García de Lomas J, Navarro D, Gimeno C
Departamento de Microbiología, Hospital Clínico Universitario, Facultad de Medicina, Valencia.
Enferm Infecc Microbiol Clin. 1997 Sep;15 Suppl 1:14-9.
The outer membrane of gramnegative bacteria cell-wall contain channels formed by proteins known as porins, which facilitate the penetration of molecules into the cell. Imipenem and meropenem possess an important intrinsic activity against most gramnegative bacteria due to their high affinity for the penicillin-binding proteins PBP-2 and/or PBP-3. Meropenem is slightly more active against certain species of Enterobacteriaceae, Pseudomonas aeruginosa and nonfermenters bacilli. In this sense the differences in the activity between the two carbapenems may be attributable to differences in their affinity for PBPs, differences in their resistance to beta-lactamases hydrolysis, or to the differences in the capacity to employ certain porin channels. OprF is the main porin channel involved in the beta-lactam penetration of bacteria, though OprC and OprD2 may also contribute to the penetration of carbapenems into P. aeruginosa. However, evidences suggest that although impenem requires the presence of OprD2, meropenem may use other pathways for penetration. In Escherichia coli both carbapenems use ompF and ompC, and no specific porin channels have been detected. Only in the case of Enterobacter cloacae may exceptions exists among Enterobacteriaceae.
革兰氏阴性菌细胞壁的外膜含有由孔蛋白形成的通道,这些孔蛋白有助于分子进入细胞。亚胺培南和美罗培南对大多数革兰氏阴性菌具有重要的固有活性,因为它们对青霉素结合蛋白PBP - 2和/或PBP - 3具有高亲和力。美罗培南对某些肠杆菌科细菌、铜绿假单胞菌和非发酵杆菌的活性略高。从这个意义上说,两种碳青霉烯类药物活性的差异可能归因于它们对PBPs亲和力的差异、对β-内酰胺酶水解的抗性差异,或利用某些孔蛋白通道能力的差异。OprF是参与β-内酰胺进入细菌的主要孔蛋白通道,尽管OprC和OprD2也可能有助于碳青霉烯类药物进入铜绿假单胞菌。然而,有证据表明,虽然亚胺培南需要OprD2的存在,但美罗培南可能使用其他途径进行渗透。在大肠杆菌中,两种碳青霉烯类药物都使用ompF和ompC,并且未检测到特定的孔蛋白通道。仅在阴沟肠杆菌的情况下,肠杆菌科中可能存在例外。