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Synthesis and antimycobacterial activity of ternatolide

Xing-Yue Ji+, Si-Yang Li+, Shuai Meng, Chun-Ling Xiao, Xue-Fu You, Zhuo-Rong Li*   

  1. Department of Medicinal Chemistry, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
  • Received:2012-01-13 Revised:2012-03-20 Online:2012-05-15 Published:2012-05-15
  • Contact: Zhuo-Rong Li*

Abstract:

Ternatolide isolated from Radix Ranuncoli Ternati is considered as the active ingredient against Mycobacterium tuberculosis. Herein, ternatolide was synthesized in four steps in 32.7% overall yield by using Yamaguchi esterification as the key step, and its antimycobacterial activity was investigated in vitro using a rapid direct susceptibility assay. It was reported that ternatolide killed the Mycobacterium tuberculosis possibly by enhancing the expression of GLS in PBLs indirectly, and our results indicated that ternatolide was weakly active against MTB H37Rv ATCC 27294 directly. Therefore, it can be concluded that its mechanism of action was possibly related to the cellular factors.

Key words: Ternatolide, Synthesis, Antimycobacterial activity

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