Stemcell, 100-0252, (Z)-Guggulsterone

(Z)-Guggulsterone is a plant steroid found in the resin of the guggul plant Commiphora mukul that acts as a selective antagonist of farnesoid X receptor (FXR; Cui et al.). It decreases chenodeoxycholic acid-induced FXR activation (IC₅₀ = 10 μM) in the presence of 100 μM chenodeoxycholic acid (Cui et al.; Urizar et al.).

DIFFERENTIATION

· Induces differentiation of human pluripotent stem cell-derived neural stem cells into dopaminergic neurons (Gonzalez et al.).

METABOLISM

· Decreases hepatic low-density lipoprotein cholesterol and triglyceride levels in rodents fed with a high-cholesterol diet (Urizar et al.).

CANCER RESEARCH

· Regulates growth and metastasis of tumor cells in human multiple myeloma cells by the expression of STAT3-regulated antiapoptotic (Bcl-2, Bcl-xL, and Mcl-1), proliferative (cyclin D1), and angiogenic (VEGF) gene products (Ahn et al.).

· Inhibits tube formation in human umbilical vein endothelial cells (HUVECs) and migration in HUVECs or a human prostate cancer cell line (Xiao et al.).