三白草酮衍生物的合成及其保肝活性研究

Study on Synthesis and Hepatoprotective Activities of Sauchinone Derivatives

目的对三白草中具有保肝活性的成分三白草酮进行结构修饰,意图得到保肝活性更强的衍生物。方法以三白草酮为原料,在四氢呋喃-甲醇碱性体系中,用NaBH4将C-2’羰基还原为羟基得衍生物A;再以乙酸酐为乙酰化试剂,DMAP为催化剂,吡啶为溶剂将该羟基酰化得衍生物B。以四氯化碳小鼠急性肝损伤模型考察衍生物的保肝降酶活性。结果得到2个尚未见文献报导的三白草酮衍生物A和B,其结构经1 H NMR,13 C NMR和Q-TOF-MS确定。药理实验表明A的降酶效果比三白草酮要好,B与三白草酮相当。结论将三白草酮中羰基还原为羟基能增强降酶活性,该羟基酰化后降酶活性与三白草酮相当。

OBJECTIVE To modify the structure of Sauchinone,an hepatoprotective ingredient,to obtain the derivatives with better hepatoprotective activity.METHODS Sauchinone was taken as the primary material and derivative A was obtained through C-2＇ hydroxyl reduction to be carbonyl with NaBH4 in tetrahydrofuran-methanol alkaline system; acetic anhydride taken as acetylating agent,DMAP as catalyst and pyridine as solvent,the hydroxyl was acylated to get derivative B.Hepatoprotective enzyme activity of derivatives was investigated with carbon tetrachloride-induced acute liver injury mice.RESULTS Saururaceae derivatives A and B were obtained unwritten in any literature,whose structures were confirmed through 1 H NMR,13C NMR and Q-TOF-MS.Pharmacological experiments showed that the lowering transaminase effect of A was better than that of Sauchinone while B has the same effect with Sauchinone.CONCLUSION The lowering transaminase effect can be enhanced through hydroxyl reduction to be carbonyl,which shows the same effect with Sauchinone after acylating.