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
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篇名: 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
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摘要: 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、120 μg/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50.72 μg/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。
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 μg/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.
期刊: 2018年第29卷第7期
作者: 张丽娟,刘永红,古同男,钟家亮
AUTHORS: ZHANG Lijuan,LIU Yonghong,GU Tongnan,ZHONG Jialiang
关键字: 精氨白桦脂酸;表征;增溶;三阴性人乳腺癌细胞MDA-MB-231;增殖抑制
KEYWORDS: Argininate betulinic acid; Characterization; Solubilization; Triple-negative human breast cancer cell MDA-MB- 231; Proliferation inhibition
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