Journal of Ethnopharmacology 139 (2012) 214–220

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Journal of Ethnopharmacology
journal homepage: www.elsevier.com/locate/jethpharm

Trillin, a steroidal saponin isolated from the rhizomes of Dioscorea nipponica,

exerts protective effects against hyperlipidemia and oxidative stress
Tiejie Wang a,d , Roy C.Y. Choi d , Jun Li a , Cathy W.C. Bi d , Wei Ran c , Xiaohui Chen b ,
Tina T.X. Dong d , Kaishun Bi b , Karl W.K. Tsim d,∗
a
Shenzhen Municipal Institute for Drug Control, Shenzhen 518029, China
b
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 10016, China
c
Center for Drug Re-evaluation, SFDA, National Center for ADR Monitoring, Beijing 100045, China
d
Division of Life Science and Center for Chinese Medicine, The Hong Kong University of Science and Technology, Clear Water Bay Road, Hong Kong, China

a r t i c l e i n f o a b s t r a c t

Article history: Ethnopharmacological evidence: Numerous efforts have been conducted in searching for effective agents
Received 10 June 2011 against cardiovascular diseases, in particular from herbal medicines. The rhizome of Dioscorea nipponica
Received in revised form 27 October 2011 (Dioscoreae Nipponicae Rhizoma) is a traditional Chinese herb being prescribed to improve the blood
Accepted 1 November 2011
circulation. Here, we identified a steroidal saponin trillin from Dioscorea nipponica, which showed robust
Available online 12 November 2011
anti-hyperlipidemic effects.
Materials and methods: Rats were induced for hyperlipidemia and subjected to the drug treatment. The
Keywords:
anti-hyperlipidemic effects of trillin were evaluated by different biochemical assays.
Trillin
Cardiovascular
Results: In hyperlipidemic rat model, fed with high-fat diet, the blood levels of cholesterol, triglyceride,
Hyperlipidemic low density lipoprotein (LDL) and high density lipoprotein (HDL) were increased. The intra-peritoneal
Anti-oxidative administration of trillin into those rats significantly improved the bleeding and blood coagulation time,
Dioscorea nipponica Makino and in parallel the treatment restored the levels of cholesterol, glyceride, LDL and HDL back to the normal
condition. In addition, the administration of trillin in rats exerted beneficial effects in improving the levels
of lipid peroxidation and superoxide dismutase activity.
Conclusion: This was the first time to reveal the anti-hyperlipidemic and anti-oxidative effects of trillin.
These results would be important in developing food supplements for health improvements and thera-
peutic drugs against hyperlipidemia and cardiovascular diseases in future.
© 2011 Elsevier Ireland Ltd. All rights reserved.

1. Introduction
Mortality from cardiovascular diseases is the second leading
cause of death worldwide (Ohlsen, 2004). Patients suffered from
cardiovascular diseases usually have an increase in blood choles-
terol and low-density lipoprotein (LDL), as well as an increased
activity of lipid peroxidation: these are the hallmarks of hyperc-
holesterolemia (Dembowski and Davidson, 2009; Zhou and Liao,
2009). Due to dramatic changes of living and food styles in the last
century, the intake of a large variety of high-lipid snack and an
excessive intake of high-lipid food could result, subsequently, in
hyperlipidemia (Sorrentino et al., 2008). Clinically, hyperlipidemia
is considered to be one of the major risk factors for cardiovascu-
lar diseases including atherosclerosis, myocardial infarction, heart
attacks, stoke and cerebrovascular diseases (McBride, 2008; Tarride
et al., 2009).
∗ Corresponding author. Tel.: +852 2358 7332; fax: +852 2358 1559.
E-mail address: botsim@ust.hk (K.W.K. Tsim).
Over the last few decades, numerous studies have been car-
ried out on the identification of novel classes of hypolipidemic
agents from both natural and synthetic sources, which possess
ability in reducing the level of lipids in blood. These studies dis-
covered a lot of anti-hyperlipidemic substances, including dietary
fibers (Yamada et al., 2003), plant sterols (Nigon et al., 2001), herbal
extracts (Megalli et al., 2005) and yeast extracts (Elwood et al.,
1982). Among these searches, traditional Chinese herb is one of the
selections. The rhizome of Dioscorea nipponica Makino (Dioscoreae
Nipponicae Rhizoma or Japan Yam Rhizome) has been consumed
as a herbal medicine for more than four thousand years in China. In
clinical practice, Dioscoreae Nipponicae Rhizoma is used for reliev-
ing cough and asthma, eliminating rheumatic aches, alleviating
pain, and improving blood circulation. The rhizome of Dioscorea
nipponica is the major part of medicine, and the identified active
components are steroidal saponins, including furostanol saponins
and isospirostanol saponins. Saponin of Dioscorea nipponica pos-
sesses various pharmacological activities. Among them, trillin, a
steroidal saponin identified from Dioscorea nipponica, has been
demonstrated to induce multi-nucleation in different cancer cell

