Anti-inflammatory, analgesic and antioxidant activities of novel kyotorphin-nitroxide hybrid molecules. Issue 8 (15th April 2016)

• Record Type: Journal Article
• Authors: Bi, Wei; Bi, Yue; Gao, Xiang; Yan, Xin; Zhang, Yanrong; Xue, Ping; Bammert, Catherine E.; Legalley, Thomas D.; Michael Gibson, K.; Bi, Lanrong; Wang, Jia-Xiang
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 8(2016)
• Page Start: 2005
• Page End: 2013
• Publication Date: 2016-04-15
• Subjects: Anti-inflammatory activity -- Analgesic activity -- Free radical scavenging activity -- Kyotorphin-nitroxide hybrid molecules -- Ischemia/reperfusion injury; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.02.086
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Mitochondrial oxidative damage contributes to a wide range of pathologies, including ischemia/reperfusion (I/R) injury, cardiovascular disorders and neurodegenerative diseases. Accordingly, protecting mitochondria from oxidative damage should possess therapeutic relevance. In the present study, we have designed and synthesized a series of novel kyotorphin-nitroxide hybrid molecules, and examined their free radical scavenging activities, in addition to their anti-inflammatory and analgesic activities. We have further characterized these compounds in a simulated I/R cellular model. Our findings suggest that the protective effects of kyotorphin-nitroxides partially reside in maintaining optimal mitochondrial function.