Ternatolide isolated from Radix Ranuncoli Ternati is considered as the active ingredient against Mycobacterium tuberculosis. Herein, tematolide was synthesized in four steps in 32.7% overall yield by using Yamaguchi e...Ternatolide isolated from Radix Ranuncoli Ternati is considered as the active ingredient against Mycobacterium tuberculosis. Herein, tematolide 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 tematolide 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.展开更多
基金National S&T Major Special Project on Major New Drug Innovation (Grant No. 2012ZX09102-101-001)
文摘Ternatolide isolated from Radix Ranuncoli Ternati is considered as the active ingredient against Mycobacterium tuberculosis. Herein, tematolide 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 tematolide 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.
