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EP-1 包合物制备及其对布氏田鼠繁殖器官的影响

王大伟, 刘琪, 刘明, 李宁, 黄宝欢, 刘晓辉   

  1. 中国农业科学院植物保护研究所,杂草害鼠生物学与治理重点开放实验室,北京 100193
  • 出版日期:2011-03-02 发布日期:2011-03-02

Preparation of hydroxypropyl-β-cyclodextrin inclusion with Levonorgestrel and Quinestrol (EP-1) and its influence on the reproductive organs Brandt’s voles (Lasiopodomys brandtii)

WANG Dawei,LIU Qi,LIU Ming,LI Ning,HUANG Baohuan,LIU Xiaohui   

  1. Key Laboratoryof W eed and Rodent Biology and Management,Institute of Plant Protection,Chinese Academy of Agricultural Sciences,Beijing 100193,China
  • Online:2011-03-02 Published:2011-03-02

摘要: EP 系列鼠类不育剂的主要成分—左炔诺孕酮和炔雌醚在常温下难溶于水,给研究和应用造成很大不便。本研究利用2 - 羟丙基-β-环糊精(HPCD)提高了EP 不育剂的水溶性,制备包合物;设置4 个浓度梯度的EP-1 包合物水溶液,分别对雌雄布氏田鼠进行灌胃,并在第2 周和第4 周测量繁殖器官指标,评价不育效果。结果表明, 在20% 的HPCD 水溶液中,左炔诺孕酮和炔雌醚的溶解度分别可达约4 mg / mL和0. 5 mg/ mL;在第2周, 2 mg/ kg EP-1 灌胃组雄鼠的繁殖器官受到了明显抑制,但各剂量组雌鼠未表现出明显影响。本研究结果说明, HPCD 与EP-1 可通过形成包合物,显著增加其常温下的溶解度;EP-1 包合物对雄性布氏田鼠的繁殖器官有抑制效果,但是对雌鼠作用不明显。本研究结果表明包合作用未影响EP 系列不育剂的不育效果。

关键词: 2-羟丙基-β-环糊精, 左炔诺孕酮, 炔雌醚, 包合物, 布氏田鼠, 不育控制

Abstract: EP series rodent contraception is mainly composed of levonorgestrel and quinestrol. However,neither component do not readily dissolves in water,which limits the precision of research and application. In the present study, solubilization was measured in hydroxypropyl-β-cyclodextrin (HPCD) inclusion complexes of levonorgestrel and quinestrol, respectively. Afterwards,the effects of treatment times (after 2 and 4 weeks)and doses (0,1, 2, 4 mg/ kg) of EP-1 inclusion complexes on reproductive organs were investigated using a gastric gavage method. The results showed that the solubility of levonorgestrel and quinestrol reached 4 mg /mL and 0. 5 mg/ mL in 20% aqueous HPCD solution,respectively. For females, there were no significant differences after 2 or 4 weeks between the control and treatment groups that received gavage. For males,the average weight of reproductive organs of the group that received gavage for 2 weeks of 2 mg/ kg group was less than that of the control group. Our results indicate that the solubility of EP-1 was significantly enhanced by forming inclusion complexes with HPCD; the suppressive effects on reproduction in male Brandt’s voles is more obvious than those in females. Moreover,inclusion did not affect the anti-fertility effect of EP-1.

Key words: Antifertility control, HPCD, Inclusion complex, Lasiopodomys brandtii, Levonorgestrel, Quinestrol