Ng Yoke Mooi, Coghi Paolo, Ng Jerome P L, Ali Fayaz, Wong Vincent Kam Wai, Coluccini Carmine
Institute of New Drug Development, College of Medicine, China Medical University, No. 91 Hsueh-Shih Road, Taichung 40402, Taiwan.
School of Pharmacy, Macau University of Science and Technology, Macau 999078, China.
Polymers (Basel). 2021 Nov 26;13(23):4133. doi: 10.3390/polym13234133.
In this study, a full organic and water-soluble material was synthesized by coupling low molecular weight polyethylenimine (PEI-800) with cyclotriveratrilene (CTV). The water-soluble cross-linked polymer contains hydrophobic holes with a high coordination capability towards different organic drug molecules. The coordinating capability towards hydrophilic drugs (doxorubicin, gatifloxacin and sinomenine) and hydrophobic drugs (camptothecin and celastrol) was analyzed in an aqueous medium by using NMR, UV-Vis and emission spectroscopies. The coordination of drug molecules with the armed CTV unit through hydrophobic interactions was observed. In particular, celastrol exhibited more ionic interactions with the PEI moiety of the hosting system. In the case of doxorubicin, the host-guest detachment was induced by the addition of ammonium chloride, suggesting that the intracellular environment can facilitate the release of the drug molecules.
在本研究中，通过将低分子量聚乙烯亚胺（PEI - 800）与环三聚藜芦烃（CTV）偶联，合成了一种全有机且水溶性的材料。这种水溶性交联聚合物含有对不同有机药物分子具有高配位能力的疏水孔。通过核磁共振（NMR）、紫外可见光谱（UV - Vis）和发射光谱等方法，在水介质中分析了其对亲水性药物（阿霉素、加替沙星和青藤碱）和疏水性药物（喜树碱和雷公藤红素）的配位能力。观察到药物分子通过疏水相互作用与带臂CTV单元的配位情况。特别地，雷公藤红素与主体体系的PEI部分表现出更多的离子相互作用。在阿霉素的情况下，加入氯化铵会诱导主客体分离，这表明细胞内环境可促进药物分子的释放。
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