Shin J S, Kim K S, Kim M B, Jeong J H, Kim B K
College of Pharmacy, Seoul National University, Korea.
Bioorg Med Chem Lett. 1999 Mar 22;9(6):869-74. doi: 10.1016/s0960-894x(99)00092-x.
A series of 18 chrysin derivatives, prepared by alkylation and condensation, were fully characterized by NMR and other techniques and tested in vivo against the diabetes mellitus. Several modified compounds especially those with propyl, butyl, octyl and tolyl groups were found to have hypoglycemic effect on diabetec mice in spite of the fact that chrysin itself had inhibited insulin release by 40-60%. None of the test animals died at the maximum dose 500mg/kg and did not cause any significant change in general feature, water and food consumption, body weight and organ weight when we examined the acute oral toxicity of those compounds having significant hypoglycemic effect.
通过烷基化和缩合反应制备的一系列18种白杨素衍生物，经核磁共振（NMR）和其他技术进行了全面表征，并在体内针对糖尿病进行了测试。尽管白杨素本身可抑制胰岛素释放40%-60%，但仍发现几种修饰化合物，特别是那些带有丙基、丁基、辛基和甲苯基的化合物，对糖尿病小鼠具有降血糖作用。在检查那些具有显著降血糖作用的化合物的急性口服毒性时，没有一只实验动物在最大剂量500mg/kg时死亡，并且在一般特征、水和食物消耗量、体重以及器官重量方面均未引起任何显著变化。
