Guggulsterone and Its Role in Chronic Diseases.

Guggulsterone is a plant sterol derived from gum resin of Commiphora wightii. The gum resin from guggul plants has been used for thousand years in Ayurveda to treat various disorders, including internal tumors, obesity, liver disorders, malignant sores and ulcers, urinary complaints, intestinal worms, leucoderma, sinuses, edema, and sudden paralytic seizures. Guggulsterone has been identified a bioactive components of this gum resin. This plant steroid has been reported to work as an antagonist of certain nuclear receptors, especially farnesoid X receptor, which regulates bile acids and cholesterol metabolism. Guggulsterone also mediates gene expression through the regulation of transcription factors, including nuclear factor-kappa B and signal transducer and activator of transcription 3, which plays important roles in the development of inflammation and tumorigenesis. Guggulsterone has been shown to downregulate the expression of proteins involved in anti-apoptotic, cell survival, cell proliferation, angiogenic, metastatic, and chemoresistant activities in tumor cells. This review aimed to clarify the cell signal pathways targeted by guggulsterone and the bioactivities of guggulsterone in animal models and humans.