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Clinical Studies

Abstracts are presented below for clinical studies on Tribulus.

  • Botanical Name: Tribulus Terrestris

  • Ayurvedic Name: Gokshura

  • Common Name: Tribulus

Tribulus Terrestris

Plant Phytonutrient Profile


1: Planta Med. 1999 Feb;65(1):68/​73.

Application of Electrospray Ionization Mass Spectrometry Combined with
Sequential Tandem Mass Spectrometry Techniques for the Profiling of Steroidal
Saponin Mixture Extracted from Tribulus terrestris.

Fang S, Hao C, Liu Z, Song F, Liu S.

Changchun Institute of Applied Chemistry, Chinese Academy of Sciences,
Changchun, People's Republic of Chin.

Using electrospray ionization mass spectrometry combined with sequential tandem
mass spectrometry (ESI/​MS (n)), the steroidal saponin mixture extracted from
TRIBULUS TERRESTRIS was studied. The structures of five known steroidal saponins
and two unknown steroidal saponins in the saponin mixture were investigated by
sequential tandem mass spectrometry experiments. All of the steroidal saponins
displayed similar fragmentation behavior in ESI/​MS (n), and the characteristic
cross ring cleavage pattern could be used as a fingerprint for the
identification of steroidal saponins. The methodology has been established as a
powerful tool for the profiling of mixtures, especially of crude plant extracts,
and the structural elucidation of compounds.

PMID: 17260238 [PubMed /​ in process]

2: Nan Fang Yi Ke Da Xue Xue Bao. 2006 Dec;26(12):1777/​9.

[Effect of Tribulus terrestris extract on melanocyte/​stimulating hormone
expression in mouse hair follicles]

[Article in Chinese]

Yang L, Lu JW, An J, Jiang X.

Department of Traditional Chinese Medicine, Southern Medical University,
Guangzhou 510515, China. yangliutcm@ 21cn.com

OBJECTIVE: To observe the effect of Tribulus terrestris extract on melanocyte
stimulating hormone (MSH) expression in C57BL/6J mouse hair follicles, and
investigate the role of Tribulus terrestris extract in activation,
proliferation, epidermal migration of dormant hair follicle melanocytes.
METHODS: The aqueous extract of Tribulus terrestris was administered orally in
specific pathogen/​free C57BL/6J mouse at the daily dose equivalent to 1 g/1 kg
in adult human, and the expression and distribution of MSH in the mouse hair
follicles was observed with immunohistochemistry. RESULTS: The positivity rate
of MSH expression in the hair follicle melanocytes was 75% in mice treated with
the extract, significantly higher than the rate of only 18.75% in the control
group (P<0.01). CONCLUSION: The aqueous extract of Tribulus terrestris can
significantly increase MSH expression in the hair follicle melanocytes by
activating tyrosinase activity and promoting melanocyte proliferation, melanine
synthesis, and epidermal migration of dormant melanocytes.

Publication Types:
English Abstract

PMID: 17259119 [PubMed /​ in process]

3: Exp Biol Med (Maywood). 2007 Jan;232(1):126/​33.

Saponins from Tribulus terrestris L are less toxic for normal human fibroblasts
than for many cancer lines: influence on apoptosis and proliferation.

Neychev VK, Nikolova E, Zhelev N, Mitev VI.

Department of Chemistry and Biochemistry, Medical University, Sofia 1431,
Bulgaria. neychev@dir.bg

The objective of the study was to explore the influence of saponins derived from
Tribulus terrestris L. (TT) on normal human skin fibroblasts and to compare it
with their anticancer properties. In this study, [3H]thymidine incorporation and
MTT to assess cell proliferation and viability, respectively, and immunoblotting
and HPLC analysis to explore intracellular signal transduction pathways have
been used. We found that TT caused a dose/​dependent decrease in [3H]thymidine
incorporation into the DNA of treated fibroblast compared to the untreated
controls. Viability of treated cells remained within the control levels with
treatment of up to 5 micro g TT/ml medium. It was significantly depressed with
incubation in > or =6 micro g TT/ml medium with an IC50 of 12.6 micro g TT/ml of
cultivating media. ERK1/2 was significantly dephosphorylated at 5 mins of
incubation with TT until the 48th hour, when phosphorylation slightly recovered,
but was still below the control levels. In contrast, p38 and JNK phosphorylation
was positively influenced, with peaks at 1 hr and 24 hrs of incubation
respectively. Phosphorylation/dephosphorylation events of SAPK/MAPK clearly
correlated with Mkp/​1 induction. Procaspase 3 was activated after 5 mins of
incubation and coincided with a rapid actin cleavage. There was a significant
decrease of putrescine concentration and a concomitant increase of spermidine
and spermine at 2 mins of treatment. According to our results, TT is less toxic
for normal human skin fibroblasts in comparison to many cancer lines
investigated in previous studies. The molecular mechanism of this cytotoxicity
involves up/​ and downregulation of polyamines' homeostasis, suppression of
proliferation, and induction of apoptosis. Further research in this field using
animal models would help to explore and interpret the potential properties of TT
as an anticancer supplement.

Publication Types:
Comparative Study
Research Support, Non/​U.S. Gov't

PMID: 17202593 [PubMed /​ indexed for MEDLINE]

4: Rapid Commun Mass Spectrom. 2007;21(3):286/​96.

Intramolecular interchain reactions in bidesmosidic glycosides, a new insight
into carbohydrate rearrangements induced by electrospray ionisation.

Dal Piaz F, De Leo M, Braca A, De Simone F, De Tommasi N.

Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Salerno, Via
Ponte Don Melillo, 84084 Fisciano (Sa), Italy. fdalpiaz@unisa.it

Glycoconjugates are a class of complex molecules that are widely distributed in
the plant kingdom and in some marine organisms. This class of compounds has a
wide range of biological activities such as anti/​inflammatory, antimicrobial,
antifungal, anticancer, antiulcer, and immunoenhancing actions.1/​3 Some of them
also show various toxic activities such as cytotoxic, hemolytic, cardiotoxic,
and teratogenic. Among these compounds, steroidal and triterpenoid saponins have
long been known as components of widely used herbal drugs and pharmaceutical
preparations; ginseng, Tribulus terrestris, Quillaja saponaria, and Digitalis
ssp. are just a few examples. Thus, identification of saponins in herbal drugs
used worldwide is of significance in phytochemical and toxicological quality
control studies, and for the production of safe health products. Therefore,
there is continuing demand for methods to rapidly identify and characterize
these natural products. Copyright 2007 John Wiley & Sons, Ltd.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 17200980 [PubMed /​ in process]

5: Ann N Y Acad Sci. 2006 Nov;1084:391/​401.

The protective effect of Tribulus terrestris in diabetes.

Amin A, Lotfy M, Shafiullah M, Adeghate E.

Biology Department, United Arab Emirates University, PO Box: 17551, Al/​Ain,
Abu/​Dhabi, United Arab Emirates. a.amin@uaeu.ac.ae

Tribulus terrestris L (TT) is used in the Arabic folk medicine to treat various
diseases. The aim of this article was to investigate the protective effects of
TT in diabetes mellitus (DM). Diabetes is known to increase reactive oxygen
species (ROS) level that subsequently contributes to the pathogenesis of
diabetes. Rats were divided into six groups and treated with either saline,
glibenclamide (Glib), or TT for 30 days. Rats in group 1 were given saline after
the onset of streptozotocin (STZ)/​induced diabetes; the second diabetic group
was administered Glib (10 mg/kg body weight). The third diabetic group was
treated with the TT extract (2 g/kg body weight), while the first, second, and
third nondiabetic groups were treated with saline solution, Glib, and TT
extract, respectively. At the end of the experiment, serum and liver samples
were collected for biochemical and morphological analysis. Levels of serum
alanine aminotransferase (ALT) and creatinine were estimated. In addition,
levels of malondialdehyde (MDA) and reduced glutathione (GSH) were assayed in
the liver. The tested TT extract significantly decreased the levels of ALT and
creatinine in the serum (P < 0.05) in diabetic groups and lowered the MDA level
in liver (P < 0.05) in diabetic and (P < 0.01) nondiabetic groups. On the other
hand, levels of reduced GSH in liver were significantly increased (P < 0.01) in
diabetic rats treated with TT. Histopathological examination revealed
significant recovery of liver in herb/​treated rats. This investigation suggests
that the protective effect of TT for STZ/​induced diabetic rats may be mediated
by inhibiting oxidative stress.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 17151317 [PubMed /​ in process]

6: Zhongguo Zhong Yao Za Zhi. 2006 Jun;31(11):910/​3.

[Inhibitory effects of saponins from Tribulus terrestris on alpha/​glucosidase in
small intestines of rats]

[Article in Chinese]

Zhang SJ, Qu WJ, Zhong SY.

School of Life Science, East China Normal University, Shanghai 200062, China.

OBJECTIVE: To determine the effects of saponins from Tribulus terrestris (STT)
on small intestinal a/​glucosidase and postprandial blood glucose levels in rats.
METHOD: The inhibitory effects of STT on a/​glucosidase extracted from small
intestines in rats were carried out in vitro. The blood glucose levels were
measured after 60 min when sucrose (2 g x kg(/​1)) or glucose (2 g x kg(/​1)) was
administered orally with STT (100 mg x kg(/​1)). After treated with STT (100 mg x
kg(/​1)) for 14 d, the activities of a/​glucosidase were determined daily, as well
as the postprandial blood glucose levels after oraly administered sucrose (2 g x
kg(/​1)). RESULT: STT at concentrations of 0.1, 1 and 10 mg x mL(/​1) reduced
significantly the activities of alpha/​glucosidase with inhibitory rates of
(20.83 +//​ 1.66)%, (43.73 +//​ 2.39)% and (52.62 +//​ 2.69)%, respectively. In
facts STT (100 mg x kg(/​1)) considerably decreased the blood glucose levels
which was 52.61% of that of the control in rats co/​administered orally with
sucrose (2 g x kg(/​1)). However, it showed no such effect on the rats
co/​administered orally with glucose (2 g x kg(/​1)). After orally administered of
STT for 14 d, the activity of alpha/​glucosidase was significantly reduced (P <
0.05) to (58.17 +//​ 3.24)% of that those in control. Meanwhile, The rats were
oral administered with sucrose, the increase of postprandial blood glucose
levels were (69.50 +//​ 4.28)% of that in control 60 min later ( P < 0.05).
CONCLUSION: It was through inhibiting the activity of a/​glucosidase in small
intestines that STT significantly retarded the increase in postprandial blood
glucose levels in rats.

Publication Types:
English Abstract

PMID: 17048632 [PubMed /​ in process]

7: Trop Biomed. 2006 Jun;23(1):45/​51.

Recovery of phosphatase and transaminase activity of mercury intoxicated Mus
musculus (Linn.) liver tissue by Tribulus terrestris (Linn.) (Zygophyllaceae)
extract.

Jagadeesan G, Kavitha AV.

Department of Zoology, Faculty of Science, Annamalai University, Annamalainagar
/​ 608 002.

The efficacy of the methanolic fraction (MF) of Tribulus terrestris fruit
extract on mercury intoxicated mice, Mus musculus has been studied. At a
median/​lethal dose of mercuric chloride (12.9 mg/kg body wt.) administration an
enhanced level of glutamate oxaloacete transaminase (GOT), glutamate pyruvate
transminase (GPT) and simultaneously decreased level of acid phosphatase (ACP)
and alkaline phosphatase (ALT) activities were noticed in the liver. Due to the
mercury toxicity the liver cells are damaged to cause the alterations in their
enzymes. During the recovery period, all the enzymological parameters are
restored to reach near normal level. The result suggested that the oral
administration of MF of T. terrestris fruit extract has (6 mg/kg body wt.)
provided protection against the mercuric chloride induced hepatic damage in the
mice, M. musculus.

