Monday, March 5, 2012

Are you buying (Z)-Guggulsterone?

Description
The trans stereoisomer of guggulsterone, (Z)-Guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50 value of 17 µM. By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet. While both cis and trans stereoisomers have been shown to directly decrease hepatic cholesterol, the Z isomer is the most studied. (Z)-Guggulsterone demonstrates antitumor-promoting effects inhibiting both constitutive and interleukin-6-induced STAT3 activation in human multiple myeloma cells and suppressing the VEGF-VEGF/R2-Akt signaling axis in DU145 human prostate cancer cells.
Guggulsterone is a plant steroid found in the resin of the guggul plant, Commiphora mukul. 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. Several studies have been published that indicate no overall reduction in total cholesterol occurs using various dosages of guggulsterone, and levels of low-density lipoprotein ("bad cholesterol") increased in many people. Nevertheless, guggulsterone is an ingredient in many nutritional supplements.
(Z)-Guggulsterone is a synthetic form of the guggul tree plant steroid that exhibits an ability to lower LDL cholesterol and triglyceride levels. Acts as a selective antagonist of farnesoid X receptor (FXR) and inhibits FXR transactivation (IC50 = 10 µM in the presence of 100 µM chenodeoxycholic acid). Does not activate or inhibit transactivation of liver X receptor α (LXRα), peroxisome proliferator activated receptor γ (PPARγ), or retinoid X receptor α (RXRα).
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