論文

査読有り 筆頭著者
2017年3月

Filamenting temperature-sensitive mutant Z inhibitors from Glycyrrhiza glabra and their inhibitory mode of action

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Takashi Matsui
  • ,
  • Subehan Lallo
  • ,
  • Khoirun Nisa
  • ,
  • Hiroyuki Morita

27
6
開始ページ
1420
終了ページ
1424
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bmcl.2017.01.095
出版者・発行元
PERGAMON-ELSEVIER SCIENCE LTD

FtsZ is an essential protein for bacterial cell division, and an attractive and underexploited novel antibacterial target protein. Screening of Indonesian plants revealed the inhibitory activity of the methanol extract of Glycyrrhiza glabra on the Bacillus subtilis FtsZ (BsFtZ) GTPase, and further bioassay-guided fractionation of the active methanol extract led to the isolation of seven known polyketides (1-7). Among them, gancaonin I (1), glycyrin (3), and isolicoflavanol (5) exhibited anti-BsFtsZ GTPase activities, at levels comparable to that of the synthetic FtsZ inhibitor, Zantrin Z3. Enzymatic assays using a BsFtsZ Va1307R mutant protein and in silico simulations suggested that 1, 3, and 5 bind to the cleft on BsFtsZ, as in the case of the previously reported uncompetitive FtsZ inhibitor, PC190723, and thereby display their significant anti-BsFtsZ inhibitory activities. Furthermore, 1 also showed significant inhibitory activity against B. subtilis, with a MIC value of 5 mu M. The present study provides new insights into the naturally occurring B. subtilis growth inhibitors. (C) 2017 Elsevier Ltd. All rights reserved.

リンク情報
DOI
https://doi.org/10.1016/j.bmcl.2017.01.095
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/28196701
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000396798800017&DestApp=WOS_CPL
ID情報
  • DOI : 10.1016/j.bmcl.2017.01.095
  • ISSN : 0960-894X
  • eISSN : 1464-3405
  • PubMed ID : 28196701
  • Web of Science ID : WOS:000396798800017

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