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。     

棉酚衍生物的合成及其抗生育作用的研究

本文报道3N-烷基-N′-氨基和N-烷基-N′-氨乙基哌嗪同棉酚的二种席夫碱的合成及其对雄性大鼠生育力的影响。每天口服15mg/kg,连续六周,记录雌性动物着床数、服药前后体重变化,以及睾丸重量和精子活力等。结果表明该二类棉酚衍生物无明显的抗生育作用。     

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。     

雷公藤单体TWl9雄性抗生育及免疫活性调节的研究

TWl9系从雷公藤根皮中提取分离出的一个二萜类化合物,本文比较了TWl9对SD大鼠、ICR小鼠和昆明种小鼠的雄性抗生育作用,以及对ICR小鼠免疫功能的影响。TWl9连续5周灌服给药,以交配试验观察抗生育效果。结果显示TWl9对SD大鼠、ICR小鼠、昆明种小鼠抗生育作用的半数有效剂量(ED50)分别为332.0μg/kg、369.9μg/kg、286.8μg/kg。TWl9在抗生育有效剂量时能使昆明种小鼠及SD大鼠附睾内精子数量和活动力下降,睾丸重量减轻,而对ICR种小鼠没有影响。TWl9对体外培养的T、B淋巴细胞具有抑制作用,而抑制ICR种小鼠体内抗体的生成,但是对于整体动物B细胞的增殖和补体C3的产生有促进作用。     

Studies on Male Antifertilitic and Immunomodulatory Effects of TW19

TW 19 is a diterpene compound isolated from the root cortex of Tripterygium Wilfordii Hood. F. . Its effects on the immune function in ICR mice and the male fertility in SD rats, ICR mice and Kunming mice were evaluated. TW19 was given orally for 5 weeks. Then the antifertilitic effect was assessed by mating test. The results showed that EDso for anti-fertilitic were 332 μg/kg, 369. 9 μg/kg and 286. 8 μg/kg per day in SD rats, ICR mice and Kunming mice respectively. After the treatment of TW 19 at anti fertility dose for 5 weeks consecutively, the spermatozoa density and motility of trial animals reduced significantly. The weight of testis also declined in SD rats and Kunming mice, but no effects were observed in ICR mice. TW 19 inhibited proliferation of splenic T and B-lymphocytes of ICR mice in vitro and hence inhibited the antibody formation in vivo, but compared with T 4, the immunosuppressive effect of TW 19 was less obvious.