Gene/Protein
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Symptom
Drug
Enzyme
Compound
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Target Concepts:
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Query: EC:3.2.1.31 (
beta-glucuronidase
)
7,680
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Castration provokes a time-related decrease in weight, protein,
beta-glucuronidase
and glucose-6-phosphate dehydrogenase activity of seminal vesicles. A dose-dependent stimulation of these parameters is obtained with 5alpha-
DHT
. Cryproterone acetate counteracts the stimulatory effects due to androgen. Acid and alkaline phosphatases remain largely unaffected by these treatments.
...
PMID:A study of the enzyme activity in the seminal vesicles of castrated and hormone-replaced castrated mice. 44 40
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.
...
PMID:Androgen metabolism by rat epididymis. 4. The formation of conjugates. 94 Nov 82
The effect of oxytetracycline (1 g/day for five days) on the enterohepatic recycling of oestrogens and on plasma sex hormone concentrations was assessed in healthy men. Plasma oestrone (E1), oestradiol-17 beta (E2), 4-androstenedione (A), 5 alpha-dihydrotestosterone (5 alpha-
DHT
), total and free testosterone (T and free T), binding capacity of sex hormone binding globulin, luteinizing hormone, dehydroepiandrosterone-sulphate, urinary total E1, E2, and oestriol (E3), and oestriol-3-glucuronide (E3-3G) and faecal unconjugated and conjugated E1, E2, and E3 were measured by radioimmunoassay (RIA). Treatment with the antibiotic significantly increased the excretion of faecal conjugated oestrogens, which parallelled a decrease in urinary oestrogen excretion, especially of E3. The effect on urinary E3 could be explained almost entirely by the simultaneous decrease of urinary E3-3G concentrations. In urine and faeces the E2/E3 and E1 + E2/E3 ratios increased, probably because of the diminished reductive metabolism of oestrogens in the gut. No significant effects on plasma unconjugated oestrogen concentrations were observed. Moreover, in the present study oxytetracycline had no remarkable effect on plasma total, or free T concentrations, nor on other plasma hormones measured. Our results suggest that enterohepatic recycling and intestinal metabolism of oestrogens may be significant in men. The mechanism of action of antibiotics on oestrogen metabolism probably involves decreased hydrolysis by
beta-glucuronidase
of oestrogen conjugates by the intestinal contents, diminishing the reabsorption of aglycones of oestrogen conjugates and resulting in faecal loss of the steroids.
...
PMID:Effect of oxytetracycline administration on intestinal metabolism of oestrogens and on plasma sex hormones in healthy men. 303 44
Daily s.c. injections of cyproterone acetate cause a time-related decrease in the weight and
beta-glucuronidase
activity of seminal vesicles in mouse. Protein content shows an initial increase and subsequently, after 120-180 days of treatment, a decline (reaching control levels). Acid phosphatase activity also decreases but only after long-term treatments. 5 alpha-
DHT
tends to bring the values of various parameters towards the control range. However, its effects are of a lesser magnitude in animals treated for 90 days with the antiandrogen. It is proposed that the antifertility action of cyproterone acetate is due mainly to its negative influence not only on the epididymis but also on seminal vesicles.
...
PMID:Effects of prolonged treatment with cyproterone acetate on hydrolytic enzymes in seminal vesicles of the mouse. 645 Nov 91
Biologically active androgens and peripheral androgen metabolites in plasma were measured in 25 women with idiopathic hirsutism (IH). Plasma testosterone was not significantly elevated. Free testosterone however was increased although the elevation was not impressive (10.9 +/- 6.6 SD vs. 3.3 +/- 1.5 ng/dl) and one-fourth of the cases had normal unbound testosterone.
Dihydrotestosterone
(
DHT
) values were elevated (23.5 +/- 14 vs. 12.5 +/- 3.59) but again over half of the values were within the normal range. In our series of mild to moderate cases, 3 alpha-diol was not at all discriminatory. However, plasma 3 alpha-diol glucuronide was markedly increased (604 +/- 376 vs. 40 +/- 10 ng/dl), and elevated in all but one mild case. Previous studies document that
DHT
is the important androgen in skin and formation of
DHT
and 3 alpha-diol is markedly increased in vitro in IH. Since 3 alpha-diol glucuronide is derived largely from extrasplanchnic events,
beta-glucuronidase
is present in skin, and androgen stimulates formation of the enzyme in extrasplanchnic tissue, we conclude that 3 alpha-diol glucuronide is a marker of peripheral androgen action and markedly elevated in IH.
...
