Abstract
The piperidine nitroxide TEMPOL induces apoptosis in a number of tumor cell lines through free radical-dependent mechanisms. As mitochondria play a major role in apoptosis as both source and target for free radicals, the present study focuses on mitochondrial effects of TEMPOL in a human promyelocytic leukemic cell line (HL-60). On 24-h exposure to TEMPOL, the following alterations were observed: 1) decrease in both the intracellular and mitochondrial glutathione pools; 2) impairment of oxidative phosphorylation; and 3) decrease in mitochondrial membrane potential. In addition, TEMPOL was found to specifically target complex I of the respiratory chain, with minor effects on complexes II and IV, suggesting that mitochondrial effects might play a role in TEMPOL-induced oxidative stress and apoptosis, and that TEMPOL might sensitize tumor cells to the pro-apoptotic effects of cytotoxic agents.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antioxidants / pharmacology*
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Apoptosis / drug effects*
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Chromatography, High Pressure Liquid
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Cyclic N-Oxides / pharmacology*
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Electron Transport Complex II
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Electron Transport Complex III / antagonists & inhibitors
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Electron Transport Complex IV / antagonists & inhibitors
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Enzyme Inhibitors / pharmacology
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Glutathione / metabolism
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HL-60 Cells / cytology
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HL-60 Cells / drug effects*
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Humans
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Intracellular Membranes / drug effects
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Membrane Potentials / drug effects
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Mitochondria / drug effects*
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Multienzyme Complexes / antagonists & inhibitors
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Neoplasm Proteins / antagonists & inhibitors
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Oxidation-Reduction
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Oxidative Phosphorylation / drug effects
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Oxidoreductases / antagonists & inhibitors
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Rotenone / pharmacology
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Sodium Azide / pharmacology
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Spin Labels
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Succinate Dehydrogenase / antagonists & inhibitors
Substances
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Antioxidants
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Cyclic N-Oxides
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Enzyme Inhibitors
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Multienzyme Complexes
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Neoplasm Proteins
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Spin Labels
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Rotenone
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Sodium Azide
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Oxidoreductases
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Electron Transport Complex II
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Succinate Dehydrogenase
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Electron Transport Complex IV
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Electron Transport Complex III
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Glutathione
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tempol