ABSTRACT
OBJECTIVE:To prepare argininate betulinic acid,and to investigate the effect of the proliferation of triple-negative human breast cancer cell MDA-MB-231. METHODS:By using argininate as the solubilization carrier,argininate betulinic acid was prepared by co-grinding equal molar ratio of betulinic acid and argininate. The argininate betulinic acid was characterized with powder X-ray diffractometry,infrared spectroscopy and differential scanning calorimetry. The solubility of betulinic acid and argininate betulinic acid were compared. MTT method was used to assay the effects of 15,30,60,120 μ g/mL betulinic acid, argininate betulinic acid and 5-FU on the proliferation of MDA-MB-231 cell. RESULTS:Prepared argininate betulinic acid was a new phase which was different from the physical mixing of argininate and betulinic acid,among which carboxyl group of betulinic acid and amino group of argininate formed as a salt,and the salt had no obvious melting peak. Betulinic acid was almost insoluble in water. The solubility of betulinic acid in argininate betulinic acid aqueous solution was 50.72 μg/mL. Compared with betulinic acid,the inhibitory rate of argininate betulinic acid on the growth of MDA-MB-231 cell was increased significantly(P<0.05), there was no statistical significance between its effect and 5-FU(P>0.05). CONCLUSIONS:Argininate betulinic acid with good solubility is prepared successfully,and can inhibit the proliferation of MDA-MB-231 cell.
ABSTRACT
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.