来自海洋海绵Dysidea的具有强效和广谱抗菌活性的多溴二苯醚

Polybrominated diphenyl ethers with potent and broad spectrum antimicrobial activity from the marine sponge Dysidea.

作者信息

Sun Shi, Canning Corene B, Bhargava Kanika, Sun Xiuxiu, Zhu Wenjun, Zhou Ninghui, Zhang Yifan, Zhou Kequan

机构信息

Department of Nutrition and Food Science, Wayne State University, 5045 Cass Ave, Detroit, MI 48202, United States.

Nutrition and Food Management, Human Environmental Sciences, Box 118, University of Central Oklahoma, 100 N. University Drive, Edmond, OK 73034, United States.

出版信息

Bioorg Med Chem Lett. 2015;25(10):2181-3. doi: 10.1016/j.bmcl.2015.03.057. Epub 2015 Mar 25.

DOI:10.1016/j.bmcl.2015.03.057

PMID:25863431

Abstract

Three polybrominated diphenyl ethers, 2-(2',4'-dibromophenoxy)-3,5-dibromophenol (1) and 2-(2',4'-dibromophenoxy)-3,4,5-tribromophenol (2) were isolated from the marine sponge Dysidea granulosa; and 2-(2',4'-dibromophenoxy)-4,6-dibromophenol (3) from Dysidea spp. They exhibited potent and broad spectrum in vitro antibacterial activity, especially against methicillin resistant Staphylococcus aureus (MRSA), methicillin sensitive Staphylococcus aureus (MSSA), Escherichia coli O157:H7, and Salmonella. Minimal inhibitory concentration (MIC) was evaluated against 12 clinical and standard strains of Gram positive and negative bacteria. The observed MIC range was 0.1-4.0mg/L against all the Gram positive bacteria and 0.1-16.0mg/L against Gram negative bacteria. 2-(2',4″-Dibromophenoxy)-3,5-dibromophenol showed stronger broad spectrum antibacterial activity than other two compounds. 2-(2',4″-Dibromophenoxy)-3,5-dibromophenol and 2-(2',4'-dibromophenoxy)-4,6-dibromophenol are thermo-stable. The results suggest that 2-(2',4'-dibromophenoxy)-3,5-dibromophenol could be used as a potential lead molecule for anti-MRSA, anti-E. coli O157:H7, and anti-Salmonella for drug development.

摘要

从海洋海绵粒皮盘海绵中分离出三种多溴二苯醚、2-(2',4'-二溴苯氧基)-3,5-二溴苯酚(1)和2-(2',4'-二溴苯氧基)-3,4,5-三溴苯酚(2)；从皮盘海绵属中分离出2-(2',4'-二溴苯氧基)-4,6-二溴苯酚(3)。它们在体外表现出强大且广谱的抗菌活性，尤其对耐甲氧西林金黄色葡萄球菌(MRSA)、甲氧西林敏感金黄色葡萄球菌(MSSA)、大肠杆菌O157:H7和沙门氏菌。针对12株革兰氏阳性和阴性细菌的临床及标准菌株评估了最低抑菌浓度(MIC)。观察到的MIC范围对所有革兰氏阳性细菌为0.1 - 4.0mg/L，对革兰氏阴性细菌为0.1 - 16.0mg/L。2-(2',4″-二溴苯氧基)-3,5-二溴苯酚比其他两种化合物表现出更强的广谱抗菌活性。2-(2',4″-二溴苯氧基)-3,5-二溴苯酚和2-(2',4'-二溴苯氧基)-4,6-二溴苯酚具有热稳定性。结果表明，2-(2',4'-二溴苯氧基)-3,5-二溴苯酚可作为抗MRSA、抗大肠杆菌O157:H7和抗沙门氏菌药物开发的潜在先导分子。