精氨白桦脂酸的制备及其对三阴性人乳腺癌细胞MDA-MB-231增殖的影响

Preparation of Argininate Betulinic Acid and Its Effect of the Proliferation of Triple-negative Human Breast Cancer Cell MDA-MB-231

目的:制备精氨白桦脂酸,并考察其对三阴性人乳腺癌细胞MDA-MB-231增殖的影响。方法:以精氨酸为增溶载体,采用共研磨法将等摩尔比的白桦脂酸与精氨酸制成精氨白桦脂酸。采用粉末X射线衍射法、红外光谱法、差示扫描量热法对精氨白桦脂酸进行表征;比较白桦脂酸和精氨白桦脂酸的溶解度;采用MTT法检测15、30、60、120μg/mL的白桦脂酸、精氨白桦脂酸和5氟尿嘧啶(5-FU)对MDA-MB-231细胞增殖的影响。结果:所制精氨白桦脂酸为不同于精氨酸与白桦脂酸物理叠加的新的物相,其中白桦脂酸的羧基与精氨酸中氨基进行了成盐反应,其未见明显的熔点峰。白桦脂酸几乎不溶于水,精氨白桦脂酸水溶液中白桦脂酸的溶解度为50.72μg/mL。与白桦脂酸比较,精氨白桦脂酸对MDA-MB-231细胞的增殖抑制率明显升高(P<0.05),且与5-FU比较差异无统计学意义(P>0.05)。结论:成功制得溶解度较好的精氨白桦脂酸,其对MDA-MB-231细胞的增殖具有抑制作用。

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 15,30,60,120μg/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 50.72μg/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.