1. Topoisomerase I inhibitor evodiamine acts as an antibacterial agent against drug-resistant Klebsiella pneumoniae
- Author
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Hsiang Ping Tsai, Jui Yu Wu, Chun Mao Lin, Che Hsiung Yang, Chien Chun Yang, Chien Shu Chen, Ming Chih Chang, and Hsiu Chen Lin
- Subjects
medicine.drug_class ,Klebsiella pneumoniae ,Antibiotics ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Topoisomerase-I Inhibitor ,Analytical Chemistry ,Microbiology ,Evodia ,Minimum inhibitory concentration ,chemistry.chemical_compound ,Evodiamine ,Drug Discovery ,Drug Resistance, Bacterial ,medicine ,Escherichia coli ,Antibacterial agent ,Pharmacology ,biology ,Plant Extracts ,Topoisomerase ,Organic Chemistry ,biology.organism_classification ,Anti-Bacterial Agents ,Complementary and alternative medicine ,chemistry ,biology.protein ,Quinazolines ,Molecular Medicine ,Topoisomerase I Inhibitors ,Topoisomerase inhibitor - 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.
- Published
- 2012