鸡血藤活性化合物儿茶素结构修饰及抗辐射作用研究

Structural Modification and Antiradiation Activity Study of Catechin from Spatholobus Suberectus

目的对儿茶素进行结构修饰,制备系列衍生物,观察其抗辐射效果。方法通过乙酸酐,丙酸酐,苯甲酰氯在碱性溶剂下与儿茶素反应,合成产物再利用硅胶层析进行分离纯化,得到纯化合物后进行结构鉴定;60Coγ射线(剂量为6Gy)照射小鼠造成辐射模型,照后给予3,5,7,3’,4’-O-五乙酰基儿茶素和儿茶素灌胃;并于照前、后1、3、7、10、14、21d取鼠尾静脉血,测外周血白细胞(WBC)、红细胞(RBC)、血红蛋白(HGB)、血小板数值(PLT)。结果合成并鉴定得到3种化合物,分别为3,5,7,3’,4’-O五-乙酰基儿茶素;5,7,3’,4’-O-四苯甲酰基儿茶素;3,5,7,3’,4’-O-五丙酰基儿茶素;全乙酰化儿茶素对于辐射小鼠WBC,HGB,RBC,PLT的升高均有一定作用,但作用强度均不及儿茶素。结论经过结构改造后的3,5,7,3’,4’-O-五乙酰基儿茶素有一定的抗辐射作用,但作用效果较儿茶素弱。

Aim To prepare derivatives of catechin and observe their antiradiation activity. Methods Catechin was treated with acetic anhydride, propionic anhydride and benzoyl chloride respectively. The reaction products were separated with various chromatographic techniques and their structures were elucidated by means of NMR spectrum. After the whole body was irradiated with 6Gy^60Coγ-rays, the peripheral WBC, RBC, HGB, PLT were detected on 1,3,7,10,14,21 d respectively. Results Three compounds were synthesized ; they were 3,5,7,3＇ ,4＇ O-Pentaacetylcatechin ,5,7,3 ＇ , 4＇ -O-Tetrabenzoylcatechin, 3,5,7,3 ＇ , 4＇ -O-Tetrapropionylcatechin. Conclusion 3,5,7,3＇ ,4＇ -O-Pentaacetylcatechin showed antiradiation activtiy, but not as strong as catechin.