碳青霉烯抗生素对质粒介导β-内酰胺酶的稳定性及抑酶效应研究  

Study of stability and inhibitory activity of carbapenems against β-lactamases

作　　者：陈勇川[1] 朱卫民[1] 钱元恕[2] 

机构地区：[1]第三军医大学西南医院,重庆400038 [2]汕头大学医学院

出　　处：《中国抗生素杂志》2003年第5期289-291,共3页Chinese Journal of Antibiotics

摘　　要：用紫外分光光度法 ,以其它 β 内酰胺抗生素为对照 ,研究碳青霉烯类抗生素亚胺培南、美洛培南和帕尼培南对 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 ,OXA 3 )的稳定性及抑酶作用。亚胺培南、美洛培南、帕尼培南和头孢西丁对 14种标准 β 内酰胺酶均高度稳定。所有抗生素对超广谱 β 内酰胺酶 (TEM 3、TEM 5、SHV 2、SHV 4、SHV 5 )的IC50 低于 3 μmol/L ;但对广谱酶 (TEM 1,TEM 2 ,SHV 1,OXA)的IC50 超过 10 0 μmol/L。整体上美洛培南对 14种 β 内酰胺酶的抑制作用强于亚胺培南和帕尼培南。The stabilities and inhibitory activities of carbapenems against 14 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) were studied, using other β lactams as control. Results showed that imipenem, meropenem, panipenem and cefoxitin were very stable to 14 β lactamases. The IC 50 s of all carbapenems against extended spectrum β lactamases (TEM 3, TEM 5, SHV 2, SHV 4 and SHV 5) were below 3μmol/L; but the IC 50 s of all carbapenems against broad spectrum β lactamases (TEM 1, TEM 2 and SHV 1) and OXA type β lactamases were beyond 100μmol/L. Overall, meropenem showed more potent inhibition activity than imipenem and panipenem against 14 β lactamases.

关 键 词：碳青霉烯类抗生素 Β-内酰胺酶 稳定性 抑酶作用 

分 类 号：R927.11[医药卫生—药学]