Kniewald J, Osredecki V, Gojmerac T, Zechner V, Kniewald Z
Faculty of Food Technology and Biotechnology, University of Zagreb, Croatia.
J Appl Toxicol. 1995 May-Jun;15(3):215-8. doi: 10.1002/jat.2550150312.
The influence of s-triazine compounds (atrazine, prometryne and deethylatrazine) on testosterone conversion and 5 alpha-dihydrotestosterone-receptor complex formation was studied in vitro and in vivo in the rat prostate. A marked in vitro influence of atrazine and prometryne (from 0.465 to 1.392 mumol) and their mixtures (in total concentration, 0.928 mumol) on 5 alpha-dihydrotestosterone formation was detected. 5 alpha-Dihydrotestosterone-specific receptor complex formation was inhibited in vitro by ca. 0.5 mumol of atrazine or deethylatrazine and only in vivo by 6 mg of atrazine 100 g-1 body wt. daily during 7 days in the prostate cytosol. The inhibition of the enzymic activities responsible for testosterone conversion and steroid hormone-receptor complex formation was non-competitive and reversible, and s-triazine compounds act as antiandrogens.
研究了s-三嗪化合物(阿特拉津、扑灭通和去乙基阿特拉津)对大鼠前列腺睾酮转化和5α-二氢睾酮-受体复合物形成的体内外影响。检测到阿特拉津和扑灭通(浓度为0.465至1.392μmol)及其混合物(总浓度为0.928μmol)对5α-二氢睾酮形成有显著的体外影响。约0.5μmol的阿特拉津或去乙基阿特拉津在体外抑制5α-二氢睾酮特异性受体复合物的形成,而仅在体内,每天以6mg/100g体重的阿特拉津处理7天可抑制前列腺胞质溶胶中的该复合物形成。负责睾酮转化和类固醇激素-受体复合物形成的酶活性抑制是非竞争性且可逆的,s-三嗪化合物可作为抗雄激素。