Advances in structural modifications of celastrol

Abstract

Celastrol, a quinone methide triterpenoid from the Chinese medicinal root bark of Tripterygium wilfordii, possesses beneficial therapeutic properties and affects numerous cellular pathways. Recently, structure and activity relation studies based on celastrol semi-synthetic derivatives have contributed greatly to our understanding of its mechanism of action and cellular targets. These modifications have resulted in better activity and improvement of the pharmacokinetic properties of celastrol. This review will mainly cover advances in the structural modifications of celastrol at the C-20 carboxylic acid functionality, alterations of the A ring, and modifications at C-6.