Jordán J, Idoate I, Urdaneta E, Larralde J
Departamento de Fisiología y Nutrición, Facultad de Farmacia, Universidad de Navarra, Pamplona, Spain.
Rev Esp Fisiol. 1996 Mar;52(1):31-6.
The effect of the broad spectrum antibiotics cefaclor, cefadroxil, cephradine, cefatrizine, cephaloglycine and cefroxadine was examined on rat intestinal brush border enzymes, aminopeptidase N (E.C. 3.4.11-2), dipeptidyl peptidase IV (E.C. 3.4.14.5) and alkaline phosphatase (E.C. 1.3.1.3.). All the cephalosporins assayed -except cefaclor- inhibit the aminopeptidase N activity, in an uncompetitive manner. Cefatrizine showed the most important inhibitory effect (52.5%; p < 0.001). Cefaclor and cefadroxil have no effect on the activity of the dipeptidyl peptidase IV, while cephaloglycine and cephradine showed a non competitive type inhibition. In contrast, cefatrizine and cefroxadine showed a competitive inhibition for this enzyme. None of the cephalosporins assayed had any effect on alkaline phosphatase activity.
研究了广谱抗生素头孢克洛、头孢羟氨苄、头孢拉定、头孢曲嗪、头孢甘氨酸和头孢沙定对大鼠肠道刷状缘酶氨肽酶N（E.C. 3.4.11-2）、二肽基肽酶IV（E.C. 3.4.14.5）和碱性磷酸酶（E.C. 1.3.1.3.）的影响。除头孢克洛外，所有检测的头孢菌素均以非竞争性方式抑制氨肽酶N的活性。头孢曲嗪显示出最重要的抑制作用（52.5%；p < 0.001）。头孢克洛和头孢羟氨苄对二肽基肽酶IV的活性没有影响，而头孢甘氨酸和头孢拉定显示出非竞争性抑制类型。相比之下，头孢曲嗪和头孢沙定对该酶表现出竞争性抑制作用。所有检测的头孢菌素对碱性磷酸酶活性均无影响。