0378-8741/$ – see front matter © 2011 Elsevier Ireland Ltd. All rights reserved.
doi:10.1016/j.jep.2011.11.001
 T. Wang et al. / Journal of Ethnopharmacology 139 (2012) 214–220 215

lines (Liu et al., 2004), suggesting its regulatory effect in arrest-

ing mitotic cells. However, the report on other biological effects
A Cholesterol
of trillin is rather limited. In the current study, we employed a rat
Triglyceride
model feeding with high-fat diet as to induce hyperlipidemia, and + High-fat diet
subsequently the anti-hyperlipidemia effects of Dioscorea nippon-
ica rhizome and trillin were tested in the rats. Thus, we revealed ***
two novel activities of trillin in against hyperlipidemia and oxi-
*

Amount of lipid (mmol)

dation. Specifically, the anti-hyperlipidemic effects, including the 8
bleeding and blood coagulation time, the blood levels of choles-
terol, triglyceride, LDL and high-density lipoprotein (HDL) were
revealed here. In addition, the anti-oxidative effects, including 6
the levels of lipid peroxidation and superoxide dismutase (SOD),
were also determined. Indeed, the oxidation of lipid molecules is
one of the initial stages in developing cardiovascular diseases and 4
atherosclerosis.

2
2. Materials and methods

2.1. Preparation of herbal extracts and purification of trillin 0

Rhizoma Dioscoreae Nipponicae was obtained from Shenyang

Pharmaceutical University with the voucher specimen #10-08-04.
The raw herbs were morphologically authenticated by one of the
authors, Dr. Wang, during the field collection. Their corresponding
voucher specimens in the form of whole plants were deposited in Extractions
Shenzhen Institute of Drug Control, Shenzhen China. For chemi-
cal extraction, dried powder (5 kg) of Dioscorea nipponica rhizomes B
was extracted by 65% ethanol under reflux for 2 h and repeated HDL
two times (2× 50 L). After evaporation of solvent under vacuum,
the extract (630 g) was re-suspended in water and then extracted LDL
+ High-fat diet
by CHCl3 and n-BuOH to yield CHCl3 (60 g), n-BuOH (160 g) and
Amount of HDL or LDL (mmol)

H2 O fractions. The n-BuOH fraction (100 g) was subjected to column

**
chromatography (Ø 8 cm × 38 cm) over a silica gel (200–300 mesh)
with a gradient of CHCl3 –MeOH–H2 O system (10:1:0; 8:2:0.2;
*
7:3:0.5; 6:4:0.8) using 8.4 L volume for elution, which yielded 30 4
sub-fractions. Octa-decyl silica (ODS) open column chromatogra-
phy (Ø 5 cm × 25 cm) using a solvent consisting of MeOH–H2 O (6:4,
7:3, 8:2) and a volume of 1.5 L for elution led to the isolation of trillin
(200 mg) with over 98% purity. The chemical structure of purified
trillin was determined by comparing their spectral data with those
2
in the literatures, including infrared spectrum, nuclear magnetic
resonances (13 C NMR and 1 H NMR) and mass spectrometry (Choi
et al., 1991; Ballabeni et al., 2004).

