page_title: Guggulsterone
hierarchical_section_title: Guggulsterone
caption_attribution_description: English: Chemical structure of (E)-guggulsterone
context_page_description: Guggulsterone is a phytosteroid found in the resin of the guggul plant, Commiphora mukul. Guggulsterone can exist as either of two stereoisomers, E-guggulsterone and Z-guggulsterone. In humans, it acts as an antagonist of the farnesoid X receptor, which was once believed to result in decreased cholesterol synthesis in the liver. Several studies have been published that indicate no overall reduction in total cholesterol occurs using various dosages of guggulsterone, and levels of low-density lipoprotein increased in many people. Nevertheless, guggulsterone is an ingredient in many nutritional supplements.
  Guggulsterone is a broad-spectrum ligand of steroid hormone receptors, and is known to possess the following activities:
  Mineralocorticoid receptor antagonist
  Progesterone receptor partial agonist
  Glucocorticoid receptor antagonist
  Androgen receptor antagonist
  Estrogen receptor agonist
  Farnesoid X receptor antagonist
  Pregnane X receptor agonist
context_section_description: Guggulsterone is a phytosteroid found in the resin of the guggul plant, Commiphora mukul.  Guggulsterone can exist as either of two stereoisomers, E-guggulsterone and Z-guggulsterone. In humans, it acts as an antagonist of the farnesoid X receptor, which was once believed to result in decreased cholesterol synthesis in the liver. Several studies have been published that indicate no overall reduction in total cholesterol occurs using various dosages of guggulsterone, and levels of low-density lipoprotein ("bad cholesterol") increased in many people.  Nevertheless, guggulsterone is an ingredient in many nutritional supplements.
  Guggulsterone is a broad-spectrum ligand of steroid hormone receptors, and is known to possess the following activities:
  Mineralocorticoid receptor antagonist (Kᵢ = 39 nM)
  Progesterone receptor partial agonist (Kᵢ = 201 nM)
  Glucocorticoid receptor antagonist (Kᵢ = 224 nM)
  Androgen receptor antagonist (Kᵢ = 240 nM)
  Estrogen receptor agonist (Kᵢ > 5 μM; EC₅₀ > 5 μM)
  Farnesoid X receptor antagonist (IC₅₀ = 5–50 μM)
  Pregnane X receptor agonist (EC₅₀ = 2.4 μM ((Z)-isomer))
  Guggulsterone has been found in animal research to be orally active; it has an absolute bioavailability of 42.9% after oral administration in rats, with a half-life of around 10 hours in this species, indicating a good pharmacokinetic profile.
caption: E-Guggulsterone
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