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作 者:宋薇 许小蓉 葛洁 李慧玲 文爱东 王婧雯 张晓梅 张娟利 SONG Wei;XU Xiaorong;GE Jie;LI Huilin;WEN Aidong;WANG Jingwen;ZHANG Xiaomei;ZHANG Juanli(Department of Pharmacy,The First Affiliated Hospital of Air Force Medical University,Xi’an 710032,China;Yunnan University of Chinese Medicine,Kunming 650500,China)
机构地区:[1]空军军医大学第一附属医院药剂科,西安710032 [2]云南中医药大学,昆明650500
出 处:《中国现代应用药学》2022年第20期2573-2577,共5页Chinese Journal of Modern Applied Pharmacy
基 金:国家自然科学基金项目(81602979,21662048)。
摘 要:目的对剑叶龙血树内生链霉菌S009中抗菌活性成分进行研究。方法采用Sephadex LH-20、反相柱色谱、硅胶柱层析及HPLC对S009菌株的发酵产物进行分离纯化,并通过MS、NMR等波谱技术鉴定其结构。结果从S009菌株中分离并鉴定了4个大环四重内酯类化合物,分别为nonactin(1)、monactin(2)、dinactin(3)和trinactin(4)。活性结果显示化合物3和4对多种G^(+)菌、G^(–)菌和白色念珠菌均显示较强的抗菌活性。另外,化合物2~4还具有很强的抗耐甲氧西林金黄色葡萄球菌(methicillin-resistant Staphylococcus aureus,MRSA)活性,其对所测试的多种MRSA菌株的最低抑制浓度(minimum inhibitory concentration,MIC)均小于或等于阳性药万古霉素(1~4μg·mL^(-1)),尤其以化合物3活性最为显著(MIC≤0.125μg·mL^(-1))。结论本研究结果不仅可为研制新型抗MRSA药物提供先导化合物,同时对有效利用和保护珍稀濒危植物剑叶龙血树资源具有重要意义。OBJECTIVE To investigate the antibacterial components of endophytic Streptomyces S009 from Dracaena cochinchinensis.METHODS The fermentation extracts of S009 were isolated and purified by Sephadex LH-20,reversed phase column chromatography,silica gel column chromatography and semi-preparative HPLC.The chemical structures were identified by MS and NMR spectral analysis.RESULTS Four macrotetrolide components,including nonactin(1),monactin(2),dinactin(3)and trinactin(4),were isolated and identifed from S009.The bioactivity results showed that compounds 3 and 4possessed strong antibacterial activity against various G^(+) bacteria,G^(-) bacteria and Candida albicans.In addition,compounds 2–4also had strong anti-methicillin-resistant Staphylococcus aureus(MRSA)activity,and the minimum inhibitory concentration(MIC)values of them against a variety of tested MRSA strains were less than or equal to that of positive drug,vancomycin(MIC:1–4μg·mL^(-1)).Especially,compound 3 had the most significant activity(MIC≤0.125μg·mL^(-1)).CONCLUSION The results of this study can not only provide lead compounds for developing new anti-MRSA drugs,but also has important meaning for the effective utilization and protection of the rare and endangered Dracaena cochinchinensis.
关 键 词:剑叶龙血树 内生链霉菌 结构鉴定 大环四重内酯类成分 耐甲氧西林金黄色葡萄球菌
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