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。     

抗人上皮性卵巢癌单克隆抗体的制备与鉴定

应用卵巢浆液性乳头状囊腺癌可溶性相关抗原ＣＡ＿（９２５）免疫ＢＡＬＢ／ｃ小鼠，与ＮＳ－１骨髓瘤细胞株融合制各单克隆抗作（ＭｃＡｂ），获得５株持续性分泌抗体的细胞株，以融合孔为代号，分别为ＯＣ＿（４Ｄ９），ＯＣ＿（７Ｅ１０），ＯＣ＿（１Ｂ４），ＯＣ＿（３Ｂ８），ＯＣ＿（９Ｂ９）。５种ＭｃＡｂ的滴度分别为１：１０￣７，１：１０￣７，１：１０￣６，１：１０￣４，１：１０￣５，免疫球蛋白亚型为ＩｇＭ和ＩｇＧ型，染色体呈双亲染色体特点。所获得５种ＭｃＡｂ与ＣＡ＿（９２５）有特异性反应（阳性反应）；与正常卵巢组织及子宫平滑肌瘤未呈阳性反应；与肺癌、胃癌、肾癌、食管癌、直肠癌组织有弱阳性反应。     

低剂量棉酚男性避孕效果和副作用的临床观察

棉酚的男性避孕作用和副作用（如：不可逆性不育和低血钾症）均为男性学学者所熟悉，其副作用使棉酚至今不能成为广泛应用的男性避孕药。本文试图通过减低棉酚的起效量和维持量以减少或避免副作用的发生。结果发现：每天服用１０ｍｇ或１２．５ｍｇ，待精子密度降为≤４００万／ｍｌ时，改服维持量（隔天１０ｍｇ，或１２．５ｍｇ）均有避孕效果，但起效期较长。服药期间血清ＦＳＨ、ＬＨ和睾酮水平无明显变化，尿β－２ＭＧ和ＮＡＧ以及血钾也无明显异常，服药者更无低血钾症状出现。服药对象的女方无妊娠。     

棉酚对体外家兔精子顶体酶类的抑制作用

本文对棉酚体外抑制１０种家兔精子顶体酶活性进行了测定。当醋酸棉酚浓度为１２～７６μｍｏｌ／Ｌ时，可完全或明显抑制顶体酶（ａｃｒｏｓｉｎ）、Ａｚｏｃｏｌｌ蛋白酶、芳香基硫酸酯酶和神经氨酸苷酶活性；而当浓度高达３８０μｍｏｌ／Ｌ时才能抑制透明质酸酶、β－葡糖苷酸酶和酸性磷酸酶，但不抑制磷酸酯酶Ｃ、碱性磷酸；酶和β－Ｎ－乙酰氨基葡糖苷酶。棉酚对芳香基硫酸酯酶的抑制作用是一种非竞争性抑制作用，Ｋｉ为１２０μｍｏｌ／Ｌ。其抑制作用是可逆的，呈剂量依赖关系。由于抑制家兔精子顶体酶所需棉酚浓度比精子糖酵解或能量代谢酶要低，因此，这些敏感酶似可作为监护棉酚引起不育的指标。     

雷公藤单体对大鼠睾丸间质细胞及支持细胞毒性与其抗生育作用不相关

本文用体外培养的睾丸间质细胞和支持细胞筛选了２２种从雷公藤根、皮中分离、纯化的单体，并选择其中对两种细胞杀伤作用强、弱不同的化合物ＴＷ－９，ＴＷ－５，ＴＷ－２８和ＴＷ－２７进行抗生育试验以及体外杀精试验。结果发现对两种细胞毒性作用最弱的ＴＷ－１９对大鼠有明显的抗生育作用；而毒性作用较强的ＴＷ－５，ＴＷ－２８和最强的ＴＷ－２７则无明显的抗生育作用。然而这四种化合物的体外杀精强度则依次为：ＴＷ－２７，ＴＷ－５，ＴＷ－１９，ＴＷ－２８。与它们的抗生育作用不相关。     

