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Celastrol is a pentacyclic triterpenoid isolated from Tripterygium wilfordii that has long been used in traditional Chinese medicine for treating rheumatoid arthritis. Previous studies showed that celastrol possessed diverse biological activities, including anti-inflammatory and anticancer properties. Interestingly, most recent literatures revealed the important role of celastrol against metabolic disorders. Herein, we provide an overview of the modes of action of celastrol for combating metabolic diseases such as obesity and type 2 diabetes. The anti-obesity effect of celastrol results from relieving endoplasmic reticulum stress in hypothalamus, regulating HSF1-PGC1α axis in the adipose tissue and muscle, and alleviating inflammation via Nur77 mediated autophagy. Celastrol also reverses insulin resistance via NF-κB signaling pathway to protect against type 2 diabetes.
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