Aquastatin A, a new inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611 = Sporothrix sp. FN611 균주가 생산하는 새로운 enoyl-acyl carrier protein reductase 저해제 Aquastatin A

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Title
Aquastatin A, a new inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611 = Sporothrix sp. FN611 균주가 생산하는 새로운 enoyl-acyl carrier protein reductase 저해제 Aquastatin A
Author(s)
Yun Ju Kwon; Y Fang; G H Xu; Won Gon Kim
Bibliographic Citation
Biological & Pharmaceutical Bulletin, vol. 32, no. 12, pp. 2061-2064
Publication Year
2009
Abstract
Bacterial enoyl-acyl carrier protein (ACP) reductase has been confirmed as a novel target for antibacterial drug development. In this study, we determined that a fungal metabolite from Sporothrix sp. FN611 potently inhibited the enoyl-ACP reductase (FabI) of Staphylococcus aureus. Its structure identified the metabolite as aquastatin A by the MS and NMR data. Aquastatin A inhibited S. aureus FabI with an IC50 of 3.2 μM. It also prevented the growth of S. aureus and methicillin-resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration of 16-32 μg/ml. Aquastatin A also exerted an inhibitory effect against the FabK isoform, an enoyl-ACP reductase of Streptococcus pneumoniae, with an IC50 of 9.2 μM. The degalactosylation of aquastatin A did not affect the FabI and FabK-inhibitory or antibacterial activities, thereby suggesting that the sugar moiety within its molecular structure was not involved in these activities. The inhibitory effects of aquastatin A and its degalactosylated derivative on enoyl-ACP reductases and bacterial viability are reported for the first time in this study; these effects point to the potential that aquastatin A may be developed into a new broad-spectrum antibacterial and anti-MRSA agent.
Keyword
Aquastatin AEnoyl-acyl carrier protein reductaseFabIFungal metaboliteInhibitorStaphylococcus aureus
ISSN
0918-6158
Publisher
Pharmaceutical Soc Japan
DOI
http://dx.doi.org/10.1248/bpb.32.2061
Type
Article
Appears in Collections:
Division of Research on National Challenges > Infectious Disease Research Center > 1. Journal Articles
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