Characterization and Online Detection of Surfactin Isomers Based on HPLC-MSn Analyses and Their Inhibitory Effects on the Overproduction of Nitric Oxide and the Release of TNF-α and IL-6 in LPS-Induced Macrophages

被引:57
作者
Tang, Jin-Shan [1 ]
Zhao, Feng [2 ]
Gao, Hao [1 ,3 ]
Dai, Yi [1 ]
Yao, Zhi-Hong [1 ]
Hong, Kui [4 ]
Li, Jia [3 ,5 ]
Ye, Wen-Cai [1 ]
Yao, Xin-Sheng [1 ]
机构
[1] Jinan Univ, Inst Tradit Chinese Med & Nat Prod, Guangzhou 510632, Guangdong, Peoples R China
[2] Yantai Univ, Sch Pharm, Yantai 206005, Shandong, Peoples R China
[3] Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
[4] Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Haikou 571101, Hainan, Peoples R China
[5] Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
基金
中国国家自然科学基金;
关键词
LC-MS; Bacillus sp; surfactin isomer; anti-inflammatory activity; TANDEM MASS-SPECTROMETRY; CYCLIC LIPOPEPTIDE; BACILLUS-SUBTILIS; MECHANISM; CELLS;
D O I
10.3390/md8102605
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A rapid method for characterization and online detection of surfactin isomers was developed based on HPLC-MSn (n = 1, 2, 3) analyses, and many surfactin isomers were detected and characterized from the bioactive fraction of the mangrove bacterium Bacillus sp. Inhibitory activities of surfactin isomers on the overproduction of nitric oxide and the release of TNF-alpha and IL-6 in LPS-induced macrophages were systematically investigated. It was revealed that the surfactin isomers showed strong inhibitory properties on the overproduction of nitric oxide and the release of IL-6 on LPS-induced murine macrophage cell RAW264.7 with IC50 values ranging from 1.0 to 7.0. mu M. Structure-activity relationship (SAR) studies revealed that the existence of the free carboxyl group in the structure of surfactin isomers was crucial. These findings will be very helpful for the development of this novel kind of natural product as new anti-inflammatory agents.
引用
收藏
页码:2605 / 2618
页数:14
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