The pharmacological suppression and recovery of male fertility potential investigated with BrdU monoclonal antibody

柳氮磺胺吡啶(SASP)的抗生育作用已有多篇报道，但其作用机制尚不清楚，靶器官也未被检测到。本实验旨在研究磺基吡啶和5-氨基水杨酸酯两种代谢物对雄性大鼠的抗生育作用，并检测磺基吡啶的靶器官。9周龄雄性SD大鼠随机分为12组，分别给予磺基吡啶250、125、62.5、31.3 mg/kg。5-氨基水杨酸(5-ASA)分别为153、76.5、38.3、19.0 mg/kg。身体重量/天和蒸馏水，在正常饮食的基础上，为期5周。比较各组的平均生育力、睾丸重量和精管直径。SP250 mg/kg组对生育能力有明显的抑制作用。D，125 mg/kg。然而，在其他组中没有观察到抑制作用。各剂量组大鼠睾丸平均重量和精管平均直径均未见抑制，睾丸、附睾头和附睾尾的乙酰磺胺吡啶(Ac-SP)浓度明显升高。结果表明，AC-SP在附睾头的浓度最高，在睾丸中的浓度最低。这些发现有力地支持了SP是SASP的代谢物，抑制男性生育，SP的主要靶器官是附睾的假说。

Antifertility effect of Sulfasalazine(SASP) has been reported by many authors, but its mechanism has not been clear, and the target organ has not been detected. Our purpose of this experiment was to study the antifertility effect of both metabolites of SASP(Sulfapyridine and 5-Aminosalicylate) in male rats and to detect the target organ of Sulfapyridine.Nine-week-old male Sprague Dawly rats, assigned at random to 12 groups, were treated with Sulfapyridine(SP) at 250, 125, 62.5, 31.3mg/kg. body wt/day, and 5-Aminosalicylate(5-ASA) at 153, 76.5, 38.3, 19.Omg/kg. body wt/day and distilled water, for a period of 5 weeks in addition to a normal diet. Mean fertility, testicular weight and diameter ot the seminal tubules in each group was compared. There was a dramatical suppression in fertility in the groups with SP 250mg/kg. day and 125mg/kg. day, however, no suppression was observed in the other groups. No suppression was observed in the mean testicular weight and the mean diameter of the seminal tubules in all groups.The concentration of Acetyl-sulfapyridiie(Ac-SP) in the testis, epididymal head and epididymal tail of the rats treated with SP(250mg/kg. for 5 weeks), were investigated by high pressure liquid chromatography.The concentration of AC-SP was confirmed to be highest in the epididymal head and lowest in the testis. These findings strongly support the hypothesis that SP is the metabolite of SASP, suppressing male fertility and that main target organ of SP is epididymis.