Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Fimasartan, Anti-hypertension Drug, Suppressed Inducible Nitric Oxide Synthase Expressions via Nuclear Factor-Kappa B and Activator Protein-1 Inactivation
Suran RyuJi-Sun ShinYoung-Wuk ChoHyoung Kook KimSoo Heui PaikJoo Han LeeYong Ha ChiJi Han KimJe Hak KimKyung-Tae Lee
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Supplementary material

2013 Volume 36 Issue 3 Pages 467-474

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Abstract

Since inhibition of angiotensin II type 1 (AT1) receptor reduces chronic inflammation associated with hypertension, we evaluated the anti-inflammatory potential and the underlying mechanism of fimasartan, a Korean Food and Drug Administration approved anti-hypertension drug, in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Fimasartan suppressed the expressions of inducible nitric oxide synthase (iNOS) by down-regulating its transcription, and subsequently inhibited the productions of nitric oxide (NO). In addition, fimasartan attenuated LPS-induced transcriptional and DNA-binding activities of nuclear factor-kappa B (NF-κB) and activator protein-1 (AP-1). These reductions were accompanied by parallel reductions in the nuclear translocation of NF-κB and AP-1. Taken together, our data suggest that fimasartan down-regulates the expression of the iNOS in macrophages via NF-κB and AP-1 inactivation.

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© 2013 The Pharmaceutical Society of Japan
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