PMID: 17041551 [PubMed /​ in process]

8: Protoplasma. 2006 Aug;228(1/​3):49/​53. Epub 2006 Aug 31.

Comparative exine ontogeny in some members of the family Zygophyllaceae sensu
lato.

Nasri/​Ayachi MB, Nabli MA.

Laboratoire de Botanique Fondamentale et Appliquee, Faculte des Sciences,
Universite de Tunis El Manar, Tunis, Tunisia.

Exine ontogeny is studied in five taxa of the family Zygophyllaceae sensu lato
(Peganum harmala L., Zygophyllum album L., Fagonia cretica L., Tribulus
terrestris L., and Nitraria retusa [Forsk.] Asch.). In the beginning of the
tetrad stage, the plasmalemma is attached to the callose wall, except in T.
terrestris, where it describes crests and hollows. The primexine matrix is
fibrillar, bilayered in T. terrestris and unilayered in the other taxa. In all
species except P. harmala, the procolumellae are heterogeneous with clear zones
and they become compact later. In T. terrestris, they are built on the crests.
In Z. album and T. terrestris, a primordial nexinic lamella is set up. It is
tripartite with a white line seen at some levels; on its external leaflet, the
foot layer is observed, and on its internal leaflet, there is the endexine with
numerous lamellae. This white line disappears often in the mature exine. In T.
terrestris, there is a thick nexine that is coarsely lamellate inside. In the
aperture zone, the columellae are lacking, the tectum and the foot layer get
thinner; they unite and form the apertural membrane with the external part of
the endexine. There is a granulolamellar endexinic zone well developed in P.
harmala, whereas it is threelayered and weakly developed in T. terrestris.

Publication Types:
Comparative Study

PMID: 16937054 [PubMed /​ indexed for MEDLINE]

9: Scanning. 2006 Jul/​Aug;28(4):233/​5.

Scanning electron microscopic observations on micro/​organisms in the root
nodules of Tribulus terrestris L. (Zygophyllaceae).

Mahmood A, Athar M.

Department of Botany, University of Karachi, Karachi, Pakistan.

Scanning electron microscopic observations were made on the micro/​organisms of
root nodules of Tribulus terrestris L. The results showed that nodules of T.
terrestris contained dual infection consisting of Rhizobium sp. and Newmania
karachiensis. Based on these observations, T. terrestris should be grouped with
nonlegume Parasponia/​type bacterial nodules.

PMID: 16898671 [PubMed /​ indexed for MEDLINE]

10: Trop Biomed. 2005 Jun;22(1):15/​22.

FT/​IR Study of the influence of Tribulus terrestris on Mercury intoxicated mice,
Mus musculus liver.

Jagadeesan G, Kavitha AV, Subashini J.

Toxicological Division, Department of Zoology, Annamalai University,
Annamalainagar/​608 002, Tamilnadu, India.

FT/​IR spectra of liver tissue isolated from mice, Mus musculus, have been
recorded in the region of 4000 /​ 400 cm/​1 for normal, mercury treated and
recovery phase. In this study, the total protein content was found to be
decreased in the liver tissues after treatment with median/​lethal dose of
mercuric chloride. The marked fall in the level of bio/​chemical constituent in
the tissue due to metal exposure indicates the rapid initiation of the breakdown
of the bio/​chemical constituents to meet the energy demand during toxic stress.
During the recovery phase, the decreased levels of bio/​chemical constituents are
restored to near normal level. Methanol fractions of Tribulus terrestris fruit
extract was administrated on mercury intoxicated mice for 15 days. After the
administration, the mercury/​intoxicated animals slowly recovered from the
adverse effect of mercury poisoning with the help of plant bio/​formulations. The
results are discussed in detail.

PMID: 16880750 [PubMed /​ indexed for MEDLINE]

11: Zhongguo Zhong Xi Yi Jie He Za Zhi. 2006 Jun;26(6):541/​4.

[Effect of xinnao shutong capsule on cardiac muscle cell apoptosis and protein
expressions of Bcl/​2 and Bax in hyperlipidemia rats after myocardial infarction]

[Article in Chinese]

Guo Y, Yin HJ, Shi DZ.

Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing.

OBJECTIVE: To investigate the effect of Xinnao Shutong Capsule, whose main
ingredients gross saponins from Tribulus Terrestris L (GSTT) on cardiac muscle
cell (CMC) apoptosis and expressions of Bcl/​2 Compound rat model of and Bax in
murine model of hyperlipemia after myocardial infarction (MI). METHODS: MI and
hyperlipemia was adopted. TUNEL assay was applied to detect CMC apoptosis after
4 weeks' administration of GSTT or simvastatin, and immunohistochemical SP
technique was used to detect the expressions of Bcl/​2 and Bax protein. RESULTS:
GSTT can relieve the damage of CMC and attenuate the ventricular remodeling
after MI; high dose of GSTT and simvastatin could decrease CMC apoptosis
(P<0.05), and lower Bax protein expression (P < 0.05); and there was no
significant difference among the effects in all the treated group (P> 0.05).
CONCLUSION: GSTT can reduce CMC apoptosis through regulating protein expressions
of Bcl/​2 and Bax, which may be one of the mechanisms of its
anti/​ventricular/​remodeling effects after MI.

Publication Types:
English Abstract

PMID: 16841674 [PubMed /​ in process]

12: Asian Pac J Cancer Prev. 2006 Apr/​Jun;7(2):289/​94.

Chemopreventive potential of Tribulus terrestris against 7,12/​ dimethylbenz (a)
anthracene induced skin papillomagenesis in mice.

Kumar M, Soni AK, Shukla S, Kumar A.

Radiation and Cancer Biology Laboratory, Department of Zoology, University of
Rajasthan, Jaipur/​302004, India.

In the present investigation, the chemopreventive potential of aqueous extracts
of the root and fruit of Tribulus terrestris (an Ayurvedic medicinal plant) on
7, 12 /​ dimethylbenz (a) anthracene (DMBA) induced papillomagenesis in male
Swiss albino mice was studied. A significant reduction in tumor incidence, tumor
burden and cumulative number of papillomas was observed, along with a
significant increase in average latent period in mice treated orally with
Tribulus terrestris suspension continuously at pre, peri and post/​initiation
stages of papillomagenesis as compared to the control group treated with DMBA
and croton oil alone. Treatment with Tribulus terrestris suspension by oral
gavage for 7 days resulted in a significant increase in the reduced glutathione
content in the liver (P< 0.001 for both root and fruit extracts). Conversely,
lipid peroxidation levels were significantly decreased (P< 0.001).

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 16839225 [PubMed /​ indexed for MEDLINE]

13: Biol Pharm Bull. 2006 Jul;29(7):1383/​6.

Effect of SA1, a herbal formulation, on sexual behavior and penile erection.

Park SW, Lee CH, Shin DH, Bang NS, Lee SM.

College of Pharmacy, Sungkyunkwan University, Suwon, South Korea.

SA1 is a mixture of 9 Oriental herbs (Korean red ginseng, fermented soybean,
Tribulus terrestris, Fructus Rubi, Fructus Lycii, Semen Cuscutae, Dioscorea
Rhizome, Fructus Corni and Fructus Crataegi) that are widely used as energizers
and vitalizers in the indigenous system of medicine and have been alleged to
improve the sexual functions in men. This study evaluated SA1 using both in
vitro and in vivo experiments on laboratory animals in order to determine its
effect on the sexual behavior and penile erection. The male rats used to examine
the copulatory behavior were administered either the vehicle or SA1 (30, 100,
300, 600 mg/kg) orally for 2 weeks. The intracavernous pressure and systemic
blood pressure were recorded in anesthetized rats. The responses to
acetylcholine and SA1 of rabbit corpus cavernosum strips were also examined.
There was an overall increase in the copulatory behavior parameters in the
SA1/​treated rats, which was reflected by a decrease in the mount and
intromission latencies and an increase in the ejaculation latency and mount
frequency. SA1 significantly increased the ratio of the intracavernous pressure
to mean arterial pressure. In vitro, SA1 significantly enhanced the relaxation
responses to acetylcholine. These results suggest that SA1 improves the sexual
activity and erectile function.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 16819173 [PubMed /​ indexed for MEDLINE]

14: Aust Vet J. 2006 Jan/​Feb;84(1/​2):53/​8.

Abnormal turning behaviour, GABAergic inhibition and the degeneration of
astrocytes in ovine Tribulus terrestris motor neuron disease.

Bourke CA.

Orange Agricultural Institute, Forest Road, Orange, New South Wales 2800.

OBJECTIVE: To observe the clinical signs of sheep affected by Tribulus
terrestris motor neuron disease, to ascertain their response to striatal
dopamine reducing drugs, and to examine their brains and spinal cords for
microscopic changes. PROCEDURES: Twenty/​eight sheep displaying well developed
clinical signs of the disorder were observed. Twenty/​two of these and 22 normal
sheep were then randomly allocated to three groups and treated with diazepam,
chlorpromazine, or xylazine. The time that it took an animal to return to a
standing position following drug administration was recorded. The brain and
complete spinal cord were removed from each of the other six affected sheep and
fixed in formalin. Brains were sectioned throughout at 5 mm intervals and spinal
cords at 10 mm intervals. All tissues were paraffin embedded and examined by
light microscopy. A few samples were examined by electron microscopy. RESULTS:
Clinical signs included postural asymmetry with a right:left body/​side dominance
within the group of 50:50, unequal flaccid paresis in the pelvic limbs, extensor
muscle atrophy and adduction of the weaker pelvic limb, and concurrent abduction
of the stronger. Forward motion followed either a fixed left or right hand
curved trajectory, the sheep no longer being able to choose which. Twelve
animals intermittently displayed rotational behaviour that involved loss of
postural balance without locomotor activation. The administration of diazepam,
chlorpromazine, or xylazine caused limb paresis and sedation, with affected
sheep being slower than normal sheep by factors of 8, 3 and 2 respectively, to
return to a standing position. There were scattered areas of mild Wallerian
degeneration throughout the spinal cord, and in both the brain and the cord
there were small numbers of degenerate astrocytes containing novel cytoplasmic
pigment granules. CONCLUSIONS: Affected sheep had a dysfunction in the control
of directional change and this provides a new insight into the normal mechanism
for 'turning' in quadrupeds. Directional change requires a functional asymmetry
or lateralisation within the upper motor neuron to accommodate a difference in
the rate of forward progression of each body side and, simultaneously, a lateral
shift of the centre of gravity. The sensitivity of affected sheep to diazepam is
consistent with a pre/​existing elevation in GABAergic neuronal inhibition,
probably as a result of a reduction in glutamatergic neuronal excitation. The
cytoplasmic pigment found in degenerate astrocytes was novel and its presence in
the brain nuclei known to contribute to turning behaviour could have
aetiological significance. The motor output of the basal ganglia in Tribulus
neurotoxicity appeared to be excessively inhibitory to the pelvic limb extensor
muscles and was asymmetric, causing fixation of the turning posture but not
locomotor activation. An intoxication of specific purine sensitive, glutamate
releasing astrocytes, located in nuclei controlling turning, was suspected.

PMID: 16498837 [PubMed /​ indexed for MEDLINE]

15: Pak J Pharm Sci. 2004 Jan;17(1):9/​17.

Bioactivity studies of the individual ingredients of the Dashamularishta.

Jabbar S, Khan MT, Choudhuri MS, Sil BK.

Pharmacology Research Lab, Faculty of Pharmaceutical Sciences, University of
Science and Technology Chittagong, Foy's Lake, Chittagong, Bangladesh.

