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Int J Biol Macromol ; 70: 241-5, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-25010476

RESUMO

Curcumin, a dietary phytopolyphenol isolated from a perennial herb (Curcuma longa), is a well-known compound effective for bacterial infections and tumors, and also as an antioxidant. In this study, we report the inhibitory effects of curcumin and its analogs on the Escherichia coli ATP synthase F1 sector. A structure-activity relationship study indicated the importance of 4'-hydroxy groups and a ß-diketone moiety for the inhibition. The 3'-demethoxy analog (DMC) inhibited F1 more strongly than curcumin did. Furthermore, these compounds inhibited E. coli growth through oxidative phosphorylation, consistent with their effects on ATPase activity. These results suggest that the two compounds affected bacterial growth through inhibition of ATP synthase. Derivatives including bis(arylmethylidene)acetones (C5 curcuminoids) exhibited only weak activity toward ATPase and bacterial growth.


Assuntos
ATPases Bacterianas Próton-Translocadoras/antagonistas & inibidores , Curcumina/análogos & derivados , Curcumina/farmacologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/enzimologia , ATPases Bacterianas Próton-Translocadoras/química , ATPases Bacterianas Próton-Translocadoras/metabolismo , Curcumina/química , Relação Dose-Resposta a Droga , Ativação Enzimática/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Fosforilação Oxidativa/efeitos dos fármacos , Relação Estrutura-Atividade
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