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首页> 外文期刊>Heterocycles: An International Journal for Reviews and Communications in Heterocyclic Chemistry >FURTHER BISINDOLE ALKALOIDS FROM CATHARANTHUS ROSEUS AND THEIR CYTOTOXICITY
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FURTHER BISINDOLE ALKALOIDS FROM CATHARANTHUS ROSEUS AND THEIR CYTOTOXICITY

机译:樟脑的双双吲哚碱及其细胞毒性

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Two novel bisindole alkaloids, cyclovinblastine A-B (1-2), together with ten known alkaloids 4-deacetoxycyclovinblastine (3), cycloleurosine (4), leurosine (5), vinblastine (6), leurosidine (7), vinblastine AVoxide (8), isoleurosine (9), 4'-deoxyleurosidine (10), 4'-deoxyleurosidine AVoxide (11) and 4-desacetoxyvinblastine (12) were isolated from the leaves of Catharanthus roseus. The structures of 1 and 2 were established by analysis of their NMR and HR-ESI-MS spectroscopic data. All alkaloids (1-12) were evaluated for their cytotoxic activities against the human hepatocellular carcinoma (HepG2) cell line, human colorectal carcinoma (Lovo) cell line, and human breast carcinoma (MCF-7) cell line by the MTT method in vitro, respectively. The results indicated that cytotoxic activities of alkaloids 9, 10 and 12 were much more potent than those of the positive control vinblastine (6). In addition, the structure-activity relationships (SAR) were conducted on the basis of the cytotoxicity of these isolated alkaloids.
机译:两个新的双吲哚生物碱,环长春碱AB(1-2)和十种已知的生物碱4-脱乙酰氧基环长春碱(3),环亮氨酸(4),亮氨酸(5),长春碱(6),亮氨酸(7),长春碱AVoxide(8) ,从长春花的叶子中分离出异芥子苷(9),4′-脱氧亮氨酸(10),4′-脱氧亮氨酸AVoxide(11)和4-脱乙酰氧长春花碱(12)。 1和2的结构通过对其NMR和HR-ESI-MS光谱数据进行分析来确定。通过MTT方法在体外评估了所有生物碱(1-12)对人肝细胞癌(HepG2),人结肠直肠癌(Lovo)和人乳腺癌(MCF-7)细胞的细胞毒活性, 分别。结果表明,生物碱9、10和12的细胞毒性活性比阳性对照长春花碱强得多(6)。另外,基于这些分离的生物碱的细胞毒性进行了构效关系(SAR)。

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