Phytopharmacological overview of Tribulus terrestris

Abstract

Tribulus terrestris (family Zygophyllaceae), commonly known as Gokshur or Gokharu or puncture vine, has been used for a long time in both the Indian and Chinese systems of medicine for treatment of various kinds of diseases. Its various parts contain a variety of chemical constituents which are medicinally important, such as flavonoids, flavonol glycosides, steroidal saponins, and alkaloids. It has diuretic, aphrodisiac, antiurolithic, immunomodulatory, antidiabetic, absorption enhancing, hypolipidemic, cardiotonic, central nervous system, hepatoprotective, anti-inflammatory, analgesic, antispasmodic, anticancer, antibacterial, anthelmintic, larvicidal, and anticariogenic activities. For the last few decades or so, extensive research work has been done to prove its biological activities and the pharmacology of its extracts. The aim of this review is to create a database for further investigations of the discovered phytochemical and pharmacological properties of this plant to promote research. This will help in confirmation of its traditional use along with its value-added utility, eventually leading to higher revenues from the plant.

Full text

Pharmacognosy Reviews | January-June 2014 | Vol 8 | Issue 15 45
PHCOG REV.
Phytopharmacological overview of Tribulus terrestris
Saurabh Chhatre, Tanuja Nesari, Gauresh Somani1, Divya Kanchan1, Sadhana Sathaye1
Department of Dravyaguana, Centre for Post Graduate Studies and Research in Ayurveda, Tilak Ayurveda Mahavidyalaya, Pune,
1Pharmaceutical Sciences and Technology, Pharmacology Research Lab‑II, Institute of Chemical Technology, (University under Section 3 of
UGC Act‑1956, Elite Status and Centre of Excellence ‑ Government of Maharashtra, TEQIP Phase II Funded), Mumbai, Maharashtra, India
Submitted: 16‑06‑2013 Revised: 16‑06‑2013 Published: 20‑01‑2014
REVIEW ARTICLE
Tribulus terrestris (family Zygophyllaceae), commonly known as Gokshur or Gokharu or puncture vine, has been used for a
long time in both the Indian and Chinese systems of medicine for treatment of various kinds of diseases. Its various parts
contain a variety of chemical constituents which are medicinally important, such as avonoids, avonol glycosides, steroidal
saponins, and alkaloids. It has diuretic, aphrodisiac, antiurolithic, immunomodulatory, antidiabetic, absorption enhancing,
hypolipidemic, cardiotonic, central nervous system, hepatoprotective, anti‑inammatory, analgesic, antispasmodic,
anticancer, antibacterial, anthelmintic, larvicidal, and anticariogenic activities. For the last few decades or so, extensive
research work has been done to prove its biological activities and the pharmacology of its extracts. The aim of this review
is to create a database for further investigations of the discovered phytochemical and pharmacological properties of this
plant to promote research. This will help in conrmation of its traditional use along with its value‑added utility, eventually
leading to higher revenues from the plant.
Key words: Pharmacology, saponin, tribulus terrestris
INTRODUCTION
The genus Tribulus, belonging to family Zygophyllaceae,
comprises about 20 species in the world, of which three species,
viz. Tribulus cistoides, Tribulus terrestris, and Tribulus alatus, are of
common occurrence in India.[1] Among them, T. terrestris (TT)
is a well‑patronized medicinal herb by Ayurvedic seers as well as
by modern herbalists.[2] The plant is used individually as a single
therapeutic agent or as a prime or subordinate component of
many compound formulations and food supplements. It is an
annual shrub found in Mediterranean, subtropical, and desert
climate regions around the world, viz. India, China, southern
USA, Mexico, Spain, and Bulgaria.[3,4]
Taxonomical classication
• Kingdom: Plantae
• Division: Phanerogams
• Subdivision: Angiospermae
• Class: Dicotyledonae
• Subclass: Polypetalae
• Series:Disciorae
• Order: Giraniales
• Family: Zygophyllaceae
• Genus: Tribulus
• Species: terrestris Linn.