2.2. Induction of hyperlipidemia by high-fat diet 0

Male Sprague–Dawley (SD) rats (180–220 g) were obtained from

the Guangdong Medical Laboratory Animal Center (Guangdong,
China). The handling of animals was according to the regulation
of Shenzhen Institute for Drug Control, Shenzhen China, and the
experimental procedures were approved by the ethical committee
of this Institute in line with the international guidelines of animal
care and welfare. In the diet-induced hyperlipidemia model, rats
were fed with normal and high-fat diet (normal diet supplemented
with 5% cholesterol (Sigma, St. Louis, MO)), 0.5% pig bile salt (Sigma)
and 0.2% thimecil (Sigma) for 1–28 days. The rats receiving the
high-fat diet were randomly divided into different groups (10 rats
each group) and subjected to drug treatments as control (without
drug administration), solvent (0.5% DMSO), positive control (Lovas-
tatin at 10 mg/kg from Sigma with >98% purity), chloroform extract
(50 mg/kg), n-butanol extract (50 mg/kg), water extract (50 mg/kg)
and trillin (0.5 mg/kg dissolved in 0.5% DMSO). The drug delivery
was conducted by intra-peritoneal administration everyday from
the period of 15 to 28 days.
Extractions
Fig. 1. The anti-hyperlipidemic effects of Dioscoreae Nipponicae Rhizoma by dif-
ferent extractions. The rhizomes of Dioscorea nipponica was extracted twice by 65%
EtOH for 2 h under reflux and then dried by rota-evaporation. The EtOH extract was
extracted by chloroform, n-butonol and water for 3 times. Solutions were dried by
either lyopholization or rota-evaporation. Experimental rats were subjected to nor-
mal or high-fat diet for 14 days, and the latter group was intra-gastric administrated
with the extracts (100 mg/kg) for 28 days. Intra-peritoneal administration of Lovas-
tatain (10 mg/kg) served as a positive control. The anti-hyperlipidemic activities
were assayed in terms of measuring the blood levels of cholesterol and triglyceride
in (A), and LDL and HDL in (B). Data were expressed as the amount of lipids or
lipoproteins, mean ± SEM, n = 10. *p < 0.05, **p < 0.01 and ***p < 0.001 as compared
to the control received high-fat diet.
216 T. Wang et al. / Journal of Ethnopharmacology 139 (2012) 214–220

A C
Capillary method
250
O ***
Trillin
200 ***
O
150

100

Coagulation time (sec)

GlcO
60

0
B 250 *** Slide method
***
Bleeding time (secc)

*** 200
200
**
150
150

100
100

60
60

0
0

+ High-fat diet
+ High-fat diet
Fig. 2. The regulatory effects of trillin on bleeding and coagulation time. (A) Trillin, ((25R)-spirost-5-en-3b-yl O-␤-d-glucopyranoside), was isolated and purified by column
chromatography as described in Section 2, with a purify of >98%. The identity was confirmed by correspondent spectra IR, NMR and MS (data not shown here). (B) Rats were
subjected to normal or high-fat diet for 1–28 days, and the latter group was intra-peritoneally injected with the trillin (0.5 mg/kg), Lovastatain (10 mg/kg), and 0.5% DMSO
solvent from 14 to 28 days. The measurement of blood clotting was represented by the bleeding time from the cut tail. (C) The blood coagulation time was determined
by using the capillary (upper panel) and slide (lower panel) methods being described in Section 2. Data were expressed as the time of bleeding or blood coagulation (s),
mean ± SEM, n = 10, **p < 0.01 and ***p < 0.001 as compared to the control received high-fat diet.

2.3. Bleeding and blood coagulation assays
At the end of the experimental period, followed by fasting for
8 h, the rats were anesthetized by isoflurane (5%) and subjected to
different blood assays, including bleeding and coagulation tests. For
bleeding assay, the rat tail was cut. The duration (in s) required from
bleeding to clotting was determined (Ballabeni et al., 2004). For
coagulation tests, the blood samples (0.5 mL) were collected from
the eye socket using a glass capillary, and the time interval required
for blood coagulation inside the capillary was measured (capillary
method). In addition, the blood samples (collected before) were
spread onto the glass slides. The duration (in s) required for blood
coagulation was also determined (slide method). The experimental
conditions of all the tests were controlled at 27 ◦ C with a humidity
of 60%.
2.4. Measurement of triglyceride, cholesterol, HDL, LDL in blood
was calculated using the equation: LDL = cholesterol − HDL − 1/5
triglyceride (Choi et al., 1991; Kim et al., 2001).
2.5. Anti-oxidative assays of lipid peroxidation and super oxide
dismutase
Followed by fasting for 8 h, the rats were anesthetized by isoflu-
rane (5%), the blood samples (0.5 mL) were withdrawn from the
veins of upper extremity, and which was centrifuged to obtain
the serum. Lipid peroxidation was measured by the formation of
malonaldehyde using thio-barbituric acid (TBA shade selection)
method (BIOMOL International Inc., Plymouth Meeting, PA), and the
enzymatic activity of superoxide dismutase (SOD) was measured
by xanthine oxidase (hydroxylamine method) method (Invitrogen,
Carlsbad, CA).

