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What is it?

Description

The plant Tribulus terrestris, commonly known as tribulus or goat’s head, has been used for thousands of years in traditional medicines. Its chemical constituents are said to have analgesic, anti-aging, anti-cancerous, anti-cariogenic, anti-inflammatory, anti-microbial, anti-oxidative, anti-spasmodic, anti-urolithic, diuretic, hepatoprotective, and immunomodulatory properties. Tribulus has known applications in sexual, cardiovascular, and anti-diabetic functions. (5)(22) A variety of tribulus products exist, containing various anatomical parts of the plant (e.g., whole plant, fruit, seeds, aerial parts, leaves, etc.). However, there is a wide discrepancy in the content of its most bioactive saponin components, particularly furostanol and spirostanol, based on the plant’s location of origin and the anatomical parts used. This may affect clinical efficacy, safety, and pharmacodynamic action. (19)

It is important to note that many tribulus products are marketed for their ability to increase testosterone, improve sexual function, and address other disorders related to male or female reproductive organs. However, a large proportion of clinical trials available to date include multi-ingredient formulations, making it unclear as to whether effects are attributable to tribulus, the other ingredients, or their combination. In this ingredient review, only single-ingredient tribulus formulations were considered.

Main uses

Raising testosterone (male and female)
Sexual dysfunction and hypoactive sexual desire

Formulations

Formulation
Comparison
Androsten®
Standardized extract containing 15% steroidal saponins (e.g., 250 mg tablet contains ~37.5 mg protodioscin) (14)
EFFEX®
Standardized extract containing 35-45% furostanol saponins
Provided similar efficacy on erectile dysfunction measures as Tribestan® (18)
Tribestan®
Standardized extract containing 35-45% furostanol saponins (e.g., 250 mg tablet contains ~112.5 mg furostanols); (10)
Provided similar efficacy on erectile dysfunction as EFFEX® (18)
Trib Gold
Standardized extract containing 45% steroidal saponins (e.g., 250 mg contains ~112.5 mg protodioscin) (7)

Dosing & administration

Adverse effects

A higher frequency of side effects do not occur compared with placebo or are reported at similar rates. (2)(6)(10)(15)(20) In one prospective, randomized, double-blind, placebo-controlled clinical trial that included 60 postmenopausal women with sexual dysfunction, the incidence of diarrhea was greater following tribulus intake compared with a placebo. (12)

Pharmacokinetics

Currently, little is known about the pharmacokinetics of tribulus and there is no available data in humans.

Absorption

  • Protodioscin, one of the main active components of tribulus, is slowly absorbed with low absolute bioavailability, as shown in rodents (21)
  • Saponins possess membrane permeabilizing effects due to its amphiphilic properties that can improve the absorption of other hydrophilic and hydrophobic compounds (19)

Distribution

  • Listed from highest to lowest concentrations, post-injection methyl-protodioscin was found in rodent womb, lung, kidney, liver, heart, spleen, small intestine, stomach, large intestine, ovary, skeletal muscle, fat and brain tissues (4)

Metabolism

  • Protodioscin may be converted to DHEA (1)
  • Methyl-protodioscin’s primary metabolite is dioscin, as shown in rats (8)

Excretion

  • Methyl-protodioscin possessed a post-injection half-life of 25 to 29 minutes, (4) and protodioscin possessed a post-oral administration half-life of approximately 12 hours in rodents (21)
  • Methyl-protodioscin is excreted primarily in bile, as well as in the urine of rodents (4)

 

