Constructing transferrin receptor targeted drug delivery system by using doxorubicin hydrochloride and vanadocene dichloride.

Abstract

Transferrin has shown potential in the delivery of anticancer drugs into primarily proliferating malignant cells that over-express transferrin receptors. Constructing transferrin receptor targeted drug delivery system has been widespread concerned. In this study, whether transferrin could transport noncovalent binding drugs into cancer cells has been investigated. Two representative compounds, doxorubicin hydrochloride (Dox) and vanadocene dichloride (Cp(2)VCl(2)), have been chosen to study the interactions with h-Tf and apo-Tf, and the influences in the presence of h-Tf and apo-Tf by using fluorescence spectroscopy, circular dichroism (CD) spectroscopy and MTT assay. The results have shown that both doxorubicin and Cp(2)VCl(2) could bind to h-Tf and apo-Tf but with different binding modes. The results of MTT assay demonstrate that the presence of both h-Tf and apo-Tf has enhanced the antiproliferative activity of Cp(2)VCl(2). However, the anticancer activity of the mixture of doxorubicin and h-Tf is basically the same as that of doxorubicin does. Our studies indicate that transferrin plays an important role in the transport and targeted delivery of Cp(2)VCl(2) into cancer cells.

• Authors: Yanxia Zhang, Junfeng Xiang, Yan Liu, Xiufeng Zhang, Yalin Tang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 19 Pg. 5982-6 (Oct 01 2011) ISSN: 1464-3405 [Electronic] England
• PMID: 21862329 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 Elsevier Ltd. All rights reserved.

Chemical References

• Antibiotics, Antineoplastic
• Antineoplastic Agents
• Drug Carriers
• Receptors, Transferrin
• Transferrin
• Vanadium Compounds
• vanadocene dichloride
• Doxorubicin

Topics

• Antibiotics, Antineoplastic (chemistry, metabolism, pharmacology)
• Antineoplastic Agents (chemistry, pharmacology)
• Biological Transport
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Doxorubicin (chemistry, metabolism, pharmacology)
• Drug Carriers
• Drug Delivery Systems
• Drug Design
• Drug Screening Assays, Antitumor
• Fluorescence
• Humans
• Molecular Conformation
• Molecular Targeted Therapy
• Protein Binding
• Receptors, Transferrin (metabolism)
• Substrate Specificity
• Transferrin (chemistry, metabolism)
• Vanadium Compounds (chemistry, metabolism, pharmacology)