title: 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.affiliation: State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
authors.forename: Yanxia
authors.initials: Y
authors.lastname: Zhang
authors.forename: Junfeng
authors.initials: J
authors.lastname: Xiang
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Xiufeng
authors.initials: X
authors.lastname: Zhang
authors.forename: Yalin
authors.initials: Y
authors.lastname: Tang
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001692:Biological Transport; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005453:Fluorescence; D006801:Humans; D008968:Molecular Conformation; D058990:Molecular Targeted Therapy; D011485:Protein Binding; D011990:Receptors, Transferrin / Q000378:metabolism*; D013379:Substrate Specificity; D014168:Transferrin / Q000737:chemistry / Q000378:metabolism*; D017968:Vanadium Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D004337:Drug Carriers; D011990:Receptors, Transferrin; D014168:Transferrin; D017968:Vanadium Compounds; C030754:vanadocene dichloride; D004317:Doxorubicin