The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria.
The inhibitory effect of the dienone-phenolic triterpene, celastrol, on lipid peroxidation in rat liver mitochondrial membranes induced by ADP and Fe2+ was studied. The anti-peroxidative effect of celastrol was very strong: its 50% inhibitory concentration was 7 microM, and it was about 15 times more effective than alpha-tocopherol. Celastrol scavenged 1.5 molar equivalents of radicals in homogeneous aqueous ethanolic solution, whereas cysteine and alpha-tocopherol scavenged one and two molar equivalents of radicals, respectively. The process of anti-peroxidation of celastrol was biphasic, possibly due to stepwise inhibitions of peroxidation in the outer and inner mitochondrial membranes.
Sassa
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Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
Takaishi
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Terada
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H
D000818:Animals; D016166:Free Radical Scavengers; D005609:Free Radicals; D007700:Kinetics; D015227:Lipid Peroxidation / Q000187:drug effects*; D008054:Lipid Peroxides / Q000032:analysis; D008297:Male; D008930:Mitochondria, Liver / Q000187:drug effects / Q000378:metabolism*; D010101:Oxygen Consumption / Q000187:drug effects; D053978:Pentacyclic Triterpenes; D051381:Rats; D011919:Rats, Inbred Strains; D013367:Submitochondrial Particles / Q000187:drug effects / Q000378:metabolism*; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D014810:Vitamin E / Q000494:pharmacology
D016166:Free Radical Scavengers; D005609:Free Radicals; D008054:Lipid Peroxides; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D014810:Vitamin E; C050414:celastrol