The bioactivity studies of the individual ingredients of Dashamularishta/​/​a
classical Ayurvedic preparation were done with the aqueous extracts of the
individual ingredients. The Aegle marmelos Correa. exhibited severe toxicity to
the brine shrimp (BST) nauplii, wheat rootlet growth (WRG) inhibition bioassay
and lettuce seed germination (LSG) bioassay. It exhibited no inhibition to the
growth of PPR and Reo virus in vero cell line. The Oroxylum indicum exhibited
moderate toxicity to the BST and WRG, but it is not toxic to the LSG. It
exhibited no inhibition to the growth of PPR and Reo virus. The Stereospermum
suaveolens exhibited severe toxicity to the BST and LSG, but it is not toxic to
the WRG. It exhibited total inhibition to the growth of Reo virus, but it has
not effect on the PPR virus. The Premna integrifolia showed severe toxicity to
the BST, but it was not toxic to the WRG and LSG. It exhibited no inhibition to
the growth of PPR and Reo virus. The Gmelina arborea exhibited severe toxicity
to the BST and WRG, but it is not toxic to the LSG. It exhibited no inhibition
to the growth of PPR and Reo virus. The Solanum xanthocarpum showed mild
toxicity to the BST, WRG and LSG. It exhibited 75% inhibition to the growth of
Reo virus. The Solanum indicum showed no toxicity to the BST, WRG and LSG. It
exhibited 75% inhibition to the growth of PPR virus. The Desmodium gangeticum
showed no toxicity to the BST, but moderate toxicity to the WRG and LSG. It
exhibited total inhibition to the growth of PPR virus. The Uraria lagopoides
showed no toxicity to the BST, WRG and LSG. It exhibited total inhibition to the
growth of Reo virus. The Tribulus terrestris showed no toxicity to the BST, but
showed moderate toxicity to the WRG and LSG. It exhibited 75% inhibition to the
growth of both PPR and Reo virus.

PMID: 16414581 [PubMed]

16: Biol Pharm Bull. 2005 Dec;28(12):2211/​5.

In vitro and in vivo antifungal activities of the eight steroid saponins from
Tribulus terrestris L. with potent activity against fluconazole/​resistant fungal
pathogens.

Zhang JD, Cao YB, Xu Z, Sun HH, An MM, Yan L, Chen HS, Gao PH, Wang Y, Jia XM,
Jiang YY.

Department of Pharmacology, College of Pharmacy, Second Military Medical
University, Shanghai, PR China.

Antifungal activity of natural products is being studied widely. Saponins are
known to be antifungal and antibacterial. We have isolated eight steroid
saponins from Tribulus terrestris L., namely TTS/​8, TTS/​9, TTS/​10, TTS/​11,
TTS/​12, TTS/​13, TTS/​14 and TTS/​15. TTS/​12 and TTS/​15 were identified as
tigogenin/​3/​O/​beta/​D/​xylopyranosyl(1/​/​>2)/​[beta/​D/​xylopyranosyl(1/​/​>3)]/​beta/​D/​g
lucopyranosyl(1/​/​>4)/​[alpha/​L/​rhamnopyranosyl(1/​/​>2)]/​beta/​D/​galactopyranoside
and
tigogenin/​3/​O/​beta/​D/​glucopyranosyl(1/​/​>2)/​[beta/​D/​xylopyranosyl(1/​/​>3)]/​beta/​D/​
glucopyranosyl(1/​/​>4)/​beta/​D/​galactopyranoside, respectively. The in vitro
antifungal activities of the eight saponins against six fluconazole/​resistant
yeasts, Candida albicans, Candida glabrata, Candida parapsilosis, Candida
tropicalis, Candida krusei, and Cryptococcus neoformans were studied using
microbroth dilution assay. The results showed that TTS/​12 and TTS/​15 were very
effective against several pathogenic candidal species and C. neoformans in
vitro. It is noteworthy that TTS/​12 and TTS/​15 were very active against
fluconazole/​resistant C. albicans (MIC(80)=4.4, 9.4 microg/ml), C. neoformans
(MIC(80)=10.7, 18.7 microg/ml) and inherently resistant C. krusei (MIC(80)=8.8,
18.4 microg/ml). So in vivo activity of TTS/​12 in a vaginal infection model with
fluconazole/​resistant C. albicans was studied in particular. Our studies
revealed TTS/​12 also showed in vivo activities against fluconazole/​resistant
yeasts. In conclusion, steroid saponins TTS/​12 and TTS/​15 from Tribulus
terrestris L. have significant in vitro antifungal activity against
fluconazole/​resistant fungi, especially TTS/​12 also showed in vivo activity
against fluconazole/​resistant C. albicans.

Publication Types:
Comparative Study
Research Support, Non/​U.S. Gov't

PMID: 16327151 [PubMed /​ indexed for MEDLINE]

17: J Ethnopharmacol. 2006 Apr 6;104(3):351/​5. Epub 2005 Nov 9.

Antihypertensive and vasodilator effects of methanolic and aqueous extracts of
Tribulus terrestris in rats.

Phillips OA, Mathew KT, Oriowo MA.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kuwait University,
P.O. Box 24923, 13110 Safat, Kuwait.

The effects of methanolic and aqueous extracts of Tribulus terrestris on rat
blood pressure (BP) and the perfused mesenteric vascular bed were investigated.
The extracts dose/​dependently reduced BP in spontaneously hypertensive rats
(SHRs) with the aqueous fraction being more potent than the methanolic fraction
at all doses tested. In vitro, the methanolic but not aqueous extract produced a
dose/​dependent increase in perfusion pressure of the mesenteric vascular bed.
When perfusion pressure was raised with phenylephrine (10(/​5) M), the aqueous
extract produced a dose/​dependent reduction in perfusion pressure at all doses.
A low dose of the methanolic extract produced a vasoconstrictor effect while
higher doses produced dose/​dependent reduction in perfusion pressure. L/​NAME
(10(/​4) M) significantly reduced but did not abolish vasodilation induced by the
extracts. Vasodilator responses to aqueous and methanolic fractions were
significantly reduced in preparations where perfusion pressure was raised with
KCl (60 mM). A combination of KCl and L/​NAME abolished the vasodilator responses
induced by the extracts. It was concluded that methanolic and aqueous extracts
of Tribulus terrestris possess significant antihypertensive activity in
spontaneously hypertensive rats. The antihypertensive effects appeared to result
from a direct arterial smooth muscle relaxation possibly involving nitric oxide
release and membrane hyperpolarization.

Publication Types:
In Vitro
Research Support, Non/​U.S. Gov't

PMID: 16289603 [PubMed /​ indexed for MEDLINE]

18: Zhongguo Zhong Yao Za Zhi. 2005 Aug;30(16):1271/​4.

[Experimental study of saponins from Tribulus terrestris on renal carcinoma cell
line]

[Article in Chinese]

Yang HJ, Qu WJ, Sun B.

School of Life Sciences, East China Normal University, Shanghai 200062, China.

OBJECTIVE: To investigate the effect of saponins from Tribulus terrestris (STT)
on the renal carcinoma cell (786/​0) in vitro, and inhibitory mechanisms. METHOD:
Effects of SIT on the cytotoxicity, morphological changes of apoptosis, cell
cycle and expression of Bcl/​2 protein in the 786/​0 were tested respectively by
MTT method, Wright and acridine orange stain assay, as well as flow cytometry
(FCM). RESULT: After the 786/​0 was treated by STY, it was shown that: 1) A
significant cytotoxic effect was observed by MTT assay; 2) Apoptosis/​induced was
viewed by Wright and acridine orange stain assay; 3) The distribution of 786/​0
on S phase was increased; 4.) The expression of Bcl/​2 protein and cyclin D1 was
decreased. CONCLUSION: STT can significantly inhibit the growth of 786/​0 in
vitro, partially, by apoptosis.

Publication Types:
English Abstract
Research Support, Non/​U.S. Gov't

PMID: 16245908 [PubMed /​ indexed for MEDLINE]

19: J Ethnopharmacol. 2006 Jan 3;103(1):76/​84. Epub 2005 Oct 5.

Antifungal activities and action mechanisms of compounds from Tribulus
terrestris L.

Zhang JD, Xu Z, Cao YB, Chen HS, Yan L, An MM, Gao PH, Wang Y, Jia XM, Jiang YY.

Department of Pharmacology, College of Pharmacy, Second Military Medical
University, Shanghai, PR China.

Antifungal activity of natural products is being studied widely. Saponins are
known to be antifungal and antibacterial. We used bioassay/​guided fractionation
to have isolated eight steroid saponins from Tribulus terrestris L., which were
identified as hecogenin/​3/​O/​beta/​D/​glucopyranosyl
(1/​/​>4)/​beta/​D/​galactopyranoside (TTS/​8), tigogenin/​3/​O/​beta/​D/​glucopyranosyl
(1/​/​>4)/​beta/​D/​galactopyranoside (TTS/​9), hecogenin/​3/​O/​beta/​D/​glucopyranosyl
(1/​/​>2)/​beta/​D/​glucopyranosyl (1/​/​>4)/​beta/​D/​galactopyranoside (TTS/​10),
hecogenin/​3/​O/​beta/​D/​xylopyranosyl (1/​/​>3)/​beta/​D/​glucopyranosyl
(1/​/​>4)/​beta/​D/​galactopyranoside (TTS/​11), tigogenin/​3/​O/​beta/​D/​xylopyranosyl
(1/​/​>2)/​[beta/​D/​xylopyranosyl (1/​/​>3)]/​beta/​D/​glucopyranosyl
(1/​/​>4)/​[alpha/​L/​rhamnopyranosyl (1/​/​>2)]/​beta/​D/​galactopyranoside (TTS/​12),
3/​O/​[beta/​D/​xylopyranosyl (1/​/​>2)/​[beta/​D/​xylopyranosyl
(1/​/​>3)]/​beta/​D/​glucopyranosyl (1/​/​>4)/​[alpha/​L/​rhamnopyranosyl
(1/​/​>2)]/​beta/​D/​galactopyranosyl]/​26/​O/​beta/​D/​glucopyranosyl/​22/​methoxy/​(3beta,5
alpha,25R)/​furostan/​3,26/​diol (TTS/​13), hecogenin/​3/​O/​beta/​D/​glucopyranosyl
(1/​/​>2)/​[beta/​D/​xylopyranosyl (1/​/​>3)]/​beta/​D/​glucopyranosyl
(1/​/​>4)/​beta/​D/​galactopyranoside (TTS/​14), tigogenin/​3/​O/​beta/​D/​glucopyranosyl
(1/​/​>2)/​[beta/​D/​xylopyranosyl (1/​/​>3)]/​beta/​D/​glucopyranosyl
(1/​/​>4)/​beta/​D/​galactopyranoside (TTS/​15). The in vitro antifungal activities of
the eight saponins against five yeasts, Candida albicans, Candida glabrata,
Candida parapsilosis, Candida tropicalis and Cryptococcus neoformans were
studied using microbroth dilution assay. In vivo activity of TTS/​12 in a Candida
albicans vaginal infection model was studied in particular. The results showed
that TTS/​12 and TTS/​15 were very effective against several pathogenic candidal
species and Cryptococcus neoformans in vitro. It is noteworthy that TTS/​12 and
TTS/​15 were very active against Candida albicans (MIC(80) = 10 and 2.3
microg/mL) and Cryptococcus neoformans (MIC(80) = 1.7 and 6.7 microg/mL). Phase
contrast microscopy showed that TTS/​12 inhibited hyphal formation, an important
virulence factor of Candida albicans, and transmission electron microscopy
showed that TTS/​12 destroyed the cell membrane of Candida albicans. In
conclusion, TTS/​12 has significant in vitro and in vivo antifungal activity,
weakening the virulence of Candida albicans and killing fungi through destroying
the cell membrane.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 16169173 [PubMed /​ indexed for MEDLINE]

20: J Ethnopharmacol. 2005 Oct 3;101(1/​3):319/​23.

