Ultrastructural, fertility, and spermicidal studies with isomers and derivatives of gossypol in male hamsters.
Ultrastructural, fertility, and spermicidal studies with isomers and derivatives of gossypol in male hamsters.
复制标题
雄性仓鼠棉酚异构体和衍生物的超微结构、生育力和杀精子研究。
DOI：
10.1095/biolreprod37.4.909
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发表时间：
1987
影响因子：
3.6
通讯作者：
Matlin,SA
中科院分区：
文献类型：
--
作者：
Hoffer,AP;Agarwal,A;Meltzer,P;Herlihy,P;Naqvi,RH;Lindberg,MC;Matlin,SA
本研究报道了14种新的口服合成棉酚类似物对仓鼠睾丸超微结构和生育力的影响，以及这些化合物的杀精特性，以及棉酚的光学异构体对仓鼠和人精子的体外杀精特性。通过每日管饲法将测试化合物以15至50 mg/kg范围内的剂量给予成年雄性仓鼠，持续9周。本研究的结果表明，本文评价的14种新的棉酚类似物作为男性抗生育剂是无效的，它们作为杀精子剂的体外活性或缺乏活性与它们的体内避孕潜力无关。此外，研究结果表明：（1）棉酚分子的异丙基部分，如醛基，是其作用机制所必需的;（2）棉酚诱导的线粒体鞘中的特异性缺陷似乎与其作为雄性抗生育剂的独特活性有关。这些发现的意义进行了讨论。
The effects of fourteen new, orally administered synthetic analogs of gossypol on testicular ultrastructure and fertility in hamsters and the spermicidal properties of these compounds, as well as of the optical isomers of gossypol against hamster and human sperm in vitro, are reported in this study. Test compounds were administered to adult male hamsters by daily gavage for 9 weeks at doses ranging from 15 to 50 mg/kg. The results of this study have demonstrated that the fourteen new gossypol analogs evaluated herein are not effective as male antifertility agents and their in vitro activity or lack of activity as spermicides is unrelated to their in vivo contraceptive potential. In addition, the results of the study suggest that (1) the isopropyl moiety of the gossypol molecule, like the aldehyde group, is essential for its mechanism of action and (2) the pathognomonic defect in the mitochondrial sheath induced by gossypol appears to be related to its unique activity as a male antifertility agent. The significance of these findings is discussed.