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Query: UMLS:C0338671 (Steroids)
 9,479 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The ability to form androgen conjugates and the hormone dependency of the conjugating enzymes have been studied in the rat epididymis. Following the in vitro incubation of 3H-testosterone with epididymal slices from intact and castrated rats, the radioactivity recovered was partitioned between water and ether. Examination of the water soluble radioactivity demonstrated the presence of glucuronides and sulfates. The total radioactivity in the conjugate fraction was the same for both intact and castrated animals. However, castrated rats showed a 3-fold increase in the glucuronide fraction with a corresponding decrease in the formation of sulfates. Characterization of the ether soluble radioactivity after solvolysis of the conjugate fraction from castrated animals, showed DHT (17beta-hydroxy-5alpha-androstan-3-one) and 3alpha-diol (5alpha-andro-stane-3alpha, 17beta-diol) to be the main metabolites. After beta-glucuronidase hydrolysis of the same, only 3alpha-diol could be demonstrated at a significant level, although traces of DHT and delta16 compounds were present. Corresponding hydrolysis of the water phase from incubation of epididymis from intact rats, demonstrated a marked quantitative difference. Here approximately 40% of the conjugated aglycones consisted of delta16 compounds, whilst only about 12% was comprised of 3alpha-diol. The preferential conjugation of DHT and 3alpha-diol to a sulfate radical was demonstrated in both intact and castrated rats. Since the conjugated delta16 compounds were detected only in the epididymis from intact animals, it is possible that these are formed by the spermatozoa.
Steroids 1976 May
PMID:Androgen metabolism by rat epididymis. 4. The formation of conjugates. 94 Nov 82

The inhibition of testosterone 5alpha-reductase activity by 3-oxo-4-androstene-17beta-carboxylic acid in the male reproductive organs of the rat was demonstrated in vitro. The medium for incubation of caput epididymis showed the highest concentration of 5alpha-dihydrotestosterone (5alpha-DHT) whereas the highest concentration of testosterone (T) was recorded in medium for incubation of decapsulated testis after two hours of incubation. The 3-oxo-4-androstene-17beta-carboxylic acid (1.58 X 10(-5)M) inhibited the conversion of T to 5alpha-DHT in all the organs tested (testis, caput and cauda epididymis and ventral prostate) under identical incubation conditions.
Steroids 1976 Jun
PMID:The inhibition of the conversion of testosterone into 5alpha-dihydrotestosterone in the reproductive organs of the male rat. 94 Nov 90

The metabolism of testosterone (T) in neonatal rat brains was measured following in vivo and in vitro incubations with 3H-testosterone.Steroids associated with nuclear and cytoplasmic fractions of brain tissue from 4, 12, and 32-day-old male and female rats were identified. Although there are quantitative differences under different methods of incubation, in all cases more than 95% of the radioactivity was recovered and identified as T, or the 5alpha-reduced metabolities, DHT and 3alpha-androstanediol. Most of the metabolism of T occurred in the cytoplasm but 5alpha-reduced metabolities were also associated with purified nuclei. Reaction kinetics indicate that the metabolic sequence is T leads to DHT leads to 3alpha DIOL. DHT levels were similar in the cytoplasmic fractions from the neonates (4 and 12-day-old animals) and prepubertal animals (32-day-old animals), but 3alpha-androstanediol was significantly reduced in these fractions from prepubertal animals compared to those from neonates. Sex differences in the metabolism of T in the various subcellular fractions were not detectable.
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PMID:Cytoplasmic and nuclear metabolism of testosterone in the brains of neonatal and prepubertal rats. 96 4

The metabolism of 3H-testosterone by the epididymis and accessory organs of adult male rats exposed continuously to microdoses of cyproterone acetate from subcutaneous capsules were studied. The major metabolite of 3H-testosterone in the epididymis, vas deferens and ventral prostate of control rat was dihydrotestosterone while the formation of androstanediol by these tissues was low. The highest percentage of DHT was formed by the ventral prostate and cauda epididymis. In rats exposed to cyproterone acetate for four months, the conversion of testosterone to DHT was inhibited in all the tissues but maximally in the ventral prostate and cauda epididymis. In these rats, the secretory function of the ventral prostate was normal while that of the epididymis was markedly decreased. These data are discussed based on the differential thresholds of androgens required to regulate the functions of the accessory organs.
Steroids 1976 Aug
PMID:Metabolism of testosterone by the epididymis and ventral prostate of rat and its inhibition by cyproterone acetate. 97 32

