男性ホルモンの肝臓内に於ける破壊について

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There has been prevailing a question why the natural estrogen displays far less effectiveness when administered per os than when it is subcutaneously or intramuscularly injected. Recent reports suggest that the sex hormones are more or less inactivated in the liver. This has been confirmed by our experimental study that the liver plays a significant role in the diminishing mechanism of the hormones when given by oral administration. Pellets made of compressed crystals of estrone exert no effect on the gonad of the experimental animal when implanted in the spleen or mesenterium connected with the portal vein in an oophorectomized rat, beaause it may be inactivated in situ or absorbed in the portal vein passing through the liver. Accordingly no oestrus is detected in the animal, its vaginal smear showing sexually quiescent stage; the patterns of the anterior lobe of the pituitary being the same as in castrated animals, the genital organs being atrophied with little findings characteristic of those induced by the estrone. On the contrary full cornification of vagina will follow in the animal when injected either subcutaneously or intramuscularly with estrone, its genital organs showing marked developement. When the spleen, implanted with the pellets, acquires collateral circulation, immediate effect of estrone will manifest itself because some of the estrone may be kept from the liver. The effect of estrone will also be observed in the animal, the liver of which has been partially excised. Thus it has been demonstrated that estrone shows no effect when implanted in the portal circulation system due to the powerful inactivating action of the liver. A similar experiment has been made with Hexestrol, a synthetical compound of the follicular hormone. It has been demonstrated that the inactivating action of the liver upon the hormone implanted in the spleen is much less so that its hormonal effect can be clearly seen. Thus it has been shown that, so far as oral administration is concerned, Hexestrol has some effect, while estrone has no effect. The same idea led us to compare progestional hypertrophy of the uterine mucosa following the implantation of progesterone pellets in the spleen and in the muscle. In the former case no change ensued because of the inactivating effect of the liver, while in the latter positive results were obtained. Thus it is to be concluded that the progesterone is similarly inactivated in the liver and may be of no use in oral administration. Testosterone acetate pellets were also examined, and the result obtained shows some similarity in its effect upon the gonad, while in case of methyl testosterone pellets the effects have been influenced very little by the liver. Accordingly, it could be reasonably assumed that methyl testosterone may well be taken orally. The foregoing results seem to coincide well with the clinical observations.
社団法人日本産科婦人科学会の論文
1951-09-01

男性ホルモンの肝臓内に於ける破壊について

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