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org/JMPR DOI: 10.5897/JMPR11.014 ISSN 1996-0875 ©2012 Academic Journals
Monograph of Tribulus terrestris
Ghazala Shaheen1*, Irshad Ahmad2, Khan Usmanghani 3 Naveed Akhter1, Mukhtiar Ahmad1, Sabira Sultana1 and M. Akram3
University College of Conventional Medicine, Faculty of Pharmacy and Alternative Medicine, The Islamia University Bahawalpur, Pakistan.
Accepted 19 December, 2011
Tribulus terrestris has long been used as a tonic and aphrodisiac, and a diuretic in Unani system of medicine. The diuretic effect was attributed to the presence of potassium salts in high concentration. So many studies have been done on pharmacological activities of T. terrestris. The major constituents of these plants are steroidal saponins namely: terrestrosins A, B, C, D and E, desgalactotigonis, Fgitonis, desglucolanatigoneis, gitnin etc. The biological activity exhibited by saponins include: pisicidal, antimicrobial, molluscicidal, haemolytic, antiviral, cytotoxic, antihepatotoxic, spermicidal, insecticidal, antioedematous, antiulcer analgesic, immunomodulatory, and sedative effects. Key words: Tribulus terrestris, steroidal saponins, aphrodisiac, diuretic.
INTRODUCTION Tribulus terrestris is a flowering plant of the family Zygophyllaceae. It is native to warm temperate and tropical regions of the Old World in Southern Europe, Southern Asia, throughout Africa, and Australia (http://en.wikipedia.org/wiki/Tribulus_terrestris). Family: Zygophyllaceae Genus: Tribulus Species: Terrestris Linn. Botanical synonym: Tribulus languinosus Linn. English: Land-caltrops, Puncture-vine Part used: Dried spiny fruit Botanical description T. terrestris is an annual or perennial, prostrate herb with many slender, spreading branches and silky-villous young parts (Matthew et al., 1983). Leaves are abruptly simple, pinnate and opposite. Leaflets almost sessile, rounded or oblique at the base, mucronate at the apex, flowers bright yellow, solitary, pseudo axillary or leaf opposed. Fruits are 5 angled or winged spinous tuberculate woody schizocarp, separating into five cocci, each coccus having two long, stiff, sharp divaricate spines towards the distal half and two shorter ones nearer the base, seeds one or more in each coccus (Matthew et al., 1983). Geographical distribution The plant grows wild throughout India, the shrub thrives in well irrigated black soil upto attitudes of 3000 m. (Matthew et al., 1983) (Figure 1). Traditional uses The roots and fruits are sweet, cooling, diuretic, aphrodisiac, emollient, appetiser, digestive, anthelmintic, expectorant, anodyne, anti-inflammatory, alterant, laxative, cardiotonic, styptic, lithotriptic and tonic. They are useful in strangury, dysuria, vitiated conditions of vata and pitta, renal and vesical calculi, anorexia, dyspepsia, helminthiasis, spermatorrhoea, anaemina, scabies, ophthalmia, ulocace and general weakness. The leaves are astringent, diuretic, aphrodisiac, depurative, anthelmenthic and tonic. They are useful in gonorrhoea, inflammation, menorrhagia, strangury, leprosy, skin diseases, verminosis and general weakness. The seeds are astringent, strengthening and are useful in epistaxis, haemorrhages and ulcerative stomatitis. The ash of the whole plant is good for external application in rheumatic-
*Corresponding author. E-mail: firstname.lastname@example.org.
J. Med. Plants Res.
Figure 1. Tribulus terrestris.
essential oil which occurs in the seeds (Nadkarni et al., 1993). Phytochemistry The major constituents of this plants are steroidal saponins 1 namely terrestrosins A, B, C, D and E, desgalactotigonis, F-gitonis, desglucolanatigoneis, gitnin etc., which on hydrolysis yield jdiosgenis, hecogenis and neotigogenin etc. (Zafar et al., 1989). There are other minor constituents like alkaloids (uncharacterised) (Yan et al., 1996) common phyto sterols namely, -sitosterol, stigmasterol, a cinnamic amide derivative - terrestiamide and 7-methylhydroisdamone (Mahato et al., 1978). Active constituents The fruit of T. terrestris contain of glycosides, especially saponin glycosides. The saponins on hydrolysis yields diosgenin, ruscogenin, gitogenin, three flavone glycosides etc. (Figures 2, 3 and 4). PHARMACOLOGY Antiurolithiatic activity
Figure 3. Ruscogenin.