The aphrodisiac herb Tribulus terrestris does not influence the androgen
production in young men.

Neychev VK, Mitev VI.

Department of Chemistry and Biochemistry, Medical University, 2 Zdrave str.,
Sofia/​1431, Bulgaria. neychev@dir.bg

OBJECTIVE: The aim of the current study is to investigate the influence of
Tribulus terrestris extract on androgen metabolism in young males. DESIGN AND
METHODS: Twenty/​one healthy young 20/​36 years old men with body weight ranging
from 60 to 125 kg were randomly separated into three groups/​two experimental
(each n=7) and a control (placebo) one (n=7). The experimental groups were named
TT1 and TT2 and the subjects were assigned to consume 20 and 10 mg/kg body
weight per day of Tribulus terrestris extract, respectively, separated into
three daily intakes for 4 weeks. Testosterone, androstenedione and luteinizing
hormone levels in the serum were measured 24 h before supplementation (clear
probe), and at 24, 72, 240, 408 and 576 h from the beginning of the
supplementation. RESULTS: There was no significant difference between Tribulus
terrestris supplemented groups and controls in the serum testosterone (TT1
(mean+//​S.D.: 15.75+//​1.75 nmol/l); TT2 (mean+//​S.D.: 16.32+//​1.57 nmol/l);
controls (mean+//​S.D.: 17.74+//​1.09 nmol/l) (p>0.05)), androstenedione (TT1
(mean+//​S.D.: 1.927+//​0.126 ng/ml); TT2 (mean+//​S.D.: 2.026+//​0.256 ng/ml);
controls (mean+//​S.D.: 1.952+//​0.236 ng/ml) (p>0.05)) or luteinizing hormone
(TT1 (mean+//​S.D.: 4.662+//​0.274U/l); TT2 (mean+//​S.D.: 4.103+//​0.869U/l);
controls (mean+//​S.D.: 4.170+//​0.406U/l) (p>0.05)) levels. All results were
within the normal range. The findings in the current study anticipate that
Tribulus terrestris steroid saponins possess neither direct nor indirect
androgen/​increasing properties. The study will be extended in the clarifying the
probable mode of action of Tribulus terrestris steroid saponins.

Publication Types:
Randomized Controlled Trial

PMID: 15994038 [PubMed /​ indexed for MEDLINE]

21: Urol Res. 2005 May;33(2):80/​6. Epub 2005 Mar 25.

Inhibition of the growth of urinary calcium hydrogen phosphate dihydrate
crystals with aqueous extracts of Tribulus terrestris and Bergenia ligulata.

Joshi VS, Parekh BB, Joshi MJ, Vaidya AD.

Crystal Growth Laboratory, Physics Department, Saurashtra University, Rajkot
360, India.

Urinary type calcium hydrogen phosphate dihydrate (CHPD) or Brushite crystals
were grown by the single diffusion gel technique in silica hydro/​gels. The gel
framework acts as a three dimensional crucible in which the crystal nuclei are
delicately held in the position of their formation and nutrients are supplied
for their growth. This technique can be utilized as a simplified screening model
to study the growth and dissolution of urinary stones in vitro. The action of
the putatively litholytic medicinal plants Tribulus terrestris and Bergenia
ligulata on the growth of CHPD crystals was studied . The effects of artificial
reference urine (ARU) and human urine (HU), along with the plant extracts, are
also reported. Attempts were made to understand the role of these inhibitors on
urinary crystal formation. HU, ARU, extracts of B. ligulata and T. terrestris
exhibit appreciable amounts of inhibition, but B.ligulata and T.terrestris with
ARU and HU do not show inhibition at all.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 15791467 [PubMed /​ indexed for MEDLINE]

22: J Ethnopharmacol. 2005 Jan 4;96(1/​2):127/​32.

Effect of Tribulus terrestris on nicotinamide adenine dinucleotide
phosphate/​diaphorase activity and androgen receptors in rat brain.

Gauthaman K, Adaikan PG.

Department of Obstetrics and Gynaecology, National University Hospital, National
University of Singapore, 5 Lower Kent Ridge Road, Singapore 119074, Singapore.

Tribulus terrestris L. (Zygophyllaceae) have been used as an aphrodisiac both in
the Indian and Chinese traditional systems of medicine. Administration of
Tribulus terrestris extract (TT) increased sexual behaviour and intracavernous
pressure both in normal and castrated rats and these effects were probably due
to the androgen increasing property of TT. The objective of the present study is
to evaluate the effect of TT on nicotinamide adenine dinucleotide
phosphate/​diaphorase (NADPH/​d) activity and androgen receptor (AR)
immunoreactivity in rat brain. Twenty/​four adult male Sprague/​Dawley rats were
divided into two groups of twelve each. Group I was treated with distilled water
and Group II was treated with TT at the dose of 5mg/kg body weight orally, once
daily for 8 weeks. Following treatment transcardiac perfusion was done with
Ringer lactate, 4% paraformaldehyde and 30% sucrose. The brain tissue was
removed and sections of the paraventricular (PVN) area of hypothalamus were
taken for NADPH/​d and AR immunostaining. There was an increase in both NADPH/​d
(67%) and AR immunoreactivity (58%) in TT treated group and these results were
statistically significant compared to the control. Chronic treatment of TT in
rats increases the NADPH/​d positive neurons and AR immunoreactivity in the PVN
region. Androgens are known to increase both AR and NADPH/​d positive neurons
either directly or by its conversion to oestrogen. The mechanism for the
observed increase in AR and NADPH/​d positive neurons in the present study is
probably due to the androgen increasing property of TT. The findings from the
present study add further support to the aphrodisiac claims of TT.

PMID: 15588660 [PubMed /​ indexed for MEDLINE]

23: Zhongguo Zhong Yao Za Zhi. 2004 Jul;29(7):681/​4.

[Investigation on inhibitory and apoptosis/​inducing effects of saponins from
Tribulus terrestris on hepatoma cell line BEL/​7402]

[Article in Chinese]

Sun B, Qu WJ, Zhang XL, Yang HJ, Zhuang XY, Zhang P.

Life Science School, East China Normal University, Shanghai 200062, China.

OBJECTIVE: To investigate the inhibitory and apoptosis/​inducing effects of
saponins from Tribulus terrestris (STT) on liver cancer cell line BEL/​7402.
METHOD: MTT, SRB, Wright staining, acridine orange staining, flow cytometry, and
Immunofluorescence microscopy were used to evaluate the effects of STT on
BEL/​7402 cell line. RESULT: SMT had potent inhibitory effect on BEL/​7402 cell
line in a concentration/​dependent manner. BEL/​7402 cells exibited typical
morphological alteration of apoptosis when sub/​G1 peak could be seen. The
expression of Bcl/​2 was decreased in STT treated cells as compared with
untreated control cells. CONCLUSION: STT exerts its cytotoxic effect on BEL/​7402
cells by inducing apoptosis.

Publication Types:
English Abstract

PMID: 15503780 [PubMed /​ indexed for MEDLINE]

24: Magn Reson Chem. 2004 Nov;42(11):990/​3.

Dependence of 1H NMR chemical shifts of geminal protons of glycosyloxy methylene
(H2/​26) on the orientation of the 27/​methyl group of furostane/​type steroidal
saponins.

Agrawal PK.

Central Institute of Medicinal and Aromatic Plants, Lucknow/​226015, India.
pkagrawal11@hotmail.com

An approach based on the difference (Delta(ab) = delta(a) /​ delta(b)) between
the 1H NMR chemical shifts (delta(a), delta(b)) of the geminal protons of
glycosyloxy methylene (H2/​26) (Delta(ab) = <0.48 for 25R; Delta(ab) = >0.57 for
25S) is proposed for ascertaining 25R/25S orientation of the 27/​methyl group of
furostane/​type steroidal saponins. These studies suggested the 25R/​orientation
of the 27/​Me group for the furostanol glycosides isolated by Wu et al. from
Tribulus terrestris. Copyright 2004 John Wiley & Sons, Ltd.

PMID: 15386548 [PubMed /​ indexed for MEDLINE]

25: J Ethnopharmacol. 2004 Mar;91(1):57/​60.

Acetylcholinesterase and butyrylcholinesterase inhibitory activity of some
Turkish medicinal plants.

Orhan I, Sener B, Choudhary MI, Khalid A.

Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330 Ankara,
Turkey. iorhan@gazi.edu.tr

The chloroform:medianol (1:1) extracts of a number of the plant species
belonging to eight families, namely Corydalis solida (L.) Swartz subsp. solida
and Glaucium corniculatum (L.) J. H. Rudolph (Papaveraceae), Rhododendron
ponticum L. subsp. ponticum and Rhododendron luteum Sweet. (Ericaceae), Buxus
sempervirens L. (Buxaceae), Vicia faba L. (Fabaceae), Robinia pseudoacacia L.
(Caeselpiniaceae), Tribulus terrestris L. and Zygophyllum fabago L.
(Zygophyllaceae), Lycopodium clavatum L. (Lycopodiaceae), Fumaria vaillantii
Lois., Fumaria capreolata L., Fumaria kralikii Jordan, Fumaria asepala Boiss.,
Fumaria densiflora DC., Fumaria flabellata L., Fumaria petteri Reichb. subsp.
thuretii (Boiss.) Pugsley, Fumaria macrocarpa Boiss. ex Hausskn., Fumaria
cilicica Hauskkn., Fumaria parviflora Lam. and Fumaria judaica Boiss.
(Fumariaceae) were screened for their anticholinesterase activity on
acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes by in vitro
Ellman method at 10 microg/ml and 1 mg/ml concentrations. The extracts did not
show any noticeable inhibitory activity against both of the enzymes at 10
microg/ml. The extracts of Rhododendron ponticum subsp. ponticum, Rhododendron
luteum, Corydalis solida subsp. solida, Glaucium corniculatum, and Buxus
sempervirens showed remarkable inhibitory activity above 50% inhibition rate on
AChE at 1 mg/ml. Among them, Rhododendron ponticum subsp. ponticum, Corydalis
solida subsp. solida and Buxus sempervirens were the most active extracts
against BChE having 95.46 +//​ 1.03%, 93.08 +//​ 0.97%, and 93.45 +//​ 0.88%
inhibition rates, respectively. Among the extracts screened, all of the Fumaria
extracts displayed highly potent inhibition against both of the enzymes at 1
mg/ml concentration compared to the standard.

PMID: 15036468 [PubMed /​ indexed for MEDLINE]

26: Fitoterapia. 2004 Mar;75(2):117/​22.

A novel furostanol saponin from Tribulus terrestris of Bulgarian origin.

Conrad J, Dinchev D, Klaiber I, Mika S, Kostova I, Kraus W.

Department of Chemistry, University of Hohenheim, 70593 Stuttgart, Germany.

The phytochemical investigation of the aerial parts of Tribulus terrestris of
Bulgarian origin has resulted in the isolation of the novel furostanol saponin
1, named tribol, together with the known spirostanol saponins 2 and 3 and
sitosterol glucoside. The structure of tribol was determined as
(25R)/​furost/​5(6)/​ene/​3beta,16,26/​triol/​3/​O/​alpha/​rhamnopyranosyl/​(1/​/​>2)/​[alpha
/​rhamnopyranosyl/​(1/​/​>4)]/​beta/​glucopyranoside (1) by spectral analysis,
including extensive 1D and 2D/​NMR experiments.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 15030914 [PubMed /​ indexed for MEDLINE]

27: J Am Soc Mass Spectrom. 2004 Feb;15(2):133/​41.