PLANT PROFILE
TT is commonly known as Gokshur (Sanskrit); puncture vine,
land (or small) caltrops (English); Gokharu (Hindi); Bethagokharu
or Nanagokharu (Gujarathi); Nerinjil (Tamil); and Khar‑e‑khusak
khurd (Urdu). It is distributed along a wide geographic perimeter.
It is found all over India up to 11,000 ft in Kashmir, Ceylon,
and all warm regions of both hemispheres. It is a common weed
ofthepasturelands,roadsides,andotherwasteplaces,chiey
in hot, dry, and sandy regions including West Rajasthan and
Gujarat in India.[5]
Botanical description T. terrestris
It is small prostrate, 10‑60 cm height, hirsute or silky hairy shrub.
Leavesareopposite,oftenunequal,paripinnate;pinnaefromve
to eight pairs, elliptical or oblong lanceolate [Figure 1]. Flowers
are yellow in color. Its carpel fruits are of characteristic, stellate
shape,somewhat round‑shaped,compressed, vecornered,
and covered with princkles of very light yellow color. There are
several seeds in each crocus with transverse partitions between
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DOI:
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ABSTRACT
Address for correspondence:
Dr. Saurabh P. Chhatre, D: 32, 2/1, Sagar Sangam CHS,
Sector ‑ 4, Nerul, Navi Mumbai ‑ 400 706, Maharashtra, India.
E‑mail: saurabh_chhatre@yahoo.com

Chhatre, et al.: Review on tribulus terrestris
46 Pharmacognosy Reviews | January-June 2014 | Vol 8 | Issue 15
them. The seeds are oily in nature. When fresh, the root is slender,
brous,cylindrical,frequentlybranched,bearinganumberof
small rootlets and is of light brown color. Fruits and roots are
mainly used as a folk medicine for the treatment of various
ailments. Root occurs in pieces, 7‑18 cm long and 0.3‑0.7 cm
indiameter,cylindrical,brous,frequentlybranched,bearinga
number of small rootlets, tough, woody, yellow to light brown
in color, surface rough due to the presence of small nodules;
fracturebrous;odor aromatic;taste sweetishastringent. The
fruits of the herb are known as “Chih‑hsing” in China or goat
head in USA. The spiky fruit looks like the cloven hoof of a
cow and, hence, is known as go‑ksura (cow‑hoof). Fruits are
faint greenish yellow with spines [Figure 2]. They are globose,
consistingof ve,nearlyglabrous,muriculate,wedge‑shaped,
woody cocci, each with two pairs of hard sharp spines, one
pair longer than the other. Tips of spines almost meet in pairs
together forming pentagonal framework around the fruit. Outer
surface of the schizocarp is rough. There are several seeds in
each coccus, with transverse partitions between them. Odor of
fruits is faintly aromatic and taste is slightly acrid.
PROPERTIES AND ACTIONS MENTIONED IN
AYURVEDA
• Rasa (taste based on activity): Madhura (sweet)
• Guna (properties): Guru (heavy to digest),
Snigdha (unctuous)
• Veerya (potency): Sheeta (cooling)
• Vipaka (taste after digestion based on activity):
Madhura (sweet)
• Karma (pharmacological actions):
Brumhana (nourishing), Vatanut (paciesVata‑dsha),
Vrusya (aphrodisiac), Ashmarihara (removes urinary
stone), Vastishodhana (cures bladder ailments).
