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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。
Objective To prepare water-soluble rhein derivatives. Methods Rhein was used as the starting material to prepare the lysine solution of rhein, which was reacted at 30 ℃ for 24 h. Then a certain amount of acetone was added to crystallize it to obtain the crystal material. According to the 2005 Pharmacopoeia method to detect its solubility in water, using MTT assay of new compounds on cell proliferation. Results The target compounds were confirmed by HPLC, IR and 1H-NMR. Lysine has a solubility in water of 15 g.L -1, which is comparable to rhein in inhibiting the proliferation of tumor cells and endothelial cells. Conclusion A good water-soluble rhein derivative, Rhein, was obtained and its activity was comparable to Rhein.