Morphologische Studie der Wirkung von Norethisteron-Oxim auf das Ovarium des Kaninchens und der Ratte

The search for antiimplantation agents has been attracting attention widely. In animal experiment it has been proven, that norethisterone oxime (NETO) showed significant antiimplantation effect with certain antigestogen activity. Rabbits and rats were used in morphological study in order to explore whether NETO also has some effect on the ovary. 20 mature female rabbits and 12 mature female rats were treated with NETO from the first day of pregnancy for three days and sacrificed on the 9th and the 7th day respectively. The ovaries and uteri were examined histologically after staining with HE and PAS, and histochemically (ACP, ALP, 3ß-HSD and SDH). It was found that NETO showed obvious antigestogen effect. The corpora lutea became flattened and the lutein cells showed obvious vacuolar degeneration. In histochemical examination, the activity of ACP was increased and 3ß-HSD decreased, but ALP and SDH had not changed. The lutein cells showed electronmicroscopically an increase of fat droplets as well as secondary lysosomes in their cytoplasm and a decrease of SER in number. The secretory granules of lutein cells were of various size and electron density, some of them even exhausted. It could be concluded that the biosynthesis of steroid hormone in ovary was blocked due to the inhibition of 3ß-HSD activity, and that NETO might be an effective contraceptive in human beings.     

炔诺酮肟对大鼠抗着床抗早孕作用机理的形态学研究

大鼠从妊娠第一天开始每日灌服炔诺酮肟4mg/kg,共3天。结果能引起早孕大鼠黄体细胞滑面内质网减少;脂滴大量积贮;抑制卵巢3β-羟基甾体脱氢酶活性,从而使卵巢孕酮生物合成受阻。药物还能引起早孕大鼠子宫蜕膜的病理改变,蜕膜细胞出现变性,坏死,宫腔内大量出血,白细胞浸润,胚胎发育不良,蜕膜细胞内糖原及碱性磷酸酶含量均下降。本文还讨论了药物引起卵巢孕酮生物合成受阻与蜕膜变化的关系。     

醋酸棉酚对大鼠孕卵转运和发育的影响

本文观察了醋酸棉酚对大鼠孕卵在输卵管内转运和早期发育的影响。结果表明,棉酚可延缓孕卵转运速度、阻滞和破坏胚胎早期发育,以对后者的作用更为显著。这可能是棉酚对雌性大鼠抗着床作用的重要原因之一。     

醋酸棉酚对大鼠孕卵转运和发育的影响

本文观察了醋酸棉酚对大鼠孕卵在输卵管内转运和早期发育的影响。结果表明,棉酚可延缓孕卵转运速度、阻滞和破坏胚胎早期发育,以对后者的作用更为显著。这可能是棉酚对雌性大鼠抗着床作用的重要原因之一。     

双炔失碳酯—PVP共沉淀物的研究

本文用差示扫描量热法(DSC)筛选确定双炔失碳酯与PVP按1:7～1:9比例以溶剂法制得共沉淀物,其中已不存在双炔失碳酯晶体。用X射线衍射法研究了1:8共沉淀物,证明无双炔失碳酯的晶体衍射峰。经溶出速率测定结果20 min的药物溶出度1:8共沉淀物比原药约大38倍。用导数热重法(DTG)求得1:8共沉淀物与双炔失碳酯的热解动力学参数,其活化能分别为182.8和133.4 kJ/mol,1:8共沉淀物的热解稳定性明显大于原药。小鼠抗着床试验结果表明空白对照组着床数为4.8,53抗孕片(剂量10.6 mg/kg)组为0.9(P<0.05),1:8共沉淀物(剂量5 mg/kg)组为0.2(P<0.01),即1:8共沉淀物抗着床的有效剂量小于53抗孕片的一半。     

3-[p-ω-取代氨基烃氧基)-苯甲酰]-吲哚衍生物的合成

本文根据某些吲哚化合物具有抗生育活性,结合多数非甾体抗生育化合物联有碱性醚链的结构特征,设计并合成了以吲哚为母核的四种类型化合物(Ⅰ_1～7,Ⅱ_1～7,Ⅲ_1～7,Ⅳ₁)22个,并验证了三个熔点与文献报道不符的关键中间体。对小白鼠的初步药理试验表明:所合成的化合物均无抗着床作用;Ⅱ₁,Ⅱ₂,Ⅱ₄和Ⅱ₅有明显的镇痛作用;Ⅲ₂和Ⅲ₃则有较强的抗电休克作用。     

Antifertility activity of hydroalcoholic extract of Ailanthus excelsa (Roxb): an ethnomedicines used by tribals of Nilgiris region in Tamilnadu

The practice of traditional medicine for the control of fertility in Nilgris is based on the use of plant medicine for many years. The aim of the present study is to evaluate the effect of hydroalcoholic extract of stem bark of Ailanthus excelsa Roxb (Simaroubaceae) (HEA) has been studied in rats to explore its antifertility activity. A strong antiimplantation (72%) and abortifacient activity (56%) was observed at the tested dose levels (200 and 400mg/kg, p.o.). The extract shows further more, significant (P<0.05) increase in uterine weight in immature ovariectomised rats. Simultaneous administration of extract with ethinyl estradiol cause significant antiestrogenic activity. All these observations suggest that hydroalcoholic extract of Ailanthus excelsa has antifertility effect.     

双炔失碳酯—PVP共沉淀物的研究

本文用差示扫描量热法(DSC)筛选确定双炔失碳酯与PVP按1:7～1:9比例以溶剂法制得共沉淀物,其中已不存在双炔失碳酯晶体。用X射线衍射法研究了1:8共沉淀物,证明无双炔失碳酯的晶体衍射峰。经溶出速率测定结果20 min的药物溶出度1:8共沉淀物比原药约大38倍。用导数热重法(DTG)求得1:8共沉淀物与双炔失碳酯的热解动力学参数,其活化能分别为182.8和133.4 kJ/mol,1:8共沉淀物的热解稳定性明显大于原药。小鼠抗着床试验结果表明空白对照组着床数为4.8,53抗孕片(剂量10.6 mg/kg)组为0.9(P<0.05),1:8共沉淀物(剂量5 mg/kg)组为0.2(P<0.01),即1:8共沉淀物抗着床的有效剂量小于53抗孕片的一半。     

非甾体抗炎药4-羟基-3-胺甲基-联苯及4(2)-环己基-2(4)-胺甲基-苯酚衍生物的合成及其生物活性

为了寻找作用强、毒副作用小的非甾体抗炎药,以取代酚类为原料,通过Mannich反应合成了26个4-羟基-3-胺甲基-联苯及4(2)-环己基-2(4)胺甲基-苯酚衍生物,对其中23个化合物进行了初步药理筛选,发现部分化合物在大鼠模型有明显的抗炎活性并有镇痛、解热作用。对其中20个化合物进行了抗着床筛选,以7.5 mg/kg剂量给予交配后的大鼠,结果均无抗着床活性。