Characterization and online detection of surfactin isomers based on HPLC-MS(n) analyses and their inhibitory effects on the overproduction of nitric oxide and the release of TNF-α and IL-6 in LPS-induced macrophages.

Characterization and online detection of surfactin isomers based on HPLC-MS(n) analyses and their inhibitory effects on the overproduction of nitric oxide and the release of TNF-α and IL-6 in LPS-induced macrophages.
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DOI:
10.3390/md8102605
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发表时间:
2010-10-11
期刊:
影响因子:
5.4
通讯作者:
Yao XS
Yao XS
中科院分区:
医学2区
文献类型:
--
作者:
Tang JS;Zhao F;Gao H;Dai Y;Yao ZH;Hong K;Li J;Ye WC;Yao XS

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基于 HPLC-MSn (n = 1, 2, 3) 分析,开发了一种快速表征和在线检测表面活性素异构体的方法,并从红树林细菌芽孢杆菌的生物活性部分中检测和表征了许多表面活性素异构体。系统地研究了 surfactin 异构体对 LPS 诱导的巨噬细胞中一氧化氮过量产生以及 TNF-α 和 IL-6 释放的抑制活性。结果表明,表面活性素异构体对 LPS 诱导的鼠巨噬细胞 RAW264.7 的一氧化氮过量产生和 IL-6 释放具有很强的抑制作用,IC50 值范围为 1.0 至 7.0 μM。构效关系(SAR)研究表明,表面活性素异构体结构中游离羧基的存在至关重要。这些发现对于开发这种新型天然产物作为新型抗炎剂非常有帮助。
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.
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