CHEMICAL CONSTITUENTS
The preliminary phytochemical study of TT revealed the
presenceof  saponins, avonoids,glycosides, alkaloids,and
tannins.[6] According to literature data, the saponin composition
and the saponin content of TT from different geographic
regions is different.[7] Kostova et al. studied the chemistry and
bioactivity of saponins in TT. They reported that furostanol
and spirostanol saponins of tigogenin, neotigogenin, gitogenin,
neogitogenin, hecogenin, neohecogenin, diosgenin, chlorogenin,
ruscogenin, and sarsasapogenin types are frequently found in
this plant. In addition, four sulfated saponins of tigogenin and
diosgenin type were also isolated. Majorly present are furostanol
glycosides including protodioscin and protogracillin, of which
protodioscin is the most dominant saponin and spirostanol
glycosides are present in small quantities.[7,8] Wu et al. found that
thequantityofmainavonoidsisabout1.5timesthatofmain
saponins.ThisindicatedthattheavonoidcontentsinTTshould
be studied, developed, and further used.[9] Bhutani et al. isolated
kaempferol, kaempferol‑3‑glucoside, kaempferol‑3‑rutinoside,
and tribuloside [kaempferol‑3‑β‑d‑(6″‑p‑coumaroyl)
glucoside]from leavesas well as fruits and identied them
by spectroscopic analysis.[10] Louveaux et al. detected 18
avonoids(caffeoylderivatives,quercetinglycosides,including
rutin and kaempferol glycosides) using high‑performance liquid
chromatography (HPLC) in four Tribulus species leaf extracts.[11]
Yang et al. optimized the extraction condition using orthogonal
experiment.[12] Matin Yekta et al. isolated three flavonoid
glycosides, viz. quercetin 3‑O‑glycoside, quercetin 3‑O‑rutinoside,
and kaempferol 3‑O‑glycoside from the aerial parts of T. terrestris
L. var. orientalis (Kerner) G. Beck in the northeast of Iran.[13]
Raja and Venkataraman identified flavonoids from the
petroleum ether and chloroform extracts of fresh fruits of
TT from India using ethyl acetate: benzene (1:9) solvent
system. These flavonoids were not detected in the fruit
extracts of other variety, namely T. alatus. Hence, presence
of such pharmacognostic constituents can be used as a
diagnostictool in the identication of  thespecies and study
of contamination/adulteration.[14,15] Tian Shung et al. isolated
and characterized three new compounds, terrestribisamide,
25R‑spirost‑4‑en‑3, 12‑dione, and tribulusterine, together with
10 known compounds, N‑p‑coumaroyltyramine, terrestriamide,
hecogenin, aurantiamide acetate, xanthosine, fatty acid ester, ferulic
acid, vanillin, p‑hydroxybenzoic acid, and β‑sitosterol, from the
dried fruits of TT.[16] The alkaloids present are harmane and
norharmane. The β‑carboline alkaloid, tribulusterine, is present
in minor quantities in fruits.[17] Gas chromatography‑mass
spectrometry analysis of methanolic extract of the whole
plant of TT revealed the presence of α‑Amyrin as the
major constituent and seven minor constituents, which are
3,7,11,15‑tetramethyl‑2‑hexadecen‑1‑ol, n‑hexadecadienoic acid,
hexadecadienoic acid ethyl ester, phytol, 9,12‑octadecadienoic
acid, 9,12,15‑octadecatrienoic acid, and 1,2‑benzenedicarboxylic
acid disoctyl ester. Sterols such as β‑sitosterols and stigmasterols
were also found to be present.[18]
TRADITIONAL USES
TT is used in folk medicines as a tonic, aphrodisiac, palliative,
astringent, stomachic, antihypertensive, diuretic, lithotriptic,
and urinary disinfectant. The dried fruit of the herb is very
effective in most of the genitourinary tract disorders. It is a vital
constituent of Gokshuradi Guggul, a potent Ayurvedic medicine
used to support proper functioning of the genitourinary
tract and to remove the urinary stones. TT has been used for
centuries in Ayurveda to treat impotence, venereal diseases, and
sexual debility. In Bulgaria, the plant is used as a folk medicine
for treating impotence. In addition to all these applications,
the Ayurvedic Pharmacopoeia of India attributes cardiotonic
properties to the root and fruit. In traditional Chinese medicine,
the fruits were used for treatment of eye trouble, edema,
abdominal distension, emission, morbid leukorrhea, and sexual
