Inhibitory effects on mitochondrial complex I of semisynthetic mono-tetrahydrofuran acetogenin derivatives |
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| Authors: | Tormo José R Gallardo Teresa Peris Eva Bermejo Almudena Cabedo Nuria Estornell Ernesto Zafra-Polo M Carmen Cortes Diego |
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| Affiliation: | Departamento de Farmacología, Laboratorio de Farmacognosia, Facultad de Farmacia, Universidad de Valencia, Avda. Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain. |
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| Abstract: | Modifications in the terminal alpha,beta-unsaturated gamma-methyl-gamma-lactone moiety or in the alkyl chain that links this terminal gamma-lactone with the alpha,alpha'-dihydroxylated THF system of the natural mono-tetrahydrofuranic acetogenins, annonacin and annonacinone, led to the preparation of eight semisynthetic derivatives. Their inhibitory effects on mitochondrial complex I is discussed and compared with that of the classical complex I inhibitor, rotenone. |
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