期刊
JOURNAL OF NATURAL PRODUCTS
卷 83, 期 9, 页码 2578-2586出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.0c00067
关键词
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资金
- National Natural Science Foundation of China [81573309, 81973206, 81773995]
- Funding of Double First-rate Discipline Innovation Team [CPU2018PZQ17, CPU2018PZQ18, CPU2018GF05]
- Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program [2017BT01Y036]
- Major National Science and Technology Projects of the Chinese Thirteen Five-year Plan [2017ZX09309024]
- National Key R&D Program of China [2017YFC1703802]
- China Postdoctoral Science Foundation [2019M662006, 2019TQ0357]
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 IC50 values ranging from 25 to 83 nM, and weak cytotoxicity (CC50 > 1 mu M). 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.
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