dysfunction. TT is described as a highly valuable drug in the

Chhatre, et al.: Review on tribulus terrestris
Pharmacognosy Reviews | January-June 2014 | Vol 8 | Issue 15 47
Shern‑Nong Pharmacopoeia (the oldest known pharmacological
work in China) in restoring the depressed liver, for treatment
offullnessinthechest,mastitis,atulence,acuteconjunctivitis,
headache, and vitiligo. In Unani medicine, TT is used as diuretic,
mild laxative, and general tonic.[19]
PHARMACOLOGICAL ACTIVITIES
Diuretic activity
The diuretic properties of TT are due to large quantities of
nitrates and essential oil present in its fruits and seeds. The
diuretic activity can also be attributed to the presence of
potassium salts in high concentration. Ali et al. tested the aqueous
extract of TT prepared from its fruit and leaves in rat diuretic
model and strips of isolated Guinea pig ileum were used for
the contractility test. The aqueous extract of TT, in oral dose
of 5 g/kg, elicited a positive diuresis, which was slightly more
than that of furosemide. Sodium and chloride concentrations in
the urine were increased. The increased tonicity of the smooth
muscles, which was produced by TT extract, together with its
diuretic activity helped in the propulsion of stones along the
urinary tract.[20] Saurabh et al. evaluated the different extracts
of TT fruits, viz. aqueous, methanolic, Kwatha‑high strength,
Kwatha‑low strength, and Ghana powder, for diuretic activity in
rats. Kwatha‑high strength showed diuretic effect comparable
to that of the reference standard frusemide and also exhibited
additional advantage of potassium‑sparing effect.[21] The diuretic
action of TT makes it useful as an anti‑hypertensive agent.
Aphrodisiac activity
Adaikan et al. reported that the TT extract exhibited a pro‑erectile
effect on rabbit corpus cavernosum smooth muscle ex vivo after
oral treatment at doses of 2.5, 5, and 10 mg/kg body weight
for8weeks.Asignicantrelaxationof24%wasobservedwith
nitroglycerine in the corpus cavernosum smooth muscle tissue.
Similarly,10%relaxationwasobservedwithbothacetylcholine
andelectricaleldstimulation,respectively,followingtheabove
treatment with TT in rabbits. The enhanced relaxant effect
observed is due to increase in the release of nitric oxide from
the endothelium and nitrergic nerve endings, which may account
for its claims as an aphrodisiac.[22] Singh et al. evaluated the acute
and repeated dose administration of lyophilized aqueous extract
of the dried fruits of TT (LAET) at doses of 50 and 100 mg/kg
of body weight as a sexual enhancer in the management of
sexual dysfunction in male rat. A dose‑dependent improvement
in sexual behavior was observed with the LAET treatment,
which was more prominent on chronic administration of LAET.
Asignicant increasein serum testosteronelevels too was
observed.Thesendingsconrmthetraditionaluseof TTas
a sexual enhancer in the management of sexual dysfunction in
males.[23] Ethanolic extract of TT exhibited protective effect
against cadmium‑induced testicular damage. The protective effect
appears to be mediated directly either through inhibition of
testicular tissue peroxidation by antioxidant and metal chelating
activity or by stimulating the testosterone production from Leydig
cells.[24]TT extract(100‑300mg/l) treatment toa sh colony
was found to be effective in increasing the proportion of males
inthepopulation.Itwasfoundthattestesof shtreatedwith
TT extract showed all stages of spermatogenesis with improved
growth performance in Poeciliata reticulatash species.[25] The
two main components of the saponin fraction from TT, namely
protodioscin and protogracillin, are responsible for the observed
biological aphrodisiac activity.[26] It is suggested that protodioscin
works by increasing the conversion of testosterone into the
potent dehydrotestosterone, which stimulates not only increase
in the sex drive but also the production of red cells from bone
marrow along with muscular developments contributing to
improvement of blood circulation and the oxygen transport
systems, leading to optimal health.
