthis, and Aloe barbadensis were reported to possess
hypoglycemic properties (Atta-Ur-Rahman and Zaman, 1989; Ziyyat et al., 1997;
Bnouham et al., 2002).
Chattapadhyay (1999) reported that the leaf extract of Azadirachta indica
significantly blocked the inhibitory effect of serotonin on insulin secretion mediated
by glucose. Moreover, A. indica leaf extract was found to have the most potent blood
sugar lowering property followed by Catharanthus roseus, Gymnema sylvestre and
Ocimum sanctum (Chattapadhyay, 1993). Uma Devi et al. (2006) reported the
anti-diabetic and hyperlipidaemic effects of Cassia auriculata in alloxan induced
diabetic rats. Effect of Ficus carica leaf decoction, as a supplement to breakfast, was
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The methanol
leaf extract of Costus pictus was investigated for its antidiabetic effect in wistar albino
rats by Jothivel et al. (2007).
extract
of
Bougainvillea
glabra
on
alloxan
induced
diabetic
rats.
Murugan et al. (2009) studied the antidiabetic and hypolipidaemic activity of Mucuna
pruriens leaves in alloxan induced diabetic rats. The antidiabetic effect of Artemisia
judaica extract on alloxan induced diabetic rats was studied by Nofal et al. (2009).
Rajalakshmi et al. (2009) studied the anidiabetic properties of various extracts
(hexane, ethyl acetate and methonal) of Tinospora cordifolia against streptozotocininduced diabetic rats.
Gurjar et al. (2010) reported the antidiabetic activity of Anthocephalus
cadamba bark in alloxan induced diabetic rats. Kumar et al. (2010) studied the
antidiabetic activity of Euphorbia hitra stem, leaf and flower extracts against normal
and streptozotocin-induced diabetic rats. Sharma et al. (2010) investigated the
antidiabetic activity of Ficus glomerata in alloxan induced diabetic rats.
Maruthupandian and Mohan (2011) studied the antidiabetic effects of ethanol wood
33
and bark extracts and combined wood and bark extract of Pterocarpus marsupium in
wistar albino rats. The ethanol leaf extract of Senna auriculata was investigated for its
antidiabetic
and
antihyperlipidaemic
activities
in
wistar
albino
rats
by
are available today to cure liver diseases. Therefore it is not surprising that a
considerable interest has been taken by researchers to examine their numerous
traditional plant remedies, used for treating liver disorders. In recent years,
investigations have been carried out to provide experimental evidences confirming
that many of these plants do have hepatoprotective properties (Sharma et al., 2003).
Mondal et al. (2005) reported that methanol extract of Diospyros malabarica
bark had a potent hepatoprotective activity against carbon tetrachloride induced liver
damage in rats. Dash et al. (2007) reported that chloroform and methanol entire plant
extracts of Ichnocarpus frutescens served as effective hepatoprotective agents in
paracetamol induced liver damage in rats. Iniaghe et al. (2008) reported that the
aqueous leaf extract of Acalypha racemosa served as an effective hepatoprotective
agent against CCl4 induced liver damage. Abdul-Razik et al. (2009) studied the effect
of ethyl acetate and n-butanol extracts and volatile oil of Juncus subulatus, in ethanolinduced hepatic injury in female rats and showed that all extracts served as potential
hepatoprotective agents. Jain et al. (2009) compared the hepatoprotective potentials
of ethanol and aqueous extracts of Amorphophallus campanulatus tubers using carbon
tetrachloride induced hepatic damage in rats. This study revealed that the ethanol
extract was more hepatoprotective than the aqueous extract.
Aqueous extracts of seeds of Areca catechu and nutgalls of Quercus infectoria
were investigated for their hepatoprotective activities against liver injury induced
by carbon tetrachloride (CCl4) in rats (Pithayanukul et al., 2009). Tiwari and Khosa
(2009) evaluated the hepatoprotective effects of aqueous and methanol extracts of
flower heads of Sphaeranthus indicus, a traditional Indian medicinal plant commonly
used to nourish and improve the liver conditions, on acetaminophen induced
hepatotoxicity in rats. Hepatoprotective activity of water and alcoholic extracts of
35
Antifertility activity
Recently, efforts are being made to explore the hidden wealth of medicinal
plants for contraceptive use. With the exciting prospects of gene therapy, herbal
medicines remain one of the commonest forms of therapy available for much of
worlds population to maintain health and to treat diseases.
