Guggulsterone health benefit and use to lower cholesterol and blood lipids, as potential for inflammation control
February 1 2017

Guggulsterone is a plant sterol present in the resin of the guggul plant, Commiphora mukul. Guggulsterone is an ingredient in many nutritional supplements.

Health benefit
Guggulsterone has been used to treat hyperlipidemia, arthritis, and obesity. Although its anti-inflammatory and anti-hyperlipidemic effects have been well documented. guggulsterone may be used to preserve functional beta-cell mass in the pancreas. These compounds may also be beneficial for the treatment of various cancers although most of the studies thus far have focused on in vitro experiments.

How do they work?
In humans, guggulsterones act as an antagonist of the farnesoid X receptor. In cells studies with adipocytes, guggulsterones may exert anti-obesity effects by inhibiting differentiation of preadipocytes, and by inducing apoptosis and promoting lipolysis of mature adipocytes.

Colon Cancer
Guggulsterone induces apoptosis in colon cancer cells and inhibits tumor growth in murine colorectal cancer xenografts.
Cancer Lett. 2009. Department of Internal Medicine and Institute of Gastroenterology, Brain Korea 21 Project for Medical Science, Yonsei University College of Medicine, 134 Shinchon-dong, Seodaemun-gu, Seoul, Republic of Korea.
The plant sterol guggulsterone has recently been shown to have anti-tumor potential. This study was designed to investigate the anti-tumor efficacy of guggulsterone and to elucidate its molecular mechanisms in colon cancer. Guggulsterone significantly increased apoptosis in HT-29 cells. The present study suggests a potential therapeutic use for this compound in the treatment of colorectal cancer.

Pancreas cancer
Cancer Lett. 2013. Guggulsterone decreases proliferation and metastatic behavior of pancreatic cancer cells by modulating JAK/STAT and Src/FAK signaling.

Prostate cancer
Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis.

Inflammatory bowel disease, anti-inflammatory
The plant sterol guggulsterone attenuates inflammation and immune dysfunction in murine models of inflammatory bowel disease.
Biochem Pharmacol. 2009; Mencarelli A, Renga B, Palladino G, Distrutti E, Fiorucci S. Dipartimento di Medicina Clinica e Sperimentale, Università di Perugia, Via E. dal Pozzo, Perugia, Italy.
Inflammatory bowel diseases (IBD) are chronic inflammatory and relapsing diseases of the gut that may manifest as either Crohn’s disease (CD) or ulcerative colitis (UC). CD and UC are immunologically different diseases characterized by exacerbated Th1 and Th2 response. T-cell resistance against apoptosis contributes to inappropriate T-cell accumulation and the perpetuation of chronic mucosal inflammation. In the present study we have investigated the effect exerted by guggulsterone in two models of intestinal inflammation induced in mice. We provided evidence that guggulsterones protect mice against development of sign and symptoms of colon inflammation. Guggulsterone is an anti-inflammatory compound with the capacity to prevent and ameliorate T-cell-induced colitis. These data ground the use of GS, a natural cholesterol-lowering agent, in the treatment of chronic inflammatory diseases.

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Molecules of guggulsterone have two stereoisomers, E-guggulsterone and Z-guggulsterone.