TY - JOUR
T1 - Enhancement of the cytotoxicity of titanocene dichloride by aging in organic co-solvent
AU - Ravera, Mauro
AU - Cassino, Claudio
AU - Monti, Elena
AU - Gariboldi, Marzia
AU - Osella, Domenico
N1 - Funding Information:
This work received the financial support of MIUR (Rome) and CIRCMSB (Bari). The research was carried out within the framework of the European Cooperation COST D20 action (Metal compounds in the treatment of cancer and viral diseases) and the COST B16 action (Multidrug resistance reversal). Thanks are due to Dr. Maurizio Aceto and Dr. Fabio Gosetti (DiSAV, Alessandria) for the GF-AAS and ESI-MS determinations, respectively. We are indebted to Dr. Laura McLean for her assistance in the revision of this manuscript.
PY - 2005/12
Y1 - 2005/12
N2 - Titanocene dichloride exhibits anti-proliferative activity in a wide spectrum of murine and human tumors. Although it is still unclear as to which species are active in biological media, they all readily deliver Ti(IV) to transferrin, the protein that transports iron in the blood. In this article, we report that aging of the complex in alcohols (namely methanol and ethanol) or dimethyl sulfoxide, the co-solvents used to prepare mother solution of the drug, leads to increased cytotoxic activity (i.e. lower IC50 values) in HCT116 colon cancer cell lines, to a different extent. The TiCp 2Cl2 solvolysis was followed by 1H NMR, ESI-MS, electrochemical and conductivity measurements, and the intracellular Ti(IV) uptake was evaluated.
AB - Titanocene dichloride exhibits anti-proliferative activity in a wide spectrum of murine and human tumors. Although it is still unclear as to which species are active in biological media, they all readily deliver Ti(IV) to transferrin, the protein that transports iron in the blood. In this article, we report that aging of the complex in alcohols (namely methanol and ethanol) or dimethyl sulfoxide, the co-solvents used to prepare mother solution of the drug, leads to increased cytotoxic activity (i.e. lower IC50 values) in HCT116 colon cancer cell lines, to a different extent. The TiCp 2Cl2 solvolysis was followed by 1H NMR, ESI-MS, electrochemical and conductivity measurements, and the intracellular Ti(IV) uptake was evaluated.
KW - Anti-proliferative agents
KW - Cellular uptake
KW - Ligand solvolysis
KW - Titanocene
UR - http://www.scopus.com/inward/record.url?scp=28444492702&partnerID=8YFLogxK
U2 - 10.1016/j.jinorgbio.2005.08.003
DO - 10.1016/j.jinorgbio.2005.08.003
M3 - Article
SN - 0162-0134
VL - 99
SP - 2264
EP - 2269
JO - Journal of Inorganic Biochemistry
JF - Journal of Inorganic Biochemistry
IS - 12
ER -