Cooke B A, Vallance D K
Biochem J. 1968 Aug;109(1):121-5. doi: 10.1042/bj1090121.
Megestrol acetate is metabolized by homogenates of rat adrenal glands to three more polar metabolites Y(2), Y(3) and Y(4). Their structures were investigated by microchemical reactions, paper chromatography, and ultraviolet and infrared spectroscopy. Metabolite Y(3) was identified as 17alpha-acetoxy-11beta-hydroxy-6-methyl-pregna-4,6-diene-3,20-dione, its oxidation product being identical with authentic 17alpha-acetoxy-6-methylpregna-4,6-diene-3,11,20-trione. It is suggested that metabolite Y(2) is 17,18-dihydroxy-6-methylpregna-4,6-diene-3,20-dione and that it also exists in the form of an alpha-ketol formed between the 18-hydroxyl and 20-oxo groups. Metabolite Y(4) is probably a tautomeric form of metabolite Y(2) as they were partially interconverted on chromatography and also have similar properties.
醋酸甲地孕酮经大鼠肾上腺匀浆代谢为三种极性更强的代谢产物Y(2)、Y(3)和Y(4)。通过微量化学反应、纸色谱法以及紫外和红外光谱对它们的结构进行了研究。代谢产物Y(3)被鉴定为17α - 乙酰氧基 - 11β - 羟基 - 6 - 甲基 - 孕甾 - 4,6 - 二烯 - 3,20 - 二酮，其氧化产物与纯品17α - 乙酰氧基 - 6 - 甲基 - 孕甾 - 4,6 - 二烯 - 3,11,20 - 三酮相同。推测代谢产物Y(2)为17,18 - 二羟基 - 6 - 甲基 - 孕甾 - 4,6 - 二烯 - 3,20 - 二酮，并且它也以18 - 羟基和20 - 氧代基团之间形成的α - 酮醇形式存在。代谢产物Y(4)可能是代谢产物Y(2)的互变异构体，因为它们在色谱上会部分相互转化，并且性质也相似。
