教員教育・研究情報 - 興村　桂子

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	2007/03
形態種別	学術論文
査読	査読あり
標題	Chemical Conversion of Natural Polymyxin B and Colistin to Their N-Terminal Derivatives
執筆形態	共著
掲載誌名	Bull. Chem. Soc. Jpn.
巻・号・頁	80,pp.543-552
著者・共著者	Keiko Okimura, Kazuhiro Ohki, Yuki Sato, Kuniharu Ohnishi, Yoshiki Uchida, and Naoki Sakura
概要	The chemical conversions of natural polymyxin B and colistin, which are fatty-acylated cyclic decapeptides, to polymyxin (2–10) and colistin (2–10) derivatives were examined. The N^α-free and side chain N^γ-protected nonapeptides, i.e., tetrakis(N^γ-trifluoroacetyl)–polymyxin B (2–10) and tetrakis(N^γ-trifluoroacetyl)–colistin (2–10), were prepared by trifluoroacetylation of polymyxin B and colistin. Further, myristoyl–polymyxin B (2–10) and myristoyl–colistin (2–10) retained their antimicrobial activity with an MIC of 2–4 nmol/mL against Escherichia coli, Salmonella Typhimurium, and Pseudomonas aeruginosa. They also retained their high lipopolysaccahride (LPS) binding activity.