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.
Keywords:
Analgesic activity; Anti-inflammatory activity; Free radical scavenging activity; Ischemia/reperfusion injury; Kyotorphin-nitroxide hybrid molecules.
Published by Elsevier Ltd.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Analgesics / chemical synthesis
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Analgesics / chemistry
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Analgesics / pharmacology*
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / pharmacology*
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Dose-Response Relationship, Drug
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Edema / chemically induced
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Edema / drug therapy
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Endorphins / chemistry
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Endorphins / pharmacology*
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Mice
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Mitochondria / drug effects
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Mitochondria / metabolism
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Molecular Structure
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Nitrogen Oxides / chemistry
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Nitrogen Oxides / pharmacology*
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Pain / drug therapy
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Pain Measurement / drug effects
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Structure-Activity Relationship
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Xylenes
Substances
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Analgesics
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Anti-Inflammatory Agents, Non-Steroidal
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Antioxidants
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Endorphins
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Nitrogen Oxides
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Xylenes
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kyotorphin