The Marine Science Institute , University of the Philippines , Diliman, Quezon City 1101 , Philippines.
Department of Medicinal Chemistry , University of Utah , Salt Lake City , Utah 84112 , United States.
J Nat Prod. 2019 Apr 26;82(4):1024-1028. doi: 10.1021/acs.jnatprod.8b00979. Epub 2019 Feb 22.
Three new pyoluteorin analogues, mindapyrroles A-C (1-3), were purified from Pseudomonas aeruginosa strain 1682U.R.0a.27, a gill-associated bacterium isolated from the tissue homogenate of the giant shipworm Kuphus polythalamius. Mindapyrroles B and C inhibit the growth of multiple pathogenic bacteria, with mindapyrrole B (2) showing the most potent antimicrobial activity and widest selectivity index over mammalian cells. Preliminary structure-activity relationship analysis showed that dimerization of the pyoluteorin moiety through a C-C linkage is detrimental to the antimicrobial activity, but addition of an aerugine unit in the methylene bridge is favorable for both the antimicrobial activity and selectivity index.
三种新的吡咯素类似物，mindapyrroles A-C（1-3），从来源于巨型船蛆 Kuphus polythalamius 组织匀浆的鳃相关细菌铜绿假单胞菌 1682U.R.0a.27 中分离纯化得到。Mindapyrroles B 和 C 抑制多种病原菌的生长，mindapyrrole B（2）对哺乳动物细胞表现出最有效的抗菌活性和最宽的选择性指数。初步的构效关系分析表明，吡咯素部分通过 C-C 键二聚化不利于抗菌活性，但在亚甲基桥中添加一个 aerugine 单元有利于抗菌活性和选择性指数。
