Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/16174
DC Field | Value | Language |
---|---|---|
dc.contributor | Department of Applied Biology and Chemical Technology | - |
dc.creator | Sun, N | - |
dc.creator | Chan, FY | - |
dc.creator | Lu, YJ | - |
dc.creator | Neves, MAC | - |
dc.creator | Lui, HK | - |
dc.creator | Wang, Y | - |
dc.creator | Chow, KY | - |
dc.creator | Chan, KF | - |
dc.creator | Yan, SC | - |
dc.creator | Leung, YC | - |
dc.creator | Abagyan, R | - |
dc.creator | Chan, TH | - |
dc.creator | Wong, KY | - |
dc.date.accessioned | 2014-12-19T07:02:26Z | - |
dc.date.available | 2014-12-19T07:02:26Z | - |
dc.identifier.uri | http://hdl.handle.net/10397/16174 | - |
dc.language.iso | en | en_US |
dc.publisher | Public Library of Science | en_US |
dc.rights | © 2014 Sun et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. | en_US |
dc.rights | The following publication Sun N, Chan FY, Lu YJ, Neves MAC, Lui HK, et al. (2014) Rational Design of Berberine-Based FtsZ Inhibitors with Broad-Spectrum Antibacterial Activity, PLOS ONE 9(5): e97514 is available at https://doi.org/10.1371/journal.pone.0097514 | en_US |
dc.title | Rational design of berberine-based FtsZ inhibitors with broad-spectrum antibacterial activity | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.identifier.volume | 9 | en_US |
dc.identifier.issue | 5 | en_US |
dc.identifier.doi | 10.1371/journal.pone.0097514 | en_US |
dcterms.abstract | Inhibition of the functional activity of Filamenting temperature-sensitive mutant Z (FtsZ) protein, an essential and highly conserved bacterial cytokinesis protein, is a promising approach for the development of a new class of antibacterial agents. Berberine, a benzylisoquinoline alkaloid widely used in traditional Chinese and native American medicines for its antimicrobial properties, has been recently reported to inhibit FtsZ. Using a combination of in silico structure-based design and in vitro biological assays, 9-phenoxyalkyl berberine derivatives were identified as potent FtsZ inhibitors. Compared to the parent compound berberine, the derivatives showed a significant enhancement of antibacterial activity against clinically relevant bacteria, and an improved potency against the GTPase activity and polymerization of FtsZ. The most potent compound 2 strongly inhibited the proliferation of Gram-positive bacteria, including methicillin-resistant S. aureus and vancomycin-resistant E. faecium, with MIC values between 2 and 4 μg/mL, and was active against the Gram-negative E. coli and K. pneumoniae, with MIC values of 32 and 64 mg/mL respectively. The compound perturbed the formation of cytokinetic Z-ring in E. coli. Also, the compound interfered with in vitro polymerization of S. aureus FtsZ. Taken together, the chemical modification of berberine with 9-phenoxyalkyl substituent groups greatly improved the antibacterial activity via targeting FtsZ. | - |
dcterms.accessRights | open access | en_US |
dcterms.bibliographicCitation | PLoS one, 2014, v. 9, no. 5, e97514 | - |
dcterms.isPartOf | PLoS one | - |
dcterms.issued | 2014 | - |
dc.identifier.scopus | 2-s2.0-84901336638 | - |
dc.identifier.pmid | 24824618 | - |
dc.identifier.eissn | 1932-6203 | en_US |
dc.identifier.rosgroupid | r70555 | - |
dc.description.ros | 2013-2014 > Academic research: refereed > Publication in refereed journal | en_US |
dc.description.validate | 201809_a bcma | en_US |
dc.description.oa | Version of Record | en_US |
dc.identifier.FolderNumber | OA_IR/PIRA | en_US |
dc.description.pubStatus | Published | en_US |
Appears in Collections: | Journal/Magazine Article |
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File | Description | Size | Format | |
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Sun_Rational_design_berberine-based.PDF | 2.62 MB | Adobe PDF | View/Open |
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