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近十余年来,为寻求毒副反应小的棉酚类男性节育药,合成并筛选了大量的棉酚类似物,但无一优于棉酚。1975年 Stipanovic 等首次从生长1周的陆地棉(Gossypium hirsutum)和海岛棉(G.barbadense)籽苗根部分离出天然棉酚类似物——6-甲氧基棉酚(即单甲醚棉酚,6-MG),然而关于6-MG 的生理活性未见报道。1991年我们从中国海岛棉籽中分离获得了6-MG的消旋体,经体外实验证实该化合物具有对人精子的杀精作用。继而又进行了消旋6-MG 的拆分,首次得到了左旋6-MG。6-MG 是以从海岛棉籽中提取的粗制乙酸棉酚为原料,采用改进的 Stipanovic 方法,分离得到黄色晶
In the past ten years, a large number of gossypol analogs have been synthesized and screened for the purpose of seeking gossypol-type male birth control drugs with little toxic side effects, but none of them is superior to gossypol. In 1975, Stipanovic et al first isolated the natural gossypol (6-methoxypicolinol) (ie, monomethyl ether gossypol) from the roots of Gossypium hirsutum and G. barbadense seedlings for one week. , 6-MG), however, the physiological activity of 6-MG has not been reported. In 1991, we isolated racemic 6-MG from Chinese island cottonseed and confirmed that the compound has spermicidal effect on human sperm in vitro. Subsequently, the resolution of racemic 6-MG was carried out and the first time, the 6-MG was obtained. 6-MG is derived from the island cottonseed crude gossypol acetate as raw material, using a modified Stipanovic method, isolated yellow crystals