Study on Synthesis and Hepatoprotective Activities of Sauchinone Derivatives

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.