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ID: ALA4665764
Journal: J Nat Prod
Title: Synthesis and Biological Evaluation of Celastrol Derivatives as Potential Immunosuppressive Agents.
Authors: He QW,Feng JH,Hu XL,Long H,Huang XF,Jiang ZZ,Zhang XQ,Ye WC,Wang H
Abstract: Celastrol, a friedelane-type triterpenoid isolated from the genus Triperygium, possesses antitumor, anti-inflammatory, and immunosuppressive activities. A total of 42 celastrol derivatives (1a-1t, 2a-2l, and 3a-3j) were synthesized and evaluated for their immunosuppressive activities. Compounds 2a-2e showed immunosuppressive effects, with IC values ranging from 25 to 83 nM, and weak cytotoxicity (CC > 1 μM). Compound 2a, with a selectivity index value 31 times higher than that of celastrol, was selected as a lead compound. Further research showed that 2a exerted its immunosuppressive effects by inducing apoptosis and inhibiting cytokine secretion via Lck- and ZAP-70-mediated signaling pathways.
CiteXplore: 32822186