Synthesis of biflavones having a 6-O-7" linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase

Che, Haiyan; Park, Byung Kyu; Lim, Hyun; Kim, Hyun Pyo; Chang, Hyeun Wook; Jeong, Jin-Hyun; Park, Haeil

doi:10.1016/j.bmcl.2008.11.017

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Synthesis of biflavones having a 6-O-7" linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase

Che, Haiyan;
Park, Byung Kyu;
Lim, Hyun;
Kim, Hyun Pyo;
Chang, Hyeun Wook;
외 2명

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18

초록

In order to establish anti-inflammatory potential of biflavonoids, 17 biflavone derivatives having a 6-O-7 '' linkage were synthesized and their effects on cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) were evaluated. The basic molecule (6-O-7 '' biflavone) potently inhibited COX-2-mediated PGE(2) production (IC50: < 2 mu M), being less active on iNOS-mediated NO production (IC50: > 50 mu M) from lipopolysaccharide-treated RAW 264.7 cells, a mouse macrophage cell line. Generally, the hydroxyl/methoxyl substitution(s) on the basic biflavone (6-O-7 '') reduced the inhibitory activity of PGE(2) production, while the effects on NO production were varied. It is suggested that the basic biflavone (6-O-7 '') may have a potential for new anti-inflammatory agent. (C) 2008 Elsevier Ltd. All rights reserved.

키워드

6-O-7 '' biflavonoid; Cyclooxygenase; Nitric oxide synthase; Anti-inflammation; PHOSPHOLIPASE A(2)

제목: Synthesis of biflavones having a 6-O-7" linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase

저자: Che, Haiyan; Park, Byung Kyu; Lim, Hyun; Kim, Hyun Pyo; Chang, Hyeun Wook; Jeong, Jin-Hyun; Park, Haeil

DOI: 10.1016/j.bmcl.2008.11.017

발행일: 2009-01-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 19

호: 1

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