title: Anti-inflammatory effects of N(1)-Benzyl-4-methylbenzene-1,2-diamine (JSH-21) analogs on nitric oxide production and nuclear factor-kappa B transcriptional activity in lipopolysaccharide-stimulated macrophages RAW 264.7.
abstract: N(1)-Benzyl-4-methylbenzene-1,2-diamine (JSH-21) and its analogs were chemically synthesized and their anti-inflammatory potentials investigated. JSH-21 inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 in a dose-dependent manner, with an IC50 value of 9.2 μM, where pyrrolidine dithiocarbamate and parthenolide as positive controls exhibited IC50 values of 29.3 and 3.6 μM, respectively. The inhibitory effect of JSH-21 on the NO production was attributable to its down-regulatory action on LPS-induc-ible NO synthase (iNOS), which was documented by iNOS promoter activity. In the mechanism of the anti-inflammatory action, JSH-21 exhibited inhibitory effects on LPS-induced DNA binding activity and transcriptional activity of nuclear factor-kappa B(NF-KB). Structural analogs of JSH-21 also inhibited both the LPS-induced NO production andNF-KB transcriptional activity, where diamine substitution at positions 1 and 2 of JSH-21 seems to play an important role in the anti-inflammatory activity.
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea.
authors: Kyung Rak
authors: KR
authors: Min
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea.
authors: Hyun-Mo
authors: HM
authors: Shin
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea.|College of Pharmacy, Chungnam National University, 305-764, Daejeon, Korea.
authors: Jee-Hyun
authors: JH
authors: Lee
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea.
authors: Byung Hak
authors: BH
authors: Kim
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea.
authors: Eun Yong
authors: EY
authors: Chung
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea.|College of Pharmacy, Chungnam National University, 305-764, Daejeon, Korea.
authors: Sang-Hun
authors: SH
authors: Jung
authors: College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, 361-763, Cheongju, Korea. youngsoo@chungbuk.ac.kr.
authors: Youngsoo
authors: Y
authors: Kim
keywords: Anti-inflammatory effect; Chemical preparation; Lipopolysaccharide; N1-Benzyl-4-methylbenzene-1,2-diamine; Nitric oxide; Nuclear factor-kappa B