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当代肿瘤药物靶点

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ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

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Research Article

6-羟基黄嘌呤二烯叠氮衍生物的合成及细胞毒活性

卷 20, 期 9, 2020

页: [666 - 674] 页: 9

弟呕挨: 10.2174/1568009620999200421200338

价格: $65

摘要

背景：已经合成并通过NMR光谱仪鉴定并合成了6-羟基黄嘌呤二烯的eremophilane系列的倍半萜内酯与氢化杂志（哌啶和哌嗪）的共轭物。 目的：从植物土木香（Inula helenium L）中提取具有异常骨架“ 6-羟基黄嘌呤二烯”的内酯，并用NMR光谱仪鉴定各种物种。 方法：研究了A549，HCT116，RD和Jurkat等不同肿瘤系的细胞毒性，线粒体和抗氧化活性，并确定了可能的机制。 结果：结果表明，最有效的化合物是IIIi，对RD细胞具有最高的细胞毒性（IC50 25.23} 0.04μM），使线粒体膜去极化，并且是一种有效的抗氧化剂（IC50抑制LP 10.68} 3.21μM），没有任何对健康细胞的毒副作用。 结论：倍半萜烯内酯6-羟基黄嘌呤二烯III与氢化叠氮的结合可能有助于设计潜在的有前途的抗癌药物。

关键词: 6-羟基黄嘌呤二烯，叠氮，细胞毒性，线粒体，细胞凋亡，抗氧化剂，抗癌药。

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