新型黄酮-Tröger's碱类衍生物的合成及其生物活性
收稿日期: 2018-05-03
修回日期: 2018-07-27
网络出版日期: 2018-09-05
基金资助
江苏省高校优势学科建设工程项目、江苏省高校自然科学研究重点项目（No.15KJA180002）和江苏师范大学博士学位教师科研支持项目（No.17XLR023）资助项目.
Synthesis and Biological Evaluation of Novel Flavonoid-Substituted Tröger's Bases
Received date: 2018-05-03
Revised date: 2018-07-27
Online published: 2018-09-05
Supported by
Project supported by the Priority Academic Program Development of Jiangsu Higher Education Institutions, the Major Project of the Natural Science Research of University in Jiangsu Province (No. 15KJA180002) and the Aid Project for PhD Faculties in Jiangsu Normal University (No. 17XLR023).
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
苑睿 , 王园江 , 黄树颖 , 窦鹏飞 , 张珑严 , 陈雯 , 任璇璇 , 周生亮 , 宛瑜 , 吴翚 . 新型黄酮-Tröger's碱类衍生物的合成及其生物活性[J]. 有机化学, 2018 , 38(12) : 3338 -3344 . DOI: 10.6023/cjoc201805011
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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