There has been a steady accumulation of information regarding the screening
of plants having anti-fertility efficacy (Hanshaw, 1953; Chopra et al., 1956;
Chopra et al., 1958; Casey, 1960; Bhakuni et al., 1969 and Farnsworth et al., 1975a;
1975b). The folklore information and the ancient literature about the herbals can help
antifertility program. In the recent past, various researchers have done a number of
works on plants and isolated, identified and evaluated active principles from different
parts of plants such as root, stem, leaves, flowers, seeds or stem barks. These reports
have been exhaustively reviewed by Orzechowski (1972); Brondegaard (1973);
Kholkute et al. (1976); Kamboj and Dhawan (1982); Zhu (1982) and Satyawati
(1983). A literature survey for the period of past 25 years (1980-2005) revealed that
there are about 105 plants possessing antifertility activity in males (Gupta and
Sharma, 2006).
Hadley et al. (1981) isolated gossypol, a yellow phenolic compound from
cotton seed oil and confirmed it as a male contraceptive drug. They found that
gossypol treatment reduced the level of serum testosterone and luteinizing hormone
levels. Gossypol acts directly on testes and induces azoospermia or oligospermia
(Xue, 1980; Xue, 1985 and Taitzoglou et al., 1999). A multi-glycoside extracted
from the root xylem of Tripterygium wilfordii was shown to have a reversible
anti-fertility action in male rats by Qian (1987) using Task-Force supported study.
37
Its antifertility activity was well documented in rats, mice and human (Qian, 1986 and
Qian et al., 1995).
Choudhary et al. (1991) studied antifertility effect of ethanol leaf extracts of
Alstonia scholaris, Cleistanthus collinus and Terminalia bellerica and root extract of
Murraya paniculata in male albino rats. Lohiya and Goyal (1992) administered
chloroform extract of Carica papaya seeds and showed a decrease in sperm count
and the suppression of caudal epididymal sperm motility in rats. They also suggested
that contraceptive effects were mainly post testicular in nature and without adverse
influence on the lipids profile of animals. Verma and Chinoy (2001) reported
that the Carica papaya seed extract altered caudal epididymal micro-environment.
Manivannan et al. (2004) observed the ultra structural changes in the testis and
epididymis of rats following treatment with the chloroform extracts of the Carica
papaya seeds. Dehghan et al. (2006) reported that the Azadirachta indica seed extract
altered vas deferens and epididymal milieu and affected the spermatozoa.
Thus the extract served as a potential anti-fertility agent. Sakthidevi et al. (2012)
reported the antifertility activity of whole plant extract of Polygala javana on male
albino rats. Thanga Krishna Kumari et al. (2012) studied the antifertility activity of
whole plant extract of Sarcostemma secamone on male albino rats.
Antiinflammatory activity
The term rheumatism embraces a variety of disorders that have in common
pain and stiffness referable to the musculoskeletal system. When such symptoms are
due to abnormality of the joint itself, the condition can be classified as arthritis.
Non-articular rheumatism includes those conditions in which the symptoms are
produced not by pathologic changes in the joints proper, but in the structures
contiguous to, or related to the joints. Although arthritis occurs in a number of
38
different forms, there are essentially two fundamental pathological processes that
affect the joints viz., inflammation, which may be exudative or proliferative or a
combination of each and degenerative changes, which are primarily dependent on the
limited capacity of articular cartilage to repair itself (Loeb, 1971). The target should
be to discover plant based new drugs which may provide therapeutic cure and would
be free from undesirable effect as well as economical, which would be accepted by
the developing nations like India (Huang, 1999).
A systematic study of antiinflammatory effects of Indian medicinal plants
began by Gujral and his associates. They screened a number of plants for their
antiarthritic effects. Subsequently, various workers from different laboratories in India
made significant contributions. In the sixties, formaldehyde induced arthritis and
croton oil induced granuloma pouch in rats were mainly used as the experimental
models of inflammation. Later, with the introduction of better and more specific
models of experimental inflammation like carrageenan induced paw edema in rats,
cotton pellet induced granuloma in rats, Freuds complete adjuvant induced arthritis
etc., and workers in different laboratories tested their drugs with the help of the later
models. Scientists in Central drugs Research Institute, Lucknow studied nearly two
thousand Indian medicinal plants for their various pharmacological properties
(Chatterjee and Pal, 1984; Shah et al., 2006). The greatest disadvantage in the
presently available potent synthetic antiinflammatory drugs lies in their toxicity and
reappearance of symptoms after discontinuation. Therefore, the search for their
antiinflammatory activity (AIA) is an unending problem (Chawla et al., 1987 and
Shen, 1981).
