文献类型：期刊文献

中文题名：单／双光子可激发的香豆素光扳机的光控抗癌前药的设计合成

英文题名：Design and synthesis of photocontrolled anticancer prodrugs based on coumarin phototrigger by one-or two-photo excitation

作者：黄琪[1];包春燕[1];吴润青[1];朱麟勇[1]

机构：[1]华东理工大学化学与分子工程学院,结构可控先进功能材料及其制备教育部重点实验室,上海200237

年份：2013

卷号：8

期号：3

起止页码：263

中文期刊名：中国科技论文

外文期刊名：China Sciencepaper

收录：北大核心:【北大核心2011】；

基金：高等学校博士学科点专项科研基金资助项目(20090074120018);国家自然科学基金资助项目(21173078,51273064);上海市教育委员会科研创新项目

语种：中文

中文关键词：有机合成;香豆素光扳机;苯丁酸氮芥;光控前药;药物释放

外文关键词：organic s ynthesis; coumarin phototrigger; chlorambucil; photocontrolled prodrug; drug release

摘要：利用取代7-氨基香豆素作为光扳机,化学键连苯丁酸氮芥抗癌药物构成光控抗癌前药(前药1～2)。一方面通过引入BOC保护的羧酸功能基团使所得的前药能进一步与载体相连构成光控药物释放体系;另一方面通过引入水溶性PEG来改性前药,使所得的光控前药具有更好的水溶性,以便更好地与生物体系相容。通过HPLC光解测试,证明该两种前药可以在单光子可见光、双光子近红外光激发下有效地释放抗癌药物,相比于其他响应体系,该类体系可以通过控制光的条件来控制药物释放的剂量,显示了其在癌症治疗方面的潜在应用。另外,与HeLa细胞作用后的荧光成像测试证明香豆素光扳机优异的发光性质也为光控前药体系提供了荧光示踪功能。
We used 7-aminocoumarin as phototrigger to cage chlorambucil anticancer drug to constitute photocontrolled anti-cancer prodrugs （prodrugs 1 2）. On the one hand, prodrug 1 was endowed to further connect with carriers to form the photocomrolled drug release system by introducing BOC protected carboxylic acid; on the other hand, in order to improve the water solubility of pmdrug, prodrug 2 was modified by introducing a water soluble PEG substituent, so as to obtain a prodrng with excellent solubility in water and biological compatibility. Photolysis tested by HPLC proved that both of the two prodrngs released the anticancer drug effectively when irradiated by either single photon visible light or two-photon near-infrared light. Compared with other response systems, these phototriggered release systems can control the dose of the drug release accurately by facially controlling the light conditions, which shows potential applications in the cancer therapy. In addition, the fluorescence imaging after cultured with HeLa cells confirmed the fluorescent tracer function of the prodrugs due to the excellent luminescence properties of the coumarin phototrigger.