银杏叶聚戊烯醇含氮和含卤素衍生物的抑菌活性研究

利用含氮和含卤素试剂对银杏叶聚戊烯醇末端羟基进行含氮和含卤素的衍生化改性,结果得到5种衍生物,分别为聚戊烯基邻苯二甲酰亚胺(GPH)、氨基聚戊烯醇(GAM)、聚戊烯基季铵盐(GAS)、聚戊烯基三氟乙酰(GTF)和聚戊烯基氯乙酰(GCH),并用~1H NMR分别表征并证实了产物结构。通过比较产物抑菌圈直径和最小抑质量浓度(MIC)来筛选出抗菌作用较强的衍生物,结果显示:GAS对于大肠杆菌和金黄色葡萄球菌的抗菌活性均为最高,其抑菌圈为19.1~19.8 mm,MIC均为31.3 mg/L。同时研究了GAS在亚抑菌质量浓度下(15.6 mg/L)对大肠杆菌和金黄色葡萄球菌的杀菌曲线,结果显示:GAS对大肠杆菌和金黄色葡萄球菌在48 h内具有一定抗菌性;在前8 h内,GAS对于大肠杆菌和金黄色葡萄球菌的杀菌作用较强,致使菌群数量迅速下降;8 h以后,两种菌群都有不同程度的再生,抑菌活性减弱。

Synthesis and Antibacterial Activity of Nitrogenated and Haloid Derivatives of Ginkgo Biloba Leaves Polyprenol

Chemical structure modification of —OH in α-terminal unit of Ginkgo biloba leaves polyprenol ( GBP) was conducted to prepare five nitrogenated and haloid derivatives of GBP ,i. e. , polyprenyl phthalimides ( GPH) , polyprenyl amines ( GAM) , polyprenyl quaternary ammonium salt ( GAS ) , polyprenyl trifluoroacetate ( GTF ) and polyprenyl chloroacetate ( GCH ) . All derivatives were identified by 1H NMR. In the study of antibacterial activity, GAS had the highest antibacterial activity against strains Escherichia coli and Staphylococcus aureus with inhibition halos of 19. 1 - 19. 8 mm and the minimal inhibitory concentration(MIC) of 31. 3 mg/L. At the same time, the time-killing curves of GAS against E. coli and S. aureus under sub-MIC of 15. 6 mg/L were drawn and studied. And the results showed that GAS possessed antibacterial activity against E. coli and S. aureus in 48 h and the bacterial number was in a rapid decline within 8 h of exposure in the time-kill studies.