人精液非精子细胞分析

采用Ｐａｐａｎｉｃｏｌａｏｕ染色、免疫荧光和电镜技术对１３例生育者、１３例不明原因不育者和８例精液脲原体阳性不育者的精液非精子细胞（ＮＳＣ）进行分析，发现生育组ＮＳＣ占精液细胞总数的１．８８％，其中未成熟生精细胞（ＩＧ）占ＮＳＣ的８３．４％，白细胞９．１％，脱落上皮细胞６．３％，支持细胞１．２％。ＩＧ中包括无核胞浆体５０．４％，初级精母细胞１０．１％，次级精母细胞２．９％，早期精子细胞６．８％，晚期精子细胞１３．２％。白细胞中多形核细胞５．４％，巨噬细胞２．６％，淋巴细胞１．１％。淋巴细胞中以ＣＤ３和ＣＤ８阳性细胞为主，ＣＤ３／ＩｇＧ阳性细胞比为１６．５；ＣＤ８／ＣＤ４细胞比为３．６。两组不育者中，ＮＳＣ总数和除支持细胞外各组分均增加，其中淋巴细胞总数和ＣＤ４细胞增加最显著，ＣＤ８／ＣＤ４比降为０．３５，两不育组间无显著差异。正常精液中ＣＤ８细胞优势可能有利于免疫抑制作用。     

四种溶脲脲原体对精子穿卵试验的作用比较

分别用血清型４、９、１０、１２四种溶脲脲原体按２０￣４０颜色变化单位（ＣＣＵ）／精子的浓度与正常生育男性精子一同孵育。结果发现，部分感染的精子尾部有绒毛状附着物；血清型４、１２溶脲脲原体与精子共同孵育后，精子活率及活力明显下降，血清型９、１０溶脲脲原体对精子活率及活力无明显影响。血清型４、９、１０、１２溶脲脲原体均使精子穿卵值（ＳＰＡ）明显降低（分别为６．５０％、１０．４５％、９．６０％和６．４０％），对照组为４９．３３％。提示溶脲脲原体不仅可能影响精子的活率与活力，而且可影响精卵相互作用乃至融合过程，溶脲脲原体的致病作用与其血清型有关。     

孕妇与胎儿巨细胞病毒感染的血清学研究

测定了１７３例孕妇及８１例胎儿血清ＣＭＶ抗体。结果：１７３例孕妇血清中ＣＭＶ－ＩｇＧ阳性率为７０．５％（１２２／１７３），ＣＭＶ－ＩｇＭ阳性率为０．５８％（１／１７３），孕妇早、中、晚孕期ＣＭＶ感染率分别为５２％、７２．９％，７４．４％，妊娠次数≥４次的孕妇ＣＭＶ感染率较高。８１例脐血血清中ＣＭＶ－ＩｇＧ阳性率为５４．３％（４４／８１），ＣＭＶ－ＩｇＭ阳性率为６．２％（５／８１），５例先天性ＣＭＶ感染儿分别为４例胎儿畸形及１例产前咨询者，后者取脐血查到ＩｇＭ阳性后１个月，胎死宫内。提示脐血中一旦查到ＣＭＶ－ＩｇＭ阳性，胎儿有严重后果。因此，产前诊断胎儿ＣＭＶ感染，早期发现ＣＭＶ感染儿，是非常重要的。     

妇科肿瘤患者治疗前后血浆FN水平的观察及意义

目的：通过比较妇科肿瘤患者纤维连结蛋白（ＦＮ）的变化，评价ＦＮ对妇科肿瘤诊断及疗效评价的意义。方法：检测妇科良性肿瘤２６例、恶性肿瘤７１例治疗前后血浆的ＦＮ值，并与健康献血员４０例血浆ＦＮ值作对照。结果：妇科恶性肿瘤组治疗前血浆ＦＮ平均值为４．５０×１０－３±１．９０×１０－３ｍｍｏｌ／Ｌ，治疗后升至６．８１×１０－３±２．２２×１０－３ｍｍｏｌ／Ｌ，治疗前后差异有显著性（Ｐ＜０．０１）。恶性肿瘤组治疗前血浆ＦＮ值与健康献血员、良性肿瘤组治疗前血浆ＦＮ值比较差异也有显著性（Ｐ＜０．０１）。结论：妇科恶性肿瘤患者血浆ＦＮ值明显低于正常，治疗效果好的患者血浆ＦＮ值总的趋势是逐渐上升，治疗效果不好的患者血浆ＦＮ值总的趋势是逐渐下降。ＦＮ可作为妇科常见恶性肿瘤诊断、疗效观察的临床参考指标。     

