Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents
Synthesis and biological evaluation of novel ocotillol-type triterpenoid derivatives as antibacterial agents
复制标题
新型抗菌奥克替醇型三萜类衍生物的合成及生物学评价
DOI：
10.1016/j.ejmech.2013.07.041
复制
发表时间：
2013-10-01
影响因子：
6.7
通讯作者：
Xu, Jinyi
中科院分区：
文献类型：
--
作者：
Zhou, Zhiwen;Ma, Cong;Xu, Jinyi
合成了一类新的油参醇型三萜衍生物，并对其对几种具有代表性的病原菌的体外抗菌活性进行了评价。化合物20(S)-protopanaxadiol （PPD）、3、5、16和24对革兰氏阳性菌具有较强的抗菌活性。化合物3和5对社区相关的耐甲氧西林金黄色葡萄球菌（CA-MRSA；菌株USA300）也显示出良好的抗菌活性。此外，化合物PPD、3和16与市售抗生素卡那霉素和氯霉素在亚mic浓度下对金黄色葡萄球菌USA300和枯草芽孢杆菌168有较强的协同抑制作用。此外，细胞毒活性测定显示，所测化合物不影响人上皮肾细胞（HEK-293）和人宫颈细胞（HeLa）的细胞活力。(C) 2013 Elsevier Masson SAS。版权所有。
A novel class of ocotillol-type triterpenoid derivatives have been synthesized and evaluated for their in vitro antibacterial activity against several representative pathogenic bacterial strains. Compounds 20(S)-protopanaxadiol (PPD), 3, 5,16 and 24 exhibited potent antibacterial activity against Gram-positive bacteria. Compounds 3 and 5 also displayed promising antibacterial activity against a community-associated methicillin-resistant Staphylococcus aureus (CA-MRSA; strain USA300). Furthermore, compounds PPD, 3 and 16 combined with two commercially available antibiotics kanamycin and chloramphenicol showed strong synergistic inhibitory effects at their sub-MIC concentrations against S. aureus USA300 and Bacillus subtilis 168. Additionally, cytotoxic activity assay showed that the compounds tested did not affect cell viability of the human epithelial kidney (HEK-293) and human cervical (HeLa) cells at their MICs. (C) 2013 Elsevier Masson SAS. All rights reserved.