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基于 HPLC-MS(n) 分析的表面活性剂异构体的表征和在线检测及其对 LPS 诱导的巨噬细胞中一氧化氮过度产生和 TNF-α及 IL-6 释放的抑制作用。

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.

机构信息

Institute of Traditional Chinese Medicine & Natural Products, Jinan University, Guangzhou 510632, Guangdong, China.

出版信息

Mar Drugs. 2010 Oct 11;8(10):2605-18. doi: 10.3390/md8102605.

DOI:10.3390/md8102605
PMID:21116409
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2992995/
Abstract

A rapid method for characterization and online detection of surfactin isomers was developed based on HPLC-MS(n) (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 IC(50) 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.

摘要

建立了基于 HPLC-MS(n)（n=1、2、3）分析的表面活性素异构体的快速鉴定和在线检测方法，并从红树林细菌芽孢杆菌的生物活性部分检测和鉴定出许多表面活性素异构体。系统研究了表面活性素异构体对脂多糖诱导的巨噬细胞中一氧化氮过量产生和 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 中一氧化氮的过量产生和 IL-6 的释放具有很强的抑制作用，IC（50）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是至关重要的。这些发现将对开发这种新型天然产物作为新型抗炎剂非常有帮助。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/d5d07465e247/marinedrugs-08-02605f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/8fe33889041f/marinedrugs-08-02605f1a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/12175dbaa4f2/marinedrugs-08-02605f2a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/9810d888fa90/marinedrugs-08-02605f3a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/b642a1f00cdc/marinedrugs-08-02605f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/523bba60395e/marinedrugs-08-02605f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/d5d07465e247/marinedrugs-08-02605f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/8fe33889041f/marinedrugs-08-02605f1a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/12175dbaa4f2/marinedrugs-08-02605f2a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/9810d888fa90/marinedrugs-08-02605f3a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/b642a1f00cdc/marinedrugs-08-02605f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/523bba60395e/marinedrugs-08-02605f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0fbb/2992995/d5d07465e247/marinedrugs-08-02605f6.jpg

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