The oleoresin fraction of Commiphora mukul possessed significant
anti-arthritic and antiinflammatory activities. A steroidal compound isolated from
39
C. mukul displayed a significant dose dependent activity which was more potent than
the resin fraction of C. mukul. A comparison between the antiinflammatory activities
of petroleum ether extract of C. mukul with standard drugs showed that the
former to be more effective. The ethyl acetate-soluble portion of the resin
(guggalipid), on fractionation, revealed that the acidic portion displayed a significant
anti-inflammatory activity (Satyavati et al., 1969).
Hye and Gafur (1975) observed the antiinflammatory activity of a flavanoid
glycoside, chrysoeriol 7-0--D glucopyranosyl-D-apiofuranoside, isolated from
Dalbergia volubilis. Magniferin, a xanthone C-glucoside isolated from Canscora
decusssata, mangostin and related compounds isolated from Garcinia mangostana
by Shankaranarayanan et al. (1979) and xanthones isolated from Calophyllum
inophyllum and Meusa ferrea by Gopalakrishnan et al. (1980) were shown to have
antiinflammatory activities. Swarnalakshmi et al. (1981) isolated epicatechin from
seed coat of Anacardium occidentale and showed it an antiinflammatory agent, as
effective as phenylbutazone, using various test models. Bergenin was isolated from
the pods of Peltophorum pterocarpum and was found to be equipmental to
phenylbutazone against carrageenan induced edema in rats (Menon et al., 1982).
A flavonoid isolated from Hedychium spicatum showed a significant activity
with less ulcerogenic index than phenylbutazone (Srimal et al., 1984). The petroleum
ether extract of Curcuma longa rhizomes showed significant antiinflammatory
activity and was effective in delayed hypersensitivity. Curcumin, chemically known
as diferuloyl methane, a constituent of turmeric, was shown to be effective by Srimal
and Dhawan, (1973). It is as potent as phenylbutazone in the carrageenan induced
edema test but half as potent in chronic tests. Srivastava and Srimal (1985) showed
that curcumin was found to be a stabilizer of lysosomal membrane (more potent than
40
3-0-acetylpadmatin
along
with
sesquiterpene
lactone
inuvisolide;
41
oleanene and ursene series were found to be active against carrageenan induced
edema, formaldehyde induced edema and formaldehyde induced arthritis in rats.
Bhargava et al. (1970) suggested that the antiinflammatory activity of the
triterpenoids of the oleanene series, with the polarity of compounds, were enhanced
by a number of hydroxyl groups in the molecule. Atal et al. (1980) observed the
antiinflammatory and antiarthritic activities of the oleogum of Boswellia serrata
in controlled clinical trials in arthritic patients. Its activity might be due to the
boswellic acids present in the oleogum. Two new triterpene saponins having
phospholipase-D inhibitory activity were isolated from extract of the leaves of
Myrsine australis. Oleanolic acid 3--glucoside isolated from the seeds of Randia
dumetorum showed a significant AIA in the exudative and proliferative phases of
inflammation in rats (Ghosh et al., 1983). Singh et al. (1970) isolated -sitosterol
from Cyperus rotendus and showed it a potent antiinflammatory agent against
carrageenan and cotton pellet-induced edema in rats. Gupta et al. (1971) compared the
antipyretic activities of hydrocortisone and oxyphenbutazone. -spinasterol obtained
from the stem-bark of Symplocos spicata showed a significant activity against acute
inflammation induced by carrageenan in rats.
Tylophorine, an alkaloid isolated from Tylophora indica, apart from
the
anaphylactic
and
immunocytoadherence
actions
significantly
inhibited
in rats (Ghosh and Kumar, 1983). Radiological findings by Hazeena Begum and
Sadique (1988) evidently supported the anti-arthritic property of Withania somnifera.
Handa et al. (1992) cited that species of 96 genera belonging to 56 families
possessed antiinflammatory activities. The triterpenes, alpha-amyrin acetate,
beta-amyrin acetate and lupeol acetate of Alstonia boonei were evaluated for their
antiarthritic activities in rats by Kweifio-Okai and Carroll (1992 and 1993).
The anti-inflammatory activity of the aqueous extract of Bridelia ferrugiana stem
bark was evaluated using carrageenan induced paw edema in rats and mice
(Olajide et al., 1999). Suleyman et al. (1999) studied the antiinflammatory activity of
the aqueous extracts of Rumex patientia roots using carrageenan, histamine, dextrane,
serotonin and formaldehyde induced edema tests. The alcoholic extract of
Clerodendron serratum roots was evaluated for its antiinflammatory activity using
animal models (Narayanan et al., 1999).
The analgesic and antiinflammatory properties of lyophilized aqueous extract
of Opuntia dillenii fruits were demonstrated by Loro et al. (1999) in rats and mice.
