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齐墩果酸衍生物的合成与表征及其抑菌活性的研究
引用本文:赵龙铉,沈平,郑昌吉,赵春晖,张晓翠,杨君微,唐尧.齐墩果酸衍生物的合成与表征及其抑菌活性的研究[J].辽宁师范大学学报(自然科学版),2012(1):63-68.
作者姓名:赵龙铉  沈平  郑昌吉  赵春晖  张晓翠  杨君微  唐尧
作者单位:辽宁师范大学化学化工学院;辽宁师范大学生物技术与分子药物研发辽宁省重点实验室;延边大学长白山生物资源与功能分子教育部重点实验室
基金项目:吉林省科技厅科技计划项目(201015250)
摘    要:齐墩果酸属于五环三萜类化合物,在自然界中分布广泛,并显示出多种生物活性,如:保肝、抗炎、抗病毒、抗癌等多种药理作用,并具有良好的抑菌活性.因此本文以齐墩果酸为先导化合物,对其结构进行了修饰,合成4个中间体和6个新的目标产物,并经过IR、1 H NMR波谱测试技术对其结构进行了表征.并以其对培养于MHB(高铁血红蛋白)的S.a(金黄色葡萄球菌)4220、S.a(金黄色葡萄球菌)209、MRSA(抗甲氧西林金黄色葡萄球菌)3167、MRSA(抗甲氧西林金黄色葡萄球菌)3506、QRSA(抗喹诺酮金黄色葡萄球菌)3505、QRSA(抗喹诺酮金黄色葡萄球菌)3519和培养于BHI中的E.coli(大肠杆菌)1682、E.coli(大肠杆菌)1356等8种菌种进行抑菌活性测试,结果表明,部分化合物的抑菌活性较标准抗菌药物有明显提高.

关 键 词:齐墩果酸  合成  抑菌活性

Synthesisand characterization of oleanolic derivatives and the study on antibacterial activities
ZHAO Long-xuan,SHEN Ping,ZHENG Chang-ji,ZHAO Chun-hui,ZHANG Xiao-cui,YANG Jun-wei,TANG Yao.Synthesisand characterization of oleanolic derivatives and the study on antibacterial activities[J].Journal of Liaoning Normal University(Natural Science Edition),2012(1):63-68.
Authors:ZHAO Long-xuan  SHEN Ping  ZHENG Chang-ji  ZHAO Chun-hui  ZHANG Xiao-cui  YANG Jun-wei  TANG Yao
Institution:1(1.School of Chemistry and Chemical Engineering,Liaoning Normal University,Dalian 116029,China; 2.Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery,Liaoning Normal University,Dalian 116029,China; 3.Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education,Yanbian University College of Pharmacy,Yanji 133002,China)
Abstract:Oleanolic acid belongs to pentacyclic triterpenoid of natural products.It widely distributed in nature and showed many bioactivities such as hepatoprotective,anti-inflammatory,anti-cancer activity,antiviral pharmacological,so oleanolic acid was taken as the lead compound for modifying its structure in this paper.Ten kinds of intermediates and final products were synthesized through modification of oleanolic acid.These compounds were characterized by IR and 1H NMR techniques.These compounds were tested antibacterial activity of eight strains,which were S.a 4220,S.a 209,MRSA 3167,MRSA 3506,QRSA 3505,QRSA 3519 cultured on MHB and E.coli 1682、E.coli 1356 cultured on BHI.The results showed that the inhibit activities of some compounds were enhanced compared with those standard antibacterial medicines.
Keywords:oleanolic acid  synthesis  antibacterial activities
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