Tamai I, Terasaki T, Tsuji A
J Antibiot (Tokyo). 1985 Dec;38(12):1774-80. doi: 10.7164/antibiotics.38.1774.
The inhibition effect of several beta-lactam antibiotics on the uptake of [14C]benzylpenicillin (PCG) into isolated rat hepatocytes was studied. Monobasic beta-lactam antibiotics such as apalcillin, cloxacillin, nafcillin, piperacillin, cefmetazole, cefoperazone, cefpiramide and cephalothin significantly inhibited the uptake of PCG, while amphoteric beta-lactam antibiotics such as amoxicillin, ciclacillin, cephradine, cephalexin and cephaloridine had a slight inhibitory effect on the uptake of PCG. Five monobasic compounds of these antibiotics used (apalcillin, nafcillin, piperacillin, cefmetazole and cefoperazone) which have a tendency to be excreted into bile to a large extent, inhibited the initial uptake rate of PCG in a fully competitive fashion according to the Lineweaver-Burk plots and the corresponding modified Inui-Christensen plots. Thus, it was concluded that almost all beta-lactam antibiotics have a common carrier system responsible for their uptake into isolated rat hepatocytes, but it is still uncertain whether or not amphoteric beta-lactam antibiotics have another specific transport system.
研究了几种β-内酰胺类抗生素对[14C]苄青霉素（PCG）进入离体大鼠肝细胞摄取的抑制作用。一元β-内酰胺类抗生素如阿帕西林、氯唑西林、萘夫西林、哌拉西林、头孢美唑、头孢哌酮、头孢匹胺和头孢噻吩显著抑制PCG的摄取，而两性β-内酰胺类抗生素如阿莫西林、环青霉素、头孢拉定、头孢氨苄和头孢硫脒对PCG的摄取有轻微抑制作用。所使用的这些抗生素的五种一元化合物（阿帕西林、萘夫西林、哌拉西林、头孢美唑和头孢哌酮）在很大程度上倾向于排入胆汁，根据Lineweaver-Burk图和相应的改良Inui-Christensen图，它们以完全竞争的方式抑制PCG的初始摄取速率。因此，得出的结论是，几乎所有的β-内酰胺类抗生素都有一个共同的载体系统负责它们进入离体大鼠肝细胞的摄取，但两性β-内酰胺类抗生素是否有另一种特异性转运系统仍不确定。
