Jones I W, Denholm A A, Ley S V, Lovell H, Wood A, Sinden R E
Department of Biology, Imperial College of Science, Technology and Medicine, London, UK.
FEMS Microbiol Lett. 1994 Jul 15;120(3):267-73. doi: 10.1111/j.1574-6968.1994.tb07044.x.
We have shown that azadirachtin, a compound from the neem tree, Azadirachta indica, and selected semi-synthetic derivatives, block the development of the motile male malarial gamete in vitro. Changes in the hemiacetal group at position C11 in the molecule result in a loss of activity in this assay. The motility of fully formed male gametes, and other selected flagellated cells, is unaffected by azadirachtin in vitro. These findings raise the possibility of developing azadirachtin-based compounds as antimalarials with transmission-blocking potential, as well as permitting the further study of structure-activity relationships in these compounds.
我们已经证明，印楝素（一种来自印楝树Azadirachta indica的化合物）及其选定的半合成衍生物在体外可阻止活动期雄性疟原虫配子的发育。分子中C11位半缩醛基团的变化导致该测定中活性丧失。在体外，印楝素不会影响完全形成的雄配子以及其他选定的鞭毛细胞的运动能力。这些发现增加了开发具有传播阻断潜力的基于印楝素的化合物作为抗疟药的可能性，同时也允许对这些化合物的构效关系进行进一步研究。