The aqueous and alcoholic extracts of Tecoma sambucifolia flowers and pods were
analysed to determine their antiinflammatory activities using carrageenan induced
edema test (Alguacil et al., 2000). Stephania tetrandrae, a traditional medicinal plant
to treat inflammatory diseases in Korea, possessed two major alkaloids namely
fangchinoline and tetraandrine. Choi et al. (2000) isolated fangchinoline and
tetraandrine and showed their anti-inflammatory potentialities of using animal
models.
The dried leaf methanol extract of Alstonia macrophylla was investigated
for its antiinflammatory activity in carrageenan induced rat paw edema
(Arunachalam et al., 2002). Antiinflammatory activity of ethanol extract of Bouchea
43
podophyllum, leaves of Hamelia patens and Piper amalago and barks of Bursera
simaruba were evaluated for their antiinflammatory activities by Sosa et al. (2002).
Mitragyna
treat
ciliata,
inflammation,
widely
hypertension,
used
headache,
traditional
medicinal
rheumatism,
plant
gonorrhoea
to
and
44
petasites was assessed by Panthong et al. (2003) for antiinflammatory and anti-pyretic
activities using experimental animals. They found that the extract possessed moderate
inhibitory activity on acute phase of inflammation. The methanol-water extract
of Barleria prionitis was evaluated for its anti-inflammatory and antiarthritic activities
against different acute and chronic animal test models (Singh et al., 2003).
The antiinflammatory activity of the alcoholic stem extract of Tabenaemontana
pandacaqui was studied using carrageenan induced rat paw edema (Taesotikul et al.,
2003). Trongsakul et al. (2003) conducted pharmacological studies using
experimental animal models and evaluated the analgesic, antipyretic and
antiinflammatory activities of hexane extract of the dried stem of
Diospyros
variegata.
Deb et al. (2007) investigated the antiinflammatory activity of the aqueous
leaf extract of Eucalyptus globulus in carrageenan induced paw edema and cotton
pellet granuloma technique in albino rats. The petroleum ether, ethyl acetate, ethanol
and aqueous leaf extracts of Calotropis gigantea were screened by Patil et al. (2007)
for their antiarthritic activities in albino rats. The petroleum ether, chloroform,
methanol and aqueous extracts of Sesbania sesban leaves were investigated for their
antiinflammatory activities in albino rats (Tatiya et al., 2007). The bark extract of
xeromphis spinosa using a mixture of equal proportions of petroleum ether, ethyl
acetate and methanol was analysed for its antiinflammatory activity by
Das et al. (2009). It exhibited a significant result at an oral dose of 200 and
400 mg/kg body weight.
The ethyl acetate and methanol extracts of Syzygium cumini leaves were
investigated for their antiinflammatory activities in carrageenan induced paw edema
in wistar rats (Jain et al., 2010). Parthasarathy (2010) using carrageenan induced paw
45
edema albino rats, studied the antiinflammatory activity of whole plant methanol
extract of Spermacoce hispida. Rajesh et al. (2010) investigated the antiinflammatory
activity of the petroleum ether, chloroform, ethyl acetate, ethanol and water leaf
extracts of Salvadora persica in albino rats. The methanol root bark and stem bark
extracts of Pittosporum tetraspermum were investigated for their antiinflammatory
activities by Rosakutty et al. (2010) in carrageenan induced paw edema in albino rats.
Sutha et al, (2011) screened the ethanol leaf extract of Alstonia venenata for its
antiinflammatory activity in carrageenan induced paw edema in albino rats.
The whole plant ethanol extracts of Polygala rosmarinifolia, P.javana and
P. chinensis were evaluated for their antiinflammatory activities using carrageenan
induced paw edema by Alagammal et al. (2012e, f, g). Balamurugan et al. (2012)
reported the anti-inflammatory activity of Polycarpea corymbosa against carrageenan
induced paw edema. Kalpanadevi et al. (2012) studied the ethanol extract of Entada
pursaetha seed for its antiinflammatory activity in carrageenan induced paw edema in
albino rats. The ethanol leaf and stem bark extracts of Naringi crenulata were
evaluated for their antiinflammatory activities using carrageenan induced paw edema
by Sarada et al. (2012). Muthulakshmi et al. (2012) studied the antiinflammatory
activity of ethanol extract of leaf and bark of Feronia elephantum against carrageenan
induced paw edema. Thanga Krishna Kumari et al. (2012a, b) reported the
antiinflammatory activity of ethanol extract of Sarcostemma secamone and Canscora
perfoliata whole plant against carrageenan induced paw edema.
46