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Int J Biol Macromol ; 70: 241-5, 2014 Sep.
Article in English | MEDLINE | ID: mdl-25010476

ABSTRACT

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.


Subject(s)
Bacterial Proton-Translocating ATPases/antagonists & inhibitors , Curcumin/analogs & derivatives , Curcumin/pharmacology , Escherichia coli/drug effects , Escherichia coli/enzymology , Bacterial Proton-Translocating ATPases/chemistry , Bacterial Proton-Translocating ATPases/metabolism , Curcumin/chemistry , Dose-Response Relationship, Drug , Enzyme Activation/drug effects , Escherichia coli/growth & development , Oxidative Phosphorylation/drug effects , Structure-Activity Relationship
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