5α-Reductase Inhibitory and Antiandrogenic Activities of Novel Steroids in Hamster Seminal Vesicles
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概要
- 論文の詳細を見る
The pharmacological activity of several 16-bromosubstituted trienediones 4 and 5, 16-methyl substituted di-enediones 6 and 7 and the 16-methyl substituted trienedione 8 was determined on gonadectomized hamster seminal vesicles by measuring the in vitro conversion of testosterone (T) to dihydrotestosterone (DHT) as 5α-reductase inhibitors and also the ability of these steroids to bind to the androgen receptor. Steroids 6 and 7 when injected together with T decreased the weight of the seminal vesicles thus showing an antiandrogenic effect. Compounds 5 and 6 reduced substantially the conversion of T to DHT and therefore can be considered good inhibitors for the enzyme 5α-reductase; however both steroids failed to form a complex with the androgen receptor. On the other hand compound 7 which showed a very small inhibitory activity for the enzyme 5α-reductase, exhibited a very high affinity for the androgen receptor and thus can be considered an effective antiandrogen. This compound also reduced substantially the weight of the seminal vesicles. Steroids 4 and 8 did not reduce the weight of the seminal vesicles and exhibited a low affinity for the androgen receptor; 8 showed a weak 5α-reductase inhibitory activity, whereas 4 exhibited a weak androgenic effect.
- 公益社団法人日本薬学会の論文
- 2002-11-01
著者
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Montes Diana
Department Of Pharmacy Faculty Of Chemistry Unam Ciudad Universitaria
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Ramirez Elena
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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BRATOEFF Eugene
Departamento de Farmacia, Facultad de Quimica, UNAM, Ciudad Universitaria
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CABEZA Marisa
Departamento de Farmacia, Facultad de Quimica, UNAM, Ciudad Universitaria
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Quiroz Alexandra
Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco
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Flores Eugenio
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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Bratoeff Eugene
Department Of Pharmacy Faculty Of Chemistry National University Of Mexico City
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Cabeza M
Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco
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Cabeza Marisa
Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria
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HEUZE Ivonne
Departments of Biological Systems and Animal Production, Metropolitan University-Xochimilco
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CALLEROS Jorge
Department of Pharmacy, Faculty of Chemistry, UNAM, Ciudad Universitaria
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Heuze Ivonne
Departments Of Biological Systems And Animal Production Metropolitan University-xochimilco
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Ramirez Elena
Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria
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Calleros Jorge
Department Of Pharmacy Faculty Of Chemistry Unam Ciudad Universitaria
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Bratoeff Eugene
Departamento De Farmacia Facultad De Quimica Unam Ciudad Universitaria
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