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Antiandrogens.

Many antiandrogens, mainly steroidal and some nonsteroidal agents, have been synthesized and tested in several available biological assays. Unfortunately, many of these compounds have other biological activities which make it difficult to ascertain the precise mechanism of antiandrogenic action. The blocking of androgen action can be accomplished by a number of ways: (1) the inhibition of gonadotropin release and/or synthesis, (2) the interference with testosterone and/or dihydrotestosterone biosynthesis, (3) the blocking of protein synthesis, and (4) the competition with androgens at receptor sites. Although the major reason for the development of antiandrogens is to utilize them in certain clinical situations, some have become important tools in studying androgen action, particularly on the molecular level. The clinical effectiveness of some antiandrogens in prostatic hyperplasias, hirsutism, and acne represents an important advance in therapeutics, but the search for more potent antiandrogens with minimal side effects should continue.

Acne Vulgaris↗

[Pityrosporum folliculitis (author's transl)].

Pityrosporum folliculitis occurs mainly among adult males on the back and may result from antibiotic and steroid administration. The lipophilic yeasts are numerous in the papulo-pustular lesions and can easily be demonstrated in the perifollicular inflammation on histological slides. 8 new cases with typical clinicopathological features are recorded by the authors. The best results are obtained with topically applied amphotericin B or econazol.

Adult↗

[Clearance of antigens by the liver (author's transl)].

The liver is not only a metabolic organ, but has also immunological properties provided by the Kupffer cells which represent the major part of the body phagocytizing capacity. In case of an impairment of this function intestinal antigens, e.g. endotoxins, may reach the systemic circulation and thus exhibit their biological properties. The function of Kupffer cells obviously depends on a slow sinusoidal blood stream which latter is provided by blood flowing to the liver via the portal venous tract. This fact may be of consequence in porto-caval shunt surgery in order to use methods by which a rest flow through the portal vein to the liver is maintained. Thus, the organism is prevented from the biological consequences of an altered phagocytic function of the liver.

Antigens↗

Inhibition of tumor cell growth by low-boiling-point-saturated fatty acids isolated by molecular distillation and reversed phase liquid chromatography of hydrolysates of uncytotoxic wool grease secreted from sheep sebaceous gland.

We showed that massive growth of mouse Ehrlich ascites carcinoma (EAC) cells was not inhibited by wool grease secreted from the sheep sebaceous gland, whereas wool fatty acids separated by saponification of wool grease was growth-inhibitory. We then fractionated wool fatty acids into 9 fractions using molecular distillation (80-200 degrees C; 1 x 10(-2) mmHg) and found a marked antitumor activity in a low-boiling-point (< 80 degrees C) fraction (MW 200-300; C10-C20), which was further separated by reversed phase liquid chromatography on an octadecylisilica gel column, resulting in 5 fractions. The second most hydrophobic fraction (C8Si-4) obtained was the most growth-inhibitory to EAC cells cultured or implanted into mice, more marked than the antitumor glycopeptide bleomycin. C8Si-4 was suggested to be a mixture of a normal-chain C16-saturated fatty acid and two branched-chain kinds of saturated C16-iso- and C19-anteiso-fatty acids without hydroxyl groups according to gas chromatography-mass spectrographic analysis. Thus low-boiling-point saturated fatty acid moieties in some wool grease molecules were shown to become growth-inhibitory in vitro and in vivo only after released in the free acid form by esterolysis.

Animals↗