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Tribulus terrestris Linn.: A review article

Article  in  Journal of Medicinal Plant Research · August 2011

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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
1
Department of Basic Medical Sciences1, Faculty of Eastern Medicine, Hamdard University Karachi, Pakistan.
2
College of Conventional Medicine, Faculty of Pharmacy and Alternative Medicine, The Islamia University of
Bahawalpur, Pakistan.
3
University College of Pharmacy, Punjab University Lahore, Pakistan.
4
Faculty 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 on liver BEL-7402 cells by inducing apoptosis (Sun et al.,
areas around the world. It is commonly known as Gokhru 2004). T. terrestris exerts significantly antihyperlipidemic
belonging to the family Zygophyllaceae, widely distributed effects (Jiji et al., 2009). Chronic intake of a complex
throughout India. The fruits of T. terrestris L. have been dietary supplement containing DHEA (Jameel et al.,
used in traditional Chinese medicine for the treatment of 2004), androstenedione and herbal extracts increases
eye trouble, edema, abdominal distention, emission, mor- serum androgen levels, it has minimal effect on immune
bid leucorrhea, sexual dysfunction and veiling. Roots and function in middle aged men (Kohut et al., 2003; Protich
fruits are useful in rheumatism, piles, renal and vesical et al., 1983). Gynaecomastia has also been reported due
calculi, menorrhagia, impotency, premature ejaculation, to intake of a T. terrestris (Jameel et al., 2004).
general weakness etc. The fruits, flowers and leaves are T. terrestris is a natural stimulant of Luteinizing hor-
shown in Figures 1 and 2. It is a very potent diuretic and mone (LH) which signals the body to produce more of its
tonic drug (Selvam, 2008). The steroidal saponin consti- own testosterone (Neychev et al., 2005; Antonio, 2000).
tuents obtained from T. terrestris exhibit antimicrobial and Clinical studies showed T. terrestris improved reproduce-
cytotoxic effects (Bedir et al., 2002; Protich et al., 1983; tive function, including increased concentration of
Chu et al., 2003; Li et al., 2002). The phytochemical hormones such as estradiol, with testosterone being very
investigation of the aerial parts of T. terrestris of has slightly influenced, thereby improving reproductive func-
resulted in the isolation of the novel furostanol saponin 1, tion, libido and ovulation (Gauthaman, 2002; Tomova,
named tribol, together with the known spirostanol 1978).
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). Tribulus terrestris Linn.
Saponins from T. terrestris (STT) exert its cytotoxic effect
Tibbi name: Gokhru
English name: Caltrop
Botanical name: T. terrestris
*Corresponding author. E-mail: [email protected]. Family: Zygphyllaceae
Tel: 92-021-6440083. Fax: 92-021-6440079. Part used: Seeds
3602 J. Med. Plant. Res.

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
Figure 1. Fruit of T. terrestris. 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
Figure 2. Leaves and flowers of T. terrestris. spines. Two of the larger spines are directed towards the
apex and other two smaller ones are directed
downwards. Each coccus contains several seeds.

Description
Active constituents
It is a tap rooted herbaceous perennial plant that grows
as a summer annual in colder climates. The stems Protodioscin, terrestrosins A-E, desgalactotigonin, F-
radiate from the crown to a diameter of about 10 cm to gitonin, desglucolanatigonin, gitonin, tigogenin, furostanol
over 1 m, often branching. They are usually prostrate, glycosides, β-Sitosterol, spirosta-3,5-diene, stigmasterol,
forming flat patches, though they may grow more diosgenin, hecogenin, ruscogenin, Kaempferol, quercetin,
upwards in shade or among taller plants. The leaves are tribulusamides A and B (Wu et al., 1999; Mahato et al.,
pinnately compound with leaflets less than a quarter-inch 1981).
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 Pharmacological action
single-seeded nut lets.
The nutlets or "seeds" are hard and bear two to three T. terrestris shows aphrodisiac, diuretic, antiseptic,
 Akram et al. 3603

