Cephalochromin, a FabI-directed antibacterial of microbial origin

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Title
Cephalochromin, a FabI-directed antibacterial of microbial origin
Author(s)
C J Zheng; Mi Jin Sohn; Sangku LeeYoung-Soo Hong; J H Kwak; Won Gon Kim
Bibliographic Citation
Biochemical and Biophysical Research Communications, vol. 362, no. 4, pp. 1107-1112
Publication Year
2007
Abstract
Microorganisms produce many kinds of antibiotics which function in an antagonistic capacity in nature where they have much competition. Bacterial enoyl-acyl carrier protein (ACP) reductase (FabI) has been demonstrated to be an antibacterial target. However, no FabI-directed antibiotic of microbial origin has been reported so far. In this study, we found that cephalochromin with a naphtho-γ-pyrone skeleton, a fungal secondary metabolite, inhibited FabI of Staphylococcus aureus and Escherichia coli with IC50 of 1.9 and 1.8 μM, respectively. The methylether derivatives of cephalochromin, however, did not inhibit FabI. The FabI-inhibitory activities of cephalochromin and its derivatives well correlated with antibacterial activity as well as the inhibition of cellular fatty acid biosynthesis. Furthermore, FabI-overexpressing S. aureus exhibited reduced susceptibility to cephalochromin compared to the wild-type strain, demonstrating that the mode of antibacterial action of cephalochromin is via the inhibition of FabI. These results indicate that cephalochromin is the first FabI-directed antibacterial of microbial origin and may have the potential for further antibacterial development.
Keyword
AntibacterialCephalochrominEnoyl-ACP reductaseFabIFatty acid synthesisNaphtho-γ-pyrone
ISSN
0006-291X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bbrc.2007.08.144
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
Division of Research on National Challenges > Infectious Disease Research Center > 1. Journal Articles
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