Strong inhibitory effects of curcumin and its demethoxy analog on Escherichia coli ATP synthase F1 sector

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 F-1 sector. A structure-activity relationship study indicated the importance of 4'-hydroxy groups and a beta-diketone moiety for the inhibition. The 3'-demethoxy analog (DMC) inhibited F-1 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 (C-5 curcuminoids) exhibited only weak activity toward ATPase and bacterial growth. (C) 2014 Elsevier B.V. All rights reserved.