2017年3月
Filamenting temperature-sensitive mutant Z inhibitors from Glycyrrhiza glabra and their inhibitory mode of action
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- ,
- ,
- ,
- 巻
- 27
- 号
- 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
- ID情報
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- DOI : 10.1016/j.bmcl.2017.01.095
- ISSN : 0960-894X
- eISSN : 1464-3405
- PubMed ID : 28196701
- Web of Science ID : WOS:000396798800017