文章摘要
徐春蕾,张芳,陈宏降,李祥.三白草酮衍生物的合成及其保肝活性研究[J].南京中医药大学学报(自然科学版),2014,30(5):465-467.
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
投稿时间:2014-04-11  修订日期:2014-07-12
DOI:
中文关键词: 三白草酮  结构修饰  衍生物  保肝活性
英文关键词: sauchinone  structural modification  derivative  hepatoprotective activity
基金项目:
作者单位
徐春蕾,张芳,陈宏降,李祥* 南京中医药大学药学院江苏 南京 ;210023 
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中文摘要:
      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1H NMR,13C 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。
英文摘要:
      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 1H 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.
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