title: Topoisomerase I inhibitor evodiamine acts as an antibacterial agent against drug-resistant Klebsiella pneumoniae.
abstract: Topoisomerase inhibitors have been developed in a variety of clinical applications. We investigated the inhibitory effect of evodiamine on E. coli topoisomerase I, which may lead to an anti-bacterial effect. Evodiamine inhibits the supercoiled plasmid DNA relaxation that is catalyzed by E. coli topoisomerase I, and computer-aided docking has shown that the Arg161 and Asp551 residues of topoisomerase I interact with evodiamine. We investigated the bactericidal effect of evodiamine against multidrug-resistant Klebsiella pneumoniae. Evodiamine showed a significantly lower minimal inhibitory concentration value (MIC 128 µg/mL) compared with antibiotics (>512 µg/mL) against the clinical isolate of K. pneumoniae. The results suggested that evodiamine is a potential agent against drug-resistant bacteria.
authors.affiliation: College of Medicine, Taipei Medical University, Taipei, Taiwan.
authors.forename: Jui-Yu
authors.initials: JY
authors.lastname: Wu
authors.forename: Ming-Chih
authors.initials: MC
authors.lastname: Chang
authors.forename: Chien-Shu
authors.initials: CS
authors.lastname: Chen
authors.forename: Hsiu-Chen
authors.initials: HC
authors.lastname: Lin
authors.forename: Hsiang-Ping
authors.initials: HP
authors.lastname: Tsai
authors.forename: Chien-Chun
authors.initials: CC
authors.lastname: Yang
authors.forename: Che-Hsiung
authors.initials: CH
authors.lastname: Yang
authors.forename: Chun-Mao
authors.initials: CM
authors.lastname: Lin
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial / Q000187:drug effects*; D004926:Escherichia coli / Q000201:enzymology; D032086:Evodia / Q000737:chemistry*; D007711:Klebsiella pneumoniae / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D010936:Plant Extracts / Q000494:pharmacology*; D011799:Quinazolines / Q000494:pharmacology*; D059004:Topoisomerase I Inhibitors / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D010936:Plant Extracts; D011799:Quinazolines; D059004:Topoisomerase I Inhibitors; C049639:evodiamine