| 小毛茛内酯的合成及抗结核活性的研究(英文) |
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| 引用本文： | 季兴跃,李思阳,孟帅,肖春玲,游雪甫,李卓荣. 小毛茛内酯的合成及抗结核活性的研究(英文)[J]. 中国药学, 2012, 21(3): 265-268. DOI: 10.5246/jcps.2012.03.034 |
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| 作者姓名： | 季兴跃 李思阳 孟帅 肖春玲 游雪甫 李卓荣 |
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| 作者单位： | 中国医学科学院医药生物技术研究所有机化学室 |
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| 基金项目： | National S&T Major Special Project on Major New Drug Innovation (Grant No. 2012ZX09102-101-001) |
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| 摘 要： | 小毛茛内酯一直被认为是猫爪草抗结核活性的有效成分。本文通过Yamaguchi酯化反应以32.7%的总收率完成了小毛茛内酯的化学合成制备,并采用直观快速药敏实验技术评价了其抗结核活性。文献报道,小毛茛内酯是通过增加外周血淋巴细胞颗粒裂解肽的表达,间接杀死结核杆菌。本文研究结果显示,小毛茛内酯在体外对分支杆菌H37Rv ATCC27294菌株表现出了微弱的抑制活性,其抗结核杆菌作用可能与细胞因子有关。
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| 关 键 词： | 小毛茛内酯 合成 抗结核活性 |
Synthesis and antimycobacterial activity of ternatolide |
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| Xing-Yue Ji,Si-Yang Li,Shuai Meng,Chun-Ling Xiao,Xue-Fu You,Zhuo-Rong Li. Synthesis and antimycobacterial activity of ternatolide[J]. Journal of Chinese Pharmaceutical Sciences, 2012, 21(3): 265-268. DOI: 10.5246/jcps.2012.03.034 |
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| Authors: | Xing-Yue Ji Si-Yang Li Shuai Meng Chun-Ling Xiao Xue-Fu You Zhuo-Rong Li |
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| Affiliation: | * Department of Medicinal Chemistry,Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China |
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| 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. |
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| Keywords: | Ternatolide Synthesis Antimycobacterial activity |
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