Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin
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| Format: | Artículo científico |
| Sprache: | en |
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Sociedad Química de México
2013
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| _version_ | 1876449401580290048 |
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| author | Jesús G. Estrada |
| author_facet | Jesús G. Estrada |
| contents | Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin Jesús G. Estrada Roberto A. Sánchez-Delgado Multidisciplinaria (Ciencias Naturales y Exactas) rin albumin transfer Ruthenium ketoconazole 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 apotransfer - rin (ATf) with six Ru II complexes containing ketoconazole (KTZ), which we have previously reported to be active against Leishmania major and Trypanosoma cruzi , has been investigated by monitor - ing the tryptophan fluorescence intensity of each protein upon in - cremental addition of the complexes. All the Ru-KTZ derivatives, namely cis-fac -[Ru II Cl 2 (DMSO) 3 (KTZ)] ( 1 ), cis -[Ru II Cl 2 (bipy)(D MSO)(KTZ)] ( 2 ), [Ru II ( η 6 - p -cymene)Cl 2 (KTZ)] ( 3 ), [Ru II ( η 6 - p - cymene)(en)(KTZ)][BF 4 ] 2 ( 4 ), [Ru II ( η 6 - p -cymene)(bipy)(KTZ)][BF 4 ] 2 ( 5 ), and [Ru II ( η 6 - p -cymene)(acac)(KTZ)][BF 4 ] ( 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 mecha - nism 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. 2013 artículo científico 1870-249X https://www.redalyc.org/articulo.oa?id=47529964003 en http://www.redalyc.org/revista.oa?id=475 Journal of the Mexican Chemical Society application/pdf Sociedad Química de México Journal of the Mexican Chemical Society (México) Num.3 Vol.57 |
| format | Artículo científico |
| id | redalyc_47529964003 |
| institution | Redalyc |
| language | en |
| publishDate | 2013 |
| publisher | Sociedad Química de México |
| spellingShingle | Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin Jesús G. Estrada Multidisciplinaria (Ciencias Naturales y Exactas) rin albumin transfer Ruthenium ketoconazole Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin Jesús G. Estrada Roberto A. Sánchez-Delgado Multidisciplinaria (Ciencias Naturales y Exactas) rin albumin transfer Ruthenium ketoconazole 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 apotransfer - rin (ATf) with six Ru II complexes containing ketoconazole (KTZ), which we have previously reported to be active against Leishmania major and Trypanosoma cruzi , has been investigated by monitor - ing the tryptophan fluorescence intensity of each protein upon in - cremental addition of the complexes. All the Ru-KTZ derivatives, namely cis-fac -[Ru II Cl 2 (DMSO) 3 (KTZ)] ( 1 ), cis -[Ru II Cl 2 (bipy)(D MSO)(KTZ)] ( 2 ), [Ru II ( η 6 - p -cymene)Cl 2 (KTZ)] ( 3 ), [Ru II ( η 6 - p - cymene)(en)(KTZ)][BF 4 ] 2 ( 4 ), [Ru II ( η 6 - p -cymene)(bipy)(KTZ)][BF 4 ] 2 ( 5 ), and [Ru II ( η 6 - p -cymene)(acac)(KTZ)][BF 4 ] ( 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 mecha - nism 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. 2013 artículo científico 1870-249X https://www.redalyc.org/articulo.oa?id=47529964003 en http://www.redalyc.org/revista.oa?id=475 Journal of the Mexican Chemical Society application/pdf Sociedad Química de México Journal of the Mexican Chemical Society (México) Num.3 Vol.57 |
| title | Spectroscopic Study of the Interactions of Ruthenium-Ketoconazole Complexes of Known Antiparasitic Activity with Human Serum Albumin and Apotransferrin |
| topic | Multidisciplinaria (Ciencias Naturales y Exactas) rin albumin transfer Ruthenium ketoconazole |
| url | https://www.redalyc.org/articulo.oa?id=47529964003 |