藤黄酸衍生物的合成与抗菌活性研究及其对拓扑异构酶的影响

Antibacterial Activity of Gambogic Acid and its Derivatives and Effects on Topoisomerase

藤黄酸分子式为C_(38)H_(44)O_9,具有较好的抗肿瘤活性,但尚无其抑制细菌生长方面活性报道.以藤黄酸为母药,合成得到藤黄酸甲酯和藤黄酸二甲基乙酰胺两种藤黄酸衍生物,考察这几种药物对革兰氏阳性细菌金黄色葡萄球菌和革兰氏阴性细菌大肠杆菌的生长的影响,并通过凝胶电泳法检测几种药物对DNA拓扑异构酶活性的影响.实验结果表明,三种药物对革兰氏阴性细菌大肠杆菌均无抑制作用,对革兰氏阳性细菌金黄酥葡萄球菌有抑制作用.藤黄酸及其衍生物可以通过抑制拓扑异构酶的活性而抑制革兰氏阳性细菌金黄酥葡萄球菌生长的作用.

Gambogic Acid(C38H44O9),a chinese midicine with good antitumoractivity,within no related reports on its inhibitory activity of bacterial.In this paper,we synthesized twoderivatives of Gambogic acid.To investigate the effects of these drugs on Gram-positive bacteria Staphylococcus aureus and Gram-negative bacteria Escherichia coli,we performed antibacterial experiments with oxford cup method.Then we performed DNA agarose gel electrophoresis to detect the effects with DNA topoisomerase Ⅰ and Ⅱ.The results showed that all of the drugs had no inhibitory effectson gram-negative bacteria Escherichia coli,but had inhibitory effects on gram-positivebacteria Staphylococcus aureus.We proved these three drugs can inhibit the activity of topoisomerase Ⅰ and Ⅱ.