[Bone tumors and androgen metabolism]. / Opukholi kostei i metabolizm androgenov.

The paper provides data of comparative assessment of activity of the key enzymes in metabolism of androgens in various morphological variants of sarcomas and benign bone tumors in 46 patients within the age range from 15 to 61, which were under treatment in the ORC named after N. N. Blokhin, RAMS, from 1996 to 1997. On the basis on publications and our own research results we can suggest that malignant human bone tumors of various histogenesis are subject to metabolic processes of testosterone (T), the principal androgen regulator in the bone tissue, as well as formation in bones of 5 alpha-dihydrotestosterone (DHT). One cannot exclude a possibility that metabolism of androgen in bone tissues is directed towards formation of other androgens (in addition to DHT), which may participate in the bone tissue regulation, for instance, 3 alpha- and 3 beta-diols; specific activity of the latter has recently been intensively scrutinized. One can expect that further research shall disclose the clinical significance of metabolism of androgens and of individual androgens in human bone formations.

[Metabolism of androgens in various histological variants of bone tumors]. / Osobennosti metabolizma androgenov v razlichnykh gistologicheskikh variantakh opukholei kostei.

The role of androgens in human normal and neoplastic bone tissues is still unclear. The paper presents data on metabolism of androgens in homogenates of malignant (osteosarcoma, chondrosarcoma, Ewing and giant cell) and benign primary tumors from 46 male and female patients aged 14-58 years. Using two substrates (testosterone and 5 alpha-dihydrotestosterone) for the first time are shown activities of main enzymes of androgen metabolism in all tumor types. 5 alpha-reductase activity was similar in all tumors, 3 alpha-hydroxysteroid dehydrogenase activity was the highest while that of 17 beta-hydroxysteroid dehydrogenase was the lowest. Unknown metabolite(s) of 5 alpha-dehydrotestosterone was discovered which may be hydroxy-metabolites of 5 alpha-androstane-3 beta, 17 beta-diol. A principal scheme of androgen metabolism in human neoplastic tissue is proposed.

[Reduction of 5alpha-dehydrotestosterone in sex steroid target cells--catabolism or directed biotransformation into hormones?]. / Vosstanovlenie 5al'fa-digidrotestosterona v kletkakh-misheniakh polovykh steroidov--katabolizm ili napravlennaia biotransformatsiia v gormony?

Based on analysis of the published experimental data, we propose a hypothetical mechanism of action of two androgens, 5 alpha-androstane-3 alpha,17 beta-diol (3 alpha-diol) and 5 alpha-androstane-3 beta,17 beta-diol (3 beta-diol), which are produced when 5 alpha-dihydrotestosterone (DHT) is reduced in sex steroids target cells. The mode of action of these diols as regulatory factors assumes that the androgens possess autocrine, paracrine, and endocrine action that differs from the action of DHT in animals and man and do not merely represent catabolites or metabolites capable of controlling the level of true androgenic hormone DHT. It is proposed that both diols should be classified as parahormones.

[Protein determination by binding with the dye Coomassie brilliant blue G-250]. / Opredelenie belka po sviazyvaniiu s krasitelem kumassi brilliantovym golubym G-250.

Possible applications of the Coomassie brilliant blue G-250 dye method for protein assay are reviewed. The physico-chemical and optical properties of the dye are considered in detail. The data on the protein-binding mechanism are generalized. Modifications of the Coomassie blue G-250 quantitative protein assays are critically considered. The applications of the method in medicine, biochemistry and biotechnology are discussed.

[Increase in the quality of determining estradiol and progesterone receptors in breast tissue cytosol in cancer]. / Povyshenie kachestva opredeleniia retseptorov éstrodiol i progesterona v tsitozole tkani molochnoi zhelezy pri rake.

Receptors of estrogens and progestins were studied in cytosol of human mammary gland cancer depending on concentration of total protein. In saturating concentrations of ligand content of these receptors might be distinctly dissimilar when concentration of total protein varied in cytosol, whereas Scatchard plot showed the same phenomena independently on concentration of total protein. Adequate and comparable result in estimation of estrogen and progestin receptors, which is of importance in treatment of mammary gland cancer, may be accomplished by calculation of total protein in cytosol within the limits 1 +/- 0.25 mg ml-1 under saturating concentrations of ligand or using the titrimetric procedure where concentration of total protein constituted 0.7-2.0 mg ml-1.

[Testosterone stimulation of the growth of a human osteogenic sarcoma strain transplanted into athymic rats]. / Stimuliatsiia testosteronom rosta shtamma osteogennoi sarkomy cheloveka, transplantirovannogo bestimusnym krysam.

Intraperitoneal testosterone administration stimulated the growth of subcutaneously transplanted cell line of human osteogenic sarcoma in nude rats but did not provoke tumour metastasizing to other organs and tissues. The specific connection of androgens with receptor proteins in the cytosol fraction was not found in the studied osteogenic sarcomas, whereas cytoplasmic estrogen receptors were revealed in all tumours. It is supposed that the mechanism of the stimulating effect of androgens on the tumour growth is mediated through other biologic systems being not related to androgen receptors.

[Statistical analysis of results in the determination of steroid hormone receptors]. / Statisticheskaia obrabotka rezul'tatov opredeleniia retseptorov steroidnykh gormonov.

