title: Antibacterial activity of synthetic curcumin derivatives: 3,5-bis(benzylidene)-4-piperidone (EF24) and EF24-dimer linked via diethylenetriaminepentacetic acid (EF2DTPA).
abstract: Curcumin is well known for its antimicrobial and anti-inflammatory properties. However, since systemic absorption and bioavailability of curcumin from gastrointestinal tract is considerably poor, synthetic curcuminoids are being developed as better alternatives. Two curcumin derivatives: 3,5-bis(benzylidene)-4-piperidone (EF24) and EF24-dimer linked via diethylenetriaminepentacetic acid (EF2DTPA), were included in this study. We investigated the antibacterial activity of EF24 and EF2DTPA against Gram-negative (Escherichia coli) and Gram-positive (Enterococcus faecalis, Staphylococcus aureus) bacteria. We also studied the effects of EF24 and EF2DTPA on uptake and localization of pHrodo-labeled E. coli in the acidic compartments (phagolysosomes) of dendritic cells (DCs) under in vitro conditions. Our results demonstrate that treatment with EF24 and EF2DTPA directly suppresses the bacterial growth. However, these compounds do not affect the bacterial uptake or localization in the DCs.
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma Health Sciences Center, 1110 N. Stonewall Avenue, Oklahoma City, OK, 73117, USA.
authors.forename: Prachi
authors.initials: P
authors.lastname: Vilekar
authors.forename: Catherine
authors.initials: C
authors.lastname: King
authors.forename: Pallavi
authors.initials: P
authors.lastname: Lagisetty
authors.forename: Vibhudutta
authors.initials: V
authors.lastname: Awasthi
authors.forename: Shanjana
authors.initials: S
authors.lastname: Awasthi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002460:Cell Line; D003474:Curcumin / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003713:Dendritic Cells / Q000187:drug effects / Q000276:immunology; D019281:Dimerization; D051379:Mice; D004369:Pentetic Acid / Q000737:chemistry*; D010587:Phagocytosis / Q000187:drug effects; D010881:Piperidones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C526290:3,5-bis(benzylidene)-4-piperidone; D000900:Anti-Bacterial Agents; D010881:Piperidones; D004369:Pentetic Acid; D003474:Curcumin