anti-inflammatory,demulcent, nervine tonic, emenagogue, divided among meals. A significant benefit of Tribulus is
alterative, astringent analgesic activities. Plant and spiny the stimulation of hormone production to a balanced
fruits are used in the form of decoction or infusions in level, without over stimulating the secretion of hormones.
cases of spermatorrhea (Georgiev et al., 1988), T. terrestris works by stimulating the anterior pituitary
phosphaturia, and diseases of the genitourinary system gland to release LH, which is responsible for stimulating
such as dysuria, gonorrhea, gleet, chronic cystitis, the testes to produce testosterone. When scientists
calculus affections, urinary disorders, gout, and began studying the curative power of Tribulus, they
impotence; also in utrine disorder after parturition, kidney discovered that it significantly elevates the level of
diseases, and gravel. It is used in northern India in several hormones: Testosterone Luteinizing Hormone;
cough, and some diseases of the heart. Follicle stimulating hormone (FSH) and estradiol. A
significant benefit of Tribulus is the stimuration on human
males and experimental animals are well known (Tomova
MEDICINAL USES et al., 1978).

T. terrestris has been used as a diuretic, tonic and

The analgesic effect of T. terrestris extract and
aphrodisiac, urinary disorders, hyperuricccemia,
impotence. Tribulus has been shown to enhance sexual comparison of gastric ulcerogenicity of the extract
behaviour in an animal model. T. terrestris has long been with indomethacine in animal experiments
a constituent in tonics in Ayurveda medicine, where in it
is used as an aphrodisiac, also used diuretic and nervine T. terrestris has been used in traditional medicine for
in tonic, where as in Unani medicine to inhibit the relieving rheumatic pain and as an analgesic plant for a
formation of kidney stone. T. terrestris contains three long time. In this investigation the analgesic effect of
groups of active phytochemicals: Dioscin, protodioscin, methanolic extract of this plant on male albino mice was
diosgenin and similar. These substances have effect on evaluated by formalin and tail flick test. Extraction of the
sexual performance and may treat various sexual fruits of the plant was done by two different methods
disorders, they regulate sexual energy level and strength (suxheletion and percolation) with methanol 80%. The
by increasing the percentage of free testosterone level for percolated extract was injected intraperitoneally in mice
men and they affect pregnenolone, progesterone and at 50, 100, 200, 400, and 800 mg/kg. The results showed
estrogen. The hormone balancing effects of Bulgarian T. that a dose of 100 mg/kg of percolated extract had the
terrestris for women makes this herb suitable for highest significant analgesic effect compared to the
premenstrual syndrome and menopausal syndrome control group (P < 0.01) in formalin and tail flick test.
(Protich et al., 1983; Huang et al., 2003). Sterols like There is no significant difference in the analgesic effect
betasitosterols or stigma substances. These protect the of suxheleted and percolated extract. The analgesic
prostate from swelling and in combination with the X effect of the extract was lower than morphine, 2.5 mg/kg
steroidal saponins, protect the prostate from cancer. in both tests, and higher than ASA 300 mg/kg in chronic
Steroidal saponins currently referred to as X steroidal phase of pain in formalin tests (P < 0.05). Pretreatment of
saponins (Sun et al., 2003). These X steroidal saponins animal with naloxone did not change the analgesia
affect the complete immune system (Toshkov et al., induced by the plant extract in both tests, therefore the
1985). They have been demonstrated to possess anti- involvement of opioid receptor in the analgesic effect of
bacterial and anti-viral effects. this plant was excluded. The results of ulcerogenic
Bulgarian T. terrestris may be used internally and studies indicate that the gastric ulcerogenecity of plant
externally to treat herpes, and virus infections such as extract is lower than the indomethacin in the rat's
influenza and the common cold. T. terristris was found to stomach. It can therefore be concluded that T. terrestris
be a rich source of calcium (Duhan et al., 1992). extract has a suitable analgesic effect and further studies
Studies have shown a more than 50% increase in testo- are required to produce a more effective product of this
sterone levels when taking the Tribulus herb studies plant to substitute for conventional analgesic drugs
show that it works very well when stacked with DHEA (Heidari et al., 2007).
and androstenedione. It increases testosterone levels in
a different way, however, than either DHEA or andro do. A novel furostanol saponin from T.terrestris of
Instead of being a testosterone precursor, it leads to the Bulgarian origin
production of the LH. When LH levels are increased, the
natural production of testosterone also increases. LH is a The phytochemical investigation of the aerial parts of T.
hormone that also deals with sex drive. T. terrestris terrestris of Bulgarian origin has resulted in the isolation
increases sperm count as well as motility levels when it is of the novel furostanol saponin 1, named tribol, together
taken for 30 days. This is a good supplement for men and with the known spirostanol Saponins 2 and 3 and
women to increase their sex drive. Most experts sitosterol glucoside. The structure of tribol was
recommend experimenting with 750 to 1,250 mg per day, 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- medicine of many countries for different purposes. The

