Inui K, Okano T, Takano M, Saito H, Hori R
Biochim Biophys Acta. 1984 Jan 25;769(2):449-54. doi: 10.1016/0005-2736(84)90329-8.
Carrier-mediated transport of aminocephalosporin antibiotics by renal brush-border membrane vesicles has been studied in relation to the transport systems for dipeptides and amino acids. Dipeptides such as L-carnosine (beta-alanyl-L-histidine) and L-phenylalanylglycine competitively inhibited the uptake of cephalexin, but amino acids did not. Cephalexin uptake was stimulated by the countertransport effect of L-carnosine in the normal and papain-treated vesicles, and by the effect of L-phenylalanylglycine only in the papain-treated vesicles. In the papain-treated vesicles, the hydrolysis of dipeptides was markedly decreased, and the specific activity for cephalexin transport was increased approx. 2-fold because of the partial removal of membrane proteins. These results suggest that carrier-mediated transport of cephalexin can be transported by the system for dipeptides in renal brush-border membranes.
已经研究了肾刷状缘膜囊泡介导的氨基头孢菌素抗生素转运与二肽和氨基酸转运系统的关系。二肽如L-肌肽（β-丙氨酰-L-组氨酸）和L-苯丙氨酰甘氨酸竞争性抑制头孢氨苄的摄取，但氨基酸则无此作用。在正常和木瓜蛋白酶处理的囊泡中，L-肌肽的逆向转运作用刺激了头孢氨苄的摄取，而L-苯丙氨酰甘氨酸仅在木瓜蛋白酶处理的囊泡中具有这种作用。在木瓜蛋白酶处理的囊泡中，二肽的水解明显减少，由于部分去除了膜蛋白，头孢氨苄转运的比活性增加了约2倍。这些结果表明，肾刷状缘膜中二肽系统可介导头孢氨苄的载体介导转运。
