guggulsterone

**Guggulsterone** is a phytosteroid isolated from the resin of the guggul plant (Commiphora mukul), primarily found in two stereoisomeric forms: E-guggulsterone and Z-guggulsterone[1][5]. It acts as a broad-spectrum ligand of steroid hormone receptors and is known for antagonizing the farnesoid X receptor (FXR), historically thought to reduce cholesterol synthesis in the liver, although clinical evidence does not support significant cholesterol-lowering effects[1][4]. Guggulsterone displays antagonist or partial agonist activity at several other nuclear receptors (mineralocorticoid, progesterone, glucocorticoid, androgen, and estrogen receptors), and acts as an agonist at the pregnane X receptor[1]. Experimental studies in cells and animals suggest anti-inflammatory, antiapoptotic, and antitumor activities, mediated through modulation of multiple signaling pathways (e.g., NF-kB, STAT3, PI3K/Akt, apoptosis regulators), but there is limited clinical evidence for these uses[3][4][7]. It is commonly present as an ingredient in nutritional supplements, especially those targeted at lipid disorders, inflammation, and purported weight management[7][10].

Other names

Pregna-4,17(20)-diene-3,16-dioneE-guggulsteroneZ-guggulsterone