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目的合成吲哚美辛-聚乙二醇-1500(polyethylene glycol,PEG-1500)酯并考察其在水中的溶解度和体外抗肿瘤活性。方法通过吲哚美辛的羰基与PEG的羟基反应合成目标化合物羧酸酯;测定吲哚美辛-PEG-1500酯和吲哚美辛在水中的溶解度和熔点;以吲哚美辛原料药作为阳性对照药,采用MTT法测试目标化合物对HCT116人结肠癌细胞的生长抑制活性。结果合成的目标化合物的结构经IR、1H-NM R得到确证;吲哚美辛-PEG-1500酯比吲哚美辛有更好的水溶性;吲哚美辛和吲哚美辛-PEG-1500酯对HCT116人结肠癌细胞有相近的抑制作用。结论吲哚美辛-PEG-1500酯的合成不仅解决了IM C水溶性差的问题,而且也为其他同属于有机弱酸类且水溶性较差的药物解决相同或相似的问题提供了一个新的思路,具有较好的发展前景。
OBJECTIVE To synthesize indomethacin polyethylene glycol (PEG-1500) and investigate its solubility in water and in vitro antitumor activity. Methods The objective carboxylic acid esters were synthesized by the reaction of carbonyl groups of indomethacin with the hydroxyl groups of PEG. The solubility and melting point of indomethacin-PEG-1500 ester and indomethacin in water were determined. The indomethacin drug substance was used as Positive control drug, the growth inhibition activity of the target compound on HCT116 human colon cancer cells was tested by MTT method. Results The structures of target compounds were confirmed by IR, 1H-NM R; indomethacin-PEG-1500 ester showed better water solubility than indomethacin; indomethacin and indomethacin-PEG- 1500 ester HCT116 human colon cancer cells have a similar inhibitory effect. Conclusion The synthesis of indomethacin-PEG-1500 ester not only solves the problem of poor aqueous solubility of IM C, but also provides a new idea for solving the same or similar problems with other drugs that belong to the class of weak organic acids and have poor water solubility. , Has a good development prospects.