Aspiotis A, Cullmann W, Dick W, Stieglitz M
Chemotherapy. 1986;32(3):236-46. doi: 10.1159/000238420.
The role of inducible chromosomally mediated beta-lactamases was studied in 22 Proteus vulgaris isolates by monitoring enzyme induction in the presence of various inducers such as ampicillin, cefalothin, cefuroxime, cefsulodin, 6-aminopenicillanic acid (6-APS), and imipenem. 20 of the isolates exhibited resistance to ampicillin, cefalothin, and cefuroxime, whereas 2 isolates were susceptible to these compounds. In all resistant isolates marked inoculum effects could be observed. Enzyme production proved to be transient, i.e. maximum of enzyme production was achieved after 2 or 3 h. In both sensitive isolates enzyme production did not exceed 0.021 U beta-lactamase/mg protein of the cell-free supernatant even after induction with 6-APS or imipenem, whereas it ranged from 0.46 to 6.3 U in the resistant ones. Moreover, enzyme induction was found to be concentration-dependent, as revealed by the extensive study of one of the isolates (No. 4917). Three different enzymes could be distinguished by means of isoelectric focusing with isoelectric points at 7.4, 8.8, and approximately 9.5. In the presence of 2.5 mg/l clavulanic acid even strains known to be strong enzyme producers became as susceptible as the sensitive ones: moreover, the inocolum effect was markedly reduced. These findings make it apparent that it is above all the production of inducible enzymes that is responsible for resistance to beta-lactam antibiotics in P. vulgaris.
通过监测在各种诱导剂(如氨苄西林、头孢噻吩、头孢呋辛、头孢磺啶、6-氨基青霉烷酸(6-APS)和亚胺培南)存在下的酶诱导情况,对22株普通变形杆菌分离株中可诱导的染色体介导β-内酰胺酶的作用进行了研究。其中20株分离株对氨苄西林、头孢噻吩和头孢呋辛耐药,而2株分离株对这些化合物敏感。在所有耐药分离株中均可观察到明显的接种量效应。酶的产生被证明是短暂的,即在2或3小时后达到酶产生的最大值。在两株敏感分离株中,即使在用6-APS或亚胺培南诱导后,无细胞上清液中β-内酰胺酶的产生量也不超过0.021 U/mg蛋白,而在耐药分离株中,该值范围为0.46至6.3 U。此外,通过对其中一株分离株(编号4917)的广泛研究发现,酶诱导呈浓度依赖性。通过等电聚焦可区分出三种不同的酶,其等电点分别为7.4、8.8和约9.5。在2.5 mg/l克拉维酸存在的情况下,即使是已知的强酶产生菌株也变得和敏感菌株一样敏感:此外,接种量效应明显降低。这些发现表明,在普通变形杆菌中,对β-内酰胺类抗生素耐药主要是由可诱导酶的产生所致。