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. Issue 11 (1st June 2017)

• Record Type: Journal Article
• Authors: An, Ji-Young; Lee, Hwi-Ho; Shin, Ji-Sun; Yoo, Hyung-Seok; Park, Jong Seon; Son, Seung Hwan; Kim, Sang Won; Yu, Jihyun; Lee, Jun; Lee, Kyung-Tae; Kim, Nam-Jung
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 11(2017)
• Page Start: 2613
• Page End: 2616
• Publication Date: 2017-06-01
• Subjects: Flavone -- Nitric oxide (NO) -- Prostaglandin E2 (PGE2) -- Anti-inflammatory -- RAW 264.7 cell; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.03.057
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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 E2 (PGE2 ), representative pro-inflammatory mediators, in LPS-induced RAW 264.7 cells. Their structure-activity relationship was also investigated. In particular, we found that compound3g 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.