Skeletal muscle homogenate of prepuberal, adult uncastrated or short-(1-4days) or long-term (20days) castrated male and female rats was incubated at 0degreesC iwth highly labeled (3H)5alpha-dihydrotestosterone (1) or (3H) testosterone. labeled (3H)5alpha-dihydrotestosterone (1) or 3H) testosterone. After incubation bound and free hormone in the 100,000 g cytosol were separated by agargel electrophoresis at low temperature. Furthermore, the percentage distribution of the main metabolites found in the cytosol was analyzed by thin-layer chromatography. Two androgen binding proteins could be found: One with high affinity (apparent dissociation and constant (Kd)= 1.4 - 6.4X10(-9)M) low capacity (receptor), the other with relative low affinity high capacity. The physico-chemical characteristics of the androgen receptor in the rat skeletal muscle cytosol are similar if not identical to those which have been described for the androgen receptor in the prostate and other androgen dependent organs. However, the amount of available 5alpha-DHT-binding sites in the skeletal muscle is about 60 times and 7 times lower than in the prostate and bulbocavernosus/levator ani muscle, respectively. No essential androgen metabolism occurs in vitro at 0degreesC in the skeletal muscle.
Steroids 1976 Aug
PMID:Characterization of the androgen receptor in the skeletal muscle of the rat. 97 39

The pattern of androgenic metabolites in blood, muscle, caput and cauda epididymidis has been investigated in functionally hepatectomized 24 hours castrated rats, 3 hours after the intra-muscular injection of 200 muCi of 3H-3H-3alpha-diol. Identification of the radioactive metabolites showed only negligible differences between the epididymal regions. In both caput and cauda the main metabolite was DHT (17beta-hydroxy-5alpha-androstane-3-one); 3alpha- and 3beta-diol, androsterone (3alpha-hydroxy-5alpha-androstane-17-one), 5-A-dione (5alpha-androsterone-3, 17-dione), delta16-3alpha-01 (kalpha-androst-16-en-3alpha-01), delta16-3beta-01 (5alpha-androst-16-en-3alpha-01) and delta16-3-one (5alpha-androst-16-en-3-one) were also present. Androsterone and 3alpha-diol were the predominant metabolites in blood and muscle. No delta16 compounds could be detected and in constrast to epididymis, more than 50% of the radioactivity was associated with polar compounds. From determination of total radioactivity, it was seen that retention by epididymis varied from two to four times that of muscle. Purification and identification of the radioactivity associated with the nuclear fraction demonstrated that DHT was the only nuclear bound androgen. It is suggested from these results that at least one effect of 3alpha-diol on the rat epididymis is exerted through its conversion to DHT.
Steroids 1976 Nov
PMID:Androgen metabolism by rat epididymis. 5. Metabolic conversion and nuclear binding after injection of 5alpha-androstane-3alpha, 17beta-diol, in vivo. 101 38

The in vivo and in vitro metabolism of 3H-testosterone by rat epididymis and the changes in epididymal weight have been studied after castration and treatment with anti-androgens. The utilization of 3H-testosterone was greatly reduced after castration as was the formation of 5alpha-reduced 17 beta-hydroxy metabolites. The formation of the 17 -keto metabolites was unaffected. Castration had no effect on the ratio between water and ether soluble radioactivity. Administration of testosterone propionate, necessary for giving normal stimulated prostate weight (150 mug/day), restored the metabolism of testosterone to approximately normal values. Estradiol benzoate and progesterone inhibited metabolism of testosterone in vitro and greatly reduced the formation of DHT (17 beta-hydroxy-5alpha-androstan-3-one) and 3 alpha-diol(5 alpha-androstane-3 alpha-17 beta-diol) by experiments both in vivo and in vitro. No effect of cyproterone acetate could be demonstrated on either the in vitro or in vivo metabolism of testosterone. Castration for 14 days reduced the epididymal weight to about 30% of that found in intact animals. Administration of testosterone propionate restored the epididymal weight to about 80% of normal. Estradiol benzoate and cyproterone acetate given to intact rats led to a decrease in the epididymal weight. Progesterone had no such effect. In 14 days castrated rats receiving testosterone propionate all three anti-androgens reduced the weight of the epididymis. In conclusion, our results show that the metabolic conversion of testosterone in epididymis to DHT and 3 alpha-diol is dramatically dependent on the hormonal status of the animal; castration or treatment with anti-androgens causes a reduced formation of the "active" androgens whilst testosterone replacement treatment restores the metabolism of testosterone to normal.
Steroids 1976 Jan
PMID:Androgen metabolism by rat epididymis. 3. Effect of castration and anti-androgens. 126 92