Structural analysis of saponins from medicinal herbs using electrospray
ionization tandem mass spectrometry.

Liu S, Cui M, Liu Z, Song F, Mo W.

Laboratory of Mass Spectrometry, Changchun Institute of Applied Chemistry,
Chinese Academy of Sciences Changchun, China. mslab@nc.ciac.jl.cn

The underivatized saponins from Tribulus terrestris and Panax ginseng have been
investigated by electrospray ionization multi/​stage tandem mass spectrometry
(ESI/​MS(n)). In ESI/​MS spectra, a predominant [M + Na](+) ion in positive mode
and [M /​ H](/​) ion in negative mode were observed for molecular mass
information. Multi/​stage tandem mass spectrometry of the molecular ions was used
for detailed structural analysis. Fragment ions from glycoside cleavage can
provide information on the mass of aglycone and the primary sequence and
branching of oligosaccharide chains in terms of classes of monosaccharides.
Fragment ions from cross/​ring cleavages of sugar residues can give some
information about the linkages between sugar residues. It was found that
different alkali metal/​cationized adducts with saponins have different degrees
of fragmentation, which may originate from the different affinity of a saponin
with each alkali metal in the gas phase. ESI/​MS(n) has been proven to be an
effective tool for rapid determination of native saponins in extract mixtures,
thus avoiding tedious derivatization and separation steps.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 14766280 [PubMed /​ indexed for MEDLINE]

28: J Asian Nat Prod Res. 2003 Dec;5(4):285/​90.

Terrestrinins A and B, two new steroid saponins from Tribulus terrestris.

Huang JW, Tan CH, Jiang SH, Zhu DY.

State Key Laboratory of Drug Research, Shanghai Institutes for Biological
Sciences, Chinese Academy of Sciences, 294 Taiyuan Road, Shanghai 200031,
People's Republic of China.

Two new steroid saponins, named terrestrinins A (1) and B (2), along with six
known compounds were isolated from the Chinese medicine herb Tribulus
terrestris, and their chemical structures were elucidated as
26/​O/​beta/​D/​glucopyranosyl/​(25S)/​furostan/​4(5),20(22)/​diene/​3,12/​dione (1) and
26/​O/​beta/​D/​glucopyranosyl/​(25S)/​5alpha/​furostane/​3beta,22alpha,26/​triol/​3/​O/​bet
a/​D/​xylopyranosyl(1 /​/​> 3)/​[(beta/​D/​xylopyranosyl(1 /​/​>
2)]/​beta/​D/​glucopyranosyl(1 /​/​> 4)/​[alpha/​L/​rhamnopyranosyl(1 /​/​>
2)]/​beta/​D/​galactopyranoside (2) on the basis of spectroscopic techniques.

PMID: 14604238 [PubMed /​ indexed for MEDLINE]

29: J Am Coll Nutr. 2003 Oct;22(5):363/​71.

Ingestion of a dietary supplement containing dehydroepiandrosterone (DHEA) and
androstenedione has minimal effect on immune function in middle/​aged men.

Kohut ML, Thompson JR, Campbell J, Brown GA, Vukovich MD, Jackson DA, King DS.

Department of Health and Human Performance, Iowa State University, Ames, Iowa
50011, USA. mkohut@iastate.edu

OBJECTIVE: This study investigated the effects of four weeks of intake of a
supplement containing dehydroepiandrosterone (DHEA), androstenedione and herbal
extracts on immune function in middle/​aged men. DESIGN: Subjects consumed either
an oral placebo or an oral supplement for four weeks. The supplement contained a
total daily dose of 150 mg DHEA, 300 mg androstenedione, 750 mg Tribulus
terrestris, 625 mg chrysin, 300 mg indole/​3/​carbinol and 540 mg saw palmetto.
MEASUREMENTS: Peripheral blood mononuclear cells were used to assess
phytohemagglutinin(PHA)/​induced lymphocyte proliferation and cytokine
production. The cytokines measured were interleukin (IL)/​2, IL/​4, IL/​10,
IL/​1beta, and interferon (IFN)/​gamma. Serum free testosterone, androstenedione,
estradiol, dihydrotestosterone (DHT) were also measured. RESULTS: The supplement
significantly increased serum levels of androstenedione, free testosterone,
estradiol and DHT during week 1 to week 4. Supplement intake did not affect LPS
or ConA proliferation and had minimal effect on PHA/​induced proliferation.
LPS/​induced production of IL/​1beta, and PHA/​induced IL/​2, IL/​4, IL/​10, or
IFN/​gamma production was not altered by the supplement. The addition of the same
supplement, DHEA or androstenedione alone to lymphocyte cultures in vitro did
not alter lymphocyte proliferation, IL/​2, IL/​10, or IFN/​gamma, but did increase
IL/​4. In addition, serum HDL/​C concentration significantly declined. CONCLUSION:
These findings suggest that, although chronic intake of a complex dietary
supplement containing DHEA, androstenedione and herbal extracts increases serum
androgen levels, it has minimal effect on immune function in middle/​aged men.

Publication Types:
Clinical Trial
Randomized Controlled Trial
Research Support, Non/​U.S. Gov't

PMID: 14559928 [PubMed /​ indexed for MEDLINE]

30: Zhong Yao Cai. 2003 May;26(5):341/​4.

[Effect of saponin from Tribulus terrestris on hyperlipidemia]

[Article in Chinese]

Chu S, Qu W, Pang X, Sun B, Huang X.

School of Life Science, East China Normal University, Shanghai 200062.

The preventive and therapeutic effects of saponin from Tribulus terrestris L. on
diet/​induced hyperlipidemia in mice have been studied. It showed that in
preventive experiment the saponin could significantly low the levels of serum TC
(P < 0.05), LDL/​c (P < 0.01) and liver TC (P < 0.05), TG (P < 0.05), and
increase the activities of superoxide/​dismutase (SOD) in liver. The therapeutic
experiment showed that the saponin could significantly reduce the contents of
serum TC (P < 0.05) and liver TC (P < 0.01).

Publication Types:
English Abstract

PMID: 14535016 [PubMed /​ indexed for MEDLINE]

31: Life Sci. 2003 Oct 24;73(23):2963/​71.

Study of antihypertensive mechanism of Tribulus terrestris in 2K1C hypertensive
rats: role of tissue ACE activity.

Sharifi AM, Darabi R, Akbarloo N.

Department of Pharmacology, Razi Institute for Drug Research and Cellular and
Molecular Research Center, School of Medicine, Iran University of Medical
Sciences, PO Box 14155/​6183 Tehran, Iran. sharifal@yahoo.com

Tribulus terrestris is a natural herb used for treating many diseases including
hypertension. According to previous reports, aqueous extract of tribulus fruits
may have some antihypertensive effect with an unknown mechanism. The present
study investigated the antihypertensive mechanism of tribulus in 2K1C
hypertensive rats by measurement of circulatory and local ACE activity in aorta,
heart, kidney and lung. Four groups of rats were selected; control, sham,
operated or hypertensive and tribulus treated hypertensive group. Hypertension
was induced using silver clip on renal artery by surgery. Four weeks after
surgery, a single daily dose of 10 mg/kg of lyophilized aqueous extract of
tribulus fruit were given orally to 2K1C rats for four weeks. ACE activity was
determined by high performance liquid chromatography (HPLC). Blood pressure was
measured by the tail/​cuff method. The systolic blood pressure (SBP) was
significantly increased in 2K1C rats compared to control rats. The SBP of
tribulus fed hypertensive rats was significantly decreased compared to
hypertensive rats. The ACE activity in all tissues of 2K1C rats including:
aorta, heart, kidney, lung as well as serum were significantly increased
compared to normal rats. The ACE activity in all tissues of tribulus fed
hypertensive rats was significantly lower than that of hypertensive rats, which
was more pronounced in kidney. These results indicated that there is a negative
correlation between consumption of tribulus and ACE activity in serum and
different tissues in 2K1C rats.

PMID: 14519445 [PubMed /​ indexed for MEDLINE]

32: Fitoterapia. 2003 Sep;74(6):583/​91.

Furostanol saponins from Tribulus terrestris.

De Combarieu E, Fuzzati N, Lovati M, Mercalli E.

Research and Development Laboratories, Indena SpA, Via Don Minzoni 6, Settala
(MI) 20090, Italy.

An HPLC/​ELSD/​ESI/​MS method has been developed for the analysis of the steroidal
saponins in the aerial parts of Tribulus terrestris. Protodioscin, a new saponin
(5,6/​dihydroprotodioscin, neoprotodioscin) and their respective sulfates were
detected. The structure of the new compound was elucidated on the basis of NMR
and ESI/​MS spectral analysis.

PMID: 12946722 [PubMed /​ indexed for MEDLINE]

33: J Altern Complement Med. 2003 Apr;9(2):257/​65.

Sexual effects of puncturevine (Tribulus terrestris) extract (protodioscin): an
evaluation using a rat model.

Gauthaman K, Ganesan AP, Prasad RN.

Department of Obstetrics and Gynaecology, National University Hospital, National
University of Singapore, Singapore.

OBJECTIVE: Apart from its claims for improvement of sexual functions in men, the
puncturevine plant (Tribulus terrestris: TT) has long been considered as an
energizer and vitalizer in the indigenous system of medicine. Sexual behavior
and intracavernous pressure (ICP) measurements were taken in rats to
scientifically validate the claim of TT [containing protodioscin (PTN)] as an
aphrodisiac. MATERIALS AND METHODS: Forty sexually mature male Sprague/​Dawley
rats were randomly divided into four groups of 10 each. Group I served as a
control group and groups II, III, and IV were treated with three different doses
of TT extract (2.5, 5 and 10 mg/kg body weight, respectively), orally, once
daily for 8 weeks. Weight was recorded and the rats from all four groups were
subjected to sexual behavior studies with primed females and various parameters
namely mount and intromission frequencies (MF and IF, respectively), mount,
intromission and ejaculation latencies (ML, IL, and EL, respectively) as well as
postejaculatory interval (PEI) were recorded. In addition, blood pressure and
ICP were recorded for all rats at the end of study. RESULTS: Increases in body
weight (by 9, 23, and 18% for groups II, III & IV) and ICP (by 43% and 26% for
groups III and IV) were statistically significant compared to the control group.
Increases in MF (by 27% and 24%) and IF (by 19% and 22%) for the groups III and
IV were statistically significant. Decreases in ML (by 16%, 23%, and 22% for
groups II, III, and IV) and PEI (by 20% for group III) were statistically
significant compared to the control. CONCLUSIONS: The weight gain and
improvement in sexual behavior parameters observed in rats could be secondary to
the androgen increasing property of TT (PTN) that was observed in our earlier
study on primates. The increase in ICP which confirms the proerectile
aphrodisiac property of TT could possibly be the result of an increase in
androgen and subsequent release of nitric oxide from the nerve endings
innervating the corpus cavernosum.

PMID: 12804079 [PubMed /​ indexed for MEDLINE]

34: Zhong Yao Cai. 2003 Feb;26(2):104/​6.

[The inhibitory effect of saponins from Tribulus terrestris on Bcap/​37 breast
cancer cell line in vitro]

[Article in Chinese]

Sun B, Qu W, Bai Z.

Life Science School of East China Normal University, Shanghai 200062.

The inhibitory effect of saponins from Tribulus terrestris (STT) on Bcap37
breast cancer cell line were determined by cell growth curve, MTT assay, protein
content assay and morphological observation. The results showed that STT had
potent inhibitory effect on Bcap/​37 cell line in a concentration/​dependent
manner. Bcap/​37 cell exhibited morphological alteration, namely, cells got round
and shrunk, nuclei contracted after treating with STT.

