Cytotoxic activity of G3 PAMAM-NH2 dendrimer-chlorambucil conjugate in human breast cancer cells

被引:37
|
作者
Bielawski, Krzysztof [1 ]
Bielawska, Anna [1 ]
Muszynska, Anna [1 ]
Poplawska, Bozena [1 ]
Czarnomysy, Robert [1 ]
机构
[1] Med Univ Bialystok, Dept Med Chem, PL-15089 Bialystok, Poland
关键词
Breast cancer; Chlorambucil; PAMAM dendrimer; Collagen biosynthesis; DRUG-DELIVERY; APOPTOSIS; ASSAY; SERA;
D O I
10.1016/j.etap.2011.08.002
中图分类号
X [环境科学、安全科学];
学科分类号
08 ; 0830 ;
摘要
Evaluation of the cytotoxicity of a novel G3 PAMAM-NH2 dendrimer-chlorambucil conjugate employing a MTT assay and inhibition of [H-3]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 breast cancer cells demonstrated that the conjugate was more potent antiproliferative agent than chlorambucil. It was found that dendrimer-chlorambucil conjugate was more active inhibitor of collagen biosynthesis than chlorambucil. Our experiments carried out with flow cytometry assessment of annexin V binding and fluorescent microscopy assay revealed that PAMAM-CH conjugate inhibited the proliferation of MCF-7 and MDA-231 malignant cells by increasing the number of apoptotic and necrotic cells. The apoptotic effect of PAMAM-CH conjugate was found to be stronger than that caused by chlorambucil. (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:364 / 372
页数:9
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