Tribulus terrestris Linn.: A review article

Abstract

Tribulus terrestris has long been used as a tonic and aphrodisiac in Unani system of medicine. It has been used in India and Pakistan as a treatment for impotence and as a stimulant to enhance sexual drive and performance (Brown et al., 2001). T. terrestris has diuretic and uricosuric effects. In this review article introduction, description, active constituents and medicinal uses of T. terrestris have been given herewith.

Full text

Journal of Medicinal Plants Research Vol. 5(16), pp. 3601-3605, 18 August, 2011
Available online at http://www.academicjournals.org/JMPR
ISSN 1996-0875 ©2011 Academic Journals
Review
Tribulus terrestris Linn.: A review article
M. Akram1, H. M. Asif2, Naveed Akhtar2, Pervaiz A. Shah3, M. Uzair4, Ghazala Shaheen2,
Tahira Shamim2, S. M. Ali Shah2 and Khalil Ahmad2
1Department of Basic Medical Sciences1, Faculty of Eastern Medicine, Hamdard University Karachi, Pakistan.
2College of Conventional Medicine, Faculty of Pharmacy and Alternative Medicine, The Islamia University of
Bahawalpur, Pakistan.
3University College of Pharmacy, Punjab University Lahore, Pakistan.
4Faculty of Pharmacy, Bahauddin Zakariya University Multan, Pakistan.
Accepted 22 February, 2011
Tribulus terrestris has long been used as a tonic and aphrodisiac in Unani system of medicine. It has
been used in India and Pakistan as a treatment for impotence and as a stimulant to enhance sexual
drive and performance (Brown et al., 2001). T. terrestris has diuretic and uricosuric effects. In this
review article introduction, description, active constituents and medicinal uses of T. terrestris have
been given herewith.
Key words: Tribulus terrestris, active constituents, medicinal uses.
INTRODUCTION
Tribulus terrestris L. is found to be growing in subtropical
areas around the world. It is commonly known as Gokhru
belonging to the family Zygophyllaceae, widely distributed
throughout India. The fruits of T. terrestris L. have been
used in traditional Chinese medicine for the treatment of
eye trouble, edema, abdominal distention, emission, mor-
bid leucorrhea, sexual dysfunction and veiling. Roots and
fruits are useful in rheumatism, piles, renal and vesical
calculi, menorrhagia, impotency, premature ejaculation,
general weakness etc. The fruits, flowers and leaves are
shown in Figures 1 and 2. It is a very potent diuretic and
tonic drug (Selvam, 2008). The steroidal saponin consti-
tuents obtained from T. terrestris exhibit antimicrobial and
cytotoxic effects (Bedir et al., 2002; Protich et al., 1983;
Chu et al., 2003; Li et al., 2002). The phytochemical
investigation of the aerial parts of T. terrestris of 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 (Conrad et al.,
2004). An HPLC-ELSD-ESI-MS method has been
developed for the analysis of the steroidal saponins in the
aerial parts of T. terrestris (De Combarieu et al., 2003).
Saponins from T. terrestris (STT) exert its cytotoxic effect
*Corresponding author. E-mail: makram_0451@hotmail.com.
Tel: 92-021-6440083. Fax: 92-021-6440079.
on liver BEL-7402 cells by inducing apoptosis (Sun et al.,
2004). T. terrestris exerts significantly antihyperlipidemic
effects (Jiji et al., 2009). Chronic intake of a complex
dietary supplement containing DHEA (Jameel et al.,
2004), androstenedione and herbal extracts increases
serum androgen levels, it has minimal effect on immune
function in middle aged men (Kohut et al., 2003; Protich
et al., 1983). Gynaecomastia has also been reported due
to intake of a T. terrestris (Jameel et al., 2004).
T. terrestris is a natural stimulant of Luteinizing hor-
mone (LH) which signals the body to produce more of its
own testosterone (Neychev et al., 2005; Antonio, 2000).
Clinical studies showed T. terrestris improved reproduce-
tive function, including increased concentration of
hormones such as estradiol, with testosterone being very
slightly influenced, thereby improving reproductive func-
tion, libido and ovulation (Gauthaman, 2002; Tomova,
1978).
Tribulus terrestris Linn.
Tibbi name: Gokhru
English name: Caltrop
Botanical name: T. terrestris
Family: Zygphyllaceae
Part used: Seeds

