Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats
Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats
复制标题
多种蛋白酶抑制剂改善大鼠肺吸收(Asu1,7)-鳗鱼降钙素
DOI：
10.1023/a:1018950429341
复制
发表时间：
1994
影响因子：
3.7
通讯作者：
H. Sezaki
中科院分区：
文献类型：
--
作者：
T. Morita;A. Yamamoto;Y. Takakura;M. Hashida;H. Sezaki
本文研究了蛋白酶抑制剂甘氨胆酸钠、杆菌肽、倍他丁、萘莫司他和大豆胰蛋白酶抑制剂（STI）对鳗鱼降钙素（ECT，分子量3363）在大鼠肺吸收的影响。ECT的肺吸收通过测量其低钙效应来估计。当ECT单独施用于肺时，ECT的药理学利用度为2.7%。与STI或bestatin联合给药不会改变ECT的药理作用。然而，钠-甘胆酸盐，杆菌肽和萘莫司他甲磺酸酯引起了显着的低钙作用后，肺吸收的ECT和最大的效果，注意到在20 mM杆菌肽的存在下，接近ECT静脉给药后的效果。杆菌肽和甘氨胆酸钠可降低111 In-ECT在大鼠肺匀浆中的降解。因此，蛋白酶抑制剂有效地改善ECT的肺吸收。
The effects of protease inhibitors, Na-glycocholate, bacitracin, bestatin, nafamostat mesilate and soybean trypsin inhibitor (STI) on the pulmonary absorption of (Asu1,7)-eel calcitonin (ECT, molecular weight 3363) were investigated in rats. The pulmonary absorption of ECT was estimated by measuring its hypocalcemic effect. When ECT alone was administered into the lung, the pharmacological availability of ECT was 2.7%. Co-administration with STI or bestatin did not change the pharmacological effect of ECT. However, Na-glycocholate, bacitracin and nafamostat mesilate caused a significant hypocalcemic effect following the pulmonary absorption of ECT and a maximal effect was noted in the presence of 20 mM bacitracin, approaching the effect after intravenous administration of ECT. Bacitracin and Na-glycocholate reduced the degradation of 111In-ECT in rat lung homogenate. Therefore, protease inhibitors effectively improved the pulmonary absorption of ECT.