glucopyranoside (1) by spectral analysis, including fruits of the plant T. terrestris has been shown to exhibit
extensive 1D and 2D-NMR experiments (Conrad J). 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
The hormonal effects of T. terrestris and its role in rats, (Zhang et al., 2006) antioxidant and antihyperten-
the management of male erectile dysfunction – an sive activity in rat heart (Ojha et al., 2006; Phillips et al.,
evaluation using primates, rabbit and rat 2006). T. terrestris contains biologiacally – rich
compounds as steroids, saponins, flavonoids, alkaloids
Effects of T. terrestris (TT) on hormonal secretion were and unsaturated acids, which are involved in promoting
evaluated in primates, rabbit and rat to evaluate its numerous physiological responses (Yan et al., 1996).
usefulness in the management of erectile dysfunction Thimation. The leaves increase the menstrual flow, cure
(ED) (Adaikan et al., 2000). TT extract was administered gonorrhea. The fruits are useful in urinary complaints,
intravenously, as a bolus dose of 7.5, 15 and 30 mg/kg, painful micturation and impotence. The fruits are also
in primates for acute study. Rabbits and normal rats were used to treat coughs, scabies and anexemia. The roots
treated with 2.5, 5 and 10 mg/kg of TT extract orally for 8 are said to be stomachic, appetizer, diuretic and
weeks, for chronic study. In addition, castrated rats were carminative. It has also been used as medicine in India,
treated either with testosterone cypionate (10 mg/kg, South Africa, and Japan. Some steroidal saponins have
subcutaneously; biweekly for 8 weeks) or TT orally (5 previously been isolated from this plant as the active
mg/kg daily for 8 weeks). Blood samples were analyzed components (Milanov et al., 1985).
for testosterone (T), dihydrotestosterone(DHT) and
dehydroepiandrosterone sulphate (DHEAS) levels using
radioimmunoassay. In primates, the increases in CONCLUSION
testosterone (T) (52%), DHT (31%) and DHEAS (29%) at
7.5 mg/kg were statistically significant. In rabbits, both The plant T. terrestris has been used since centuries in
testosterone (T) and dihydrotestosterone were increased Unani system of Medicine. It has been used in the
compared to control, however, only the increases in DHT treatment of sexual disorders. T. terrestris has also been
(by 30 and 32% at 5 and 10 mg/kg) were statistically used in traditional medicine for relieving rheumatic pain
significant. In castrated rats, increases in T levels by 51 and as an analgesic plant for a long time. It is concluded
and 25% were observed with T and TT extract respect- that T. terrestris has analgesic, diuretic and uricosuric
tively that were statistically significant. TT increases effects.
some of the sex hormones, possibly due to the presence
of protodioscin in the extract. TT may be useful in mild to
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