Novel 3-Substituted Ocotillol-Type Triterpenoid Derivatives as Antibacterial Candidates
Novel 3-Substituted Ocotillol-Type Triterpenoid Derivatives as Antibacterial Candidates
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DOI：
10.1111/cbdd.12337
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发表时间：
2014-10-01
影响因子：
3
通讯作者：
Xu, Jinyi
中科院分区：
文献类型：
--
作者：
Bi, Yi;Ma, Cong;Xu, Jinyi
植物源性三萜皂苷通过靶向细菌膜参与植物防御系统。以人参主要成分PPD为原料，合成了一系列奥克替醇型三萜类衍生物，并评价了其对几种代表性细菌的抗菌活性。化合物5和11表现出优异的抗菌活性，对金黄色葡萄球菌的MIC值分别为1μg/mL，对枯草芽孢杆菌的MIC值分别为8μg/mL和4μg/mL。此外，当化合物5和11与两种市售抗生素卡那霉素和氯霉素组合时，它们在亚MIC水平下对金黄色葡萄球菌USA300和枯草芽孢杆菌168表现出很强的协同活性。此外，当与化合物11组合时，氯霉素从抑菌剂转变为杀菌剂，对抗枯草芽孢杆菌168。
Plant-derived triterpenoid saponins are involved in the plant defense system by targeting bacterial membranes. A series of ocotillol-type triterpenoid derivatives were synthesized starting from PPD, one of the main components of Panax ginseng and their antibacterial activity against several representative bacteria were evaluated. Compounds 5 and 11 exhibited excellent antibacterial activity with MIC values of 1 mu g/mL against Staphylococcus aureus and 8 mu g/mL and 4 mu g/mL against Bacillus subtilis, respectively. Furthermore, when compounds 5 and 11 were combined with two commercial antibiotics kanamycin and chloramphenicol, they showed strong synergistic activity at sub-MIC levels against S. aureus USA300 and B. subtilis 168. Moreover, chloramphenicol turned from a bacteriostatic to a bactericidal agent when combined with compound 11 against B. subtilis 168.