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一种新型非激素抗生育药物DL 111-IT:II. 对雄性大鼠睾丸透明质酸酶活性的影响

A new non-hormonal antifertility drug DL 111-IT: II. Effects on testicular hyaluronidase activity in male rats.

作者信息

Prasad R S, Vijayan E

出版信息

Contraception. 1986 Jan;33(1):89-99. doi: 10.1016/0010-7824(86)90036-3.

Abstract

Effects of DL-111, [3-(2-ethylphenyl)-5-(3-methoxyphenyl-1H-1,2,4-triazole] a non-hormonal antifertility agent, on testicular hyaluronidase activity, an accurate biochemical marker for testicular function, were evaluated in male rats. Treatment of 21-day-old rats with DL-111 sc for 7 or 15 days resulted in a significant fall in testicular weight and complete suppression of hyaluronidase activity. During the 30-day post-treatment the enzyme activity was restored to normal levels. Treatment of 40-day-old rats for 7 or 15 days also produced a significant decrease in testicular weight and hyaluronidase activity. Simultaneous administration of LH, PMSG or T with DL-111 to 21-day-old rats blocked the inhibitory activity of the drug as the enzyme activity was restored to untreated control levels. Administration of FSH along with DL-111 had no effect on suppressive action of the drug. These results suggest that in male rats DL-111 inhibits testicular activity by reducing LH levels, thereby reducing T levels as observed by reduced weights of testes and accessory glands of reproduction and hyaluronidase activity.

摘要

在雄性大鼠中评估了非激素抗生育剂DL-111,即[3-(2-乙基苯基)-5-(3-甲氧基苯基-1H-1,2,4-三唑)]对睾丸透明质酸酶活性(一种用于评估睾丸功能的准确生化标志物)的影响。给21日龄大鼠皮下注射DL-111,持续7天或15天,会导致睾丸重量显著下降,并完全抑制透明质酸酶活性。在停药后的30天内,酶活性恢复到正常水平。给40日龄大鼠注射7天或15天,也会使睾丸重量和透明质酸酶活性显著降低。将促黄体生成素(LH)、孕马血清促性腺激素(PMSG)或睾酮(T)与DL-111同时给予21日龄大鼠,可阻断该药物的抑制活性,因为酶活性恢复到未处理的对照水平。同时给予促卵泡生成素(FSH)和DL-111对该药物的抑制作用没有影响。这些结果表明,在雄性大鼠中,DL-111通过降低LH水平来抑制睾丸活性,从而降低T水平,这可通过睾丸和生殖附属腺重量减轻以及透明质酸酶活性降低观察到。

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