At the end of the experimental period, followed by fasting for 8 h,
the rats were anesthetized by isoflurane (5%), and blood samples
(1 mL) were collected from the eye socket. The levels of choles-
terol, triglyceride and HDL in serum were determined by enzymatic
colorimetric methods using the commercial kits (Jiangcheng Bio-
engineering Institute, Nanjing, China). The concentration of LDL
2.6. Statistical analysis
All data were analyzed by one-way ANOVA (analysis of F-test,
q-test and t-test) using the SPSS version 13 statistical analysis pro-
gram. Statistical significance was considered as ** for p < 0.01 and
*** for p < 0.001.
 T. Wang et al. / Journal of Ethnopharmacology 139 (2012) 214–220
3. Results
In order to test the anti-hyperlipidemia property of Dioscoreae
Nipponicae Rhizoma, the ethanol extracts were subjected to fur-
ther extraction by three different solvents: chloroform, n-butanol
and water. Different extracts were intra-gastrically administrated
to the rats that previously fed with normal, or high-fat, diet. The
results showed that administration of n-butanol extract in rats
exerted the best effect in reducing the high-fat diet-induced up reg-
ulation of lipid, including cholesterol and triglyceride (Fig. 1A). On
the other hand, the administration of n-butanol extract could also
restore the levels of HDL and LDL back to normal status (Fig. 1B).
Thus, the n-butanol extract was subjected to further purification.
Among various chemicals identified in the extract, trillin (chemical
structure see Fig. 2A) was the predominant chemical being isolated
from the extract, and about 200 mg of highly purified chemical was
achieved from 5 kg of dried herb, which therefore was chosen for
pharmacological characterization.
The regulatory effects of trillin on blood circulation were firstly
evaluated. Rats were subjected to high-fat, or normal, diet for
4 weeks. During this hyperlipidemic-inducing period, trillin was
intra-peritoneal administrated into the animals from week 2 to
week 4. At the end of the experiments, the animals were subjected
to fasting for 8 h and then anesthetized for blood clotting analysis,
including (i) the blood clotting time (indicated by the interval of
bleeding until clotting at the cutting tail); and (ii) the time of blood
coagulation (using capillary and slide methods). The results showed
that upon the receiving of high-fat diet (control), the bleeding time
in tail of the rat was dramatically reduced, as compared to that of
the normal-diet fed rat (normal). In contrast, the injection of trillin
could increase the bleeding time for more than 50% (Fig. 2B). Sim-
ilar effects were observed in blood coagulation tests that the time
interval of blood coagulation, being lowered by high-fat diet, could
be greatly restored by the administration of trillin (Fig. 2C, upper
and lower panels). In all the experiments, Lovastatin, a frequently
used statin, was used as the positive control to indicate the respon-
siveness of our model system. These results indicated that trillin
did possess promising effects in enhancing the bleeding time and
blood clotting time in the hyperlipidemic condition.
Clinically, the reduction of bleeding time and blood clotting time
under hyperlipidemic condition can be attributed to hypercholes-
terolemia. Based on this rationale, the regulatory effect of trillin
in reducing the blood cholesterol was examined. Blood samples
from the experimental rats were collected and subjected to differ-
ent biochemical assays. Results showed that the amount of blood
cholesterol was increased by ∼1.8 folds in the control group having
the high-fat diet (Fig. 3, upper panel): this increase could be attenu-
ated by the administration of trillin, with more than 90% reduction
of the level of cholesterol. In addition, high level of triglyceride in
blood stream could be linked with atherosclerosis. Therefore, the
regulatory effect of trillin on blood triglyceride was also investi-
gated. To our expectation, the content of blood triglyceride could
be elevated by the high-fat diet. The administration of trillin was
able to suppress the high level of triglyceride under high-fat diet
treatment (Fig. 3, lower panel). These results were similar to that of
Lovastatin in reducing the levels of both cholesterol and triglyceride
in high-fat diet rat.
HDL and LDL function as a cholesterol carrier in our body, and
which could serve as a diagnostic index in assessing the riskiness
of hyperlipidemia and other cardiovascular diseases. In the con-
trol rats receiving high-fat diet, the contents of LDL and HDL were
dramatically increased by ∼3.5 folds and ∼1 fold, respectively,
as compared with that of normal diet (Fig. 4A). Interestingly, the
administration of trillin was shown to reduce the level of LDL com-
pletely and HDL partially (Fig. 4A). These results were similar to that
of Lovastatin administration. In addition to the absolute amount of
217
Cholesterol
**
***
8
6
4
nt of lipid (mmol)
2
0
4 Triglyceride
Amoun
**
**
2
0
+ High-fat diet
Fig. 3. Reduction of blood cholesterol and triglyceride by trillin. Experimental rats
were subjected to a high-fat diet and then treated with solvent, Lovastatin or with
trillin, as in Fig. 2B. The amounts of cholesterol and triglyceride in the blood sam-
ples were determined. Lovastatin (10 mg/ml) served as a positive control. Data
were expressed as the amount of lipid (mmol), mean ± SEM, n = 10, **p < 0.01 and
***p < 0.001 as compared to the control received high-fat diet.
the lipoproteins in blood stream, the ratio of HDL/LDL is another
useful index for health assessment, e.g. a high ratio of HDL/LDL
refers to a better health condition with relatively low risk in suf-
fering cardiovascular diseases. The rats receiving the high-fat diet
had a low ratio of HDL/LDL, indicating the potential risk of body
health (Fig. 4B). However, the intra-peritoneal administration of
trillin was able to significantly raise the ratio to ∼4.5 (Fig. 4B). Such
promising results could be attributed to the differential regulation
of HDL and LDL by trillin that simultaneously reduced the amounts
of LDL completely and HDL partially in blood stream.
In the development of cardiovascular diseases and atherosclero-
sis by hyperlipidemia, oxidative damage of lipid molecules is one
of the initial steps of pathogenesis (Gamkrelidze et al., 2008). In
order to evaluate the anti-oxidative effects of trillin, the lipid per-
oxidation in blood was measured. Upon the treatment of high-fat
diet, the lipid peroxidation activity was increased by ∼50% (Fig. 5,
upper panel). Such deteriorate effect could be recovered by the
administration of trillin, and the level of lipid peroxidation was
totally restored to normal condition (Fig. 5, upper panel). Similar
result was observed in Lovastatin treatment. This result indicated
that trillin possessed the biological activity in suppressing the lipid
peroxidation in vivo. To partly account for this phenomenon, the
218 T. Wang et al. / Journal of Ethnopharmacology 139 (2012) 214–220

