赖氨甘草次酸增溶及对结肠癌HCT-8细胞增殖抑制作用∗

摘要

目的：制备赖氨甘草次酸，研究其增溶作用及其对结肠癌HCT-8细胞增殖的抑制作用。方法采用共研磨法制备赖氨甘草次酸，采用粉末X射线衍射法与红外光谱法对制备的赖氨甘草次酸进行表征，采用高效液相色谱法测定赖氨甘草次酸的增溶作用，采用噻唑蓝( MTT)法评价赖氨甘草次酸对结肠癌HCT-8细胞增殖的抑制作用。结果制备获得赖氨甘草次酸。通过与赖氨酸成盐，甘草次酸溶解度提高约260倍，对结肠癌HCT-8细胞增殖的抑制作用提高约7倍。结论赖氨甘草次酸较甘草次酸溶解度高，抗结肠癌HCT-8细胞效果好。%Objective To prepare,characterize glycyrrhetinic acid lysinate,and study the solubilization and inhibitory action antitumor activity of glycyrrhetinic acid lysinate on cell proliferation of colorectal cancer cell line HCT-8. Methods Glycyrrhetinic acid lysinate was prepared by co-grinding glycyrrhetinic acid with lysine in 1∶1 molar mixture for 10 hours. Characterization of glycyrrhetinic acid lysinate was achieved by X-ray powder diffraction, infrared spectroscopy, and ultraviolet spectrum techniques.HPLC method was used to study the solubilization of glycyrrhetinic acid lysinate.The MTT method was used to assay the inhibitory action of glycyrrhetinic acid lysinate on cell proliferation. Results The solubility of glycyrrhetinic acid lysinate was enhanced 260 folds,compared with glycyrrhetinicacid in water. The inhibitory cell proliferation action on HCT-8 of glycyrrhetinic acid lysinate was 7 times higher than that of glycyrrhetinic acid. Conclusion The satisfactory water solubility and antitumor activity of glycyrrhetinic acid lysinate will be potentially useful for its application as a new pharmaceutical formulation in cancer treatment in the future.