3602 J. Med. Plant. Res.
Figure 1. Fruit of T. terrestris.
Figure 2. Leaves and flowers of T. terrestris.
Description
It is a tap rooted herbaceous perennial plant that grows
as a summer annual in colder climates. The stems
radiate from the crown to a diameter of about 10 cm to
over 1 m, often branching. They are usually prostrate,
forming flat patches, though they may grow more
upwards in shade or among taller plants. The leaves are
pinnately compound with leaflets less than a quarter-inch
long. The flowers are 4 to10 mm wide, with five lemon-
yellow petals. A week after each flower blooms, it is
followed by a fruit that easily falls apart into four or five
single-seeded nut lets.
The nutlets or "seeds" are hard and bear two to three
sharp spines, 10 mm long and 4 to 6 mm broad point-to-
point. It is a trailing and spreading herb, densely covered
with minute hair. Leaves compound, in opposite pairs,
leaflets 3 to 6 pair, upto 8 cm long. Flowers are usually
silky, white or yellow, solitary, arises from the axils of
leaves. Ovary briskly, style short and stout. Fruits are
globose, spinous or tuberculate; consisting of fine hairy or
nearly glabrous, often muriculate and woodi cocci, each
with two pairs of hard sharp spines, one pair longer than
the other. Fruit often cling to clothes and bodies of
animals. Seeds are many in woodi cocci. Plant is widely
distributed in different parts of India upto 3000 m altitude.
Steroidal saponin and diosgenin is isolated from this
plant. It is very rich in protein and calcium. Dried fruit
contain semi-drying oil, peroxides, diastase, traces of
glucosides, resins, protein and large amount of inorganic
matters. From the roots, stem and leaves, sitosterol and
srtigmasterol were also isolated.
MECHANISM OF ACTION
T. terrestris extract has been shown to stimulate
luteinizing hormone (LH) release from the pituitary gland.
It may also have some peripheral effects as manifested
by increased pubic hair in some hypogonadal test
subjects.
It is speculated that the metabolites of protodioscine
may also have mild androgenic properties. The exact
mechanisms are still vague and current explanations are
speculative at best.
ANALYTICAL SPECIFICATION FOR THE CRUDE
DRUG
Macroscopic characters
Yellowish globose and spiny, each having five woody,
spiny cocci and each coccus has four pointed rigid
spines. Two of the larger spines are directed towards the
apex and other two smaller ones are directed
downwards. Each coccus contains several seeds.
Active constituents
Protodioscin, terrestrosins A-E, desgalactotigonin, F-
gitonin, desglucolanatigonin, gitonin, tigogenin, furostanol
glycosides, β-Sitosterol, spirosta-3,5-diene, stigmasterol,
diosgenin, hecogenin, ruscogenin, Kaempferol, quercetin,
tribulusamides A and B (Wu et al., 1999; Mahato et al.,
1981).
Pharmacological action
T. terrestris shows aphrodisiac, diuretic, antiseptic,

