title: Inhibitory effect of 2'-hydroxycinnamaldehyde on nitric oxide production through inhibition of NF-kappa B activation in RAW 264.7 cells.
abstract: Cinnamomum cassia has been widely used for treating dyspepsia, gastritis, and inflammatory disease. In the present study, several of cinnamaldehyde derivatives were synthesized from various cinnamic acid based on the 2'-hydroxycinnamaldehyde isolated from the bark C. cassia Blume was investigated to compare their NO production and NF-kappa B activity from Raw 264.7 cell since nitric oxide (NO) and NF-kappa B have been shown to be implicated factors in the inflammatory disease. The results show that HCA, among the derivatives, most significantly inhibited lipopolysaccharide (LPS)-induced NO production and NF-kappa B transcriptional activity in a dose-dependent manner with an IC(50) value of 8 and 22 microM, respectively. We next investigated putative possible mechanisms of inhibitory effect of HCA on NO production. The inhibition of NO by HCA was consistent with the inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) expression. Moreover, HCA inhibited LPS-induced p50 and p65 translocation resulting in the inhibition of the DNA binding activity of the NF-kappa B, a central regulator of iNOS. The present results provided evidence that HCA, among cinnamaledhyde derivatives, has the most inhibitory effect on NO production through inhibition of NF-kappa B activation, and thus can be used as an anti-inflammatory agent.
authors.affiliation: College of Pharmacy, Chungbuk National University, Heungduk-gu, Cheongju 361-763, South Korea.
authors.forename: Seung Ho
authors.initials: SH
authors.lastname: Lee
authors.forename: Sun Young
authors.initials: SY
authors.lastname: Lee
authors.forename: Dong Ju
authors.initials: DJ
authors.lastname: Son
authors.forename: Heesoon
authors.initials: H
authors.lastname: Lee
authors.forename: Hwan Soo
authors.initials: HS
authors.lastname: Yoo
authors.forename: Sukgil
authors.initials: S
authors.lastname: Song
authors.forename: Ki Wan
authors.initials: KW
authors.lastname: Oh
authors.forename: Dong Cho
authors.initials: DC
authors.lastname: Han
authors.forename: Byoung Mog
authors.initials: BM
authors.lastname: Kwon
authors.forename: Jin Tae
authors.initials: JT
authors.lastname: Hong
mesh_terms: D000171:Acrolein / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D002460:Cell Line; D032904:Cinnamomum aromaticum / Q000737:chemistry*; D051546:Cyclooxygenase 2; D004247:DNA / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D051550:I-kappa B Kinase; D020672:I-kappa B Proteins / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009569:Nitric Oxide / Q000096:biosynthesis*; D019001:Nitric Oxide Synthase / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II; D011451:Prostaglandin-Endoperoxide Synthases / Q000096:biosynthesis; D017346:Protein Serine-Threonine Kinases / Q000502:physiology
chemical_list: D000893:Anti-Inflammatory Agents; D020672:I-kappa B Proteins; D008070:Lipopolysaccharides; D016328:NF-kappa B; D009569:Nitric Oxide; D000171:Acrolein; D004247:DNA; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases; D017346:Protein Serine-Threonine Kinases; C496564:Chuk protein, mouse; D051550:I-kappa B Kinase; C496562:Ikbkb protein, mouse; C496566:Ikbke protein, mouse; C012843:cinnamaldehyde