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Post-functionalization of drug-loaded nanoparticles prepared by polymerization-induced self-assembly (PISA) with mitochondria targeting ligands
Beilstein Journal of Organic Chemistry ( IF 2.7 ) Pub Date : 2021-09-03 , DOI: 10.3762/bjoc.17.148
Janina-Miriam Noy 1 , Fan Chen 1 , Martina Stenzel 1
Affiliation  

Herein, the postfunctionalization of different non-fouling PISA particles, prepared from either poly(oligo ethylene glycol methyl ether methacrylate) (pPEGMA) and the anticancer drug PENAO (4-(N-(S-penicillaminylacetyl)amino)phenylarsenonous acid) or zwitterionic 2-methacryloyloxyethyl phosphorylcholine (MPC) and PENAO were reported. Both PISA particles were reacted with triphenylphosphonium (TPP) as mitochondria targeting units in order to evaluate the changes in cellular uptake or the toxicity of the conjugated arsenic drug. Attachment of TPP onto the PISA particles however was found not to enhance the mitochondrial accumulation, but it did influence overall the biological activity of pMPC-based particles in 2D and 3D cultured sarcoma SW982 cells. When TPP was conjugated to the pMPC PISA particles more cellular uptake as well as better spheroid penetration were observed, while TPP on PEG-based PISA had only little effect. It was hypothesized that TPP on the micelle surface may not be accessible enough to allow mitochondria targeting, but more structural investigations are required to elucidate this.

中文翻译:

通过聚合诱导自组装 (PISA) 与线粒体靶向配体制备的载药纳米颗粒的后功能化

在此,由聚(低聚乙二醇甲基醚甲基丙烯酸酯)(pPEGMA)和抗癌药物 PENAO(4-(N -(S-青霉胺基乙酰基)氨基)苯基砷酸)或两性离子 2-甲基丙烯酰氧基乙基磷酰胆碱 (MPC) 和 PENAO。两种 PISA 颗粒都与作为线粒体靶向单元的三苯基鏻 (TPP) 反应,以评估细胞摄取的变化或结合砷药物的毒性。然而,发现将 TPP 附着在 PISA 颗粒上不会增强线粒体积累,但它确实影响了基于 pMPC 的颗粒在 2D 和 3D 培养的肉瘤 SW982 细胞中的整体生物活性。当 TPP 与 pMPC PISA 颗粒结合时,观察到更多的细胞摄取以及更好的球体渗透,而 TPP 对基于 PEG 的 PISA 的影响很小。假设胶束表面上的 TPP 可能无法足够接近以允许线粒体靶向,
更新日期:2021-09-03
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