Exploring the anti-inflammatory activity of a novel 2-phenylquinazoline analog with protection against inflammatory injury
详细信息 查看全文
- 作者：Nabanita Chatterjee ; Subhadip Das ; Dipayan Bose ; Somenath Banerjee ; Sujata Das ; Debprasad Chattopadhyay ; Krishna Das Saha
- 关键词：CFA ; complete Freund's adjuvant ; ELISA ; Enzyme-linked immunosorbent assay ; I-¦ÊB ; inhibitor of kappa B ; IL ; Interleukin ; LPS ; lipopolysaccharide ; NF-¦ÊB ; Nuclear factor-¦ÊB ; NO ; Nitric oxide ; PBS ; Phosphate buffer saline ; PGE2 ; Prostaglandin-E2 ; RAW 264.7
- 刊名：Toxicology and Applied Pharmacology
- 出版年：2012
- 出版时间：15 October, 2012
- 年：2012
- 卷：264
- 期：2
- 页码：182-191
- 全文大小：1368 K
文摘
Inflammation is a protective immune response against harmful stimuli whose long time continuation results in host disease. Quinazolinones are nitrogen containing heterocyclic compounds with wide spectrum of biological activities. The anticancer effect of a 3-(arylideneamino)©\phenylquinazoline-4(3H)-one derivative was reported earlier. The anti-inflammatory effect of these quinazolinone derivatives has now been examined in endotoxin stimulated macrophages and in different in vivo models of inflammation by measuring the proinflammatory cytokines (TNF-¦Á, IL-1¦Â and IL-6), mediators NO and NF-¦ÊB (by ELISA and western blot), and translocation of the nuclear factor kB (by immunocytochemical analysis). To elucidate the in vivo effect, mice endotoxin model was and the various levels of edema, inflammatory pain and vascular permeability were studied. One of the quinazolinone derivatives showed significant anti-inflammatory activity in stimulated macrophage cells by inhibiting the expression of TNF-¦Á, IL-1¦Â, IL-6, iNOS, COX-2, p-I¦ÊB and NF-¦ÊBp65. Significant (P < 0.01) improvement was observed in the mortality of endotoxemic mice. The carrageenan and formalin-induced paw edema thicknesses were found to be reduced significantly (P < 0.01) along with the reduction of pain, vascular permeability and edema induced by complete Freund's adjuvant (P < 0.01). These findings indicate that 3-(arylideneamino)©\phenylquinazoline-4(3H)-one derivative as a potential anti-inflammatory agent.