anti-inflammatory,demulcent, nervine tonic, emenagogue,
alterative, astringent analgesic activities. Plant and spiny
fruits are used in the form of decoction or infusions in
cases of spermatorrhea (Georgiev et al., 1988),
phosphaturia, and diseases of the genitourinary system
such as dysuria, gonorrhea, gleet, chronic cystitis,
calculus affections, urinary disorders, gout, and
impotence; also in utrine disorder after parturition, kidney
diseases, and gravel. It is used in northern India in
cough, and some diseases of the heart.
MEDICINAL USES
T. terrestris has been used as a diuretic, tonic and
aphrodisiac, urinary disorders, hyperuricccemia,
impotence. Tribulus has been shown to enhance sexual
behaviour in an animal model. T. terrestris has long been
a constituent in tonics in Ayurveda medicine, where in it
is used as an aphrodisiac, also used diuretic and nervine
in tonic, where as in Unani medicine to inhibit the
formation of kidney stone. T. terrestris contains three
groups of active phytochemicals: Dioscin, protodioscin,
diosgenin and similar. These substances have effect on
sexual performance and may treat various sexual
disorders, they regulate sexual energy level and strength
by increasing the percentage of free testosterone level for
men and they affect pregnenolone, progesterone and
estrogen. The hormone balancing effects of Bulgarian T.
terrestris for women makes this herb suitable for
premenstrual syndrome and menopausal syndrome
(Protich et al., 1983; Huang et al., 2003). Sterols like
betasitosterols or stigma substances. These protect the
prostate from swelling and in combination with the X
steroidal saponins, protect the prostate from cancer.
Steroidal saponins currently referred to as X steroidal
saponins (Sun et al., 2003). These X steroidal saponins
affect the complete immune system (Toshkov et al.,
1985). They have been demonstrated to possess anti-
bacterial and anti-viral effects.
Bulgarian T. terrestris may be used internally and
externally to treat herpes, and virus infections such as
influenza and the common cold. T. terristris was found to
be a rich source of calcium (Duhan et al., 1992).
Studies have shown a more than 50% increase in testo-
sterone levels when taking the Tribulus herb studies
show that it works very well when stacked with DHEA
and androstenedione. It increases testosterone levels in
a different way, however, than either DHEA or andro do.
Instead of being a testosterone precursor, it leads to the
production of the LH. When LH levels are increased, the
natural production of testosterone also increases. LH is a
hormone that also deals with sex drive. T. terrestris
increases sperm count as well as motility levels when it is
taken for 30 days. This is a good supplement for men and
women to increase their sex drive. Most experts
recommend experimenting with 750 to 1,250 mg per day,
Akram et al. 3603
divided among meals. A significant benefit of Tribulus is
the stimulation of hormone production to a balanced
level, without over stimulating the secretion of hormones.
T. terrestris works by stimulating the anterior pituitary
gland to release LH, which is responsible for stimulating
the testes to produce testosterone. W hen scientists
began studying the curative power of Tribulus, they
discovered that it significantly elevates the level of
several hormones: Testosterone Luteinizing Hormone;
Follicle stimulating hormone (FSH) and estradiol. A
significant benefit of Tribulus is the stimuration on human
males and experimental animals are well known (Tomova
et al., 1978).
The analgesic effect of T. terrestris extract and
comparison of gastric ulcerogenicity of the extract
with indomethacine in animal experiments
T. terrestris has been used in traditional medicine for
relieving rheumatic pain and as an analgesic plant for a
long time. In this investigation the analgesic effect of
methanolic extract of this plant on male albino mice was
evaluated by formalin and tail flick test. Extraction of the
fruits of the plant was done by two different methods
(suxheletion and percolation) with methanol 80%. The
percolated extract was injected intraperitoneally in mice
at 50, 100, 200, 400, and 800 mg/kg. The results showed
that a dose of 100 mg/kg of percolated extract had the
highest significant analgesic effect compared to the
control group (P < 0.01) in formalin and tail flick test.
There is no significant difference in the analgesic effect
of suxheleted and percolated extract. The analgesic
effect of the extract was lower than morphine, 2.5 mg/kg
in both tests, and higher than ASA 300 mg/kg in chronic
phase of pain in formalin tests (P < 0.05). Pretreatment of
animal with naloxone did not change the analgesia
induced by the plant extract in both tests, therefore the
involvement of opioid receptor in the analgesic effect of
this plant was excluded. The results of ulcerogenic
studies indicate that the gastric ulcerogenecity of plant
extract is lower than the indomethacin in the rat's
stomach. It can therefore be concluded that T. terrestris
extract has a suitable analgesic effect and further studies
are required to produce a more effective product of this
plant to substitute for conventional analgesic drugs
(Heidari et al., 2007).
A novel furostanol saponin from T.terrestris of
Bulgarian origin
The phytochemical investigation of the aerial parts of T.
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-3β,16,26-triol-3-O-

