Schein L G, Donovan M P, Thomas J A, Felice P R
J Environ Pathol Toxicol. 1979 Dec;3(1-2):461-70.
These in vitro studies, utilizing cytosols prepared from various tissues (viz. anterior prostate gland, seminal vesicle, kidney and liver) taken from mice 3 days post-castration, were undertaken in order to determine whether or not certain pesticides could alter the binding of 3H-DHT to cytosolic androgen binding components. Estrone, cyproterone acetate, and unlabeled DHT were employed to confirm the presence of specific 3H-DHT binding components in the cytosols. The effects of various pesticides on 3H-DHT binding in these tissue cytosols were then assessed. Parathion (10(-8)--10(-5) M) was found to be an effective inhibitor of total 3H-DHT binding in the prostate, seminal veiscle, kidney and liver. This organophosphate was unable to compete with 3H-DHT for cytosol binding sites in the intestine. Similar in vitro binding studies using dieldrin, DDT, or carbaryl failed to reveal any interference with 3H-DHT binding in any of the tissue studied. The mechanism of parathion's interference with 3H-DHT binding is unclear.
这些体外研究使用了从阉割3天后的小鼠身上获取的各种组织（即前列腺前部、精囊、肾脏和肝脏）制备的胞质溶胶，目的是确定某些农药是否会改变³H-双氢睾酮与胞质雄激素结合成分的结合。使用雌酮、醋酸环丙孕酮和未标记的双氢睾酮来确认胞质溶胶中存在特异性³H-双氢睾酮结合成分。然后评估了各种农药对这些组织胞质溶胶中³H-双氢睾酮结合的影响。发现对硫磷（10⁻⁸ - 10⁻⁵ M）是前列腺、精囊、肾脏和肝脏中³H-双氢睾酮总结合的有效抑制剂。这种有机磷酸酯不能与³H-双氢睾酮竞争肠道中的胞质溶胶结合位点。使用狄氏剂、滴滴涕或西维因进行的类似体外结合研究未能揭示对所研究的任何组织中³H-双氢睾酮结合的任何干扰。对硫磷干扰³H-双氢睾酮结合的机制尚不清楚。