Statistical evaluation of the data of steroid hormone receptors estimation involved the principle of dependence of each experimentally obtained magnitude of total binding (in presence of a single labelled ligand) on the magnitude of unspecific binding (at the similar content of labelled ligand but in addition of unlabelled substance excess). The principle enabled to calculate: individual values of specific binding as a difference between each value for total and unspecific binding independently on amount of parallel probes of total and unspecific bindings, mean value of specific binding using the calculated magnitudes, standard deviation (dispersion) and standard error of mean value. Statistical method allowed to determine differences between magnitudes of specific binding (content of receptors) at saturating concentrations of ligand as well as to estimate standard deviation of KD and Vmax in a plot. The statistical principles were used for estimation of specific binding of 3H-estra dil-17 beta, 3H-dihydrotestosterone and 3H-5 alpha-and-rostan-3 beta, 17 beta-diol in various rat tissues (hypophysis, prostate, uterus) and human tissues (mammary gland tissue tumor, prostate adenoma). The principle developed may be used for estimation of various receptors of biologically active substances, where the specific binding is calculated as a difference between total and unspecific binding.

[Action of 5 alpha-reduced diols on the uterus of sexually immature rats]. / Deistvie 5 al'fa-vosstanovlennykh diolov na matku nepolovozrelykh krys.

The effect of testosterone (T), 5 alpha-androstane-3 alpha, 17 beta-diol (3 alpha-diol) and 5 alpha-and-rostane-3 beta, 17 beta-diol (3 beta-diol) on the uterus of immature rats was studied in combined with estradiol-17 beta (E2) and separate intraperitoneal administration. Repeated administration of T (100 micrograms per 100 g of body mass) caused no changes in the uterine mass whereas a similar dose of 3 alpha-diol resulted in a noticeable effect (0.05 greater than greater than p less than 0.1). 3 beta-diol administered repeatedly at a dose of 1.00 microgram per 100 g of body mass, produced the same uterotropic effect like E2. In combined administration of the above androgens (100 micrograms) and E2 (10 micrograms) 3 alpha-diol only inhibited the uterotropic effect of E2.

[Effect of a new peptide morphogen on androgen metabolism in the gonads during sexual maturation in the rat]. / Vliianie novogo peptidnogo morfogena na metabolizm androgenov v gonadakh pri polovom sozrevanii krys.

After chronic administration of a new neuropeptide (hydra growth activator--HGA) to male and female Wistar rats from the 29th to 43rd day of life at a dose of 30 micrograms X kg-1 of body mass a study was made of [3H] testosterone, [3H] 5 alpha-dehydrotestosterone [( 3H] DHT) and [3H] 5 alpha-androstane-3 beta, 17 beta-diol metabolism in gonadal homogenates of the animals. In testis homogenates HGA administration was shown to influence the production of [3H] 3 beta-diol from [3H] DHT only. In female rats HGA administration made an effect on the majority of enzymes of androgen metabolism in the ovaries of animals with the closed and open vagina. Basing on changes in enzymatic activity of androgen metabolism in the gonads of rats in chronic HGA administration in the period of male pubescence a conclusion was made that it acted as a pubescence accelerating factor.

[Purification of radioactive sex hormones as receptor ligands]. / Ochistka radioaktivnykh polovykh steroidov kak ligandov retseptorov.

A system (mobile phase) containing benzene:acetone:absolute ethanol 9:1:0.5, respectively, is described for thin-layer chromatography on Silufol plates of ligand receptors of sex steroid hormones 3H-5 alpha-androstan-3 beta, 17 beta-diol, 3H-estradiol-17 beta, 3H-5 alpha-dihydrotestosterone, 3H-methyltrienolone (R 1881), 3H-OPG 2058 and 3H-progesterone. A purity of commercially available 3H-steroids was decreased in storage, therefore they should be purified before use. The system described enabled to produce the 3H-steroids studied of high purity.

[Effect of testosterone, its 5 alpha-reduced metabolites, estradiol and progesterone on the formation of an experimental duodenal ulcer in male rats]. / Vliianie testosterona, ego 5 al'fa-vosstanovlennykh metabolitov, éstradiola i progesterona na obrazovanie éksperimental'noi duodenal'noi iazvy u krys-samtsov.

The influence of different doses (0.01, 0.1, 1.0, 10.0, 100.0, 250.0, 1,000.0, 2,500.0 gamma/kg body weight) of testosterone, dihydrotestosterone, 5 alpha-androstane-3 alpha, 17 beta-diol, 5 alpha-androstane-3 beta, 17 beta-diall, 4-androsterone-3,17-dione, estradiol and progesterone on the formation of cysteamine-induced duodenal ulcer was studied in mature male rats. It has been shown that all the steroids, but for progesterone, bring down the ulcer index after six days of i/p administration, the effect depending on the nature and dose of a steroid. Estradiol and 4-androstene-3,17-dione proved to be the most effective in the given dose range. The results do not only confirm the role of androgens and estradiol in the pathogenesis of duodenal ulcer, but also indicate the participation of their precursors and metabolites in the ulcer induction. The prospects of using steroids in the treatment of ulcer are discussed.

[3H-estradiol-17 beta in laboratory diagnosis]. / 3H-éstradiol-17 beta v laboratornoi diagnostike.

USSR made [3H]estradiol-17 beta was shown to be no inferior in quality to [3H]estradiol-17 beta produced by Amersham Int., Gr. Britain, for the determination of estrogen protein receptors in target tissues and for radioimmunoassay methods.

[Use of protamine sulfate in a method for determining the hormonal sensitivity of breast cancer]. / Ispol'zovanie sul'fata protamina v metodike opredeleniia gormonal'noi chuvstvitel'nosti raka molochnoi zhelezy.

A new procedure for estrogen receptor assay in breast cancer tissue is discussed. According to the method cytosol receptor level is interpreted as the estradiol binding capacity of protein which is precipitated by protamine sulfate from the cytosol fraction of tumor.