PMID- 11357890 OWN - NLM STAT- MEDLINE DCOM- 20010913 LR - 20191104 IS - 1567-5769 (Print) IS - 1567-5769 (Linking) VI - 1 IP - 4 DP - 2001 Apr TI - Capsazepine, a vanilloid receptor antagonist, inhibits the expression of inducible nitric oxide synthase gene in lipopolysaccharide-stimulated RAW264.7 macrophages through the inactivation of nuclear transcription factor-kappa B. PG - 777-84 AB - High amounts of nitric oxide (NO) production following the induction of inducible NO synthase (iNOS) gene expression has been implicated in the pathogenesis of inflammatory diseases. Capsaicin, a vanilloid receptor agonist, is known to have an inhibitory effect on NO production in macrophages. In the present study, we have found that capsazepine (CAPZ), a vanilloid receptor antagonist, also inhibited NO and iNOS protein syntheses induced by lipopolysaccharide in RAW264.7 macrophages via the suppression of iNOS mRNA. The mechanistic studies showed that CAPZ inhibited the expression of iNOS mRNA through the inactivation of nuclear transcription factor-kappa B (NF-kappa B). Thus, capsazepine may be a useful candidate for the development of a drug to treat inflammatory diseases related to iNOS gene overexpression. FAU - Oh, G S AU - Oh GS AD - Medicinal Resources Research Center (MRRC), Wonkwang University, Chonbuk, South Korea. FAU - Pae, H O AU - Pae HO FAU - Seo, W G AU - Seo WG FAU - Kim, N Y AU - Kim NY FAU - Pyun, K H AU - Pyun KH FAU - Kim, I K AU - Kim IK FAU - Shin, M AU - Shin M FAU - Chung, H T AU - Chung HT LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Netherlands TA - Int Immunopharmacol JT - International immunopharmacology JID - 100965259 RN - 0 (Lipopolysaccharides) RN - 0 (NF-kappa B) RN - 0 (RNA, Messenger) RN - 0 (Receptors, Drug) RN - 31C4KY9ESH (Nitric Oxide) RN - EC 1.14.13.39 (Nitric Oxide Synthase) RN - EC 1.14.13.39 (Nitric Oxide Synthase Type II) RN - EC 1.14.13.39 (Nos2 protein, mouse) RN - LFW48MY844 (capsazepine) RN - S07O44R1ZM (Capsaicin) SB - IM MH - Animals MH - Capsaicin/*analogs & derivatives/*pharmacology MH - Cell Line MH - Gene Expression Regulation, Enzymologic/drug effects MH - Lipopolysaccharides/*pharmacology MH - Macrophages/*enzymology MH - Mice MH - NF-kappa B/*antagonists & inhibitors MH - Nitric Oxide/biosynthesis MH - Nitric Oxide Synthase/*antagonists & inhibitors/genetics MH - Nitric Oxide Synthase Type II MH - RNA, Messenger/analysis MH - Receptors, Drug/*antagonists & inhibitors EDAT- 2001/05/19 10:00 MHDA- 2001/09/14 10:01 CRDT- 2001/05/19 10:00 PHST- 2001/05/19 10:00 [pubmed] PHST- 2001/09/14 10:01 [medline] PHST- 2001/05/19 10:00 [entrez] AID - S1567576901000121 [pii] AID - 10.1016/s1567-5769(01)00012-1 [doi] PST - ppublish SO - Int Immunopharmacol. 2001 Apr;1(4):777-84. doi: 10.1016/s1567-5769(01)00012-1.