Preparation of [1,2-^3H,4-^<14>C]16α-Hydroxyandrostenedione and Its Use for Radiometric Determination of Human Placental Aromatase Activity(Analytical,Chemical)

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[l,2-^3H,4-^<14>C]16aα-Hydroxyandrostenedione (4) (^3H, 3.20mCi/mmol; ^3H/^<14>C=222) was synthesized from commercially available [1,2-^3H,4-^<14>C]dehydroepiandrosterone (1) through bromination at C-16α of the 17-ketone 1 and controlled alkaline hydrolysis of the 16α-bromoketone 3, obtained from the brominated product 2 by 8_N CrO_3 oxidation followed by p-toluenesulfonic acid treatment, as key reactions. The tritium distribution of the labeled 16α-ketol 4 was determined by chemical and biochemical methods to be 47% at C-1α, 18% at C-2α, and 35% at the β-side of C-1 and C-2. When the labeled ketol 4 was incubated with human placental microsomes and reduced nicotinamide adenine dinucleotide phosphate, the rate of ^3H_2O release into the medium was dependent upon protein concentration and incubation time. Aromatase activity obtained by the radiometric assay was comparable to that determined by the high-performance liquid chromatographic method.
公益社団法人日本薬学会の論文
1987-06-25