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Tadpole-shaped beta-cyclodextrin-tagged poly(N-vinylpyrrolidone): synthesis, characterization and studies of its complexation with phenolphthalein and anti tumor activities

机译:形β-环糊精标记的聚(N-乙烯基吡咯烷酮):其合成,表征及其与酚酞的络合和抗肿瘤活性的研究

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摘要

Tadpole-shaped beta-cyclodextrin-tagged poly(N-vinylpyrrolidone) (beta-CD-PNVP) has been synthesised via the click reaction of alkyne-terminated PNVP and azide-functionalized beta-CD. The formed polymer is characterized by H-1 NMR, FTIR, and TGA study. The complexing ability of such a polymer with phenolphthalein is considerably lower with respect to that with beta-CD alone. Doxorubicin (DOX)-loaded beta-CD-PNVP (DOX-beta-CD-PNVP) exhibits higher tumoricidal activity against a panel of tumor cell lines derived from sarcoma (U2-OS) and carcinomas (MCF-7 and HEPG2), causing significant lysis of tumor cells compared to free DOX. The formulation also demonstrates significantly higher uptake by the tumor cells and enhances apoptosis compared to free DOX.
机译:via形的β-环糊精标记的聚(N-乙烯基吡咯烷酮)(β-CD-PNVP)是通过炔基封端的PNVP和叠氮化物官能化的β-CD的点击反应合成的。通过H-1 NMR,FTIR和TGA研究对形成的聚合物进行表征。相对于单独的β-CD,这种聚合物与酚酞的络合能力要低得多。装载阿霉素(DOX)的β-CD-PNVP(DOX-β-CD-PNVP)对来自肉瘤(U2-OS)和癌症(MCF-7和HEPG2)的一组肿瘤细胞系表现出更高的杀伤活性与游离DOX相比,肿瘤细胞发生了明显的裂解。与游离DOX相比,该制剂还显示出明显更高的被肿瘤细胞摄取并增强了细胞凋亡。

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