Publication Types:
English Abstract

PMID: 12795220 [PubMed /​ indexed for MEDLINE]

35: J Ethnopharmacol. 2003 Apr;85(2/​3):257/​60.

Tribulus terrestris: preliminary study of its diuretic and contractile effects
and comparison with Zea mays.

Al/​Ali M, Wahbi S, Twaij H, Al/​Badr A.

Department of Urology, St. Bartholomew's, The Royal London & Homerton University
Hospitals, 224B East End Road, East Finchley, N2 8AX, London, UK.
alalimun@hotmail.com

OBJECTIVES: Tribulus terrestris L. (Zygophyllaceae) which is called Al/​Gutub (in
Iraqi dialect) or Quti;ba (in classical Arabic medicine), and Zea mays were both
used alone or in combination by Iraqi herbalists to propel urinary stones. We
studied the aqueous extract of the leaves and fruits of T. terrestris and the
hair of Z. mays, to determine their diuretic activity and the contractile effect
of T. terrestris. METHODS: The aqueous extract was filtered and the solvent was
evaporated to produce a dry crude extract. The dry extract was then dissolved in
physiological saline to make the required concentrations. Wistar male rats were
used for the diuresis test and strips of isolated Guinea pig ileum were used for
the contractility test. RESULTS: The aqueous extract of T. terrestris, in oral
dose of 5g/kg elicited a positive diuresis, which was slightly more than that of
furosemide. Z. mays aqueous extract did not result in significant diuresis when
given alone in oral dose of 5g/kg, while combination of Z. mays and T.
terrestris extracts produced the same extent of diuresis as that produced by T.
terrestris alone. Na(+), K(+) and Cl(+) concentrations in the urine had also
much increased. In addition to its diuretic activity T. terrestris had evoked a
contractile activity on Guinea pig ileum. CONCLUSION: T. terrestris has long
been used empirically to propel urinary stones. The diuretic and contractile
effects of T. terrestris indicate that it has the potential of propelling
urinary stones and merits further pharmacological studies.

Publication Types:
Comparative Study

PMID: 12639749 [PubMed /​ indexed for MEDLINE]

36: Vet Res Commun. 2003 Jan;27(1):53/​62.

Experimental Tribulus terrestris poisoning in sheep: clinical, laboratory and
pathological findings.

Aslani MR, Movassaghi AR, Mohri M, Pedram M, Abavisani A.

Department of Clinical Studies, School of Veterinary Medicine, Ferdowsi
University of Mashhad, PO Box 91775/​1793, Mashhad, Iran

Eleven native sheep, 1/​2 years old, of both sexes were randomly divided into two
groups, 6 sheep being allocated to the experimental group and 5 serving as
controls. The sheep in the experimental group were fed 80% Tribulus terrestris
and 20% alfalfa hay and wheat straw, while the control sheep were given a
mixture of 40% alfalfa hay and 60% wheat straw. Clinical signs of hepatogenous
photosensitivity were observed from day 11, including reddening and crust
formation on the muzzle, nose, ears and eyelids, depression, weight loss,
icterus, conjunctivitis, and yellow discoloration of the urine. Laboratory
findings on weekly samples indicated significant differences (p < 0.05) in white
blood cell count, total plasma protein and fibrinogen, total and direct
bilirubin, blood urea nitrogen and creatinine concentrations, and aspartate
aminotransferase and alkaline phosphatase activities. There were no significant
differences in the packed cell volume, in the neutrophil, lymphocyte or
eosinophil counts, or in the serum calcium, phosphorus, potassium, sodium or
chloride concentrations. At necropsy of the experimental animals, there were
various degrees of generalized icterus and the livers were swollen and
discolored by bile pigment. Histopathological examination revealed varying
amounts of crystalloid material in the bile ducts and renal tubules,
hepatocellular degeneration, biliary fibrosis and proliferation, renal tubular
necrosis and focal necrosis of cardiac muscle.

PMID: 12625403 [PubMed /​ indexed for MEDLINE]

37: Phytomedicine. 2002 Dec;9(8):753/​6.

Tribulosin and beta/​sitosterol/​D/​glucoside, the anthelmintic principles of
Tribulus terrestris.

Deepak M, Dipankar G, Prashanth D, Asha MK, Amit A, Venkataraman BV.

Phytochemistry Laboratory, R&D Centre, Natural Remedies Pvt. Ltd., Veerasandra
Indl. Area, Bangalore, India.

Successive extracts of Tribulus terrestris prepared using petroleum ether,
chloroform, 50% methanol and water were tested for anthelmintic activity
in/​vitro using the nematode Caenorhabditis elegans. The activity could be
detected only in 50% methanol extract which on further bioactivity guided
fractionation and chromatographic separation yielded a spirostanol type saponin,
tribulosin and beta/​sitosterol/​D/​glucoside. Both the compounds exhibited
anthelmintic activity with ED50 of 76.25 and 82.50 microg/ml respectively.

PMID: 12587699 [PubMed /​ indexed for MEDLINE]

38: Zhong Yao Cai. 2002 Jun;25(6):420/​2.

[Hypoglycemic effect of saponin from Tribulus terrestris]

[Article in Chinese]

Li M, Qu W, Wang Y, Wan H, Tian C.

School of Life Science, East China Normal University, Shanghai 200062.

OBJECTIVE: To study the hypoglycemic effect of saponin from Tribulus terrestris
L. METHOD: Alloxan was used to establish the diabetic model in mice. Phenformin
Hydrochlride Tables was used as the positive control. The level of glucose,
triglyceride, cholesterol and SOD in serum were determined. RESULTS: The level
of serum glucose could be significantly reduced by saponin from Tribulus
terrestris, which was the rate of 26.25% and 40.67% in normal mice and diabetic
mice in respectively. The level of serum triglyceride could be reduced 23.35%.
The saporin could also decrease the content of serum cholesterol. Serum SOD
activity of the mice was increased by the saponin. CONCLUSION: Saponin from
Tribulue terrestris could significantly reduce the level of serum glucose.

Publication Types:
English Abstract

PMID: 12583337 [PubMed /​ indexed for MEDLINE]

39: Yao Xue Xue Bao. 2001 Oct;36(10):750/​3.

[Studies on the chemical constituents from Tribulus terrestris]

[Article in Chinese]

Xu YJ, Xie SX, Zhao HF, Han D, Xu TH, Xu DM.

Academy of Traditional Chinese Medicine and Materia Medica of Jilin Province,
Changchun 130021, China. yajuanxu@Yahoo.com

AIM: To investigate the chemical constituents of the fruit of Tribulus
terrestris J.. METHODS: Various chromatographic techniques were used to separate
the chemical constituents. ESIMS, IR, 1HNMR, 13CNMR and HMBC were used to
determine the structures of the isolated constituents. RESULTS: Two new
compounds were isolated from the fruits of Tribulus terrestris J. and were
identified as neohecogenin/​3/​O/​beta/​D/​glucopyranosyl
(1/​/​>2)/​beta/​D/​glucopyranosyl (1/​/​>4)/​beta/​D/​galactopyranoside (I);
neohecogenin/​3/​O/​beta/​D/​glucopyranosyl (1/​/​>4)/​beta/​D/​galactopyranoside (II).
CONCLUSION: Compounds I and II are new steroidal saponins.

Publication Types:
English Abstract
Research Support, Non/​U.S. Gov't

PMID: 12579974 [PubMed /​ indexed for MEDLINE]

40: Zhong Yao Cai. 2000 Nov;23(11):675/​7.

[The descriptions, microscopic and TLC identification of Tribulus terrestris L.]

[Article in Chinese]

Zhang J, Wang Z, Zhang X, Jin J, Yang F.

Hongqi Pharmaceutical Factory, Shanghai Medical University, Shanghai 201111.

The descriptions, microscopic and TLC identification of Tribulus terrestris L.
were carried out. It provided evidences for the identification of Tribulus
terrestris L.

Publication Types:
English Abstract

PMID: 12575256 [PubMed /​ indexed for MEDLINE]

41: Di Yi Jun Yi Da Xue Xue Bao. 2002 Nov;22(11):1017/​9.

[Effect of Tribulus terrestris L decoction of different concentrations on
tyrosinase activity and the proliferation of melanocytes]

[Article in Chinese]

Deng Y, Yang L, An SL.

Department of Traditional Chinese Medicine, First Military Medical University,
Guangzhou 510515, China.

OBJECTIVE: To study the effects of the decoction of Tribulus terrestris L on
tyrosinase activity and melanogenesis. METHODS: MTT was employed to study the
proliferation of human melanocytes cultured in vitro, and tyrosinase activity
was estimated by measuring the rate of oxidation of DL/​dopa, after the cells
were treated with different concentrations of decoction of Tribulus terrestris
L. RESULTS: The treatment with the decoction increased the amount of melanin at
higher concentrations but act to the reverse effect at lower concentrations,
with the best concentrations for promoting and inhibiting the cell growth being
1.5 mg/ml (P<0.05) and 0.5 mg/ml (P<0.05) respectively. At high concentrations
the decoction enhanced the tyrosinase activity that was inhibited at low
concentrations. The best concentrations for enhancing and inhibiting tyrosinase
activity were 100 mg/ml (P<0.05) and 10 mg/ml (P<0.05) respectively. CONCLUSION:
Tribulus terrestris L decoction exercises a two/​way regulation on the activity
of tyrosinase and the proliferation of melanocytes.

Publication Types:
English Abstract

PMID: 12433636 [PubMed /​ indexed for MEDLINE]

42: J Ethnopharmacol. 2002 Nov;83(1/​2):153/​9.

Evaluation of natural products on inhibition of inducible cyclooxygenase (COX/​2)
and nitric oxide synthase (iNOS) in cultured mouse macrophage cells.

Hong CH, Hur SK, Oh OJ, Kim SS, Nam KA, Lee SK.

Department of Pharmacy, College of Pharmacy, Ewha Womans University, 11/​1
Daehyun/​dong, Seodaemun/​ku, 120/​750, Seoul, South Korea.

The inhibitors of prostaglandin biosynthesis and nitric oxide production have
been considered as potential anti/​inflammatory and cancer chemopreventive
agents. In this study, we evaluated approximately 170 methanol extracts of
natural products including Korean herbal medicines for the inhibition of
prostaglandin E(2) production (for COX/​2 inhibitors) and nitric oxide formation
(for iNOS inhibitors) in lipopolysaccharide (LPS)/​induced mouse macrophages
RAW264.7 cells. As a result, several extracts such as Aristolochia debilis,
Cinnamomum cassia, Cinnamomum loureirii, Curcuma zedoaria, Eugenia
caryophyllata, Pterocarpus santalius, Rehmania glutinosa and Tribulus terrestris
showed potent inhibition of COX/​2 activity (>80% inhibition at the test
concentration of 10 micro g/ml). In addition, the extracts of A. debilis,
Caesalpinia sappan, Curcuma longa, C. zedoaria, Daphne genkwa and Morus alba
were also considered as potential inhibitors of iNOS activity (>70% inhibition
at the test concentration of 10 micro g/ml). These active extracts mediating
COX/​2 and iNOS inhibitory activities are warranted for further elucidation of
active principles for development of new cancer chemopreventive and/or
anti/​inflammatory agents.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 12413723 [PubMed /​ indexed for MEDLINE]

43: Zhongguo Zhong Yao Za Zhi. 1998 Dec;23(12):709/​11, 762.

[Investigation on resources and commodities of Chinese medicinal herbs of Jili]

[Article in Chinese]

Shi Q, Yu B, Xu L, Xu G.

Department of Pharmacognosy, China Pharmaceutical University, Nanjing 210038.

