Kimura T, Yamamoto T, Ishizuka R, Sezaki H
Biochem Pharmacol. 1985 Jan 1;34(1):81-4. doi: 10.1016/0006-2952(85)90103-0.
The transport characteristics of cefadroxil, an aminocephalosporin antibiotic, across the brush border membrane of rat small intestine were investigated by a rapid filtration technique. The uptake of cefadroxil was not affected by Na+ gradient, suggesting the absence of a cotransport system between cefadroxil and Na+ in the brush border membrane. The uptake was slightly inhibited by HgCl2 pretreatment and stimulated by the countertransport effect, where cyclacillin played a role as an elicitor. These results suggest the existence of a carrier-mediated transport system for cefadroxil in the brush border membrane, which is shared with cyclacillin. Papain treatment increased the specific transport activities for the antibiotic. This may be the first step of purification of the cefadroxil transport carrier.
采用快速过滤技术研究了氨基头孢菌素类抗生素头孢羟氨苄在大鼠小肠刷状缘膜上的转运特性。头孢羟氨苄的摄取不受Na⁺梯度影响,这表明在刷状缘膜中头孢羟氨苄与Na⁺之间不存在协同转运系统。摄取受到HgCl₂预处理的轻微抑制,并受到反向转运效应的刺激,其中环青霉素起到诱导剂的作用。这些结果表明在刷状缘膜中存在头孢羟氨苄的载体介导转运系统,该系统与环青霉素共用。木瓜蛋白酶处理增加了抗生素的特异性转运活性。这可能是头孢羟氨苄转运载体纯化的第一步。