Antiurolithic activity
An ethanolic extract of TT fruits was tested in urolithiasis induced
by glass bead implantation in albino rats by Anand et al. It exhibited
signicantdose‑dependent protection againstdeposition of 
calculogenic material around the glass bead, leukocytosis, and
elevation in serum urea levels. Subsequent fractionation of
the ethanol extract led to decrease in activity.[27] Various other
biochemical parameters in urine, serum, and the histopathology
of urinary bladder were restored in a dose‑dependent manner.
A novel antilithic protein having cytoprotective potency and of
molecularweight~60kDawaspuriedfromTT.[28] Aggarwal
tested the activity of TT on the nucleation and growth of calcium
oxalate (CaOx) crystals as well as on oxalate‑induced cell injury of
NRK 52E renal epithelial cells. The experiments revealed that TT
extract not only has a potential to inhibit nucleation and growth
of the CaOx crystals but also has a cytoprotective role.[28] TT was
found to inhibit stone formation in various models of urolithiasis
using sodium glycolate and ethylene glycol.[29]
Glycolate oxidase (GOX) is one of the principal enzymes
involved in the pathway of oxalate synthesis converting glycolate
toglyoxylatebyoxidationandnallytooxalate.Theantiurolithic
activity of TT is attributed to its GOX inhibition. Quercetin
and kaempherol, the active components of TT, were found
to be non‑competitive and competitive inhibitors of GOX,
respectively.[30]
Immunomodulatory activity
Saponins isolated from the fruits of TT demonstrated
dose‑dependent increase in phagocytosis, indicating stimulation
of nonspecic immune response.Analcoholic extract of the
wholeplantof TTexhibitedasignicantdose‑dependentincrease
in humoral antibody titre and delayed type hypersensitivity
response,indicatingincreasedspecicimmuneresponse.[31]
Antidiabetic activity
Saponin from TT possesses hypoglycemic properties.[32]
TTsignicantly reducedthe levelof serumglucose, serum
triglyceride, and serum cholesterol, while serum superoxide
dismutase (SOD) activity was found to be increased in
alloxan‑induced diabetic mice. The decoction of TT showed

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48 Pharmacognosy Reviews | January-June 2014 | Vol 8 | Issue 15
inhibition of gluconeogenesis in mice.[33,34] TT ethanolic
extract at 2 g/kg body weight produced protective effect in
streptozotocin‑induced diabetic rats by inhibiting oxidative
stress.Ethanolicextract of  TT exhibited 70% inhibitionof 
α‑glucosidase at 500 µg/ml using maltose as the substrate and
100%inhibition of  aldose reductaseat adose of  30 µg/ml
using dl‑glyceraldehyde as the substrate.[35]Asignicantdecrease
in the postprandial blood glucose level of rats was found after
administration of saponin from TT. TT produced dilation of
coronary artery and improved the coronary circulation. It is
therefore recommended in Ayurveda for the treatment of angina
pectoris and other cardiac complications of diabetes. Thus, TT
couldbebenecialinthetreatmentof diabetesbyloweringblood
glucose, lipid levels, and by its antioxidant mechanism.