OBJECTIVE: To make clear the current situation of application of the Chinese
medicinal herbs of Jili. METHOD: The medicinal resources and commodities of the
berbs in some provinces and cities in China were investigated. RESULT: The
species Tribulus terrestris included in <Pharmacopolia of the Peoples Republic
of China> is widely distributed in China. The fruit of T. terrestris which is
widely used in China as a traditional medicine is commonly called Yingjili.
Being only the fruit of Atriplex entralasiatica Ruanjili is produced mainly in
Shandong Province and customarily used as Fructus Tribuli in some areas of
Shandong and Hebei Provinces. CONCLUSION: The current situation of medicinal
application of Jili basically conforms to the requirements of <Pharmacopolia of
the Peoples Republic of China>. The main variety is Yingjili.

Publication Types:
Comparative Study
English Abstract
Research Support, Non/​U.S. Gov't

PMID: 12242817 [PubMed /​ indexed for MEDLINE]

44: Nat Prod Lett. 2002 Aug;16(4):243/​7.

A new steroidal saponin from Tribulus terrestris Linn.

Sun W, Gao J, Tu G, Guo Z, Zhang Y.

Department of Biology, Northwest University, Xi'an, China.

A new steroidal saponin containing six monosaccharides was obtained from the
total plant of Tribulus terrestris and elucidated based on chemical
spectroscopic analysis, especially on 2D/​NMR technology as
26/​0/​beta/​D/​glucopyranosyl/​22/​methoxy/​furostane/​3/​O/​[beta/​D/​xylopyranosyl(l /​/​>
3)/​[beta/​D/​xylopyranosyl(l /​/​> 2)/​beta/​D/​glucopyranosyl(1 /​/​>
4)]]/​[alpha/​L/​rhamnopyranosy(l /​/​> 2)]/​beta/​D/​galactopyranoside.

PMID: 12168759 [PubMed /​ indexed for MEDLINE]

45: Pharmazie. 2002 Jul;57(7):491/​3.

Biologically active steroidal glycosides from Tribulus terrestris.

Bedir E, Khan IA, Walker LA.

National Center for Natural Products Research, University of Mississippi, USA.

The steroidal saponin constituents obtained from Tribulus terrestris were tested
for their antimicrobial and cytotoxic effects. The spirostanol/​based steroidal
saponins 1/​3 exhibited remarkable activity against fungal organisms (Candida
albicans and Cryptococcus neoformans) and cancer cell lines [human malignant
melanoma (SK/​MEL), human oral epidermoid carcinoma (KB), human breast ductal
carcinoma (BT/​549), and human ovary carcinoma (SK/​OV/​3)], while none of the
compounds possessing the furostanol framework 4/​7 showed activity. The most
active spirostanol glycoside, compound 3 exhibited a broad range of anticancer
activity against cell lines, SK/​MEL, KB, BT/​549 and SK/​OV/​3 at IC50s of 6.0,
7.0, 6.0 and 8.2 micrograms/ml, respectively, while compounds 1 and 2 showed
selective cytotoxicity against SK/​MEL at 6.7 and 9.1 micrograms/ml,
respectively. The minimum inhibitory concentrations (MIC) in antifungal bioassay
for compounds 1/​3 varied from 1.5 to 6.2 micrograms/ml, which prompted to
conclude certain structural features are required for these bioactivities.

Publication Types:
Research Support, U.S. Gov't, Non/​P.H.S.

PMID: 12168535 [PubMed /​ indexed for MEDLINE]

46: Life Sci. 2002 Aug 9;71(12):1385/​96.

Aphrodisiac properties of Tribulus Terrestris extract (Protodioscin) in normal
and castrated rats.

Gauthaman K, Adaikan PG, Prasad RN.

Department of Obstetrics and Gynaecology, National University Hospital, National
University of Singapore, Singapore 119704, Singapore.

Tribulus terrestris (TT) has long been used in the traditional Chinese and
Indian systems of medicine for the treatment of various ailments and is
popularly claimed to improve sexual functions in man. Sexual behaviour and
intracavernous pressure (ICP) were studied in both normal and castrated rats to
further understand the role of TT containing protodioscin (PTN) as an
aphrodisiac. Adult Sprague/​Dawley rats were divided into five groups of 8 each
that included distilled water treated (normal and castrated), testosterone
treated (normal and castrated, 10 mg/kg body weight, subcutaneously, bi/​weekly)
and TT treated (castrated, 5 mg/kg body weight, orally once daily). Decreases in
body weight, prostate weight and ICP were observed among the castrated groups of
rats compared to the intact group. There was an overall reduction in the sexual
behaviour parameters in the castrated groups of rats as reflected by decrease in
mount and intromission frequencies (MF and IF) and increase in mount,
intromission, ejaculation latencies (ML, IL, EL) as well as post/​ejaculatory
interval (PEI). Compared to the castrated control, treatment of castrated rats
(with either testosterone or TT extract) showed increase in prostate weight and
ICP that were statistically significant. There was also a mild to moderate
improvement of the sexual behaviour parameters as evidenced by increase in MF
and IF; decrease in ML, IL and PEI. These results were statistically
significant. It is concluded that TT extract appears to possess aphrodisiac
activity probably due to androgen increasing property of TT (observed in our
earlier study on primates).

PMID: 12127159 [PubMed /​ indexed for MEDLINE]

47: Z Naturforsch [C]. 2002 Jan/​Feb;57(1/​2):33/​8.

Two new sulfated furostanol saponins from Tribulus terrestris.

Kostova I, Dinchev D, Rentsch GH, Dimitrov V, Ivanova A.

Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy
of Sciences, Sofia, Bulgaria. kostiv1@yahoo.com

The known furostanol saponins methylprotodioscin and protodioscin and two new
sulfated saponins, sodium salt of
26/​O/​beta/​glucopyranosyl/​22alpha/​methoxy/​(25R)/​furost/​5/​ene/​3beta,26/​diol/​3/​O/​al
pha/​rhamnopyranosyl/​(1/​/​>2)/​beta/​4/​O/​sulfo/​glucopyranoside
(methylprototribestin) and sodium salt of
26/​O/​beta/​glucopyranosyl/​22alpha/​hydroxy/​(25R)/​furost/​5/​ene/​3beta,26/​diol/​3/​O/​al
pha/​rhamnopyranosyl/​(1/​/​>2)/​beta/​4/​O/​sulfo/​glucopyranoside (prototribestin) have
been isolated from the aerial parts of Tribulus terrestris L. growing in
Bulgaria. The structures of the new compounds were elucidated on the basis of 1D
and 2D (DQF/​COSY, TOCSY, HSQC/​TOCSY, HSQC, HMBC, ROESY) NMR data, ESI mass
spectra and chemical transformation.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 11926540 [PubMed /​ indexed for MEDLINE]

48: J Pharm Sci. 2001 Nov;90(11):1752/​8.

Determination of steroidal saponins in Tribulus terrestris by reversed/​phase
high/​performance liquid chromatography and evaporative light scattering
detection.

Ganzera M, Bedir E, Khan IA.

National Center for Natural Products Research, Research Institute of
Pharmaceutical Sciences, The University of Mississippi, University, Mississippi
38677, USA.

This paper describes the first analytical method suitable for the determination
of steroidal saponins in Tribulus terrestris. A separation by high performance
liquid chromatography (HPLC) was achieved by using a reversed/​phase (RP/​18)
column, evaporative light scattering (ELS) detection, and a water/acetonitrile
gradient as the mobile phase. The marker compound, protodioscin, was detected at
a concentration as low as 10.0 microg/mL. Several different samples of plant
material were successfully analyzed, and depending on origin and plant part used
for extraction, significant differences in the composition of the saponins were
observed. The analysis of market products showed considerable variations of 0.17
to 6.49% in the protodioscin content. Copyright 2001 Wiley/​Liss, Inc. and the
American Pharmaceutical Association

Publication Types:
Research Support, Non/​U.S. Gov't
Research Support, U.S. Gov't, Non/​P.H.S.

PMID: 11745732 [PubMed /​ indexed for MEDLINE]

49: Lijec Vjesn. 2001 Jul/​Aug;123(7/​8):177/​8.

[A bronchial polyp and foreign body in an adolescent]

[Article in Croatian]

Raos M, Bumber Z, Kovac K.

Specijalna bolnica za bolesti disnog sustava djece i mladezi, Srebrnjak 100,
10000 Zagreb.

A fifteen/​year/​old adolescent with recurrent pneumonia in the last two years is
presented. The polyp in the lobar bronchus for the right inferior lobe and a
foreign body in posterobasal segmental bronchus were found on bronchoscopy. The
polyp (patHohistologically confirmed granulomatous tissue) and foreign body
(thorny fruit of small caltrops, Tribulus terrestris) were extracted through a
rigid ventilatory bronchoscope. The polyp presumably developed from the thorn of
the fruit stuck in bronchial mucosa.

Publication Types:
Case Reports
English Abstract

PMID: 11729612 [PubMed /​ indexed for MEDLINE]

50: Int J Vitam Nutr Res. 2001 Sep;71(5):293/​301.

Effects of androstenedione/​herbal supplementation on serum sex hormone
concentrations in 30/​ to 59/​year/​old men.

Brown GA, Vukovich MD, Martini ER, Kohut ML, Franke WD, Jackson DA, King DS.

Exercise Biochemistry Laboratory, Department of Health and Human Performance,
Iowa State University, Ames, IA, USA.

The effectiveness of a nutritional supplement designed to enhance serum
testosterone concentrations and prevent the formation of dihydrotestosterone and
estrogens from the ingested androgens was investigated in healthy 30/​ to 59/​year
old men. Subjects were randomly assigned to consume DION (300 mg
androstenedione, 150 mg dehydroepiandrosterone, 540 mg saw palmetto, 300 mg
indole/​3/​carbinol, 625 mg chrysin, and 750 mg Tribulus terrestris per day; n =
28) or placebo (n = 27) for 28 days. Serum free testosterone, total
testosterone, androstenedione, dihydrotestosterone, estradiol, prostate/​specific
antigen (PSA), and lipid concentrations were measured before and throughout the
4/​week supplementation period. Serum concentrations of total testosterone and
PSA were unchanged by supplementation. DION increased (p < 0.05) serum
androstenedione (342%), free testosterone (38%), dihydrotestosterone (71%), and
estradiol (103%) concentrations. Serum HDL/​C concentrations were reduced by 5.0
mg/dL in DION (p < 0.05). Increases in serum free testosterone (r2 = 0.01),
androstenedione (r2 = 0.01), dihydrotestosterone (r2 = 0.03), or estradiol (r2 =
0.07) concentrations in DION were not related to age. While the ingestion of
androstenedione combined with herbal products increased serum free testosterone
concentrations in older men, these herbal products did not prevent the
conversion of ingested androstenedione to estradiol and dihydrotestosterone.

Publication Types:
Clinical Trial
Randomized Controlled Trial
Research Support, Non/​U.S. Gov't

PMID: 11725694 [PubMed /​ indexed for MEDLINE]

51: Zhong Yao Cai. 2001 Aug;24(8):586/​8.

[Effect of the decoction of tribulus terrestris on mice gluconeogenesis]

[Article in Chinese]

Li M, Qu W, Chu S, Wang H, Tian C, Tu M.

School of Life Science, East China Normal University, Shanghai 200062.

The decoction of Tribulus terresteis could significantly inhibit the
gluconeogenesis and influence glycometabolism on normal mice. The decoction
could also reduce the level of triglyceride and the content of cholesterol in
the plasma.

Publication Types:
English Abstract

PMID: 11715199 [PubMed /​ indexed for MEDLINE]

52: J Am Coll Nutr. 2001 Oct;20(5):520/​8.

Endocrine and lipid responses to chronic androstenediol/​herbal supplementation
in 30 to 58 year old men.

