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。 Small Ranunculus lactone has long been considered as the active ingredient of the anti-tuberculosis activity of cat’s claw. In this paper, the chemical synthesis and preparation of Ranoutula lactone were completed by Yamaguchi esterification in a total yield of 32.7%, and the anti-TB activity was evaluated by an intuitive and rapid antimicrobial susceptibility test. Reported in the literature, small Ranunculus lactone is by increasing the expression of granulocyte lysates of peripheral blood lymphocytes, indirectly kill Mycobacterium tuberculosis. In this paper, the results showed that the small Ranunculus lactone against Mycobacterium H37Rv ATCC27294 strains showed a weak inhibitory activity against Mycobacterium tuberculosis may be related cytokines.