腺病毒/HSV_1-tk/GCV、ACV系统对卵巢上皮癌细胞旁观者效应的研究

目的：研究腺病毒／ＨＳＶ１－ｔｋ／ＧＣＶ、ＡＣＶ系统对卵巢上皮癌细胞旁观者效应。方法：常规重组腺病毒扩增纯化后,测病毒滴度。Ｘ－ｇａｌ染色法测定转染效率,ＰＣＲ检测ＨＳＶ１－ｔｋ的表达,混合细胞培养实验观察旁观者效应。结果：重组腺病毒扩增纯化后测定滴度分别为Ａｄ／ｔｋ*"６２×１０９ｐｆｕ／ｍｌ,ＡｄＬａｃＺ*"１４×１０９ｐｆｕ／ｍｌ。当感染复数为１００时,近１００％的细胞可被感染。ＰＣＲ结果显示,Ａｄｔｋ转染ＴＹＫ后,可见４０４ｂｐ的特异性条带,在同一ＭＯＩ中,有１０％的Ａｄｔｋ／ＴＹＫ细胞存在,ＧＣＶ就可杀死近５０％左右的混合细胞。ＡＣＶ的作用约为ＧＣＶ的１／１０。结论：重组腺病毒Ａｄ／ｔｋ可有效地感染人卵巢上皮癌细胞,腺病毒／ＨＳＶ１ ｔｋ／ＧＣＶ、ＡＣＶ系统存在着旁观者效应。     

非表面活性杀精子剂SM-3的体外杀精研究

本文采用一种非表面活性杀精子剂-1-取代咪唑衍生物SM-3,按照国际计划生育基金会认可的杀精子实验方法,对20例大鼠精液、20例人精液进行了体外杀精试验,并观察了药物与粘液(新鲜鸡蛋清)混合后的杀精效果.结果表明,SM-3与人精液作用20秒时,最低有效杀精浓度为0.09±0.03mg/ml;SM-3与大鼠精液作用20秒时,最低有效杀精浓度为0.78±0.15mg/ml;SM-3与代粘液混合后对大鼠与人精子的杀精效应没有明显改变.SM-3可望成为一种新型、高效、安全的阴道避孕剂,值得进一步研究.     

Efficacy of spermicides

Spermicidal contraceptives, after falling out of favor in the 1960s, are once again being sought be women desiring a natural and safe method. 2-6% of couples in France and other European countries are estimated to use spermicidal contraceptive methods. There is a wide an puzzling gap between the theoretical efficacy of spermicides tested in vitro and efficacy in actual practice. The theoretical failure rate of spermicides used regularly and correctly is 0-7.6%. The principal spermicides used in France at present are the ionic surfactant agent benzalkonium chloride and the nonionic surfactant nonoxynol 9, which destroy the cellular membranes of the sperm. Several tests are used to determine the spermicidal activity of a contraceptive. They include the International Planned Parenthood Federation test which is considered positive if 1 ml of a 1/11 solution immobilizes the sperm in .2 ml solution of selected sperm within 10 seconds in a reproducible fashion; the study of the minimal concentration that completely inhibits .2 ml of fresh sperm in less than 20 seconds; the absence of penetration of sperm in hamster eggs after contact with the products tested, and the Huhner test consisting of a search for sperm in the cervical mucus in the hours following intercourse. The 4 tests have demonstrated that the spermicidal efficacy of benzalkonium chloride is 4 times greater than that of nonoxynol 9. The spermicidal action is reinforced by thickening and coagulation of the mucus on contact with benzalkonium chloride, and the action of the spermicide covering the vaginal mucus. The practical efficacy of spermicides, which takes into account failures attributable to the method itself as well as failures due to incorrect use, is reflected in Pearl indexes ranging from 0.3-30. The efficacy of spermicides is closely related to their correct use. The method should be used regularly and systematically and the product inserted before initiation of sexual contact. Most products require renewed application if intercourse is repeated. Package instructions about duration of action and waiting times for the product to become fully effective should be carefully followed. The product should be left in place at least 2 hours. Baths and vaginal douches should be avoided for 4 hours after intercourse. Products such as soaps which neutralize the ionic surfactants should be avoided. Spermicidal contraceptives are recommended only for women capable of understanding and following the use instructions. Women who find the idea of spermicides distasteful and those requiring absolute efficacy should select another method. Vaginal spermicides may be suggested for women over 40 and those with contraindications to oral contraceptives and IUDs. They provide some protection against sexually transmitted diseases, and have no effects on the vaginal mucus or menstrual cycle and no carcinogenic effect.     

In vitro method for evaluation of spermicides by hemolytic potency

Nonoxynol-9 immobilizes sperm and hemolyzes erythrocytes at analogous concentrations; therefore, erythrocytes may be utilized for predicting in vitro spermicidal potency. Since erythrocytes (human or rabbit) are usually more readily available in larger quantities than are spermatozoa, this method permits extensive in vitro testing of different formulations of vaginal spermicides.     

