Title of article :
Antimicrobial natural products as β-ketoacyl-acyl carrier protein synthase III inhibitors Original Research Article
Author/Authors :
Jee-Young Lee، نويسنده , , Ki-Woong Jeong، نويسنده , , Soyoung Shin، نويسنده , , Ju-Un Lee، نويسنده , , Yangmee Kim، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2009
Abstract :
β-Ketoacyl-acyl carrier protein synthase III (KAS III) initiates bacterial fatty acid biosynthesis, making it one of the most promising condensing enzymes. In a previous study, we developed three pharmacophore maps from receptor-oriented pharmacophore-based in silico screening and proposed a potent antimicrobial inhibitor for KAS III. Using these pharmacophore maps, we examined a natural product database and chose 4 natural compounds as possible KAS III inhibitors. Here, we propose that YKAF01 (3,6-dihydroxyflavone) and YKAF04, 3-(4-hydroxyphenyl)-1-(2,4,6-tri-hydroxyphenyl)propan-1-one (or 4,2′,4′,6′-tetra-hydroxychalcone, phloretin) are potent antimicrobial inhibitors of KAS III with high binding affinity. In particular, these compounds display an excellent antimicrobial effect against Staphylococcus aureus and MRSA in the range of 16–32 μM.
Keywords :
KAS , Phloretin , Antibiotics , Flavonoid , in silico screening
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry