title: Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation.
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.
authors: Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul 130–701, Republic of Korea.
authors: Suran
authors: S
authors: Ryu
authors: Ji-Sun
authors: JS
authors: Shin
authors: Young-Wuk
authors: YW
authors: Cho
authors: Hyoung Kook
authors: HK
authors: Kim
authors: Soo Heui
authors: SH
authors: Paik
authors: Joo Han
authors: JH
authors: Lee
authors: Yong Ha
authors: YH
authors: Chi
authors: Ji Han
authors: JH
authors: Kim
authors: Je Hak
authors: JH
authors: Kim
authors: Kyung-Tae
authors: KT
authors: Lee
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000494:pharmacology*; D002478:Cells, Cultured; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D009569:Nitric Oxide / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors*; D011743:Pyrimidines / Q000494:pharmacology*; D013777:Tetrazoles / Q000494:pharmacology*; D018808:Transcription Factor AP-1 / Q000037:antagonists & inhibitors*
chemical_list: D000959:Antihypertensive Agents; D001713:Biphenyl Compounds; D008070:Lipopolysaccharides; D016328:NF-kappa B; D011743:Pyrimidines; D013777:Tetrazoles; D018808:Transcription Factor AP-1; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; C558933:fimasartan