Manankova N M, Salganik R I
Vopr Med Khim. 1977 Jul-Aug;23(4):458-63.
A possibility to increase 7alpha-hydroxylation of 4-14C-cholesterol was studied in vitro, using microsomal enzymes from rat liver tissue, under effect of such inductors of these enzymes as 5-ethyl-5-phenyl barbituric acid (phenobarbital), pregnenolone-16alpha-carbonitrile, 16-dehydropregnenolone, 3-acetate-16alpha-isothiocyanogen pregnenolone. These inductors were administered per os within 5 days as an aqueous suspension, stabilized with Tween 80 at a dose 50 mg/kg daily; ethyl ester alpha-(p-chlorophenhydroxy)-isobutyric acid (klofibrate "Miskleron*) was administered at a dose of 150 mg/kg daily within 5 days. All the inductors studied increased the activity of cholesterol 7alpha-hydroxylase: pregnenolone-16alpha-carbonitrile--by 50%, 16-dehydropregnenolone--by 80%, 3-acetate-16alpha-isthiocyanogen pregnenolone--by 110% and phenobarbital--by 200%. Klofibrate did not affect the intensity of the cholesterol hydroxylation.
利用大鼠肝脏组织中的微粒体酶,在5-乙基-5-苯基巴比妥酸(苯巴比妥)、孕烯醇酮-16α-腈、16-脱氢孕烯醇酮、3-醋酸酯-16α-异硫氰基孕烯醇酮等这些酶的诱导剂作用下,体外研究了增加4-¹⁴C-胆固醇7α-羟化作用的可能性。这些诱导剂以水悬浮液形式经口给药5天,用吐温80稳定,每日剂量为50 mg/kg;α-(对氯苯氧异丁酸)乙酯(氯贝丁酯“米斯克隆”)在5天内每日剂量为150 mg/kg给药。所有研究的诱导剂均增加了胆固醇7α-羟化酶的活性:孕烯醇酮-16α-腈增加了50%,16-脱氢孕烯醇酮增加了80%,3-醋酸酯-16α-异硫氰基孕烯醇酮增加了110%,苯巴比妥增加了至200%。氯贝丁酯不影响胆固醇羟化的强度。