Kazan Federal University, A.M. Butlerov Chemistry Institute, 420008 Kremlevskaya, 18, Kazan, Russian Federation.
Kazan Federal University, A.M. Butlerov Chemistry Institute, 420008 Kremlevskaya, 18, Kazan, Russian Federation.
Bioorg Chem. 2021 Dec;117:105415. doi: 10.1016/j.bioorg.2021.105415. Epub 2021 Oct 11.
Pillar[5]arenes containing sulfonate fragments have been shown to form supramolecular complexes with therapeutic proteins to facilitate targeted transport with an increased duration of action and enhanced bioavailability. Regioselective synthesis was used to obtain a water-soluble pillar[5]arene containing the fluorescent label FITC and nine sulfoethoxy fragments. The pillar[5]arene formed complexes with the therapeutic proteins binase, bleomycin, and lysozyme in a 1:2 ratio as demonstrated by UV-vis and fluorescence spectroscopy. The formation of stable spherical nanosized macrocycle/binase complexes with an average particle size of 200 nm was established by dynamic light scattering and transmission electron microscopy. Flow cytometry demonstrated the ability of macrocycle/binase complexes to penetrate into tumor cells where they exhibited significant cytotoxicity towards A549 cells at 10-10 M while maintaining the enzymatic activity of binase.
含磺酸酯片段的支柱芳烃已被证明可以与治疗性蛋白质形成超分子复合物，从而促进靶向运输，延长作用时间并提高生物利用度。采用区域选择性合成方法得到了一种含有荧光标记物 FITC 和九个磺乙氧基片段的水溶性支柱[5]芳烃。紫外可见光谱和荧光光谱表明，该支柱[5]芳烃与酶制剂枯草溶菌素、博来霉素和溶菌酶以 1:2 的比例形成配合物。动态光散射和透射电子显微镜表明，形成了稳定的球形纳米大环/枯草溶菌素复合物，平均粒径为 200nm。流式细胞术表明，大环/枯草溶菌素复合物能够穿透肿瘤细胞，在 10-10 M 时对 A549 细胞表现出显著的细胞毒性，同时保持枯草溶菌素的酶活性。
