Shanghai Key Laboratory of Functional Materials Chemistry, Institute of Fine Chemicals, East China University of Science and Technology, Shanghai 200237, PR China.
Org Biomol Chem. 2012 Jul 21;10(27):5238-44. doi: 10.1039/c2ob25701g. Epub 2012 May 31.
A series of anticancer prodrugs with different chemical functional groups were prepared, in which the styryl conjugated 2-nitrobenzyl derivatives were introduced as the phototrigger to regulate the drug (chlorambucil) release. Compared to the common 4,5-dimethoxy-2-nitrobenzyl caged compounds, most of the prodrugs exhibited large and redshifted one-photon absorption within the visible range. One-photon excitation for the drug release was studied by measuring UV-vis absorption, FT-IR, and HPLC spectra, which suggested that chlorambucil was released effectively and precisely by manipulating external light conditions. And the introduction of different functional groups made this type of prodrug a good platform to further react with some typical drug carriers and to further form excellent visible light responsive drug delivery systems. Moreover, the drug also could be effectively released under the excitation of two-photon at 800 nm with comparable photorelease efficiencies.
一系列具有不同化学官能团的抗癌前药被制备出来，其中引入了苯乙烯共轭 2-硝基苄基衍生物作为光触发物来调节药物（苯丁酸氮芥）的释放。与常见的 4,5-二甲氧基-2-硝基苄基笼状化合物相比，大多数前药在可见光范围内表现出较大的红移单光子吸收。通过测量紫外-可见吸收、傅里叶变换红外和高效液相色谱谱图来研究药物释放的单光子激发，结果表明通过操纵外部光照条件可以有效地、精确地释放苯丁酸氮芥。并且，引入不同的官能团使得这种类型的前药成为一个很好的平台，可以进一步与一些典型的药物载体反应，并进一步形成优异的可见光响应药物传递系统。此外，在 800nm 的双光子激发下，药物也能有效地释放，光释放效率相当。