Absorption enhancer
Ethanolic extract of TT enhanced the absorption of metformin
hydrochloride,aBiopharmaceuticsClassicationSystem(BCS)
class III drug, in everted sac technique using goat intestine, due
to the presence of saponins in the extract.[36]
Hypolipidemic activity
The aqueous extract of the fruits of TT was evaluated for
their hypolipidemic activity in Wistar albino rats. A dose of
580 mg/kg of the extract was found to decrease cholesterol‑induced
hyperlipidemia, with a decrease in cholesterol, triglycerides, low
density lipoprotein (LDL), very low density lipoprotein (VLDL),
and atherogenic index (AI), and an increase in high density
lipoprotein (HDL) levels in the blood. Hypolipidemic activity
may be due to the presence of phenolic compounds leading to
increased lipoprotein lipases in the muscles and decreased activity
in the adipose tissues, thus indicating that plasma triglycerides are
utilized for energy production by the muscle and not for energy
storage by the adipose tissue.[37] The pleotropic effect of TT at
5mg/kg/daydosefor8weeksonthelipidproleandvascular
endothelium of the abdominal aorta in New Zealand rabbits fed
on a cholesterol‑rich diet was studied. It was found that dietary
intakeoftheherbsignicantlyloweredtheserumlipidprole,
decreased endothelial cellular surface damage as well as ruptures,
and partially repaired the endothelial dysfunction resulting from
hyperlipidemia.[38]
Saponins from TT were studied on diet‑induced hyperlipidemia
in mice for its preventive and therapeutic effect. The preventive
effect was demonstrated by decrease in the levels of serum total
cholesterol (TC) and LDL‑cholesterol. It also reduced the liver
TC and triglycerides and increased the activity of SOD in the
liver.Itshowedtherapeuticeffectbysignicantlyreducingthe
serum TC and liver TC.[39]
Activity in cardiac disorders
TTshowedsignicanteffectinthetreatmentof variouscardiac
diseases including coronary disease, myocardial infarction,
cerebral arteriosclerosis, and the sequelae of cerebral thrombosis.
Zhang et al. evaluated the protective effect of tribulosin from
TT against cardiac ischemia/reperfusion injury to study the
underlying mechanism in rats. Tribulosin protected myocardium
against ischemia/reperfusion injury through protein kinase C
epsilon activation.[40]Tribulosintreatmentresultedinasignicant
reduction of malondialdehyde, aspartate transaminases, creatine
kinase, lactate dehydrogenase activity, and myocardial apoptosis
rate. It increased the activity of SOD. Crude saponin fraction of
thisplanthasshownsignicanteffectsinthetreatmentofvarious
cardiac diseases including hypertension, coronary heart disease,
myocardial infarction, cerebral arteriosclerosis, and thrombosis.
It also has been shown that the aqueous extract of TT fruits has
signicantacetylcholinesterase (ACE) inhibitoryeffects in vitro.
Methanolic and aqueous extracts of TT are shown to possess
signicantantihypertensiveactivitybydirectarterialsmoothmuscle
relaxation and membrane hyperpolarization in spontaneously
hypertensive rats.[41] TT also appears to protect the heart cells and
may even improve the heart function following a heart attack.[42]
Central nervous system (CNS) activity
Swiss Albino mice demonstrated antidepressant and anxiolytic
activity on administration of 260 mg/kg dose of Rasayana Ghana
tablet comprising three potent well‑established rejuvenator
herbs, viz. Tinospora cordifolia (stem), Emblica ofcinalis (fruit), and
TT (fruit and root), present in equal quantities in the tablet.
It was suggested that harmine, a β‑carboline alkaloid present
in TT, is one of the main active constituents that contributes
to the above‑mentioned activities. Harmine is an inhibitor of
monoamine oxidase which helps to increase level of dopamine
in the brain.[43]
Hepatoprotective activity
The TT extract (250 mg/kg) showed a remarkable hepatoprotective
activity against acetaminophen‑induced hepatotoxicity in
Oreochromis mossambicussh.Theelevatedbiochemicalparameters
and decreased level of reduced glutathione enzymes were
normalized by treatment with TT extract (250 mg/kg) for
acetaminophen‑inducedtoxicityinfreshwatersh.[44]
Antiinammatory activity
The ethanolic extract of TT inhibited the expression of
cyclooxygenase‑2 (COX‑2) and inducible nitric oxide
synthase (iNOS) in lipopolysaccharide‑stimulated RAW264.7 cells.