Based on histological criteria, Kingsley and Bogdanove (3) reported that the benzoate ester of 17beta-hydroxy-5alpha-androstan-3-one (5alpha-DHT), unlike testosterone propionate, is unable to induce vaginal mucification when given subcutaneously to rats. In contrats, Kennedy (4) found in estrogen-pretreated rats that both 5alpha-DHT and testosterone induced vaginal mucification as indicated by increased vaginal sialic acid concentration. To determine if esterification of these androgens altered their ability to induce vaginal mucification, ovariectomized rats, pretreated for 3 days with 0.25 mug estradiol-17beta, were treated for 8 days with either sesame oil or 7 mumoles of testosterone, 5alpha-DHT and their respective propionate and benzoate esters. All treatments except 5-alpha-DHT benzoate increased vaginal weight and vaginal mucification, as assessed histochemically and biochemically. 5alpha-DHT propionate was less effective than 5alpha-DHT while testosterone benzoate, but not propionate was less effective than testosterone. To determine if estrogens are necessary for the vaginal effects of androgens, ovariectomized and ovariectomized-adrenalectomized rats were treated with testosterone or 5alpha-DHT. Adrenalectomy did not significantly affect the vaginal response to either androgen. It is therefore concluded that androgens are capable of inducing vaginal mucification in the absence of estrogens.
Steroids 1976 Mar
PMID:Induction of vaginal mucification in rats with testosterone and 17beta-hydroxy-5alpha-androstan-3-one. 126

Prodynorphin is expressed by neurons of the hypothalamus and gonadotrophs of the anterior pituitary gland (AP) and plays a role in the negative feedback regulation of the reproductive neuroendocrine axis. The present study examined whether gonadal steroid hormones are capable of modulating pituitary prodynorphin expression in immature, female rats. Steroids were administered via subcutaneous Silastic implants and rats were killed at 29 days of age. Northern blot analysis was used to measure AP prodynorphin, luteinizing hormone-beta (LH beta), follicle-stimulating hormone-beta (FSH beta), and common alpha-subunit mRNA levels (normalized to 18S ribosomal RNA). Treatment groups (n = 5-6) consisted of control (CNT; empty implants), estradiol (E2; 4 days), E2 + progesterone (E2 + P4; 8 days and 4 days, respectively), and dihydrotestosterone (DHT; 4 days). Pituitary prodynorphin mRNA was significantly suppressed in only the DHT-treated animals (26 +/- 10% of CNT, p < 0.01). LH beta mRNA was suppressed by all steroid treatments (p < 0.01), FSH beta was lower in only the E2 group, and alpha-subunit was reduced in both the E2 + P4 and DHT groups (p < 0.01). Serum LH was suppressed by all steroid treatments but FSH was reduced in only the E2 and E2 + P4 groups (p < 0.01). Treatment of prepubescent rats with continuous high levels of gonadal steroids is known to severely reduce endogenous hypothalamic gonadotropin releasing hormone (GnRH) release and this is supported by our observation of reduced gonadotropin-subunit gene expression.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Differential regulation of anterior pituitary prodynorphin and gonadotropin-subunit gene expression by steroid hormones. 145 42

All the classes of hormonal steroids physiologically produced in the body (androgens, estrogens, progestagens, and corticosteroids) are able to exert important effects on the brain, but the mechanisms of their actions are not always well understood. Steroids may interact with intracellular receptors to activate the genome, but some of their effects are probably extragenomic and involve interactions with cellular membranes. Moreover, not all the steroids act always in their native molecular form; a large group of them must actually be transformed into "active" metabolites. This may occur at the level of their respective target structures. For example, androgens are metabolized in the brain into estrogens and into 5 alpha-reduced androgens, like 5 alpha-androstan-17 beta-ol-3-one (dihydrotestosterone; DHT) and 5 alpha-androstan-3 alpha, 17 beta-diol (3 alpha-diol). Progesterone, and possibly corticosteroids, may also be transformed into their corresponding 5 alpha-reduced metabolites. Also the cellular target (neurons and/or glial cells) of the hormonal steroids in the brain is not always clear. This review analyzes in detail one of the two major enzymatic systems that transform steroids in the brain, namely the 5 alpha-reductase-3 alpha-(3 beta)-hydroxysteroid dehydrogenase pathway. An active 5 alpha-reductase-3 alpha-hydroxysteroid dehydrogenase system is widely distributed in practically all CNS structures in all phases of development. In the brain, this enzymatic system is not regulated by castration or sex steroid administration; furthermore, neural inputs seem to be ineffective at the hypothalamic level. A recent interesting finding is the presence of high concentrations of the 5 alpha-reductase in the white matter. This probably is due to the fact that the white matter is particularly rich in myelin membranes, with which the enzymatic activity appears to be associated. An active 5 alpha-reductase activity has also been shown to be present in peripheral myelinated nerves. The localization in myelin membranes may suggest a possible involvement of 5 alpha-reduced metabolites of the different steroids in the process of myelination. The presence of the 5 alpha-reductase was analyzed in neurons, astrocytes, and oligodendrocytes isolated from the brains of male rats, as well as in neurons and glial cells grown in culture. Neurons appear to be more active than glial cells in converting testosterone into DHT. Only neurons possess aromatase activity.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:The 5 alpha-reductase in the brain: molecular aspects and relation to brain function. 146 1


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