Madurahydroxylactone, an Inhibitor of Staphylococcus aureus FtsZ from Nonomuraea sp AN100570

作者:Kim, Bo-Min; Choi, Ha-Young; Kim, Geon-Woo; Zheng, Chang-Ji; Kim, Young-Ho; Kim, Won-Gon*
来源:Journal of Microbiology and Biotechnology, 2017, 27(11): 1994-1998.
DOI:10.4014/jmb.1708.08044

摘要

FtsZ, a bacterial cell-division protein, is an attractive antibacterial target. In the screening for an inhibitor of Staphylococcus aureus FtsZ, madurahydroxylactone (1) and its related derivatives 2-5 were isolated from Nonomuraea sp. AN100570. Compound 1 inhibited S. aureus FtsZ with an IC50 of 53.4 mu M and showed potent antibacterial activity against S. aureus and MRSA with an MIC of 1 mu g/ml, whereas 2-5 were weak or inactive. Importantly, 1 induced cell elongation in the cell division phenotype assay, whereas 2-5 did not. It indicates that 1 exhibits its potent antibacterial activity via inhibition of FtsZ, and the hydroxyl group and hydroxylactone ring of 1 are critical for the activity. Thus, madurahydroxylactone is a new type of inhibitor of FtsZ.