Al-Nawas B, Swantes J, Shah P M
Dept. of Oral and Maxillofacial Surgery, Johannes Gutenberg University, Mainz, Germany.
Infection. 2000 Jul-Aug;28(4):214-8. doi: 10.1007/s150100070038.
The objectives of the study were to observe the activity of LY333328, a new semisynthetic glycopeptide, compared to that of vancomycin against six strains of Enterococcus faecium and Enterococcus faecalis, including four vancomycin-resistant strains. Bacteria ingested by polymorphonuclear leukocytes (PMN) as well as extracellular bacteria were studied using a colony count method. The activity against intracellular bacteria was tested with the drugs present in the extracellular medium, as well as after preincubating the PMN and removal of the drugs. LY333328 is active against the tested enterococci, regardless of their susceptibility to vancomycin, with MICs of 1-2 mg/l. It is bacteriostatic against extracellular enterococci at concentrations of 2 microg/ml and above regardless of their resistance to vancomycin. After 4 h incubation at 10 MIC, vancomycin-resistant strains of E. faecium and E. faecalis located intracellularly were reduced by 55% and 90%, respectively. Even after preincubation and removal of the drug, LY333328 had an effect at 10 MIC with a 20-30% reduction in the inoculum. The results suggest that in contrast to vancomycin, LY333328 is active against intracellular vancomycin-resistant enterococci, particularly E. faecalis, even after removal of the extracellular drug.
本研究的目的是观察一种新型半合成糖肽LY333328与万古霉素相比，对6株粪肠球菌和屎肠球菌（包括4株耐万古霉素菌株）的活性。使用菌落计数法研究了多形核白细胞（PMN）摄取的细菌以及细胞外细菌。通过检测细胞外培养基中存在的药物以及PMN预孵育并去除药物后，测试了对细胞内细菌的活性。LY333328对受试肠球菌具有活性，无论它们对万古霉素的敏感性如何，其最低抑菌浓度（MIC）为1 - 2mg/l。无论其对万古霉素的耐药性如何，在浓度为2μg/ml及以上时，它对细胞外肠球菌具有抑菌作用。在10倍MIC浓度下孵育4小时后，细胞内的耐万古霉素屎肠球菌和粪肠球菌菌株分别减少了55%和90%。即使经过预孵育并去除药物，LY333328在10倍MIC浓度下仍有作用，接种量减少20 - 30%。结果表明，与万古霉素不同，即使去除细胞外药物后，LY333328对细胞内耐万古霉素肠球菌，特别是粪肠球菌仍具有活性。
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