6-甲氧基棉酚的分离及其抗生育作用的初步探讨  

Isolation and preliminary antifertility test of 6-methoxygossypol

作　　者：周瑞华 沙玉申 汪利强 万阳 赵安娜 

机构地区：[1]国家计划生育委员会科学技术研究所,北京100081 [2]河南省计划生育研究所

出　　处：《生殖医学杂志》1993年第3期169-172,共4页Journal of Reproductive Medicine

摘　　要：从我国海岛棉籽中分离出6-甲氧基棉酚(6-MG),经光谱鉴定确证其结构。所得为6-MG的消旋体,拆分后的两个对映体的比旋光值分别为[α]27/D=-324°(C=0.2,CHCL_3)。体外杀精试验表明,(±)6-MG(-)6-MG及(+)6-MG对人精于活力均有抑制作用,(-)6-MG的作用较强。(±)6-MG与棉酚相比作用较弱。雄性大鼠抗生育试验说明6-MG具有抗生育活性,起效略迟于棉酚。服药(每天30mg/kg)8周的大鼠睾丸切片结果显示,6-MG对曲细精管的损伤比棉酚弱得多。Pure 6-methoxygossypol(6-MG)hsa been isolated from cottonseed of G. barbadense produced in Xinjiang Autonomous Region. The structure of 6-MG was confirmed by NMR and MS. The racemic form of 6-MG has been resolved into two enantiomers with specific rotation of [α]_D^(31)=+334° and [α]_D^(27)=-325°respectively. The spermicidal effects of (±)6-MG, (+)6-MG and(-) 6-MG were evaluated. It was evident that both enantiomers of 6-MG had inhibitory effect on human sperm motility,but the (-)form had a stronger effect,while the racemic 6-MG had a weaker effect than gossypol. The antifertility test in male rats showed that 6-MG was clearly active,but with a slightly slower response rate, when compared with gossypol acetic acid. The results also showed that the damage of seminiferous tubule of rat testis by 6-MG and gossypol were time dependent, but the damage by 6-MG was significantly weaker than that by gossypol.

关 键 词：棉酚 杀精作用 抗生育活性 分离 

分 类 号：R979.21[医药卫生—药品]