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Antimicrobial Flavonoid, 3,6-Dihydroxyflavone, Have Dual Inhibitory Activity against KAS III and KAS I
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  • Antimicrobial Flavonoid, 3,6-Dihydroxyflavone, Have Dual Inhibitory Activity against KAS III and KAS I
  • Antimicrobial Flavonoid, 3,6-Dihydroxyflavone, Have Dual Inhibitory Activity against KAS III and KAS I
저자명
Lee. Jee-Young,Lee. Eun-Jung,Jeong. Ki-Woong,Kim. Yang-Mee
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2011년|32권 9호|pp.3219-3222 (4 pages)
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대한화학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

Three types of ${eta}$-ketoacyl acyl carrier protein synthase (KAS) are important for overcoming the bacterial resistance problem. Recently, we reported the discovery of a antimicrobial flavonoid, YKAF01 (3,6-dihydroxyflavone), which exhibits antibacterial activity against Gram-positive bacteria through inhibition of ${eta}$-ketoacyl acyl carrier protein synthase III (KAS III). In this report, we suggested that YKAF01 can be an inhibitor ${eta}$-ketoacyl acyl carrier protein synthase I (KAS I) with dual inhibitory activity for KAS I as well as KAS III. KAS I is related to the elongation of unsaturated fatty acids in bacterial fatty acid synthesis and can be a good therapeutic target of designing novel antibiotics. We performed docking study of Escherichia coli KAS I (ecKAS I) and YKAF01, and determined their binding model. YKAF01 binds to KAS I with high binding affinity ($2.12{ imes}10^6$) and exhibited an antimicrobial activity against the multidrug-resistant E. coli with minimal inhibitory concentration (MIC) value of 512 ${mu}g$/mL. Further optimization of this compound will be carried out to improve its antimicrobial activity and membrane permeability against bacterial cell membrane.