双炔失碳酯或丙睾配伍dl-15甲基PGF_(2α)抗早孕的临床比较

本文报告65例双炔失碳酯配伍d1-15甲基PGF_(2α)(以下简称PG)抗早孕结果并与33例丙睾配伍PG抗早孕结果进行比较。结果显示,双炔失碳酯组完全流产59例,占90%;不全流产3例,占5%;失败3例,占5%;总有效率95%。丙睾组完全流产27例,占82%;不全流产6例,占18%;总有效率100%。两组总有效率无显著差异;完全流产率无显著差异;但不全流产率有明显差异(P<0.05)。药流后点滴出血天数,双炔失碳酯组平均为8.1±5.0天;丙睾组平均为18.9±19.1天;两组有明显差别(P<0.05)。双炔失碳酯经阴道给药后无一例发生心、肝、肾功能变化。     

顶体蛋白酶抑制剂KF-950对大鼠精子的影响

本文采用体外杀精实验检查ＫＦ－９５０对大鼠精子活力的影响和明胶底物膜法测定 ＫＦ－９５０对精子顶体蛋白酶活性的抑制作用。结果表明,ＫＦ－９５０与大鼠精液作用 ２０ ｓｅｅ 及 １２０ ｓｅｅ,最低杀精浓度分别为 １． ５６±０． １３ ｍｇ／ｍｌ和 ０． ７３±０． ０７ ｍｇ／ｍｌ,其杀精能力 明显低于壬苯醇醚（Ｐ＜０．０１）;当ＫＦ－９５０浓度为１× １０－１２ｍｇ／ｍｌ时,平均晕轮阳性率 （％）及平均晕轮直径（μｍ）分别为８３．００±７．１０及１８．２７±１．９４（与对照组比较Ｐ＜ ０．０１）,完全抑制浓度为 １×１０－３ｍｇ／ｍｌ。抑制平均晕轮阳性率和平均晕轮直径的半数有效 浓度ＥＤ５０分别为４．１５×１０－７ｍｇ／ｍｌ和２．３４×１０-7 ｍｇ／ｍｌ。本实验证明ＫＦ－９５０对精子顶 体蛋白酶具有高效抑制作用,而杀精子作用较弱,是一种新型的顶体蛋白酶抑制剂。     

棉酚单侧衍生物的合成及其口服抗生育活性研究

本文报道单醛棉酚和单苯胺棉酚合成工艺的改进,即采用新的有效的分离方法,提高收率,从而首次完成了这两个化合物的雄性大鼠口服抗生育实验。文中还首次报道了单醛棉酚的mp,UV,IR,MS及完整的~1H-NMR数据并阐明了单醛棉酚在DMSO-d_6溶剂中同时共存着醛式与内醚式两种互变异构体。     

多种化合物对体外培养人滋养层细胞 和蜕膜细胞的损伤作用

Objective　To observe the detrimental effects of 6 known antifertility compounds and 22 natural compounds which may have the antifertility activity to the human trophoblast cells and decidual cells, to check the model for screening new antifertility drugs, and to screen new active antifertility compounds.Methods　The culture method for human trophoblast cells and decidual cells and hCG radioimmunoassay were applied to observe and screen antifertility activity of microcompounds.Results　Antifertility compound R_u486 (100　μg/ml), Tamoxifen (20　μg/ml), Anordrin (100　μg/ml) and Trichothanthin (50　μg/ml) not only injured the morphology of human trophoblast cells, but also inhibited the hCG secretion of them, whereas Pseudolaric acid B (100　μg/ml) and Yuanhuacine A ( 0.5　μg/ml) only altered the morphology of trophoblast cells.Among 22 natural compounds detected, 100　μg/ml of Hml, Hmlo, TR₄, T₂ were not only detrimental to the trophoblast cells but also inhibitory to the hCG secretion.Antifertility compounds R_u486(10　μg/ml), Anordrin (60　μg/ml), Pseudolaric acid B (50　μg/ml) and Yuanhuacine Ⅰ (0.5　μg/ml) were detrimental to human decidual cells, whereas Trichothanthin did not alter the morphology of decidual cells.Among 22 natural compounds detected, TR₄ was evidently detrimental to decidual cells, whereas Zh-1 and other 19 compounds had no effect.Conclusion　Human trophoblast cells and decidual cells in vitro may be taken as the model for screening antifertility drugs; TR₄ was evidently detrimental to the trophpblast cells and decidual cells and deserves further research.     

The Effects of Anordrin on Luteal Cells, Decidual Cells and Trophoblast Cells in Vitro

ＡｎｏｒｄｒｉｎｉｓａｓｔｅｒｏｉｄｗｉｔｈａｌｏｓｓｏｆｏｎｅｃａｒｂｏｎａｔｏｍａｔＡｒｉｎｇ（２α,１７α－ｄｉ－ｅｔｈｙｎｙｌ－Ａ－ｎｏｒ－ａｎｄｒｏｓｔａｎｅ,２β,１７β－ｄｉｏｌｄｉｐｒｏｐｉｏｎａｔｅ）．Ｒｅｓｅａｒｃｈｐｅｒｆｏｒｍｅｄｐｒｅｖｉｏｕｓ－ｌｙｈａｓｄｅｍｏｎｓｔｒａｔｅｄｔｈａｔｉｔｈａｓａｎｔｉｆｅｒｔｉｌｉｔｙａｎｄｔｅｒｍｉｎａｔｉｏｎｏｆｅａｒｌｙ－ｐｒｅｇｎａｎｃｙｆｕｎｃ－ｔｉｏｎｏｂｖｉｏｕｓｌｙ［１－３］．Ｃｌｉｎｉｃａｌｏｂｓｅｒｖａｔｉｏｎｃ…     

甲基磺酸甲酯和环磷酰胺抑制小鼠精子的受精能力

本文应用小鼠卵子体外受精的方法,研究了诱变剂甲基磺酸甲酯和环磷酰胺对小鼠精子受精能力的影响.结果显示,以上两种诱变剂能明显抑制小鼠精子的受精能力,与对照组相比有显著性差异(P<0.01),同时受精后的胚胎发育延缓,但对精子的活力和密度无明显影响.     

小鼠卵在体内外受精和胚胎发育的比较

比较了人工促排的小鼠卵在体内和体外的受精和受精后的胚胎发育情况。结果表明：两者的受精率无明显差别，各为４９．４％和５５．０％，但受精卵在体外的发育速度明显慢于体内。