肝素-紫杉醇抗癌药物系统的合成及其对癌细胞生长抑制的研究

Study of the Synthetic of Heparin-Paclitaxel Anti-cancer Drug and Its Inhibitory Effect to Cancer Cells

为解决紫杉醇作为抗癌药物水溶性差毒性大的缺点,采用天然生物大分子肝素为载体,利用其具有良好的生物相容性、生物降解性以及良好的水溶性特征,选用三种带有不同a-取代基的氨基酸作为连接臂,设计合成了一类新型肝素-氨基酸-紫杉醇药物输送系统,目标产物用1H NMR进行了结构表征.体外水解动力学测试结果表明该系统水溶性好,MTT法测试结果表明所有化合对MCF-7(乳腺癌细胞)细胞毒活性优于紫杉醇.

To improve the poor water solubility and toxicity of paclitaxel as an anticancer drug,the novel drug delivery systems of heparin-paclitaxel-amino acids has been designed.The natural biomacromolecule of heparin is used as the carrier for its better biocompatibility,biodegradability and water solubility,and three amino acids with different-substituents are used as linking arms in the novel drug delivery,and desired products are characterized by 1H NMR.Experimental results of hydrolysis kinetics show the novel drug delivery system has better water solubility,and experimental results of MTT show all chemical combination is better than paclitaxel for MCF-7.