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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Antitubercular and cytotoxic tigliane-type diterpenoids from Croton tiglium
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Antitubercular and cytotoxic tigliane-type diterpenoids from Croton tiglium

机译:巴豆虎耳草的抗结核和细胞毒性虎胆碱型二萜

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Five new tigliane diterpene esters (1-5), highly oxygenated tetracyclic diterpenoid carbon skeleton, together with three known analogues (6-8) were isolated from the leaves of Croton tiglium. Extensive NMR and mass spectroscopic analysis were used to elucidate their structures. Most of the isolated compounds were tested for their cytotoxic and antitubercular activities. Among them, the cytotoxic activities of these tigliane-type diterpenes strongly depend on the species of the tumor cells. Especially, these bioactivity compounds showed strong cytotoxic activities against the K562 cell line, and their inhibition effects were close to the positive control Taxol. Furthermore, compounds 1, 2, 6, and 7 showed potent antitubercular activities with MIC values of 19.5, 20.9, 20.5, and 13.4 mu M, respectively. (C) 2016 Elsevier Ltd. All rights reserved.
机译:从巴豆虎的叶子中分离出了五种新的tigliane二萜酯(1-5),高度氧化的四环二萜碳骨架以及三种已知的类似物(6-8)。广泛的NMR和质谱分析被用来阐明它们的结构。测试了大多数分离出的化合物的细胞毒性和抗结核活性。其中,这些蒂利亚内型二萜的细胞毒活性强烈依赖于肿瘤细胞的种类。特别地,这些生物活性化合物显示出对K562细胞系的强细胞毒性活性,并且它们的抑制作用接近于阳性对照紫杉醇。此外,化合物1、2、6和7表现出有效的抗结核活性,MIC值分别为19.5、20.9、20.5和13.4μM。 (C)2016 Elsevier Ltd.保留所有权利。

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