Cellular Internalization and Cytotoxicity of Aptamers Selected from Lung Cancer Cell

¹ Beijing National Laboratory for Molecular Sciences，Key Laboratory of Molecular Nanostructure and Nanotechnology, Institute of Chemistry, Chinese Academy of Sciences, Beijing, P. R. China

² Biomedicine Engineering Center of Hunan University, Changsha, China
^*Corresponding author:

Xiaohong Fang, PhD

Beijing National Laboratory for Molecular Sciences

Key Laboratory of Molecular Nanostructure and Nanotechnology

Institute of Chemistry

Chinese Academy of Sciences

Beijing 100190, P. R. China

Email: xfang@iccas.ac.cn

Abstract

       In this work, single-stranded DNA (ssDNA) aptamers against EGFR-transfected A549 cells, one type of non-small cell lung cancer (NSCLC) cells, were selected by cell-SELEX (systematic evolution of ligands by exponential enrichment) and were evaluated. The selected aptamers had high affinity to the A549 cells with dissociation constants in the nanomolar rang. Moreover, the aptamers were able to internalize into the cells, which is advantageous over most of the other existing aptamers. One of the selected aptamers showed significant cytotoxicity by inhibiting the cell proliferation and inducing cell apoptosis. These aptamers are expected to be new molecular probes for cancer cell targeting and drug delivery.

Keywords: aptamer, cell-SELEX, lung cancer cell, internalization, proliferation inhibition.

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