2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2613-2616. doi: 10.1016/j.bmcl.2017.03.057.
Ji-Young An 1,  Hwi-Ho Lee 2,  Ji-Sun Shin 2,  Hyung-Seok Yoo 1,  Jong Seon Park 1,  Seung Hwan Son 1,  Sang Won Kim 1,  Jihyun Yu 1,  Jun Lee 1,  Kyung-Tae Lee 3,  Nam-Jung Kim 4
Affiliations

Affiliations

  • 1 Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
  • 2 Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea.
  • 3 Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: ktlee@khu.ac.kr.
  • 4 Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Dongdaemun-gu, Seoul 130-701, Republic of Korea. Electronic address: kimnj@khu.ac.kr.
PMID: 28408221 DOI: 10.1016/j.bmcl.2017.03.057
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 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.

Keywords

Anti-inflammatory; Flavone; Nitric oxide (NO); Prostaglandin E(2) (PGE(2)); RAW 264.7 cell.

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