Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin

Authors

  • Jesús G. Estrada The City University of New York
  • Roberto A. Sánchez-Delgado The City University of New York

DOI:

https://doi.org/10.29356/jmcs.v57i3.203

Keywords:

Ruthenium, ketoconazole, antiparasitic, albumin, transferrin, fluorescence

Abstract

The pharmacological properties of any drug are related to its ability to interact with macromolecular blood components. The interaction of human serum albumin (HSA) and apotransferrin (ATf) with six RuII complexes containing ketoconazole (KTZ), which we have previously reported to be active against Leishmania major and Trypanosoma cruzi, has been investigated by monitoring the tryptophan fluorescence intensity of each protein upon incremental addition of the complexes. All the Ru-KTZ derivatives, namely cis-fac-[RuIICl2(DMSO)3(KTZ)] (1), cis-[RuIICl2(bipy)(DMSO)(KTZ)] (2), [RuII(η6-p-cymene)Cl2(KTZ)] (3), [RuII(η6-p-cymene)(en)(KTZ)][BF4]2 (4), [RuII(η6-p-cymene)(bipy)(KTZ)][BF4]2 (5), and [RuII(η6-p-cymene)(acac)(KTZ)][BF4] (6) are able to quench the intrinsic fluorescence of HSA and ATf at 27 ºC. Analysis of the spectroscopic data using Stern-Volmer plots indicates that in both cases the quenching takes place principally through a static mechanism involving the formation of Ru complex-protein adducts; further analysis of the fluorescence data allowed the estimation of apparent association constants and the number of binding sites for each protein and each compound. The results indicate that both HSA and ATf are possible effective transporters for Ru-KTZ antiparasitic drugs.

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Author Biographies

Jesús G. Estrada, The City University of New York

Brooklyn College and The Graduate Center

Roberto A. Sánchez-Delgado, The City University of New York

Brooklyn College and The Graduate Center

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Published

2017-10-12

Issue

Vol. 57 No. 3 (2013): Special Issue on Bioinorganic Chemistry

Section

Regular Articles

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