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Abstract:

The mechanism of the antiandrogenic effect of 5,10-seco-19-norpregnane-4,5-diene-3,10,20-trione (secosteroid), reputedly an irreversible inhibitor of 5α -reductase, was investigated. Its addition (10 μM) to culture media effectively suppressed the synthesis of rat epididymal proteins specifically induced by 0.1 μM testosterone (T) or dihydrotestosterone (DHT). Under the same conditions, secosteroid did not change the rate at which labeled T was metabolized to 5α -reduced compounds. In a comparative study, secosteroid inhibited 5α -reductase in an isolated microsomal fraction while not affecting the enzyme activity in minced tissue. Secosteroid was shown to be a competitor of the binding of [3H]T and [3H]DHT (both at 4nM) to the epididymal cytosol androgen receptor, with ID50 of 1 μM for the former and 4μM for the latter, thus explaining the mechanism involved in its antiandrogenic properties. © 1987.

Registro:

Documento: Artículo
Título:Studies on the mechanism of the antiandrogenic effect of a putative 5α -reductase inhibitor
Autor:Vazquez, M.H.; Tezon, J.G.; Blaquier, J.A.
Filiación:Instituto de Biologia y Medicina Experimental, Obligado 2490, Buenos Aires, 1428, Argentina
Palabras clave:antiandrogen; enzyme inhibitor; steroid 5alpha reductase; animal cell; biological model; cell culture; endocrine system; epididymis; in vitro study; male genital system; nonhuman; rat; Androgen Antagonists; Animal; Binding, Competitive; Cytosol; Depression, Chemical; Epididymis; Gene Expression Regulation; Male; Microsomes; Norpregnadienes; Proteins; Rats; Rats, Inbred Strains; Receptors, Androgen; Stanolone; Support, Non-U.S. Gov't; Testosterone; Testosterone 5-alpha-Reductase
Año:1987
Volumen:28
Número:2
Página de inicio:227
Página de fin:231
DOI: http://dx.doi.org/10.1016/0022-4731(87)90381-5
Título revista:Journal of Steroid Biochemistry
Título revista abreviado:J. Steroid Biochem.
ISSN:00224731
CODEN:JSTBB
CAS:(4R)-5,10-seco-19-norpregna-4,5-diene-3,10,20-trione, 60398-19-8; Androgen Antagonists; Norpregnadienes; Proteins; Receptors, Androgen; Stanolone, 521-18-6; Testosterone 5-alpha-Reductase, EC 1.3.99.5; Testosterone, 57-85-2
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00224731_v28_n2_p227_Vazquez

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Citas:

---------- APA ----------
Vazquez, M.H., Tezon, J.G. & Blaquier, J.A. (1987) . Studies on the mechanism of the antiandrogenic effect of a putative 5α -reductase inhibitor. Journal of Steroid Biochemistry, 28(2), 227-231.
http://dx.doi.org/10.1016/0022-4731(87)90381-5
---------- CHICAGO ----------
Vazquez, M.H., Tezon, J.G., Blaquier, J.A. "Studies on the mechanism of the antiandrogenic effect of a putative 5α -reductase inhibitor" . Journal of Steroid Biochemistry 28, no. 2 (1987) : 227-231.
http://dx.doi.org/10.1016/0022-4731(87)90381-5
---------- MLA ----------
Vazquez, M.H., Tezon, J.G., Blaquier, J.A. "Studies on the mechanism of the antiandrogenic effect of a putative 5α -reductase inhibitor" . Journal of Steroid Biochemistry, vol. 28, no. 2, 1987, pp. 227-231.
http://dx.doi.org/10.1016/0022-4731(87)90381-5
---------- VANCOUVER ----------
Vazquez, M.H., Tezon, J.G., Blaquier, J.A. Studies on the mechanism of the antiandrogenic effect of a putative 5α -reductase inhibitor. J. Steroid Biochem. 1987;28(2):227-231.
http://dx.doi.org/10.1016/0022-4731(87)90381-5