洗必泰醋酸盐和洗必泰葡萄糖酸盐的杀精子效果及阻抑精子对宫颈粘液穿透力的比较研究

本文比较了洗必泰醋酸盐和洗必泰葡萄糖酸盐的杀精子效力和阻抑人精子穿透动情期牛宫颈粘液的作用。结果表明,两种形式的洗必泰盐类均有良好的杀精子效力和阻止精子穿透牛宫颈粘液的作用。应用Sander-Cramer杀精子试验法测定洗必泰醋酸盐和洗必泰葡萄糖酸盐的最低杀精子浓度分别为2.5mg/ml,5.0mg/ml。应用Cremer′s精子穿透法测定两种洗必泰盐类阻止人精子穿透牛宫颈粘液的作用很相似,当药物浓度是0.25%或0.5%时人精子穿透牛宫颈液的距离是0mm(对照是48mm)。     

Studies on the male antifertility agent gossypol acetic acid: in vitro studies on the effect of gossypol acetic acid on human spermatozoa

The hypothesis that gossypol (an active ingredient associated with cottonseed oil) affects enzymes and other constituents of spermatozoa, resulting in alterations in motility and sperm viability after in vitro treatment, was tested using human semen samples. At a gossypol acetic acid concentration (and a 30 minute incubation) of .01 mcg, the percent motility was 71+ or -2.5 (P .01); at .1 mcg concentration, percent motility was 69+ or -4 (P .01); at 1 mcg motility was 66+ or -5 (P .005); at 10 cg, motility was 38.5+ or -3.5 (P .001). Control values for sperm motility were 77+ or -3. These investigations suggested that treatment with gossypol depletes production of adenosine triphosphate in the sperms and thus their metabolism does not proceed normally, rendering them immotile. It appears that the high vulnerability of the testis to gossypol and the uncoupling of oxidative phosphorylation in the respiratory chain of mitochondria of germ cells may be the mechanism responsible for infertility induction.     

Effect of optical isomers of gossypol on mammalian spermatozoa: an in vitro study

Human, bull and monkey spermatozoa were treated with different optical isomers of gossypol in vitro. The spermatozoa (concentration 50 x 10(8)) were incubated with gossypol for 15, 30, 45 and 60 min. at 37 degrees C. The concentration of gossypol employed in the experiment was from 5-50 micrograms/ml. A marked inhibition in sperm motility was observed following gossypol treatment; levorotatory gossypol had more pronounced effect on sperm motility in comparison to dextrorotatory and racemic gossypol. Scanning electron microscope study revealed degenerative changes in the sperm head surface. Dextrorotatory gossypol, hitherto known to be non-effective in suppressing the fertility in vivo was found to be equally effective in inhibiting the motility and LDH-X activity of the spermatozoa. Both racemic and dextrorotatory gossypol inhibited fructolysis in bull spermatozoa. Our data suggest that whatever the mechanism of action of enantiomers of gossypol on sperm motility, fructolysis and LDH-X may be, it is evidently clear that dextrorotatory gossypol is equally active in inhibiting the sperm motility and enzyme active in vitro. The action of optical isomers of gossypol on spermatozoa in vitro, appears to be unrelated to the mechanism of orally administered gossypol.     

Vaginal contraception and tensio-actives (author's transl)

247 women using local contraception with a vaginal tampon impregnated with benzalkonium chloride were observed for 2597 cycles; there was only 1 pregnancy. After accurate anamnesis it appeared that the patient had neutralized the cationic spermicidal agent through postcoital douching with a liquid anoionic soap. The use of tensioactive agents in products for female hygiene is widespread, since they have active foaming and detergent properties. Spermicidal vaginal agents must never be diluted by a vaginal douche, or modified by chemical products with antagonizing properties. The use of tensioactive anionic products for female hygiene and their contact with spermicidal cationic ammonium derivates, results in the deactivation of such derivates, while nonanionic tensioactives provoke no action on cationic spermicidal agents. This brief article includes a list of different types of tensioactives, and divides them in anionic, cationic, and nonanionic categories.     

心得安体外抑精子作用的研究

30份取自健康志愿受试者的精液标本,在其自然液化后,按其精液中的精子数量和/或质量分为四组,并分别加入各不同浓度的心得安溶液剂,尔后在各个规定的时间内观察其杀精子效果。实验发现:心得安在体外对人类精子具有肯定的抑杀作用。其抑杀精子的效果与药物浓度和用药时间及精子的数量或质量有关。因此,初步认为:心得安可能作为一种安全、有效、经济和使用方便的女性阴道用杀精子避孕药,很值得进一步研究。