Clinical Chemistry
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Clinical Chemistry 55: 955-963, 2009. First published March 12, 2009; 10.1373/clinchem.2008.113423
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(Clinical Chemistry. 2009;55:955-963.)
© 2009 American Association for Clinical Chemistry, Inc.

Automation and Analytical Techniques

Tumor Cell Targeting Using Folate-Conjugated Fluorescent Quantum Dots and Receptor-Mediated Endocytosis

Er-Qun Song1, Zhi-Ling Zhang1, Qing-Ying Luo1, Wen Lu1, Yun-Bo Shi2 and Dai-Wen Pang1,a

1 College of Chemistry and Molecular Sciences, Key Laboratory of Analytical Chemistry for Biology and Medicine of the Ministry of Education and State Key Laboratory of Virology, Wuhan University, Wuhan, People’s Republic of China; 2 Section on Molecular Morphogenesis, Program on Cell Regulation and Metabolism, National Institute of Child Health and Human Development, NIH, Bethesda, MD.

aAddress correspondence to this author at: College of Chemistry and Molecular Sciences, Key Laboratory of Analytical Chemistry for Biology and Medicine of the Ministry of Education and State Key Laboratory of Virology, Wuhan University, Wuhan 430072, P. R. China. Fax +86-27-6875-4067; e-mail dwpang{at}whu.edu.cn.

Background: Luminescent nanobioprobes with cell-targeting specificity are likely to find important applications in bioanalysis, biomedicine, and clinical diagnosis. Quantum dots (QDs) are unique and promising materials for such a purpose because of their fluorescence and large surface area for attaching cell-targeting molecules.

Methods: We produced water-dispersible QDs by coating hydrophobic QDs with small amphiphilic polyethylene glycol (PEG) molecules via hydrophobic interactions. We covalently coupled folate (FA) onto the water-dispersible PEG-coated QDs (PEG-QDs) to produce FA-coupled PEG-QDs (FA-PEG-QDs).

Results: These FA-PEG-QD nanoparticles functioned as fluorescent nanobioprobes that specifically recognized folate receptors (FRs) overexpressed in human nasopharyngeal cells (KB cells) but not in an FR-deficient lung carcinoma cell line (A549 cells). Using confocal fluorescence microscopy, we demonstrated uptake of FA-PEG-QDs by KB cells but no uptake of folate-free PEG-QDs. The specificity of this receptor-mediated internalization was confirmed by comparing the uptake by KB vs A549 cells.

Conclusions: Our results suggest that such cell-targeting fluorescent nanobioprobes are potentially very powerful tools for recognizing target cells and delivering and tracking drugs and other therapeutic materials.






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Copyright © 2009 by the American Association for Clinical Chemistry.