It also suppressed the expression of proinflammatory
cytokines such as tumor necrosis factor‑alpha (TNF‑α) and
interleukin (IL)‑4 in macrophage cell line. Thus, the ethanolic
extract of TT inhibits the expression of mediators related to
inammationandexpressionofinammatorycytokines,which
hasabenecialeffectonvariousinammatoryconditions.[45] The
methanolic extract of TT showed a dose‑dependent inhibition of
ratpawvolumeincarrageenan‑inducedinammationinrats.[46]
Analgesic activity
Analgesic activities of TT were studied in male mice using
formalin and tail flick test. The study indicated that the
methanolic extract of TT at a dose of 100 mg/kg produced
analgesic effect. This analgesic effect of the TT extract may be
mediated centrally and/or peripherally. Effect of the extract was

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Pharmacognosy Reviews | January-June 2014 | Vol 8 | Issue 15 49
lower than morphine and higher than acetylsalicylic acid (aspirin)
in both tests. Pretreatment of animals with opioid receptor
antagonist, naloxone, did not change the analgesic effect of
the extract in both tests; therefore, the involvement of opioid
receptors in the analgesic effect of TT is excluded. However,
the other mechanisms responsible for the analgesic effect of
TT remain to be investigated. The results of ulcerogenic studies
indicate that the gastric ulcerogenecity of TT is lower than
indomethacin in the rat’s stomach.[47]
Antispasmodic activity
The lyophilized saponin mixture of the plant exhibited a
signicantdecreaseinperistalticmovementsofrabbitjejunum
preparation in a dose‑dependent manner. These results showed
that the saponin mixture may be useful for smooth muscle spasms
or colic pains.[48]
Anticancer activity
Chemopreventive potential of the aqueous extract of the
root and fruit of TT at 800 mg/kg on 7,12‑dimethylbenz
(a) anthracene (DMBA) and croton oil induced papillomagenesis
inSwissalbinomalemicedepictedsignicantreductionintumor
incidence, tumor burden, and cumulative number of papillomas,
alongwith asignicant increase in the average latentperiod in
mice treated orally with TT suspension continuously at pre‑, peri‑,
and post‑initiation stages of papillomagenesis, as compared to the
control group treated with DMBA and croton oil alone. The root
extract of TT exhibited better chemopreventive potential than the
fruit extract at the same concentration (800 mg/kg body weight) in
skin papillomagenesis in mice.[49] The aqueous extract of TT blocked
proliferation in HepG2 cells and could also induce apoptosis
through the inhibition of nuclear factor kappa‑light‑chain‑enhancer
of activatedB cells (NF‑ĸB) signaling. Thus,TT has clinical
therapeutic effects against liver cancer cells.[50] The aqueous root
extractof  TT produced signicant radioprotection whengiven
orally (800 mg/kg) for seven consecutive days prior to gamma
irradiation. TT extract pretreatment protected against radiation
damage by inhibiting radiation‑induced glutathione depletion
and decreasing lipoperoxidation level in the liver of mice.[51]
Saponins isolated from the aerial parts of TT were studied for their
cytostatic/cytototoxicactivityonhumanbroblasts.Theeffectswere
determined by 3‑(4,5‑dimethylthiazol‑2‑yl)‑2,5‑diphenyltetrazolium
bromide (MTT) analysis and 3Hthymidine incorporation to assess
cell viability and proliferation, respectively. Saponins showed a
dose‑dependent decrease in 3Hthymidine incorporation into the
DNA, indicating decreased proliferation. Similarly, they were found
tobelesstoxicfornormalhumanskinbroblasts.Themechanism
of action involves up‑ and down regulation of polyamines’
homeostasis, suppression of proliferation, and induction of
apoptosis.[52]
Antibacterial activity
All parts (fruits, stems, leaves, and roots) of Turkish and Iranian
TT showed antibacterial activity against Enterococcus faecalis,
Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa, in
contrast to the aerial parts of Yemeni TT which had no detectable
antibacterial activity against these bacteria, while only the fruits
and leaves of Indian TT were active exclusively against E. coli and
S. aureus. These different results relating to the antibacterial activity
of TT may be due to using different geographic sources of the
plant, types of strains, and assay methods. The methanolic extract
of fruits of TT was found to be most active against gram‑positive
and gram‑negative bacteria, while moderate activity was observed
in its petroleum ether extract and chloroform extract.[53,54]
Anthelmintic activity
The methanolic extract of TT was found to be more effective
than the petroleum ether, chloroform, and water extracts for
in vitro anthelmintic activity on the nematode Caenorhabditis elegans.
