The Hypoglycemic Effect of (7R*,9aS*)-7-Phenyl-octahydroquinolizin-2-one in Mice.
作者:Hajime KUBO、Junji KOBAYASHI、Kimio HIGASHIYAMA、Junzo KAMEI、Yuji FUJII、Shigeru OHMIYA
DOI:10.1248/bpb.23.1114
日期:——
(-)-Multiflorine (1), which was isolated from leguminous plants, produced a hypoglycemic effect when administered to mice with streptozotocin-induced diabetes. (-)-Multiflorine has an enaminone type conjugation on the A-ring, which is unusual in lupine alkaloids. Proceeding on the assumption that the A-B ring is responsible for the activity, several compounds bearing quinolizidin-2-one were synthesized
从豆科植物中分离出来的(-)-Multiflorine(1)对链脲佐菌素诱发的糖尿病小鼠给药后产生降血糖作用。(-)-Multiflorine在A环上具有一个烯胺酮型结合物,这在羽扇豆生物碱中是不常见的。在假设AB环负责该活性的前提下,合成了几种带有喹喔啉-2-酮的化合物,并研究了它们的降血糖作用。在正常小鼠中,经口服葡萄糖耐量试验测得的(7R *,9aS *)-7-苯基-八氢喹啉嗪-2-酮的降血糖作用比(-)-多花青碱强约4倍。该结果表明,具有喹啉齐丁-2-酮环体系作为基本结构的化合物可能是新型糖尿病药物的先导化合物。