Last updated: July 28th, 2020

References
  1. Adimoelja, A. (2000). Phytochemicals and the breakthrough of traditional herbs in the management of sexual dysfunctions. International Journal of Andrology, 23 Suppl 2, 82–84. ()
  2. Akhtari, E., Raisi, F., Keshavarz, M., Hosseini, H., Sohrabvand, F., Bioos, S., Kamalinejad, M., & Ghobadi, A. (2014). Tribulus terrestris for treatment of sexual dysfunction in women: Randomized double-blind placebo - controlled study. Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 22, 40. ()
  3. Borrelli, F., Colalto, C., Delfino, D. V., Iriti, M., & Izzo, A. A. (2018). Herbal dietary supplements for erectile dysfunction: A systematic review and meta-analysis. Drugs, 78(6), 643–673. ()
  4. Cao, X., Yao, Z., Shao, M., Chen, H., Ye, W., & Yao, X. (2010). Pharmacokinetics of methyl protodioscin in rats. Die Pharmazie, 65(5), 359–362. ()
  5. Chhatre, S., Nesari, T., Somani, G., Kanchan, D., & Sathaye, S. (2014). Phytopharmacological overview of Tribulus terrestris. Pharmacognosy Reviews, 8(15), 45–51. ()
  6. de Souza, K. Z. D., Vale, F. B. C., & Geber, S. (2016). Efficacy of Tribulus terrestris for the treatment of hypoactive sexual desire disorder in postmenopausal women: A randomized, double-blinded, placebo-controlled trial. Menopause , 23(11), 1252–1256. ()
  7. GamalEl Din, S. F., Abdel Salam, M. A., Mohamed, M. S., Ahmed, A. R., Motawaa, A. T., Saadeldin, O. A., & Elnabarway, R. R. (2019). Tribulus terrestris versus placebo in the treatment of erectile dysfunction and lower urinary tract symptoms in patients with late-onset hypogonadism: A placebo-controlled study. Urologia, 86(2), 74–78. ()
  8. He, X., Qiao, A., Wang, X., Liu, B., Jiang, M., Su, L., & Yao, X. (2006). Structural identification of methyl protodioscin metabolites in rats’ urine and their antiproliferative activities against human tumor cell lines. Steroids, 71(9), 828–833. ()
  9. Ismail, S. B., Bakar, M. B., Nik Hussain, N. H., Norhayati, M. N., Sulaiman, S. A., Jaafar, H., Draman, S., Ramli, R., & Wan Yusoff, W. Z. (2014). Comparison on the effects and safety of tualang honey and tribestan in sperm parameters, erectile function, and hormonal profiles among oligospermic Males. Evidence-Based Complementary and Alternative Medicine: eCAM, 2014, 126138. ()
  10. Kamenov, Z., Fileva, S., Kalinov, K., & Jannini, E. A. (2017). Evaluation of the efficacy and safety of Tribulus terrestris in male sexual dysfunction- A prospective, randomized, double-blind, placebo-controlled clinical trial. Maturitas, 99, 20–26. ()
  11. Kuchakulla, M., Narasimman, M., Soni, Y., Leong, J. Y., Patel, P., & Ramasamy, R. (2020). A systematic review and evidence-based analysis of ingredients in popular male testosterone and erectile dysfunction supplements. International Journal of Impotence Research. ()
  12. Postigo, S., Lima, S. M. R. R., Yamada, S. S., dos Reis, B. F., da Silva, G. M. D., & Aoki, T. (2016). Assessment of the effects of Tribulus terrestris on sexual function of menopausal women. Revista Brasileira de Ginecologia E Obstetricia, 38(3), 140–146. ()
  13. Qureshi, A., Naughton, D. P., & Petroczi, A. (2014). A systematic review on the herbal extract Tribulus terrestris and the roots of its putative aphrodisiac and performance enhancing effect. Journal of Dietary Supplements, 11(1), 64–79. ()
  14. Salgado, R. M., Marques-Silva, M. H., Gonçalves, E., Mathias, A. C., Aguiar, J. G., & Wolff, P. (2017). Effect of oral administration of Tribulus terrestris extract on semen quality and body fat index of infertile men. Andrologia, 49(5). ()
  15. Samani, N. B., Jokar, A., Soveid, M., Heydari, M., & Mosavat, S. H. (2016). Efficacy of the Hydroalcoholic extract of Tribulus terrestris on the serum glucose and lipid profile of women with diabetes mellitus: A double-blind randomized placebo-controlled clinical trial. Journal of Evidence-Based Complementary & Alternative Medicine, 21(4), NP91–NP97. ()
  16. Sanagoo, S., Sadeghzadeh Oskouei, B., Gassab Abdollahi, N., Salehi-Pourmehr, H., Hazhir, N., & Farshbaf-Khalili, A. (2019). Effect of Tribulus terrestris L. on sperm parameters in men with idiopathic infertility: A systematic review. Complementary Therapies in Medicine, 42, 95–103. ()
  17. Sellandi, T. M., Thakar, A. B., & Baghel, M. S. (2012). Clinical study of Tribulus terrestris Linn. in oligozoospermia: A double blind study. Ayu, 33(3), 356–364. ()
  18. Spivak, L. G., Platonova, D. V., Enikeev, D. V., Rapoport, L. M., Vinarov, A. Z., & Demidko, Y. L. (2018). [Results of a comparative multi-center randomized clinical study of efficacy and safety of EFFEX Tribulus and Tribestan in patients with erectile dysfunction]. Urologiia , 2, 54–61. ()
  19. Ștefănescu, R., Tero-Vescan, A., Negroiu, A., Aurică, E., & Vari, C.-E. (2020). A comprehensive review of the phytochemical, pharmacological, and toxicological properties of Tribulus terrestris L. Biomolecules, 10(5). ()
  20. Vale, F. B. C., Zanolla Dias de Souza, K., Rezende, C. R., & Geber, S. (2018). Efficacy of Tribulus terrestris for the treatment of premenopausal women with hypoactive sexual desire disorder: A randomized double-blinded, placebo-controlled trial. Gynecological Endocrinology: The Official Journal of the International Society of Gynecological Endocrinology, 34(5), 442–445. ()
  21. Zhang, X., Guo, Z., Li, J., Ito, Y., & Sun, W. (2016). A new quantitation method of protodioscin by HPLC-ESI-MS/MS in rat plasma and its application to the pharmacokinetic study. Steroids, 106, 62–69. ()
  22. Zhu, W., Du, Y., Meng, H., Dong, Y., & Li, L. (2017). A review of traditional pharmacological uses, phytochemistry, and pharmacological activities of Tribulus terrestris. Chemistry Central Journal, 11(1), 60. ()

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