赖氨大黄酸盐的合成工艺及活性研究

目的制备水溶性大黄酸衍生物。方法以大黄酸为起始原料,制备大黄酸的赖氨酸水溶液,在30℃反应24 h,然后加入一定量丙酮使其结晶析出,得到晶体物质。根据2005年药典方法检测其在水中溶解度,用MTT法检测新化合物对细胞增殖的影响。结果目标化合物经HPLC、红外光谱和1H-NMR确证。赖氨大黄酸在水中溶解度为15 g.L？1,其在抑制肿瘤细胞和内皮细胞增殖方面与大黄酸相当。结论获得了水溶性好的大黄酸衍生物——赖氨大黄酸,并且其活性与大黄酸相当。

Synthesis and Activity of Rhein Lysinate

OBJECTIVE To prepare the derivate of Rhein dissoluble in water.METHODS The target compound was prepared from Rhein,reacted at 30 ℃ for 24 h.Then it was precipitated and dried.The determination of the dissolubility of Rhein lysinate was based on Ch.P（2005）.The effect of Rhein lysinate on cell proliferation was detected by MTT.RESULTS The structure of new compound was confirmed by HPLC,IR and 1H-NMR.The dissolubility of Rhein lysinate in water was 15 g.L？1.CONCLUSION The derivate of Rhein,Rhein lysinate,can dissolve in water and have the same effect on cell proliferation with Rhein.