摘要/Abstract

通过多步反应合成了一系列类黄酮取代的Tröger's base衍生物，测试了其对HepG2肝癌细胞的抗癌活性和四种细菌（铜绿假单胞菌PAM1032、野生型金黄色葡萄球菌，野生型大肠杆菌和大肠杆菌-大肠杆菌NMD-1）的抗菌活性.实验结果表明，该系列中有两种化合物在1 μg/mL下对金黄色葡萄球菌有很高的抑制率，有五种产物对HepG2肝癌细胞的IC₅₀值低于阳性对照紫杉醇（30.87 μg/mL），表现出较高的抑制活性，显示了其在新药研发领域潜在的应用价值.
关键词: Tröger's base, 黄酮类, 生物活性
A series of flavonoid-substituted Tröger's base analogues were synthesized via multi-step reaction. Their anti-cancer activities on the HepG2 hepatocellular carcinoma cell and antibacterial activities on four bacterial (Pseudomonas aeruginosa PAM1032, wild type Staphylococcus aureus, wild type Escherichia coli and Escherichia.coli-NMD-1) were evaluated. Two compounds were screened out because of their high inhibitory rate on Staphylococcus aureus at 1 μg/mL. The IC₅₀ values of five products on the HepG2 (hepatocellular carcinoma cell) were lower than that of positive control paclitaxel (30.87 μg/mL), displaying their high inhibitory activity. The results indicated their potential applications in new drug development.
Key words: Tröger's base, flavonoid, bioactivity


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