【作者】 杨洋； 张瀛溟； 刘育；

【Author】 Yang Yang;Ying-Ming Zhang;Yu Liu;School of Chemical Engineering and Technology, Hebei University of Technology;Department of Chemistry, Nankai University;

【机构】 河北工业大学化工学院； 南开大学化学学院；

【摘要】 喜树碱及其类似物是一类重要的抗癌药物,但其不良的水溶性、不稳定性和缺乏靶向性限制了喜树碱的疗效和应用。我们将天然环糊精通过"click"方法连接到喜树碱上,大大增加了喜树碱在水中的溶解度,然后将其与金刚烷修饰透明质酸^[1]混合,利用环糊精与金刚烷间强烈的主客体包结作用以及包合物的两亲性作用构筑以亲水的和靶向性的透明质酸为外壳,疏水喜树碱为内核的纳米粒子。该纳米粒子经过核磁滴定,AFM,TEM和DLS的表征,证明其大小在100 nm左右,表面带有负电荷。该纳米粒子不但能够增强喜树碱的水溶性,而且使得喜树碱处于疏水环境中,使其不易水解失活。细胞实验表明该纳米粒子展现出与喜树碱相类似的抗癌活性和对正常细胞更低的毒副作用,归因于纳米粒子表面透明质酸的靶向识别癌细胞作用。更多还原

【Abstract】 Cyclodextrin modified camptothecin(CPT-CD) was synthesized by "click chemistry", and then was mixed with adamantane modified hyaluronic acid(HA-ADA). After that, a novel supramolecular nanoparticle was obtained based on supramolecular interactions and amphiphilic interactions. Moreover, the nanoparticles were characterized by means of ~1H NMR titration, AFM, TEM, and DLS, and exhibited similar anti-cancer activities with, but much lower side effects than camptothecin through the cytotoxicity experiments.更多还原