PMID:3 alpha, 17 beta-androstanediol glucuronide in plasma. A marker of androgen action in idiopathic hirsutism. 706 55
Dihydrotestosterone
(
DHT
), a biologically active metabolite of testosterone, may be misused in sports to benefit from its anabolic and psychotropic effects. After
DHT
application, a significant increase of the glucuronides of
DHT
and its metabolites can be expected for a certain time period depending upon dose, formulation, route of administration, and in case of percutaneous administration the chainlength of the ester.
DHT
and its metabolites can be monitored by gas-chromatography/mass spectrometry (GC/MS) after enzymatic hydrolysis and trimethylsilylation. To investigate the extent of the alteration of the urinary steroid profile after
DHT
application, timely controlled experiments have been performed with: a) oral application of [16,16,17-2H3]-
DHT
, and b) sublingual application of a 25 mg dose of
DHT
. In the experiment with [16,16,17-2H3]-
DHT
within 24 hours about 44% of the applied dose was recovered after hydrolysis with
beta-glucuronidase
from E. coli as di- or tri-deuterated 5 alpha-androstane glucuronides: androsterone (33.2%), 5 alpha-androsta-ne-3 alpha,17 beta-diol (2.5%), 5 alpha-androstane-3 beta, 17 beta-diol (0.9%),
DHT
(7.2%). Hydrolysis with
beta-glucuronidase
/arylsulfatase from Helix Pomatia resulted in a about 10% higher yield except for
DHT
. In the study with sublingual application of 25 mg of
DHT
the extent of the recovery of
DHT
and its metabolites was in the same range as for the deuterated
DHT
. The urinary glucuronide concentrations of
DHT
, androsterone (AND), 5 alpha-androstane-3 alpha, 17 beta-diol (5 alpha A3 alpha D) and 5 alpha-androstane-3 beta,17 beta-diol (5 alpha A3 beta D) and their ratios to etiocholanolone (ETIO), 5 beta-androstane-3 alpha, 17 beta-diol (5 beta A3 alpha D) and epitestosterone (EPIT) were increased for up to 48 hours after application. For doping control purposes concentrations of
DHT
, 5 alpha A3 alpha D, 5 alpha A3 beta D and ratios of 5 alpha-metabolites to non 5 alpha-metabolites such as
DHT
/ETIO,
DHT
/EPIT, 5 alpha A3 alpha D/5 beta A3 alpha D, 5 alpha A3 beta D/5 beta A3 alpha D, and AND/ETIO outside the reference ranges are a proof for
DHT
application. Reference ranges for Asian and Caucasian male and female athletes are calculated from data bases of the Asian Games 1994, the previous Asian Games 1990 and the routine doping control samples of Caucasian athletes measured in Cologne 1994. At the occasion of the 1994 Asian Games in Hiroshima alterations in the concentrations and ratios of the
DHT
depending parameters for outside there reference ranges have been found and have been sanctioned on this basis by the Medical Commission of the Organisation of Olympic Council of Asia (OCA).
...
PMID:Detection of dihydrotestosterone (DHT) doping: alterations in the steroid profile and reference ranges for DHT and its 5 alpha-metabolites. 877 70
Dihydrotestosterone
(
DHT
) binding studies and the effects of
DHT
on the expression of
beta-glucuronidase
(Gus) and kidney androgen-regulated protein (KAP) genes and cell growth were investigated in immortalized early PKSV-PCT and late PKSV-PR proximal tubule cells, derived from transgenic mice carrying the L-pyruvate kinase/SV40 hybrid gene. [3H]
DHT
binding studies indicated that both cell lines have conserved substantial amounts of androgen receptors. The levels of KAP and Gus transcripts in PKSV-PCT cells, and those of KAP transcripts in PKSV-PR cells, decreased when cells were shifted from a serum-supplemented to a steroid-free medium. The addition of 30 nM
DHT
to the steroid-free medium resulted in a slight increase in Gus and in a more marked increase in KAP transcripts in both cell lines.
Dihydrotestosterone
also affected the growth of PKSV-PCT and PKSV-PR cells, since this hormone added to the steroid-free medium stimulated the incorporation of [3H]thymidine in a dose-dependent manner and induced the formation of domes, which represent indicators of ionic transport processes. Thus, because these early and late mouse proximal tubule cells have conserved androgen receptors, they represent attractive cell systems to analyze the action of androgens on specific functions of the mouse proximal tubule.
...
PMID:Pleiotropic effects of dihydrotestosterone in immortalized mouse proximal tubule cells. Technical note. 945