A *** LDL Lipid peroxidation

3
*** **

Amount of MDA ((mmol/L)

**
2
protein (mmol)

30

1
20
Amount of lipop

0
** HDL 10
4 **

0
3 SOD
**
400

SOD level (U/mL)

**
2
300

1
200

0 S 100

+ High-fat diet

B + High-fat diet
***
6
Fig. 5. Anti-oxidative effects of trillin on lipid peroxidation and SOD activity. Exper-
DL

imental rats were subjected to a high-fat diet and then treated with solvent,
Ratio of HDL/LD

Lovastatin or with trillin, as in Fig. 2B. The amount of MDA (lipid peroxidation) and
SOD activity in the blood samples were determined. Lovastatin (10 mg/ml) served as
4 a positive control. Data were expressed as the amount of SOD or MDA, mean ± SEM,
n = 10, **p < 0.01 and ***p < 0.001 as compared to the control received high-fat diet.

enzymatic activity of SOD was revealed since it participated in the

2 anti-oxidant defense in nearly all cells exposed to oxygen. To our
expectation, the activity of SOD, being reduced by high-fat diet, was
enhanced in the presence of trillin (Fig. 5, lower panel). Serving as
the positive control, Lovastatin also suppressed lipid oxidation and
0 elevated SOD activity. Taken together, the anti-oxidation effects of
trillin in vivo might be a part of molecular mechanisms in protecting
body health against hyperlipidemia.

