Abstract：
Most supramolecular systems were discovered by using a trial-and-error approach, leading to numerous synthetic efforts to obtain optimal supramolecular building blocks for selective guest encapsulation. Here, we report a simple coassembly strategy for preparing tamoxifen-selective supramolecular nanomaterials in an aqueous solution. The synthetic amphiphile molecule, 1,1,2,2-tetraphenylethylene (TPE), promotes large tamoxifen aggregate disassembly into smaller, discrete aggregates such as ribbon-like and micellar assemblies in coassembled solutions, enhancing the solubility and dispersion. The TPE moiety exhibits enhanced emission upon tamoxifen interaction, enabling the observation of the coassembled species in an aqueous solution for cell imaging. The tamoxifen-selective fluorescent micelles in the presence of a 1:1 molar ratio of TPE derivative with tamoxifen show enhanced tamoxifen absorption and anticancer effects against MCF-7 breast cancer cells. These supramolecular approaches, based on the coassembly of building blocks with molecular structural similarity, can provide a novel strategy for the efficient development of selective molecular carriers with enhanced biological activities.
摘要：
大多数超分子系统是通过反复试验的方法发现的，导致许多合成努力，以获得最佳的超分子结构单元用于选择性客体封装。这里,我们报道了一种在水溶液中制备他莫昔芬选择性超分子纳米材料的简单共组装策略。合成两亲物分子，1,1,2,2-四苯基乙烯(TPE),促进大的他莫昔芬聚集体分解为较小的，离散聚集体，如共组装溶液中的带状和胶束组件，提高溶解性和分散性。TPE部分在他莫昔芬相互作用时表现出增强的发射，能够观察水溶液中的共组装物种以进行细胞成像。在TPE衍生物与他莫昔芬的摩尔比为1:1的情况下,他莫昔芬选择性荧光胶束显示出增强的他莫昔芬吸收和对MCF-7乳腺癌细胞的抗癌作用。这些超分子方法，基于具有分子结构相似性的结构单元的共同组装，可以为高效开发具有增强生物活性的选择性分子载体提供新的策略。
