生物活性：
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.

体内活性：
GugguLsterone (口服；100 mg/kg，每天一次，持续 8 天) 显著提高了患有 TNBS 诱导的结肠炎的野生型小鼠的存活率。

体外活性：
GugguLsterone (0.5 -20 μM；24 小时) 抑制 TREM-1、TLR4 和 TNF-α 的表达以及 LPS 对 IκBα 和 NF-κB p65 的磷酸化。