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

Marine Drugs

Jin-Shan Tang¹  Feng Zhao³  Hao Gao¹  Yi Dai¹  Zhi-Hong Yao¹  Kui Hong²  Jia Li⁴  Wen-Cai Ye¹ 

[1] Institute of Traditional Chinese Medicine & Natural Products, Jinan University, Guangzhou 510632, Guangdong, China; E-Mails:;Institute of Tropical Biosciences and Biotechnology, Chinese Academy of Tropical Agriculture Sciences, Haikou 571101, Hainan, China; E-Mail:;School of Pharmacy, Yantai University, Yantai 206005, Shandong, China; E-Mail:;State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China; E-Mail:

关键词: LC-MS;    Bacillus sp.;    surfactin isomer;    anti-inflammatory activity;   

DOI  :  10.3390/md8102605

来源: mdpi

【 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-α 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 μM. 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.

【 授权许可】

CC BY   
© 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland