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.
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Guggulsterone is a phytosterol extracted from the gum resin of the Commiphora wightii tree. Guggulsterone inhibits the growth of many tumour cells. It induces apoptosis by down-regulating anti-apoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP, and survivin), regulating cell cycle proteins (cyclin D1 and c-Myc), activating caspases and JNK, and inhibiting Akt[1].Guggulsterone acts as an FXR antagonist and reduces CDCA-induced FXR activation, with IC50 values of 17 and 15 μM for Z-Guggulsterone and E-Guggulsterone, respectively[2].Guggulsterone inhibited LPS-induced expression of TREM-1, TLR4 and TNF-α as well as phosphorylation of IκBα and NF-κB p65 in RAW 264.7 cells at concentrations ranging from 0.5-20 μM for 24 hours of treatment[2].
Guggulsterone 动物研究
Animal study
Administered orally at a dose of 100 mg/kg once daily for 8 days, Guggulsterone significantly increased the survival rate of TNBS-induced colitis in wild-type mice[2].
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