SciELO - Scientific Electronic Library Online

 
vol.57 issue3Transfer Hydrogenation Reactions of Photoactivatable N,N'-Chelated Ruthenium(II) Arene ComplexesSpectroscopic Characterization of an Oxovanadium(IV) Complex of Oxodiacetic Acid and 2,2'-Bipyridine: Bioactivity on Osteoblast-Like Cells in Culture author indexsubject indexsearch form
Home Pagealphabetic serial listing  

Services on Demand

Journal

Article

Indicators

Related links

  • Have no similar articlesSimilars in SciELO

Share


Journal of the Mexican Chemical Society

Print version ISSN 1870-249X

Abstract

ESTRADA, Jesús G.  and  SANCHEZ-DELGADO, Roberto A.. Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin. J. Mex. Chem. Soc [online]. 2013, vol.57, n.3, pp.169-174. ISSN 1870-249X.

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), [RuII6-p-cymene)Cl2(KTZ)] (3), [RuII6-p-cymene)(en)(KTZ)][BF4]2 (4), [RuII6-p-cymene)(bipy)(K TZ)][BF4]2 (5), and [RuII6-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.

Keywords : Ruthenium; ketoconazole; antiparasitic; albumin; transferrin; fluorescence.

        · abstract in Spanish     · text in English     · English ( pdf )

 

Creative Commons License All the contents of this journal, except where otherwise noted, is licensed under a Creative Commons Attribution License