熊果酸衍生物的合成及其抗菌活性评价

被引：9

作者：

孟英才

詹济华

肖水平

谭洋

廖美芳

张雨林

李玲

裴刚

机构：

[1] 湖南中医药大学药学院

来源：

湖南中医药大学学报 | 2017年 / 37卷 / 05期

关键词：

熊果酸; 衍生物; 抗菌药; 合成; 抑制;

D O I：

暂无

中图分类号：

R284 [中药化学]; R285 [中药药理学];

学科分类号：

100804 [中药化学]; 100806 [中药药理学];

摘要：

目的对熊果酸A环进行结构修饰,并研究其体外抗菌活性。方法以熊果酸(1)为原料,合成A环不同的熊果酸衍生物2-13,并用大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌、表皮葡萄球菌、藤黄微球菌和枯草杆菌这6种细菌对熊果酸衍生物进行体外抗菌活性筛选。结果大部分熊果酸衍生物显示很强的抗菌活性,其中化合物7对金黄色葡萄球菌的MIC值为6.3μmol/L,化合物8和化合物9对藤黄微球菌的MIC值分别为12.5μmol/L和6.3μmol/L,化合物11对六个菌种的MIC值均为3.1μmol/L,化合物12对大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌、表皮葡萄球菌的MIC值为3.1μmol/L。结论熊果酸A环化学结构修饰能够有效提高其抗菌活性,尤其是A环引入双键或环氧基,可为熊果酸抗菌衍生物的进一步研发提供依据。

引用

页码：493 / 498

页数：6

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