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Effects of training and methandrostenolone (an anabolic steroid) on energy metabolism in the guinea pig: changes in enzyme activities in gastrocnemius muscle and myocardium.

Modifications of enzyme activities (creatine kinase and its B subunit; adenylate kinase; hexokinase; phosphofructokinase; lactate dehydrogenase; malate dehydrogenase, isocitrate dehydrogenase; citrate synthase; acetylcarnitine transferase; beta-hydroxyacetyl-CoA dehydrogenase; cytochrome c oxidase) in gastrocnemius muscle and myocardium were reported after two forms of training with or without administration of anabolic steroid. Endurance training was on a horizontal motor-driven treadmill, 2 km X hr-1, 5 days a week for 0.5 hr per day for 5 weeks. In the case of power endurance training there was a slope of 45 degrees. Enzyme activities in controls and treated guinea pigs, as well as treatment-induced enzyme activity changes are time dependent. Some of these activities correlate linearly with one another; such correlations characterize the effect of adaptation. Endurance training and power endurance training in this study induce similar modifications and seem to differ essentially in the daily work load. The anabolic steroid methandrostenolone (dianabol) induces modifications which training does not bring about but which training at least partially eliminates.

Animals↗

Metabolism of methandrostenolone in the horse: a gas chromatographic-mass spectrometric investigation of phase I and phase II metabolism.

The phase I and phase II metabolism of the anabolic steroid methandrostenolone was investigated following oral administration to a standardbred gelding. In the phase I study, metabolites were isolated from the urine by solid-phase extraction, deconjugated by acid catalysed methanolysis and converted to their O-methyloxime trimethylsilyl derivatives. GC-MS analysis indicated the major metabolic processes to be sequential reduction of the A-ring and hydroxylation at C6 and C16. In the phase II study, unconjugated, beta-glucuronidated and sulfated metabolites were fractionated and deconjugated using a combination of liquid-liquid extraction, enzyme hydrolysis, solid-phase extraction and acid catalysed methanolysis. Derivatization followed by GC-MS analysis revealed extensive conjugation to both glucuronic and sulfuric acids, with only a small proportion of metabolites occurring in unconjugated form.

Administration, Oral↗

The effects of large doses of the anabolic steroid, methandrostenolone, on an athlete.

Doses of the anabolic steroid, methandrostenolone, nearly ten times greater than those used therapeutically, have resulted in a marked depression of levels of testosterone in urine and blood, and in some depression of gonadotrophin excretion by a male athlete. The administration of the drug has been checked and its metabolism studied from the pattern of urinary metabolites.

Adult↗

Effects of 5 alpha-dihydrotestosterone and methandrostenolone in male guinea pigs.

Young adult guinea pigs were studied 6 and 9 weeks after silastic capsules containing 5 alpha-hydrotestosterone (5 alpha-DHT) and methandrostenolone (Dianabol) were implanted. DHT was more effective in causing testicular atrophy and was apparently more androgenically potent in sustaining the size of the seminal vesicles. Both steroids led to hypertrophy of the masseter muscle and increase in gastrocnemius protein concentration. Cardiac tissue was sensitive to the effects of these steroids, particularly to the larger amounts of absorbed Dianabol, in terms of increases in DNA concentration and transient loss of tissue sodium, potassium, and calcium. All alterations in muscle composition occurred in the total absence of change in tissue water. Hypernatremia and hyperkalemia was present in steroid-treated animals with significant loss of urinary potassium in DHT-treated guinea pigs. Adrenal atrophy and the lowering of circulating cortisol was further indicative of effects upon adrenocortical function and the regulation of electrolyte balance.

Adrenal Glands↗

Effect of methandrostenolone on serum triglyceride and cholesterol levels in diabetic patients.

Eighteen adult diabetic patients were treated with methandrostenolone in daily doses of 15 mg for 3 weeks. Serum triglyceride and cholesterol levels and lipoprotein lipase activity were determined before and after treatment. In patients with intense hypertriglyceridaemia, triglyceride concentration decreased and, with the exception of a single patient, lipoprotein lipase activity returned to normal. Cholesterol concentration did not change characteristically.

Blood Glucose↗

[The action of methandrostenolone and ecdysterone on the physical endurance of animals and on protein metabolism in the skeletal muscles].

The results of the comparative study on the myotropic activity of methandrostenolone and ecdysterone and their effects on physical endurance of animals suggested that ecdysterone possessing a wider spectrum of the anabolic action on the contractile proteins of the skeletal muscles exerts a more pronounced influence on physical endurance of animals without their preliminary training.

Animals↗

[Radiomodifying effect of methandrostenolone on laryngeal cancer cells].

The property of methandrostenolone, a synthetic male hormone, as a stimulator of proliferative activity of tumour cells was studied in experimental analyses, conducted on the transplanted culture of HEP-2 cells and on xenografts of the human larynx cancer cultured in diffusive chambers. This property of the hormone was used to increase the sensitivity of human laryngeal tumour, to ionizing emission. The morphological study of histological specimens prepared from xenografts and histological specimens of patients with laryngeal tumour, who received preoperative distant gamma-therapy against a background of the methadrostenolone use, gave the results which allow recommending this hormone to be used during radiotherapy of patients with the laryngeal cancer.

Adult↗

The effect of methandrostenolone on nitrogen excretion following open-heart surgery.

An attempt was made to assess the effect of an anabolic hormone in the postoperative phase. Methandrostenolone (Danabol) was given to groups of adults and children undergoing open-heart surgery, and the results were compared with those obtained in control groups. No difference in the clinical picture could be found between the treated and the untreated groups, or in the total amount of nitrogen excreted during six days following the operation. In both treated groups the urinary volume was increased, resulting in a decreased urinary nitrogen concentration.

Adult↗

[Heterologous expression of functionally active human cytochrome P-450s. Cytochrome P-450IIIA4 catalyzes the biotransformation of the anabolic steroid hormone methandrostenolone].

The expression of the cytochrome P450IIIA4 gene in the Saccharomyces cerevisiae yeast using the shuttle vector pYeDP1-8/2 has been carried out. The microsomal fraction isolated from the transformed yeast cells was used for biotransformation of the anabolic steroid hormone-methandrostenolone (MA). The microsomal oxidation products were analyzed by HPLC and two-dimensional TLC. It was shown that microsomes of the yeasts expressing human cytochrome P450IIIA4 catalyze the MA conversion into its 6 beta-hydroxy derivative. An identical product is formed via a reaction catalyzed by human liver microsomes. The use of the heterological system of cytochrome P450IIIA4 expression has made it possible to establish its role in MA metabolism. The experimental system simulates the first phase of the drug biotransformation in liver cells.

Biotransformation↗