Furtherbioactivity‑guidedfractionationconrmedtribulosinand
β‑sitosterol‑d‑glucoside to be the active components with ED50
of 76.25 and 82.50 µg/ml, respectively.[55,56]
Larvicidal activity
The petroleum ether extract of the leaves of TT exhibited better
larvicidal activity against the third instar larvae and adults of
the mosquito, Aedes aegypti, which is the vector of dengue fever,
with LC50 of 64.6 ppm as compared to the crude ethanol and
Figure 1: Whole plant of tribulus terrestris Figure 2: Fruit of tribulus terrestris plant

Chhatre, et al.: Review on tribulus terrestris
50 Pharmacognosy Reviews | January-June 2014 | Vol 8 | Issue 15
acetone extracts.[57,58]
Anticariogenic activity
The ethanolic extract of fruits of TT (0.1‑0.5 mg/ml) possesses
signicantanticariogenic activityagainst Streptococcus mutans,
the pathogen responsible for dental caries. The growth, acid
production, adhesion, and water‑insoluble glucan synthesis of
S. mutans were signicantly inhibited in the presence of the
ethanol extract of TT. Further studies are necessary to elucidate
the active constituents of TT responsible for such activities.[59]
Recommended dose of TT in Ayurveda
• Fruit: 3‑6 g of the drug in powder form; 20‑30 g of
the drug for decoction
• Root: 20‑30 g of the drug for decoction[60].
Important formulations
Gokshuradi Guggulu, Trikantak Ghruta, Drakshadi Choorna, Rasayana
Choorna, Gokshuradi Kwatha, Dashamoola Kwatha[60]
CONCLUSION
TT,a commonly available weed,is of signicant value in the
traditional systems of medicine, viz. Ayurveda, Chinese, Siddha,
and Unani. TT is also a reputed herb in the folk medicine of
many countries for a number of diseases. The whole plant of
TT has been explored exhaustively for its phytochemical and
pharmacological activities such as diuretic, aphrodisiac, antiurolithic,
immunomodulatory, antihypertensive, antihyperlipidemic,
antidiabetic, hepatoprotective, anticancer, anthelmintic, antibacterial,
analgesic, and anti‑inflammatory. Considering the available
literature on TT, the plant could have a potential as a herbal
medicine for effective blood pressure control due to its diuretic
activity (potassium sparing), antihyperlipidemic activity, and
cardioprotective activity. Though TT has been used extensively over
thecenturiesandcurrentlyscienticevidencewithrespecttoits
pharmacological activities is also being generated, more studies at
the molecular level are needed to further understand the mechanism
bywhichitmodiesthediseasecondition.Thepharmacological
experiments performed on the plant must be extended to the next
level of clinical trials to generate novel drugs. This will help TT
in achieving a status of medicine or to be prescribed as a dietary
supplement in various disease conditions.
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How to cite this Article: Chhatre S, Nesari T, Somani G, Kanchan
D, Sathaye S. Phytopharmacological overview of
Tribulus
terrestris
. Phcog Rev 2014;8:45‑51.
Source of Support: Nil, Conict of Interest: None declared