PMID: 33205002Nov 19, 2020Paper

Interaction of metallocene dichlorides with apo-human transferrin: A spectroscopic study and cytotoxic activity against human cancer cell lines

International Journal of Molecular Biology : Open Access
Jorge R Güette FernándezElsie I Parés Matos

Abstract

Metallocene dichlorides (Cp2M(IV)Cl2) are the first class of small and hydrophobic organometallic compounds classified as anticancer agents against numerous cancer cell lines and tumors. In this study, the antiproliferative activities of Cp2VCl2,Cp2NbCl2, Cp2HfCl2 and Cp2ZrCl2were assessed on two human cancer cell lines (HT-29 and MCF-7) using MTT assay. Spectroscopic studies were also conducted using these and other known metallocene dichlorides on apo-human transferrin (apo-hTf) at pH 7.4. UV-Vis and CD showed that their interaction with apo-hTf could induce conformational changes of its secondary structure during binding process. In fluorescence, a decrease in intensity of the emission peak was observed when the apo-hTf:Cp2M(IV)Cl2 complex is being formed, probably due to changes in the microenvironment of its tyrosine and tryptophan residues. Among all metallocene dichlorides studied, Cp2VCl2 has the strong ability to quench the intrinsic fluorescence of apo-hTf through a static quenching mechanism. The association constants for each protein-compound complex were also determined at different temperatures (296 K, 303 K, 310 K, and 317 K) based on fluorescence quenching results. Positive enthalpy changes (ΔH) and entropy chan...Continue Reading

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