法罗培南对质粒介导β-内酰胺酶的稳定性及抑酶作用研究  

Study of stability and inhibitory activity of faropenem against plasmid-mediated β-lactamases

作　　者：陈勇川[1] 朱卫民[2] 钱元恕[3] 

机构地区：[1]第三军医大学西南医院,重庆400038 [2]重庆医科大学附属第一医院,重庆400042 [3]汕头大学医学院,汕头515031

出　　处：《中国抗生素杂志》2006年第12期717-720,共4页Chinese Journal of Antibiotics

摘　　要：目的研究青霉烯类抗生素法罗培南对14种标准β-内酰胺酶(TEM-1、TEM-2、TEM-3、TEM-5、SHV-1、SHV-2、SHV-4、SHV-5、PSE-1、PSE-2、PSE-3、OXA-1、OXA-2和OXA-3)的稳定性及抑酶作用。方法采用紫外分光光度法,以其它β-内酰胺抗生素(亚胺培南、美罗培南、头孢噻啶、头孢西丁、头孢呋辛、头孢噻肟、头孢哌酮、氨曲南、克拉维酸、舒巴坦、三唑巴坦)为对照。结果所有抗生素对超广谱β-内酰胺酶(TEM-3、TEM-5、SHV-2、SHV-4和SHV-5)的IC50低于1.9μmol/L;但对广谱酶TEM-1、TEM-2和SHV-1的IC50超过100μmol/L。法罗培南对OXA-1、OXA-2和OXA-3的IC50低于1.0μmol/L。法罗培南、亚胺培南、美罗培南和头孢西丁对14种标准β-内酰胺酶均稳定。结论法罗培南对14种β-内酰胺酶的抑制作用强于亚胺培南和美罗培南。Objective To study the stability and inhibitory activity of faropenem against 14 plasmid- mediated standard β-lactamases （TEM-1, TEM-2, TEM-3, TEM-5, SHV-1, SHV-2, SHV-4, SHV-5, PSE- 1, PSE-2, PSE-3, OXA-1, OXA-2 and OXA-3）. Method The ultraviolet spectrophotometry was used with other β-lactams （imipenem,. meropenem, cephaloridine, cefoxitin, cefuroxime, cefotaxime, cefoperazone, aztreonam, clavulanic acid, sulbactam and tazobactam） as control. Results Faropenem, imipenem, meropenem and cefoxitin were very stable to 14 plasmid-mediated β-lactamases. The IC50s of all tested antibiotics against extended-spectrum β-lactamases （TEM-3, TEM-5, SHV-2, SHV-4 and SHV-5） were below 1.9 μmol/L. The ICs0s of all antibiotics against broad-spectrum β-lactamases （TEM-1, TEM-2 and SHV-1） were beyond 100μmol/L. The IC50s of faropenem against OXA β-lactamases （OXA-1, OXA-2 and OXA-3） were below 1.0μmol/L. Conclusion Faropenem showed stronger inhibitory activity than imipenem and mero -penem against 14 plasmid-mediated β-lactamases.

关 键 词：法罗培南 Β-内酰胺酶 稳定性 抑酶作用 

分 类 号：R978.11[医药卫生—药品]