3604 J. Med. Plant. Res.
α-rhamnopyranosyl-(1→2)-[α-rhamnopyranosyl-(1→4)]-β-
glucopyranoside (1) by spectral analysis, including
extensive 1D and 2D-NMR experiments (Conrad J).
The hormonal effects of T. terrestris and its role in
the management of male erectile dysfunction – an
evaluation using primates, rabbit and rat
Effects of T. terrestris (TT) on hormonal secretion were
evaluated in primates, rabbit and rat to evaluate its
usefulness in the management of erectile dysfunction
(ED) (Adaikan et al., 2000). TT extract was administered
intravenously, as a bolus dose of 7.5, 15 and 30 mg/kg,
in primates for acute study. Rabbits and normal rats were
treated with 2.5, 5 and 10 mg/kg of TT extract orally for 8
weeks, for chronic study. In addition, castrated rats were
treated either with testosterone cypionate (10 mg/kg,
subcutaneously; biweekly for 8 weeks) or TT orally (5
mg/kg daily for 8 weeks). Blood samples were analyzed
for testosterone (T), dihydrotestosterone(DHT) and
dehydroepiandrosterone sulphate (DHEAS) levels using
radioimmunoassay. In primates, the increases in
testosterone (T) (52%), DHT (31%) and DHEAS (29%) at
7.5 mg/kg were statistically significant. In rabbits, both
testosterone (T) and dihydrotestosterone were increased
compared to control, however, only the increases in DHT
(by 30 and 32% at 5 and 10 mg/kg) were statistically
significant. In castrated rats, increases in T levels by 51
and 25% were observed with T and TT extract respect-
tively that were statistically significant. TT increases
some of the sex hormones, possibly due to the presence
of protodioscin in the extract. TT may be useful in mild to
moderate cases of erectile dysfunction (Kalamegam et
al., 1988).
Testosterone enhancer
T. terrestris is a testosterone enhancer. T. terrestris
saponins appear to bind with the receptors of the
hypothalamus that detect sex hormones. It in-part blocks
the receptors leading to the hypothalamus misinterpreting
the body’s sex hormone levels as being lower than they
really are. The hypothalamus signals to start the
production of LH. When LH levels are increased, the
natural production of testosterone also increases (Sun et
al., 2003). LH is a hormone that also deals with sex drive
(Milanov et al., 1985).
Effective dose
Effective doses used in clinical settings are 750 to 1500
mg per day.
DISCUSSION
Gokhru, an important herb commonly used in the folk
medicine of many countries for different purposes. The
fruits of the plant T. terrestris has been shown to exhibit
diuretic, (Sangeeta et al., 1994) anti-urolithiatic, (Anand
et al., 1994) CNS stimulant, (Prakash et al., 1985)
antimicrobial, (Dhar et al., 1968) antifungal activities in
rats, (Zhang et al., 2006) antioxidant and antihyperten-
sive activity in rat heart (Ojha et al., 2006; Phillips et al.,
2006). T. terrestris contains biologiacally – rich
compounds as steroids, saponins, flavonoids, alkaloids
and unsaturated acids, which are involved in promoting
numerous physiological responses (Yan et al., 1996).
Thimation. The leaves increase the menstrual flow, cure
gonorrhea. The fruits are useful in urinary complaints,
painful micturation and impotence. The fruits are also
used to treat coughs, scabies and anexemia. The roots
are said to be stomachic, appetizer, diuretic and
carminative. It has also been used as medicine in India,
South Africa, and Japan. Some steroidal saponins have
previously been isolated from this plant as the active
components (Milanov et al., 1985).
CONCLUSION
The plant T. terrestris has been used since centuries in
Unani system of Medicine. It has been used in the
treatment of sexual disorders. T. terrestris has also been
used in traditional medicine for relieving rheumatic pain
and as an analgesic plant for a long time. It is concluded
that T. terrestris has analgesic, diuretic and uricosuric
effects.
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