Abstract
Seven diterpenes isolated of the latex of the Euphorbia obtusifolia were evaluated as inhibitors of the NADH oxidase activity in submitochondrial particles from bovine heart. Compound 2, 2,3,5,7,8,9,15-heptahydroxyjatropha-6(17),11-diene-14-one 8,9-diacetate 7-isobutyrate 2,3-bis(2-methylbutyrate), was the most potent inhibitor with an inhibitory concentration (IC 50 ) value of 5.1 +/- 0.2 microM. In the present study, some structure-activity trends are suggested for the inhibitory activity of these natural products on the mammalian mitochondrial respiratory chain.
MeSH terms
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Animals
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Cattle
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Diterpenes / administration & dosage
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Diterpenes / pharmacology*
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Diterpenes / therapeutic use
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Dose-Response Relationship, Drug
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Euphorbia*
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Humans
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Inhibitory Concentration 50
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Latex / chemistry
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Mitochondria, Heart / drug effects*
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Mitochondria, Heart / enzymology
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Multienzyme Complexes / antagonists & inhibitors*
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Multienzyme Complexes / metabolism
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NADH, NADPH Oxidoreductases / antagonists & inhibitors*
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NADH, NADPH Oxidoreductases / metabolism
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Oxygen Consumption / drug effects
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Phytotherapy*
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Structure-Activity Relationship
Substances
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Diterpenes
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Latex
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Multienzyme Complexes
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NADH oxidase
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NADH, NADPH Oxidoreductases