Figure 2. Diosgenin.
arthritis. The diuretic properties of the plant are due to the large quantities of the nitrates present as well as the
In a preliminary study the diuretic effect of T. terrestris and Hygrophila spinosa water extracts in albino rats was evaluated. The diuretic effect was attributed to the presence of potassium salts in high concentration (Kumari and Iyer, 1967). The diuretic action with minimal side effect of T. terrestris in albino rats was confirmed
Shaheen et al.
Figure 4. Gitogenin.
LDH5 fraction (Sangeeta et al., 1994). Activity guided fractionation was conducted on fruits of T. terrestris. The ethanolic extract showed significant dose dependent protection against uroliths induced by glass bead implantation in albino rats. On subsequent fractionation of the ethanolic extract, maximum activity was localized in the 10% aqueous methanol fraction which provided significant protection against deposition of calculogenic material around the glass bead and it also protected leucocytosis and elevation in serum urea levels. Further fractionation bead to decreased activity which was attributed to the loss of active compounds during fractionation or due to combined effect of several constituents in the methanolic fraction (Anand et al., 1994). Aphrodisiac activity
(Singh et al., 1991). Further studies were conducted to evaluate the therapeutic use of T. terrestris in various urinary disorders including urolithiasis. The ethanol extract was tested for activity against artificially induced urolithiasis in albino rats. The extract was administered orally at 25, 50 and 100 mg/kg daily for 4 months. It exhibited dose dependent antiurolithiatic activity and almost completely inhibited stone formation. Other biochemical parameters in urine and serum which were altered during the process of stone formation were normalized by the plant extract in a dose dependent manner (Anand et al., 1994). The effect of an aqueous extract of T. terrestris administered orally at a dose of 5 g/kg body weight was studied in rats with induced hyperoxaluria (Intraperitoneal injection of 4 –OH proline at a dose of 2.5 g/kg body weight for three successive days) and maintained by sodium glycolate, twenty four hour urine was collected and analyzed for creatinine and oxalate. The oxalate excretion reversed to normal from 1.97 + 0.314 to 0.144 + 0.004 mg/mg creatinine (P<0.01) within 21 days of administration of T. terrestris extract and remained so until 15 days after withdrawal of extract and sodium glycolate (Sangeeta et al., 1993). To confirm the earlier studies, the effect of feeding aqueous extract of T. terrestris on the metabolism of oxalate in rats fed with sodium glycolate was evaluated. Glycolate feeding resulted in hyperoxaluria as well as increased activities of oxalate synthesizing enzymes of the liver namely glycolate oxidase (GAO), glycolate dehydrogenase (GAD) and lactate dehydrogenase (LDH) and decreased kidney LDH activity. T. terrestris fed rats produced a significant decrease in urinary oxalate exertion and a significant increase in urinary glycoxylate excretion, as compared to sodium glycolate fed animals. The supplementation of T. terrestris extract also caused a reduction in liver GAO and GAD activities, where as liver LDH activity remained unaltered. The isoenzyme pattern of kidney LDH revealed that normalization of kidney LDH by T. terrestris was mainly due to an increase in the
A study was conducted to investigate the effect of oral treatment of T. terrestris extract on the isolated corpus carvenosal tissue of rabbits to determine the mechanism by which protodioscin (PTN) a constituent of T. terrestris exerted its pharmacological activity. The animals were treated with extracts at different dose levels that is, 2.5, 5, 10 mg/kg body weight which was administered orally, once daily for a period of 8 weeks. The penile tissue from the sacrificed animals were subjected for responses to both contractions and relaxing pharmacological agents and electrical field stimulation (EFS). The results indicating the relaxant responses to acetyl chloline, nitroglycerin and EFS by more than 10, 24 and 10% respectively compared to their control values and the lack of such effect on the contractile response to noradrenaline and histamine indicated that PTN had a proerectile activity. The enhanced relaxant effect was attributed to the increase of nitric oxide from the endothelium and nitrergic nerve endings, which may account for its claims as an aphrodisiac (Adaikan et al., 2000). CNS activity The pharmacological screening of the T. terrestris extract showed marked CNS stimulant activity at a dosage of 20 mg/kg in albino rats (Prakash et al., 1985). Cardiotonic activity In a clinical trial 406 patients with coronary heart disease were treated with saponins of T. terrestris. The results showed that the total efficacious rate of remission angina pectoris was 82.3%. The total efficacious rate of ECG improvement (52.7%) was even higher than that of control group (35.8%). It is shown that saponin of
