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硼载脂质体的内吞作用机制及细胞毒性

The Endocytic Mechanism and Cytotoxicity of Boron-Containing Vesicles.

机构信息

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College.

Beijing Key Laboratory of Molecular Pharmaceutics and State Key Laboratory of Natural and Biomimetic Drugs, Peking University.

出版信息

Chem Pharm Bull (Tokyo). 2020 Jul 1;68(7):618-627. doi: 10.1248/cpb.c19-00971. Epub 2020 May 12.

DOI:10.1248/cpb.c19-00971
PMID:32404579
Abstract

A novel polymer (PEG-carborane), self-assembling into spherical vesicles (boron-containing vesicles, BCVs), could be quickly taken up by tumor cells and had an enhance stability in the bloodstream in previous study. To have more comprehensive understanding of BCVs, endocytic mechanism and cytotoxicity assessment were conducted. The results showed that BCVs were taken up in the intact form with cholesterol-dependent pathway during endocytosis, and BCVs exhibited nearly no cytotoxicity. BCVs could accumulate within tumors for at least 24 h. The data would provide reference information and guidance for BCVs' multifunctional application serving as a boron delivery agent for boron neutron capture therapy (BNCT), a hydrophilic and/or hydrophobic drug carrier and a diagnostic imaging fluorescent probe.

摘要

一种新型聚合物(PEG-卡硼烷)可以自组装成球形囊泡(含硼囊泡,BCVs),在之前的研究中,它可以被肿瘤细胞快速摄取,并在血液中具有增强的稳定性。为了更全面地了解 BCVs,进行了内吞作用机制和细胞毒性评估。结果表明,BCVs 通过胆固醇依赖性途径以内吞作用的完整形式被摄取,并且 BCVs 几乎没有细胞毒性。BCVs 可以在肿瘤内至少积累 24 小时。这些数据将为 BCVs 的多功能应用提供参考信息和指导,作为硼中子俘获治疗(BNCT)的硼供体、亲水性和/或疏水性药物载体以及诊断成像荧光探针。

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