Miyazaki M, Komori T, Okunishi H, Toda N
Jpn Circ J. 1979 Sep;43(9):818-23. doi: 10.1253/jcj.43.818.
The inhibitory effect of pepstatin A, an isovaleryl pentapeptide isolated from streptmyces, was studied. Pepstatin A inhibited the action of dog renin on homologus substrate. The Ki value was 7.7 X 10(-7) M and the mode of the inhibition was non-competitive. Pestatin A suppressed angiotensin I generation in dog plasma. Dose-dependent hypotensive effect of pepstatin A was observed in rats with sustained increase in blood pressure during continuous infusion of dog renin. It is concluded that pepstatin A inhibits the dog renin activity in vitro and in vivo.
研究了从链霉菌中分离出的异戊酰五肽胃蛋白酶抑制剂A的抑制作用。胃蛋白酶抑制剂A抑制犬肾素对同源底物的作用。Ki值为7.7×10(-7)M,抑制模式为非竞争性。胃蛋白酶抑制剂A抑制犬血浆中血管紧张素I的生成。在持续输注犬肾素期间血压持续升高的大鼠中观察到胃蛋白酶抑制剂A的剂量依赖性降压作用。得出结论,胃蛋白酶抑制剂A在体外和体内均抑制犬肾素活性。