J. Med. Plants Res.
T. terrestris has the action of dilating coronary artery and improving coronary circulation and thus has better effects on improving ECG of mycocardial ischemia. No adverse reaction on blood system, hepatic and renal functions were noticed (Bowen et al., 1990). Safety profile The ethanolic (95%) extract was tested in rats intraperitoneally and the LD50 was found to be 56.4 mg/kg (Dhar et al., 1968). The maximum tolerated dose in mouse was 100 g/kg, the extract used ethanol and water (1:1) intraperitoneally (Chakraborty and Neogi, 1978).
REFERENCES Adaikan PG, Gauthaman K, Prasad RN, Ng SC (2000). "Projectile pharmacological effects of Tribulus terrestris extract on the rabbits corpus carvenosum" Ann. Acad. Med. Singapore, 29(1): 22-26. Anand R, Patnaik GK, Kulshreshtha DK, Dhawan BN, (1994). " Activity of certain fractions of Tribulus terrestris fruits against experimentally induced urolithiasis in rats" Int. J. Exp. Biol., 32: 548-552. Anand R, Patnaik GK, Srivastava S, Kulshreshtha DK, Dhawan BN (1994). " Evaluation of antiurolithiatic activity of Tribulus terrestris". Int. J. Pharmacog., 32(3): 217-224. Bowen W, Long'en M, Tongku L (1990). “Clinical observation on 406 cases of angina pectoris of coronary heart disease treated with saponins of Tribulus terrestris”. Chin. J. Int. Trad. West Med., 10(2): 85-87.
Chakraborty B, Neogi NC (1978). 'Pharmacological properties of Tribulus terrestris '. Ind. J. Pharm. Sci., 40: 50-52. Dhar ML, Dhar MM, Dhawan BN, Mehrotra BN, Ray C (1968). ''Screening of Indian plants of biological activity: part 1''. Ind. J. Exp. Biol., 6: 232-247. Kumari GS, Iyer GYN (1967). "Preliminary studies on the diuretic effect of Hygrophila spinosa and Tribulus terrestris" Ind. J. Med. Res., 55(7): 714-716. Mahato SB, Sahu NP, Pal BC (1978). " Screening of Tribulus terrestris plants for diosgenis "J. Ind. Chem. (India), 50(1): 49-50. Matthew KM (1983). The flora of the Tamilnadu Carnatic Part-I, Published by The Rapinat Herbarium St.Joseph’s College Tiruchirapalli, p. 185. Nadkarni KM (1993). Popular prakashan, Bombay, Ind. Mater. Med., 1: 1230. Prakash D, Singh PN, Wahi SP (1985). “An evaluation of Tribulus terrestris Linn (Chota Gokharu)” . Ind. Drugs, 22(6): 332 -333. Sangeeta D, Sidhu H, Third SK, Nath R (1994). Effect of Tribulus terrestris on oxalate metabolism in rats”. J. Ethnopharmacol., 44: 6166. Sangeeta D, Sidhu H, Thind SK, Nath R, Vaidyanathan S (1993). “Therapeutic response of Tribulus terrestris (Gokhru) aqueous extract on hyperoxaluria in male adult rats”. Phytother. Res., 7: 116-119. Singh RG, Singh RP, Usha KP, Shukla KP, Singh P (1991). “Experimental evaluation of diuretic action of herbal drug (Tribulus terrestris Linn.) on albino rats", J. Res. Educ. Ind. Med., 10(1): 19-21. Yan W, Ohtani K, Kasai R, Yamasaki K (1996). " Steroidal saponin from fruits of Tribulus terrestris”. Phytochemistry, 42(5): 1417-1422. Zafar R, Lalwani M (1989). “Tribulus terrestris Linn - a review of current knowledge". Ind. Drugs, 27(3): 148-158. http://en.wikipedia.org/wiki/Tribulus_terrestris
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