4. Discussion

Saponins, a class of glycoside having structural diversity, have

+ High-fat diet
Fig. 4. Trillin suppresses the blood levels of LDL and HDL in high-fat diet treated
rats. (A) Experimental rats were subjected to a high-fat diet and then treated with
solvent, Lovastatin or with trillin, as in Fig. 2B. The amounts of HDL and LDL in the
blood samples were determined. (B) The ratio of HDL/LDL was calculated from the
data as listed in (A). Lovastatin (10 mg/ml) served as a positive control. Data were
expressed as the amount of HDL or LDL (mmol), mean ± SEM, n = 10, **p < 0.01 and
***p < 0.001 as compared to the control received high-fat diet.
attracted more and more attention in the last decade due to their
promising biological activities (Hostettmann and Marston, 1995;
Wang et al., 2001). Isospirostanol saponins are often found to be
the major ingredients in traditional Chinese herbs, with diosgenin
as the steroidal sapogenin. Most of them are deriving chemically
from trillin, while their structural diversities are attributed to
the difference in their sugar moieties. Some of the isospirostanol
glycosides in medicinal herbs have been used to treat malaria,
 T. Wang et al. / Journal of Ethnopharmacology 139 (2012) 214–220
helminthes infections and snake bites (Espejo et al., 1982; Ma and
Lau, 1985). Besides, anti-fungal and anti-bacterial effects were also
documented (Hufford et al., 1988; Li et al., 2001). Moreover, the
cytotoxic property of isospirostanol saponins has been shown in
againsting different strains of human cancer cells (Beneytout et al.,
1995; Ma et al., 2000). Among various biological properties, dioscin
(Cai et al., 2002) and trillin (Li et al., 1998) are the best known
isospirostanol saponins having these pharmacologically properties.
In addition to the aforementioned physiological effects, dioscin also
possesses the lipase-inhibitory activity, which is beneficial to car-
diovascular system (Kwon et al., 2003). Here, we reported the novel
biological activities of trillin in mediating the anti-hyperlipidemic
and anti-oxidative effects in vivo.
The intra-peritoneal administration of trillin improved the
blood circulation in terms of the time of bleeding and coagula-
tion. Under high-fat-diet condition, the blood viscosity would be
changed resulting in shorter blood coagulation time. The benefi-
cial effect of trillin in restoring the blood coagulation abnormality
in high-fat diet fed rat was accounted for its ability in reducing the
levels of blood cholesterol, triglyceride and two critical lipoproteins
(HDL and LDL). For oxidative damage caused by hyperlipidemia,
the level of lipid oxidation was increased in high-fat diet rats. The
anti-oxidative effect of trillin was revealed by its ability to lower
lipid peroxidation, probably via the enhancement of SOD level in
blood.
In addition to the effects of trillin against hyperlipidemia and
oxidative stress, we also found that the biological activities of
trillin in our tested parameters were rather similar to that of
Lovastatin. Lovastatin is known to be an inhibitor of 3-hydroxy-
3methylglutaryl-coenzyme A reductase (HMG-CoA reductase),
which catalyzes the conversion of HMG-CoA to mevalonate dur-
ing cholesterol synthesis (Alberts, 1998). Although the molecular
target(s) of trillin has not been determined yet in this study, the
combination of trillin and Lovastatin in treating hyperlipidemia
would provide another direction in developing a novel approach
for effective therapy in future.
Dioscin, diosgenin and protodioscin, purified from the methanol
extract of Dioscorea nipponica, have been demonstrated to possess
anti-hyperlipidemic effects including the suppression of time-
dependent increase of triglycerol in blood under the high-fat diet
treatment (Kwon et al., 2003; Wang et al., 2010). Such lipid-
reducing effect was also observed in the total extract of Dioscorea
nipponica. Among different extraction solvents, the n-butanol
extract showed better anti-hyperlipidemic effects in terms of reg-
ulating the blood cholesterol, triglyceride, HDL and LDL, than those
of chloroform and water extracts. These findings greatly support
the significant role of Dioscorea nipponica in protecting the car-
diovascular system in vivo against hyperlipidemia. It is interesting
to know if trillin, like other members of isospirostanol saponins,
would exert similar anti-lipase activity, which therefore could dis-
sect the mechanism of trillin in mediating the anti-hyperlipidemic
effect in vivo.
Natural products provide one of the most important sources
for the development of novel chemotherapeutics. These secondary
metabolites are widely distributed in plants and marine organisms
(Mahato et al., 1992). In vivo study has established that they could
be partially absorbed through intestine and distributed to various
tissues, indicating their excellent bioavailability (Nibbering et al.,
2001). In recent years, the use of herbal medicines has been
proposed as a novel strategy for maintaining a healthy life and
defeating metabolic diseases. Taking the advantage of thousand
years of experience with accumulated valuable cultural heritage of
Chinese herbal medicine, the potential usage of Chinese medicine
is huge. Therefore, the identification of active components
from Chinese herbs, the verification of their biological efficacy
and the resolution of action mechanisms are necessary for
219
internationalization and modernization of Chinese herbal
medicine, as well as for the development of drugs against
different diseases in future.
Acknowledgements
This research was supported by grants from Research Grants
Council of Hong Kong (N HKUST629/07, 662608), Croucher Foun-
dation (CAS-CF07/08.SC03) to Karl Tsim, and Shenzhen Bureau
Science Technology and Information to Jun Li (2005).
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