What is the mechanism of action of Tribulus terrestris?

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From the Guidelines

Tribulus terrestris is a plant-based supplement with a proposed mechanism of action involving the stimulation of luteinizing hormone release, potentially leading to increased testosterone production, but its efficacy and safety are not well-documented in high-quality clinical trials 1. The primary active ingredients in Tribulus terrestris are saponins, particularly protodioscin, which are believed to be responsible for its effects on sexual function and testosterone levels.

  • The stimulation of luteinizing hormone (LH) release from the pituitary gland is thought to be a key mechanism by which Tribulus terrestris may influence testosterone production in men.
  • Additionally, some research suggests that Tribulus terrestris may act as a mild PDE-5 inhibitor, potentially improving blood flow to genital tissues, although this effect is likely to be weaker than that of prescription medications like sildenafil.
  • Other potential effects of Tribulus terrestris include anti-inflammatory, antioxidant, and diuretic properties, although these are not well-studied in the context of human health. Despite its popularity as a supplement for enhancing athletic performance, sexual function, and testosterone levels, the scientific evidence supporting the effectiveness of Tribulus terrestris is inconsistent, with some studies showing modest benefits while others show no significant effect compared to placebo 1.
  • Typical supplement doses range from 250-750 mg daily, standardized to contain 45-60% saponins, but the lack of regulation in the manufacture and distribution of herbal therapies, including Tribulus terrestris, can lead to disparities in product potency and quality.
  • Side effects of Tribulus terrestris are generally mild but may include stomach discomfort, sleep disturbances, or interactions with medications like antidiabetics or blood thinners, highlighting the need for caution when using this supplement, especially in the absence of strong evidence supporting its benefits 1.

From the Research

What is Tribulus Terrestris

  • Tribulus terrestris (TT) is a dicotyledonous herbal plant of the Zygophyllaceae family 2
  • It has been used in ancient medicine for its diuretic, tonic, and aphrodisiac properties 2
  • Today, TT is widely used by athletes and bodybuilders based on the belief that it can enhance testosterone concentrations 2, 3

Mechanism of Action

  • The nitric oxide release effect of TT may offer a plausible explanation for the observed physiological responses to TT supplementation, independent of the testosterone level 2
  • TT contains several organic compounds including alkaloids and steroidal glycosides, of which pharmacological action in humans is not completely explained 3
  • Emerging evidence from experimental studies in animals suggests possible endothelium and nitric oxide-dependent mechanisms underlying TT aphrodisiac and pro-erectile activities 4

Effects on Testosterone Levels

  • Literature available for the effectiveness of TT on enhancing testosterone concentrations is limited 2
  • Evidence to date suggests that TT is ineffective for increasing testosterone levels in humans, thus marketing claims are unsubstantiated 2, 3
  • However, some studies have shown that TT can increase testosterone levels in animals, and in humans when combined with other supplements 2, 3

Clinical Trials

  • A prospective, randomized, double-blind, placebo-controlled clinical trial found that TT improved sexual function in men with mild to moderate erectile dysfunction 5
  • A systematic review found that TT may be effective in treating female sexual dysfunction, but the certainty of the evidence was very low 6

References

1
Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

6
Research

Tribulus Terrestris for Female Sexual Dysfunction: A Systematic Review.

Revista brasileira de ginecologia e obstetricia : revista da Federacao Brasileira das Sociedades de Ginecologia e Obstetricia, 2020

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This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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