Brown GA, Vukovich MD, Martini ER, Kohut ML, Franke WD, Jackson DA, King DS.

Department of Health and Hunan Performance, Iowa State University, Ames 50011,
USA.

OBJECTIVE: The effectiveness of an androgenic nutritional supplement designed to
enhance serum testosterone concentrations and prevent the formation of
dihydrotestosterone and estrogen was investigated in healthy 3 to 58 year old
men. DESIGN: Subjects were randomly assigned to consume a nutritional supplement
(AND/​HB) containing 300/​mg androstenediol, 480/​mg saw palmetto, 450/​mg
indole/​3/​carbinol, 300/​mg chrysin, 1,500 mg gamma/​linolenic acid and 1.350/​mg
Tribulus terrestris per day (n = 28), or placebo (n = 27) for 28 days. Subjects
were stratified into age groups to represent the fourth (30 year olds, n = 20),
fifth (40 year olds, n = 20) and sixth (50 year olds, n = 16) decades of life.
MEASUREMENTS: Serum free testosterone, total testosterone, androstenedione,
dihydrotestosterone, estradiol, prostate specific antigen and lipid
concentrations were measured before supplementation and weekly for four weeks.
RESULTS: Basal serum total testosterone, estradiol, and prostate specific
antigen (PSA) concentrations were not different between age groups. Basal serum
free testosterone concentrations were higher (p < 0.05) in the 30/​ (70.5 +//​ 3.6
pmol/L) than in the 50 year olds (50.8 +//​ 4.5 pmol/L). Basal serum
androstenedione and dihydrotestosterone (DHT) concentrations were significantly
higher in the 30/​ (for androstenedione and DHT, respectively, 10.4 +//​ 0.6
nmol/L and 2198.2 +//​ 166.5 pmol/L) than in the 40/​ (6.8 +//​ 0.5 nmol/L and
1736.8 +//​ 152.0 pmol/L) or 50 year olds (6.0 +//​ 0.7 nmol/L and 1983.7 +//​
147.8 pmol/L). Basal serum hormone concentrations did not differ between the
treatment groups. Serum concentrations of total testosterone and PSA were
unchanged by supplementation. Ingestion of AND/​HB resulted in increased (p <
0.05) serum androstenedione (174%), free testosterone (37%), DHT (57%) and
estradiol (86%) throughout the four weeks. There was no relationship between the
increases in serum free testosterone, androstenedione, DHT, or estradiol and age
(r2 = 0.08, 0.03, 0.05 and 0.02, respectively). Serum HDL/​C concentrations were
reduced (p < 0.05) by 0.14 mmol/L in AND/​HB. CONCLUSIONS: These data indicate
that ingestion of androstenediol combined with herbal products does not prevent
the formation of estradiol and dihydrotestosterone.

Publication Types:
Clinical Trial
Randomized Controlled Trial
Research Support, Non/​U.S. Gov't

PMID: 11601567 [PubMed /​ indexed for MEDLINE]

53: Planta Med. 2001 Mar;67(2):196/​8.

Steroidal saponins from Tribulus terrestris.

Cai L, Wu Y, Zhang J, Pei F, Xu Y, Xie S, Xu D.

Three new steroidal saponins were isolated from the fruits of Tribulus
terrestris, and their structures were elucidated as (25R,S)/​5
alpha/​spirostane/​12/​one/​3 beta/​ol/​3/​O/​beta/​xylopyranosyl(1/​/​>2)/​
[beta/​xylopyranosyl(1/​/​>3)]/​beta/​glucopyranosyl(1/​/​>4)/​[alpha/​rhamno/​
pyranosyl(1/​/​>2)]/​beta/​galactopyranoside; 26/​O/​beta/​glucopyranosyl/​(25S)/​5
alpha/​furostane/​12/​one/​3 beta,22
alpha,26/​triol/​3/​O/​beta/​glucopyranosyl(1/​/​>2)/​beta/​galactopyranoside;
26/​O/​beta/​glucopyranosyl/​(25S)/​5 alpha/​furostane/​12/​one/​3 beta,22
alpha,26/​triol/​3/​O/​beta/​glucopyranosyl(1/​/​>4)/​[alpha/​
rhamnopyranosyl(1/​/​>2)]/​beta/​galactopyranoside, respectively, by spectroscopic
analysis and color reaction.

Publication Types:
Letter

PMID: 11301880 [PubMed /​ indexed for MEDLINE]

54: J Vet Diagn Invest. 2001 Mar;13(2):170/​2.

Experimentally induced cholangiohepatopathy by dosing sheep with fractionated
extracts from Brachiaria decumbens.

Cruz C, Driemeier D, Pires VS, Schenkel EP.

Department of Veterinary Pathology, Federal University of Rio Grande do Sul,
Porto Alegre, Brazil.

Cholangiohepatopathy was induced in 5 lambs by oral administration of extracts
from signal grass (Brachiaria decumbens) in Brazil. Grossly there were pale foci
multifocally distributed throughout the hepatic parenchyma in 4 lambs. The
microscopic changes, which were similar to those produced by other steroidal
sapogenins/​containing plants such as Tribulus terrestris and Panicum spp.,
included multifocal cholangitis, bile duct proliferation, and the presence of
crystals in the biliary system.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 11289217 [PubMed /​ indexed for MEDLINE]

55: J Ethnopharmacol. 2001 Feb;74(2):173/​9.

Screening of Yemeni medicinal plants for antibacterial and cytotoxic activities.

Ali NA, Julich WD, Kusnick C, Lindequist U.

Pharmacognosy Department, Faculty of Medicine and Health Sciences, Sana'a
University, Sana'a, Yemen.

Ethanolic extracts of 20 selected plant species used by Yemeni traditional
healers to treat infectious diseases were screened for their antibacterial
activity against both Gram/​positive and Gram/​negative bacteria, as well as for
cytotoxic activity. Fourteen of the ethanolic extracts showed variable degrees
of antibacterial activity. The active ethanolic extracts were partitioned
between ethyl acetate and water for a first separation. The ethyl acetate
extract of Lawsonia inermis was found to be the most active one against all
bacteria in the test system. Other promising results could be obtained from
extracts of Aloe perryi, Indigofera oblongifolia, Meriandra benghalensis and
Ziziphus spina christi. Additionally, the ethanolic extracts of the 20 plants
under investigation were tested for their cytotoxic effects on FL/​cells using
the neutral red assay. Extracts of Calotropis procera, Chenopodium murale,
Pulicaria orientalis, Tribulus terrestris and Withania somniferum displayed a
remarkable activity.

Publication Types:
Research Support, Non/​U.S. Gov't

PMID: 11167035 [PubMed /​ indexed for MEDLINE]

56: J Nat Prod. 2000 Dec;63(12):1699/​701.

New steroidal glycosides from the fruits of Tribulus terrestris.

Bedir E, Khan IA.

National Center for Natural Products Research, Research Institute of
Pharmaceutical Sciences, and Department of Pharmacognosy, School of Pharmacy,
University of Mississippi, University, Mississippi 38677, USA.

Three new steroidal saponins (1/​3) were isolated from the fruits of Tribulus
terrestris. Their structures were assigned by spectroscopic methods (IR,
HRESIMS, 1D/​ and 2D/​NMR) as
26/​O/​beta/​D/​glucopyranosyl/​(25S)/​5beta/​furost/​20(22)/​en/​3bet a,
26/​diol/​3/​O/​alpha/​L/​rhamnopyranosyl/​(1/​/​>2)/​[alpha/​L/​rhamnopyranosyl/​
(1/​/​>4)]/​beta/​D/​glucopyranoside (1),
26/​O/​beta/​D/​glucopyranosyl/​(25S)/​5beta/​furost/​20(22)/​en/​3bet a,
26/​diol/​3/​O/​alpha/​L/​rhamnopyranosyl/​(1/​/​>2)/​[beta/​D/​glucopyranosyl/​(1
/​/​>4)]/​beta/​D/​galactopyranoside (2), and
25(S)/​5beta/​spirostan/​3beta/​ol/​3/​O/​alpha/​L/​rhamnopyranosyl/​( 1/​/​>2)/​[b
eta/​D/​glucopyranosyl/​(1/​/​>4)]/​beta/​D/​galactopyranoside (3). Compound 3 showed
cytotoxicity against a human malignant melanoma cell line (SK/​MEL).

Publication Types:
Research Support, U.S. Gov't, Non/​P.H.S.

PMID: 11141122 [PubMed /​ indexed for MEDLINE]

57: Int J Sport Nutr Exerc Metab. 2000 Sep;10(3):340/​59.

Effects of anabolic precursors on serum testosterone concentrations and
adaptations to resistance training in young men.

Brown GA, Vukovich MD, Reifenrath TA, Uhl NL, Parsons KA, Sharp RL, King DS.

Exercise Biochemistry Laboratory, Department of Health and Human Performance,
Iowa State University, Ames, IA 50011, USA.

The effects of androgen precursors, combined with herbal extracts designed to
enhance testosterone formation and reduce conversion of androgens to estrogens
was studied in young men. Subjects performed 3 days of resistance training per
week for 8 weeks. Each day during Weeks 1, 2, 4, 5, 7, and 8, subjects consumed
either placebo (PL; n = 10) or a supplement (ANDRO/​6; n = 10), which contained
daily doses of 300 mg androstenedione, 150 mg DHEA, 750 mg Tribulus terrestris,
625 mg Chrysin, 300 mg Indole/​3/​carbinol, and 540 mg Saw palmetto. Serum
androstenedione concentrations were higher in ANDRO/​6 after 2, 5, and 8 weeks (p
<.05), while serum concentrations of free and total testosterone were unchanged
in both groups. Serum estradiol was elevated at Weeks 2, 5, and 8 in ANDRO/​6 (p
<.05), and serum estrone was elevated at Weeks 5 and 8 (p <.05). Muscle strength
increased (p <.05) similarly from Weeks 0 to 4, and again from Weeks 4 to 8 in
both treatment groups. The acute effect of one third of the daily dose of
ANDRO/​6 and PL was studied in 10 men (23 +//​ 4 years). Serum androstenedione
concentrations were elevated (p <.05) in ANDRO/​6 from 150 to 360 min after
ingestion, while serum free or total testosterone concentrations were unchanged.
These data provide evidence that the addition of these herbal extracts to
androstenedione does not result in increased serum testosterone concentrations,
reduce the estrogenic effect of androstenedione, and does not augment the
adaptations to resistance training.

Publication Types:
Clinical Trial
Randomized Controlled Trial
Research Support, Non/​U.S. Gov't

PMID: 10997957 [PubMed /​ indexed for MEDLINE]

58: Planta Med. 2000 Aug;66(6):545/​50.

Three new saponins from Tribulus terrestris.

Xu YX, Chen HS, Liang HQ, Gu ZB, Liu WY, Leung WN, Li TJ.

Department of Phytochemistry, College of Pharmacy, Second Military Medical
University, Shanghai, People's Republic of China.

Three new steroidal saponins 1/​3, together with five known steroidal saponins,
L/​mannitol and an inorganic salt were isolated from Tribulus terrestris L.
(Zygophyllaceae). The structures of the new steroidal saponins were elucidated
as hecogenin
3/​O/​beta/​xylopyranosyl(1/​/​>3)/​beta/​glucopyranosyl(1/​/​>4)/​beta/​galactopyr anoside
(1), hecogenin 3/​O/​beta/​glucopyranosyl(1/​/​>2)/​beta/​glucopyranosyl(1/​/​>4)/​
beta/​galactopyranoside (2) and
3/​O/​[beta/​xylopyranosyl(1/​/​>2)/​[beta/​xylopyranosyl(1/​/̴