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

Int J Biol Macromol. 2014 Sep:70:241-5. doi: 10.1016/j.ijbiomac.2014.06.055. Epub 2014 Jul 7.

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 β-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.

Keywords: ATP synthase; Curcumin; F-ATPase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

  • Bacterial Proton-Translocating ATPases
  • Curcumin