Raab W P, Gmeiner B M
Arch Dermatol Res (1975). 1976 Jun 21;255(3):265-70. doi: 10.1007/BF00561497.
In fresh human skin homogenates, the activities of four enzymes, lactate dehydrogenase (LDH), glucose-6-phosphate dehydrogenase (G-6-PDH), "acid" phosphatase (AcP), and "leucine aminopeptidase" (LAP) were assayed following an incubation with hydrocortisone, hydrocotisone acetate, or hydrocortisone-17-butyrate, respectively. Concentration of the three compounds measured 2.75 mMol/l. Hydrocortison butyrate inhibited LDH-G-6-PDH-, and AcP-activities. Hydrocortisone and hydrocortisone acetate exerted a significant inhibitory action only in the case of G-6-PDH-activity.--On pure G-6-PDH from yeast, the inhibition exerted by hydrocortisone butyrate was significantly stronger than the inhibition exerted by the two other steroids. Time/action diagrams revealed the fact that hydrocortisone butyrate is superior to the other two compounds from the beginning of the incubation period.--The date sustain the assumption that hydrocortisone butyrate exerts biochemical-pharmacological actions of its own and that it may not be considered just as an esterified transport form of hydrocortisone.
在新鲜的人体皮肤匀浆中,分别与氢化可的松、醋酸氢化可的松或氢化可的松-17-丁酸酯孵育后,测定了四种酶的活性,即乳酸脱氢酶(LDH)、葡萄糖-6-磷酸脱氢酶(G-6-PDH)、“酸性”磷酸酶(AcP)和“亮氨酸氨肽酶”(LAP)。三种化合物的浓度均为2.75毫摩尔/升。氢化可的松丁酸酯抑制LDH、G-6-PDH和AcP的活性。氢化可的松和醋酸氢化可的松仅在G-6-PDH活性方面有显著的抑制作用。——对于来自酵母的纯G-6-PDH,氢化可的松丁酸酯的抑制作用明显强于其他两种类固醇。时间/作用图显示,从孵育期开始,氢化可的松丁酸酯就优于其他两种化合物。——这些数据支持了这样一种假设,即氢化可的松丁酸酯具有自身的生化药理作用,不能仅仅被视为氢化可的松的酯化转运形式。