Anti-inflammatory potential of thienopyridines as possible alternative to NSAIDs

作者：Madhusudana Kuncha; Shireesha Boyapati; Naidu Vegi Ganga Modi; Ramakrishna Sistla^*; Narsaiah Banda; Rao Akkinepally Raghuram; Diwan Prakash V

来源：European Journal of Pharmacology, 2012, 678(1-3): 48-54.

DOI：10.1016/j.ejphar.2011.12.019

• Thienopyridine analog
• Anti-inflammatory
• Carrageenan
• Dextran
• Arachidonic acid
• Freund%26apos
• s complete adjuvant induced arthritis

The present study was designed to evaluate the anti-inflammatory and antiarthritic activity of the new synthetic thienopyridine analogs. The anti-inflammatory activity of thienopyridines was assayed by using carrageenan; dextran and arachidonic acid induced paw edema models (acute), cotton pellet granuloma model (Sub acute) and Freund%26apos;s complete adjuvant induced arthritis (chronic) in experimental rats. The compounds BN-4, BN-14 and BN-16 have shown significant inhibition of edema in carrageenan and arachidonic acid induced paw edema model at a dose of 100 mg/kg compared to the dextran induced paw edema model and also showed significant inhibition in granuloma tissue formation and Freund%26apos;s complete adjuvant induced arthritis in experimental rats. These thienopyridine analogs also inhibited the proinflammatory mediators such as Tumor necrosis factor (TNF)-alpha, Interleukin (IL)-1 beta and Nitric Oxide (NO) in Lipopolysaccharide (LPS) challenged murine macrophages. Ulcerogenecity study results revealed less ulcerogenic potential of BN-4, BN-14 and BN-16 compared to nonsteroidal anti-inflammatory drug (NSAID) indomethacin in rats. In conclusion, the new thienopyridine analogs were promising for the potential use as anti-inflammatory agents for both acute and chronic inflammatory disorders with low toxic effects.

• 出版日期2012-3-5