title: Anti-inflammatory, analgesic and antioxidant activities of novel kyotorphin-nitroxide hybrid molecules.
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.
authors.affiliation: Department of Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan 450052, PR China; Second Hospital of HeBei Medical University, Shijiazhuang, HeBei 050000, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Bi
authors.affiliation: Second Hospital of HeBei Medical University, Shijiazhuang, HeBei 050000, PR China.
authors.forename: Yue
authors.initials: Y
authors.lastname: Bi
authors.affiliation: Department of Chemistry, Michigan Technological University, Houghton, MI 49931, United States.
authors.forename: Xiang
authors.initials: X
authors.lastname: Gao
authors.affiliation: Department of Chemistry, Michigan Technological University, Houghton, MI 49931, United States.
authors.forename: Xin
authors.initials: X
authors.lastname: Yan
authors.affiliation: Second Hospital of HeBei Medical University, Shijiazhuang, HeBei 050000, PR China.
authors.forename: Yanrong
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Second Hospital of HeBei Medical University, Shijiazhuang, HeBei 050000, PR China.
authors.forename: Ping
authors.initials: P
authors.lastname: Xue
authors.affiliation: Department of Biological Sciences, Michigan Technological University, Houghton, MI 49931, United States.
authors.forename: Catherine E
authors.initials: CE
authors.lastname: Bammert
authors.affiliation: Marquette General Heart and Vascular Institute, Marquette, MI 49855, United States.
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Legalley
authors.affiliation: Section of Experimental and Systems Pharmacology, College of Pharmacy, Washington State University, Spokane, WA 99202, United States.
authors.forename: K
authors.initials: K
authors.lastname: Michael Gibson
authors.affiliation: Department of Chemistry, Michigan Technological University, Houghton, MI 49931, United States.
authors.forename: Lanrong
authors.initials: L
authors.lastname: Bi
authors.affiliation: Department of Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan 450052, PR China.
authors.forename: Jia-Xiang
authors.initials: JX
authors.lastname: Wang
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D004723:Endorphins / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008928:Mitochondria / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D009589:Nitrogen Oxides / Q000737:chemistry / Q000494:pharmacology*; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement / Q000187:drug effects; D013329:Structure-Activity Relationship; D014992:Xylenes
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D004723:Endorphins; D009589:Nitrogen Oxides; D014992:Xylenes; C019448:kyotorphin
keywords: Analgesic activity; Anti-inflammatory activity; Free radical scavenging activity; Ischemia/reperfusion injury; Kyotorphin-nitroxide hybrid molecules