Meleagrin, a new FabI inhibitor from Penicillium chryosogenum with at least one additional mode of action

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dc.contributor.authorC J Zheng-
dc.contributor.authorM J Sohn-
dc.contributor.authorSangku Lee-
dc.contributor.authorWon Gon Kim-
dc.date.accessioned2017-04-19T09:47:56Z-
dc.date.available2017-04-19T09:47:56Z-
dc.date.issued2013-
dc.identifier.issn19326203-
dc.identifier.uri10.1371/journal.pone.0078922ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/11720-
dc.description.abstractBacterial enoyl-acyl carrier protein reductase (FabI) is a promising novel antibacterial target. We isolated a new class of FabI inhibitor from Penicillium chrysogenum, which produces various antibiotics, the mechanisms of some of them are unknown. The isolated FabI inhibitor was determined to be meleagrin by mass spectroscopy and nuclear magnetic resonance spectral analyses, and its more active and inactive derivatives were chemically prepared. Consistent with their selective inhibition of Staphylococcus aureus FabI, meleagrin and its more active derivatives directly bound to S. aureus FabI in a fluorescence quenching assay, inhibited intracellular fatty acid biosynthesis and growth of S. aureus, and increased the minimum inhibitory concentration for fabI-overexpressing S. aureus. The compounds that were not effective against the FabK isoform, however, inhibited the growth of Streptococcus pneumoniae that contained only the FabK isoform. Additionally no resistant mutant to the compounds was obtained. Importantly, fabK-overexpressing Escherichia coli was not resistant to these compounds, but was resistant to triclosan. These results demonstrate that the compounds inhibited another target in addition to FabI. Thus, meleagrin is a new class of FabI inhibitor with at least one additional mode of action that could have potential for treating multidrug-resistant bacteria-
dc.publisherPublic Library of Science-
dc.titleMeleagrin, a new FabI inhibitor from Penicillium chryosogenum with at least one additional mode of action-
dc.title.alternativeMeleagrin, a new FabI inhibitor from Penicillium chryosogenum with at least one additional mode of action-
dc.typeArticle-
dc.citation.titlePLoS One-
dc.citation.number11-
dc.citation.endPagee78922-
dc.citation.startPagee78922-
dc.citation.volume8-
dc.contributor.affiliatedAuthorSangku Lee-
dc.contributor.affiliatedAuthorWon Gon Kim-
dc.contributor.alternativeNameZheng-
dc.contributor.alternativeName손미진-
dc.contributor.alternativeName이상구-
dc.contributor.alternativeName김원곤-
dc.identifier.bibliographicCitationPLoS One, vol. 8, no. 11, pp. e78922-e78922-
dc.identifier.doi10.1371/journal.pone.0078922-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
Division of Research on National Challenges > Infectious Disease Research Center > 1. Journal Articles
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