【摘要】 <正> 抗生素广泛应用之后,细菌普遍产生抗药性,更为严重的是有些细菌的药物抗性基因可以在细菌之间进行转移,使原来敏感的细菌也变成耐药菌,限制了抗生素的临床应用,威胁着人民的保健工作。因而如何筛选新的药物以对付细菌耐药性是药物研究工作者的一项迫切任务。青霉素钝化酶β-内酰胺酶抑制剂棒酸的发现并在临床应用上获得成功,为其它抗生素钝化酶抑制剂的寻找打开了视野。磷酸化转移酶是使新霉素(NM)、卡那霉素(KM)、巴龙霉素(PM)、核糖霉素(RM)、链霉素(SM)等失效的重要钝化酶,这类酶广泛存在于微生物中,许多链霉菌都能产生磷酸化转移酶(APH),它们还参与抗生素合成及代谢调节作用。人们发现有的微生更多还原

【Abstract】 Phosphotransferase inhibitor 80-506 is produced by Str, sp. 506 in submerge culture. The active component is isolated by precipitation with sodium chloride and is further purified by dialysis and chromato-graphy on a column of Sephadex G-75 or Sephadex G-100.Phosphotransferase inhibitor 80-506 is a polypeptide, consisting of at least eight amino acids:Asp. Gly.Ala. Glu.Val. Lys.and Thr.It is inactive against bacteria and fungi, but it strongly inhibits the activity of 3’-phosphotransferase, which is isolated from various resistance bacteria and is active against the following aminoglyco-side antibiotics:KM, RM,PM,NM, LM,SM. The physicochemical properties of the corn-pound are given.更多还原