Benson C A, Beaudette F, Trenholm G
Department of Medicine, Rush-Presbyterian-St. Luke's Medical Center, Chicago, Illinois 60612.
J Antimicrob Chemother. 1987 Aug;20(2):191-6. doi: 10.1093/jac/20.2.191.
The in-vitro activity of LY146032, a new biosynthetic peptolide antibiotic, was compared with vancomycin and eight other antibiotics against 190 Gram-positive bacteria. Organisms tested included streptomycin-susceptible and resistant enterococci, nafcillin-susceptible and resistant Staphylococcus aureus, and nafcillin-susceptible and resistant Staph. epidermidis. LY146032 had excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistant staphylococci (MIC90 less than or equal to 0.5 mg/l) and against enterococci (MIC90 less than or equal to 2.0 mg/l). LY146032 was more active than vancomycin against the majority of isolated tested. With the exception of trimethoprim-sulphamethoxazole, LY146032 was the most active agent in vitro against enterococci, and was the most active against nafcillin-resistant staphylococci. LY146032 and vancomycin showed a marked increase in MIC when the inoculum was increased from 10(5) to 10(7) cfu/ml. LY146032 and vancomycin were bactericidal at concentrations within two dilutions of the MIC for staphylococci. LY146032 was bactericidal at less than or equal to 8 mg/l for all enterococcal isolates tested.
将新型生物合成缩酚肽类抗生素LY146032的体外活性与万古霉素及其他8种抗生素针对190株革兰氏阳性菌进行了比较。所测试的菌株包括对链霉素敏感和耐药的肠球菌、对萘夫西林敏感和耐药的金黄色葡萄球菌以及对萘夫西林敏感和耐药的表皮葡萄球菌。LY146032对萘夫西林敏感和耐药的葡萄球菌（MIC90小于或等于0.5毫克/升）以及肠球菌（MIC90小于或等于2.0毫克/升）具有出色的体外抑制和杀菌活性。在大多数分离测试菌株中，LY146032比万古霉素更具活性。除复方新诺明外，LY146032是体外对肠球菌活性最强的药物，且对耐萘夫西林葡萄球菌活性最强。当接种量从10^5增至10^7 cfu/毫升时，LY146032和万古霉素的MIC显著升高。LY146032和万古霉素在针对葡萄球菌的MIC的两个稀释度范围内的浓度时具有杀菌作用。对于所有测试的肠球菌分离株，LY146032在小于或等于8毫克/升时具有杀菌作用。
