用生物素-树枝状聚合物偶联物靶向癌细胞。

Targeting cancer cells with biotin-dendrimer conjugates.

作者信息

Yang Wenjun, Cheng Yiyun, Xu Tongwen, Wang Xueyuan, Wen Long-Ping

机构信息

Hefei National Laboratory for Physical Sciences at Microscale and School of Life Sciences, University of Science and Technology of China, Hefei, Anhui 230027, China.

出版信息

Eur J Med Chem. 2009 Feb;44(2):862-8. doi: 10.1016/j.ejmech.2008.04.021. Epub 2008 May 9.

DOI:10.1016/j.ejmech.2008.04.021

PMID:18550227

Abstract

Star-burst dendrimers represent a superior carrier platform for targeted drug delivery. Partially acetylated generation 5 (G5) polyamidoamine (PAMAM) dendrimer was conjugated with the targeting moiety (biotin) and the imaging moiety (fluoresceinisothiocyanate, FITC), and the resulting dendrimer-biotin conjugate was characterized by (1)H NMR, UV-vis spectrum. As revealed by flow cytometry and confocal microscopy, the bifunctional conjugate (dendrimer-biotin-FITC) exhibited much higher cellular uptake into HeLa cells than the conjugate without biotin. The uptake was energy-dependent, dose-dependent, and could be effectively blocked by dendrimer-conjugated biotin. Our results indicated that the biocompatible biotin-dendrimer conjugate might be a promising nano-platform for cancer therapy and cancer diagnosis.

摘要

星爆树枝状大分子是一种用于靶向药物递送的优质载体平台。将部分乙酰化的第5代（G5）聚酰胺-胺（PAMAM）树枝状大分子与靶向部分（生物素）和成像部分（异硫氰酸荧光素，FITC）偶联，通过1H NMR、紫外可见光谱对所得树枝状大分子-生物素偶联物进行表征。流式细胞术和共聚焦显微镜显示，双功能偶联物（树枝状大分子-生物素-FITC）对HeLa细胞的细胞摄取比不含生物素的偶联物高得多。摄取是能量依赖性和剂量依赖性的，并且可以被树枝状大分子偶联的生物素有效阻断。我们的结果表明，生物相容性生物素-树枝状大分子偶联物可能是一种用于癌症治疗和癌症诊断的有前景的纳米平台。