Guggulsterone health benefit and
use to lower cholesterol and blood lipids, as potential for inflammation control
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 of guggulsterones
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 guggulsterones work?
In humans, guggulsterones act as an antagonist of the farnesoid X receptor. In
cells studies with adipocytes, guggulsterones may exert antiobesity 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 February. 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 120-752, 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 by activating
caspases-3 and -8. Furthermore, guggulsterone decreased cIAP-1, cIAP-2, and
Bcl-2 levels and increased the levels of truncated Bid, Fas, p-JNK, and p-c-Jun.
The present study suggests a potential therapeutic use for this compound in the
treatment of colorectal cancer.
Inflammatory bowel disease
The plant sterol guggulsterone attenuates inflammation and immune dysfunction in
murine models of inflammatory bowel disease.
Biochem Pharmacol. 2009 November; 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 (GS) a plant derived steroid isolated from the
gum resin of the Commiphora mukul tree, in two models of intestinal inflammation
induced in mice by trinitro-benzene sulfonic acid (TNBS) and oxazolone. We
provided evidence that E-GS protects mice against development of sign and
symptoms of colon inflammation. E-GS effectively attenuated the severity of
wasting disease and the fecal score and colon inflammation as assessed by
measuring the macroscopic- and microscopic-damage scores. Administration Z-GS
failed to ameliorate colon inflammation in TNBS-induced colitis and had a
partial effect in oxazolone-induced colitis. In vitro, mechanistic studies
carried out using CD4+ cells isolated from the intestinal lamina propria
demonstrate that GS effectively regulates the function of effector T cells by
modulating cell signaling activation pathway caused by CD3/CD28. The net
biological effects resulting from exposure to GS includes attenuation of
generation of interleukin-2 and -4 and interferon-gamma as well as T cell
proliferation. In conclusion, 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.
Guggulsterone and prostate cancer
Z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora
mukul, inhibits the growth of human prostate cancer cells by causing apoptosis.
Molecules of guggulsterone have two stereoisomers, E-guggulsterone and Z-guggulsterone.
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