Guggulsterone

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Guggulsterone is a phytosteroid found in the resin of the guggul plant, Commiphora wightii. 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. However, clinical trials have shown that consumption of guggulsterone does not lead to decreased levels of cholesterol.

Chemistry[edit | edit source]

Guggulsterone is a phytosteroid, a plant steroid, and is present in the guggul plant, Commiphora wightii. It can exist in two forms, E-guggulsterone and Z-guggulsterone. The two forms are geometric isomers, meaning they have the same molecular formula but a different arrangement of atoms.

Pharmacology[edit | edit source]

In humans, guggulsterone acts as an antagonist of the farnesoid X receptor (FXR). FXR is a nuclear receptor that regulates the synthesis and transport of bile acids. Guggulsterone's antagonistic action on FXR was once believed to result in decreased cholesterol synthesis in the liver.

Clinical significance[edit | edit source]

Despite the pharmacological action of guggulsterone on FXR, clinical trials have shown that consumption of guggulsterone does not lead to decreased levels of cholesterol. This suggests that the mechanism of action of guggulsterone on cholesterol levels is not well understood.

See also[edit | edit source]

Guggulsterone Resources
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Contributors: Prab R. Tumpati, MD