Silva M, Jacobus N V, Gorbach S L
Department of Community Health, Tufts University School of Medicine, Boston, MA 02111.
Diagn Microbiol Infect Dis. 1988 Feb;9(2):79-85. doi: 10.1016/0732-8893(88)90100-9.
The activity of LY146032 (LY) was evaluated against 269 clinical isolates: 150 Staphylococcus spp. (Staph), 45 enterococci, 51 Clostridium spp., and 23 peptostreptococci. LY was compared to penicillin, metronidazole, imipenem, clindamycin, oxacillin, ciprofloxacin, vancomycin, and ampicillin. LY and oxacillin were tested against Staph by microdilution in cation-supplemented Mueller-Hinton broth (CSMHB), and in unsupplemented Mueller-Hinton broth (MHB). For LY, the MIC 90s in CSMHB were 16-32 dilutions lower. Among the Staph, the MIC 90s for LY, vancomycin, and ciprofloxacin were 4 micrograms/ml, 4 micrograms/ml, and 2 micrograms/ml respectively. The MIC 90s for enterococci by agar dilution were as follows: LY 8 micrograms/ml; ampicillin 4 micrograms/ml; imipenem 4 micrograms/ml; vancomycin 4 micrograms/ml; and ciprofloxacin 2 micrograms/ml. Clindamycin and penicillin were the most effective drugs against peptostreptococci and Clostridia spp., but LY was the most active drug against Clostridium difficile. The bactericidal activity of LY was determined by 24-hr time-kill curves in MHB. These showed a bactericidal effect against enterococci, and a bacteriostatic effect against three of four strains of Staph. Synergy was demonstrated against enterococci and Staph when LY was tested with aztreonam, ceftriaxone, or tobramycin. LY is a promising new agent against gram-positive bacteria, including methicillin resistant strains of staphylococci and enterococci.
对LY146032（LY）针对269株临床分离菌的活性进行了评估，这些分离菌包括：150株葡萄球菌属（葡萄球菌）、45株肠球菌、51株梭菌属和23株消化链球菌。将LY与青霉素、甲硝唑、亚胺培南、克林霉素、苯唑西林、环丙沙星、万古霉素和氨苄西林进行了比较。通过在补充阳离子的穆勒-欣顿肉汤（CSMHB）和未补充的穆勒-欣顿肉汤（MHB）中进行微量稀释法，对LY和苯唑西林针对葡萄球菌进行了测试。对于LY，在CSMHB中的MIC90低16 - 32倍稀释。在葡萄球菌中，LY、万古霉素和环丙沙星的MIC90分别为4微克/毫升、4微克/毫升和2微克/毫升。通过琼脂稀释法测得肠球菌的MIC90如下：LY为8微克/毫升；氨苄西林为4微克/毫升；亚胺培南为4微克/毫升；万古霉素为4微克/毫升；环丙沙星为2微克/毫升。克林霉素和青霉素是针对消化链球菌和梭菌属最有效的药物，但LY是针对艰难梭菌最具活性的药物。通过在MHB中绘制24小时时间-杀菌曲线来测定LY的杀菌活性。这些曲线显示对肠球菌有杀菌作用，对四株葡萄球菌中的三株有抑菌作用。当LY与氨曲南、头孢曲松或妥布霉素一起测试时，显示出对肠球菌和葡萄球菌有协同作用。LY是一种有前景的新型抗革兰氏阳性菌药物，包括耐甲氧西林的葡萄球菌和肠球菌菌株。
