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

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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