Madurahydroxylactone, an Inhibitor of FtsZ from sp. AN100570.

Bo-Min Kim, Ha-Young Choi, Geon-Woo Kim, Chang-Ji Zheng, Young-Ho Kim, Won-Gon Kim
Author Information
  1. Bo-Min Kim: Superbacteria Research Center, Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon 34141, Republic of Korea.
  2. Ha-Young Choi: Superbacteria Research Center, Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon 34141, Republic of Korea.
  3. Geon-Woo Kim: Superbacteria Research Center, Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon 34141, Republic of Korea.
  4. Chang-Ji Zheng: Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, P.R. China.
  5. Young-Ho Kim: Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, P.R. China.
  6. Won-Gon Kim: Superbacteria Research Center, Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon 34141, Republic of Korea.

Abstract

FtsZ, a bacterial cell-division protein, is an attractive antibacterial target. In the screening for an inhibitor of FtsZ, madurahydroxylactone () and its related derivatives 2-5 were isolated from sp. AN100570. Compound 1 inhibited FtsZ with an IC of 53.4 μM and showed potent antibacterial activity against and MRSA with an MIC of 1 μg/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.

Keywords

MeSH Term

Actinobacteria
Anti-Bacterial Agents
Bacterial Proteins
Cytoskeletal Proteins
Lactones
Methicillin-Resistant Staphylococcus aureus
Microbial Sensitivity Tests
Staphylococcal Infections
Staphylococcus aureus

Chemicals

Anti-Bacterial Agents
Bacterial Proteins
Cytoskeletal Proteins
FtsZ protein, Bacteria
Lactones
madurahydroxylactone

Word Cloud

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