オキムラ　ケイコ   Keiko Okimura
  興村　桂子
   所属   薬学部 薬学科
   職種   准教授
言語種別 英語
発行・発表の年月 2009/03
形態種別 学術論文
査読 査読あり
標題 Contribution of Each Amino Acid Residue in Polymyxin B3 to Antimicrobial and Lipopoly-saccharide Binding Activity
執筆形態 共著
掲載誌名 Chem. Pharm. Bull.
巻・号・頁 57,pp.240-244
著者・共著者 Kazushi Kanazawa, Yuki Sato, Kazuhiro Ohki, Keiko Okimura, Yoshiki Uchida, Mitsuno Shindo, and Naoki Sakura
概要 This study on the structure-activity relationship of polymyxin B, a cyclic peptide antibiotic, used sixteen synthetic polymyxin B3 analogs including alanine scanning analogs to elucidate the contribution of the side chains to antimicrobial activity and lipopolysaccharide (LPS) binding. Of these analogs, [Ala5]-polymyxin B3 showed greatly reduced antimicrobial activity against Escherichia coli (E. coli), Salmonella Typhimurium (S. Typhimurium) and Pseudomonas aeruginosa (P. aeruginosa) with MIC values of 4-16 nmol/mL, suggesting that the Dab (α,γ-diaminobutyric acid) residue at position 5 is the most important residue contributing to bactericidal activity.