Takatsu T, Katayama T, Nakajima M, Takahashi S, Haneishi T, Magaribuchi T, Tajima M
J Antibiot (Tokyo). 1987 Jul;40(7):946-52. doi: 10.7164/antibiotics.40.946.
Chloropolysporins A, B and C, as well as derivatives prepared from this group and alpha- and beta-avoparcins by enzymatic and mild acid hydrolysis, were active against Gram-positive bacteria including clinically isolated methicillin-resistant Staphylococci (MIC 0.39-6.25 micrograms/ml) and anaerobic enterobacteria (MIC 0.10-1.56 micrograms/ml). Derhamnosyl and demannosyl derivatives from both groups of antibiotics showed stronger activities than the parent compounds. The MIC and MBC values against Staphylococci were similar and were not effected by the presence of serum. Moreover, chloropolysporin C exhibited very strong synergistic effects with various beta-lactam antibiotics against methicillin-resistant strains of Staphylococcus aureus. Some of these compounds also protected mice from experimental infection with S. aureus. Acute toxicities of chloropolysporin by intravenous administration ranged from 215-290 mg/kg in mice. Chloropolysporin B as well as other glycopeptide antibiotics, showed distinctive growth promoting activity in broiler chickens.
氯多孢菌素A、B和C，以及由该组化合物和α-和β-阿伏霉素经酶促和温和酸水解制备的衍生物，对革兰氏阳性菌具有活性，包括临床分离的耐甲氧西林葡萄球菌（MIC为0.39 - 6.25微克/毫升）和厌氧肠杆菌（MIC为0.10 - 1.56微克/毫升）。两组抗生素的去鼠李糖基和去甘露糖基衍生物显示出比母体化合物更强的活性。针对葡萄球菌的MIC和MBC值相似，且不受血清存在的影响。此外，氯多孢菌素C与各种β-内酰胺抗生素对耐甲氧西林金黄色葡萄球菌菌株表现出非常强的协同作用。其中一些化合物还能保护小鼠免受金黄色葡萄球菌的实验性感染。小鼠静脉注射氯多孢菌素的急性毒性范围为215 - 290毫克/千克。氯多孢菌素B以及其他糖肽类抗生素在肉鸡中表现出独特的促生长活性。
