Identification and structure activity relationship of novel flavone derivatives that inhibit the production of nitric oxide and PGE2 in LPS-induced RAW 264.7 cells

被引：12

作者：

An, Ji-Young ^{[1
]}

Lee, Hwi-Ho ^{[2
]}

Shin, Ji-Sun ^{[2
]}

Yoo, Hyung-Seok ^{[1
]}

Park, Jong Seon ^{[1
]}

Son, Seung Hwan ^{[1
]}

Kim, Sang Won ^{[1
]}

Yu, Jihyun ^{[1
]}

Lee, Jun ^{[1
]}

Lee, Kyung-Tae ^{[2
]}

Kim, Nam-Jung ^{[1
]}

机构：

[1] Kyung Hee Univ, Coll Pharm, Dept Pharm, 26 Kyungheedae Ro, Seoul 130701, South Korea

[2] Kyung Hee Univ, Dept Life & Nanopharmaceut Sci, 26 Kyungheedae Ro, Seoul 130701, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 11期

基金：

新加坡国家研究基金会;

关键词：

Flavone; Nitric oxide (NO); Prostaglandin E-2 (PGE(2)); Anti-inflammatory; RAW; 264.7; cell; COX-2; ACTIVITY; INFLAMMATION; CANCER; POLYPHENOLS; ANTICANCER; PATHWAY; CHRYSIN; ACID; INOS; NO;

D O I：

10.1016/j.bmcl.2017.03.057

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an effort to identify novel anti-inflammatory compounds, a series of flavone derivatives were synthesized and biologically evaluated for their inhibitory effects on the production of nitric oxide (NO) and prostaglandin E-2 (PGE(2)), representative pro-inflammatory mediators, in LPS-induced RAW 264.7 cells. Their structure-activity relationship was also investigated. In particular, we found that compound 3g displayed more potent inhibitory activities on PGE2 production, similar inhibitory activities on NO production and less weak cytotoxicity than luteolin, a natural flavone known as a potent anti-inflammatory agent. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：2613 / 2616

页数：4

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