Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System
Metal complexation in general improves the biological properties of ligands. We have previously measured the anticancer effects of the oxidovanadium(IV) cation with chrysin complex, VO(chrys)<sub>2</sub>. In the present study, we synthesized and characterized a new complex generated by t...
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-12-01
|
| Series: | Inorganics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2304-6740/10/1/4 |
| _version_ | 1797493141573468160 |
|---|---|
| author | Agustin Actis Dato Luciana G. Naso Marilin Rey Pablo J. Gonzalez Evelina G. Ferrer Patricia A. M. Williams |
| author_facet | Agustin Actis Dato Luciana G. Naso Marilin Rey Pablo J. Gonzalez Evelina G. Ferrer Patricia A. M. Williams |
| author_sort | Agustin Actis Dato |
| collection | DOAJ |
| description | Metal complexation in general improves the biological properties of ligands. We have previously measured the anticancer effects of the oxidovanadium(IV) cation with chrysin complex, VO(chrys)<sub>2</sub>. In the present study, we synthesized and characterized a new complex generated by the replacement of one chrysin ligand by phenanthroline (phen), VO(chrys)phenCl, to confer high planarity for DNA chain intercalation and more lipophilicity, giving rise to a better cellular uptake. In effect, the uptake of vanadium has been increased in the complex with phen and the cytotoxic effect of this complex proved higher in the human lung cancer A549 cell line, being involved in its mechanisms of action, the production of cellular reactive oxygen species (ROS), the decrease of the natural antioxidant compound glutathione (GSH) and the ratio GSH/GSSG (GSSG, oxidized GSH), and mitochondrial membrane damage. Cytotoxic activity studies using the non-tumorigenic HEK293 cell line showed that [VO(chrys)phenCl] exhibits selectivity action towards A549 cells after 24 h incubation. The interaction with bovine serum albumin (BSA) by fluorometric determinations showed that the complex could be carried by the protein and that the binding of the complex to BSA occurs through H-bond and van der Waals interactions. |
| first_indexed | 2024-03-10T01:15:45Z |
| format | Article |
| id | doaj.art-099b4e068f5b45f18996b01457e06f9d |
| institution | Directory Open Access Journal |
| issn | 2304-6740 |
| language | English |
| last_indexed | 2024-03-10T01:15:45Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Inorganics |
| spelling | doaj.art-099b4e068f5b45f18996b01457e06f9d2023-11-23T14:09:02ZengMDPI AGInorganics2304-67402021-12-01101410.3390/inorganics10010004Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin SystemAgustin Actis Dato0Luciana G. Naso1Marilin Rey2Pablo J. Gonzalez3Evelina G. Ferrer4Patricia A. M. Williams5Centro de Química Inorgánica (CEQUINOR, UNLP, CONICET), Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bv. 120 No 1465, La Plata CP B1906CXS, ArgentinaCentro de Química Inorgánica (CEQUINOR, UNLP, CONICET), Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bv. 120 No 1465, La Plata CP B1906CXS, ArgentinaDepartamento de Física, Facultad de Bioquímica y Ciencias Biológicas, Universidad Nacional del Litoral and CONICET, Santa Fe S3000ZAA, ArgentinaDepartamento de Física, Facultad de Bioquímica y Ciencias Biológicas, Universidad Nacional del Litoral and CONICET, Santa Fe S3000ZAA, ArgentinaCentro de Química Inorgánica (CEQUINOR, UNLP, CONICET), Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bv. 120 No 1465, La Plata CP B1906CXS, ArgentinaCentro de Química Inorgánica (CEQUINOR, UNLP, CONICET), Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bv. 120 No 1465, La Plata CP B1906CXS, ArgentinaMetal complexation in general improves the biological properties of ligands. We have previously measured the anticancer effects of the oxidovanadium(IV) cation with chrysin complex, VO(chrys)<sub>2</sub>. In the present study, we synthesized and characterized a new complex generated by the replacement of one chrysin ligand by phenanthroline (phen), VO(chrys)phenCl, to confer high planarity for DNA chain intercalation and more lipophilicity, giving rise to a better cellular uptake. In effect, the uptake of vanadium has been increased in the complex with phen and the cytotoxic effect of this complex proved higher in the human lung cancer A549 cell line, being involved in its mechanisms of action, the production of cellular reactive oxygen species (ROS), the decrease of the natural antioxidant compound glutathione (GSH) and the ratio GSH/GSSG (GSSG, oxidized GSH), and mitochondrial membrane damage. Cytotoxic activity studies using the non-tumorigenic HEK293 cell line showed that [VO(chrys)phenCl] exhibits selectivity action towards A549 cells after 24 h incubation. The interaction with bovine serum albumin (BSA) by fluorometric determinations showed that the complex could be carried by the protein and that the binding of the complex to BSA occurs through H-bond and van der Waals interactions.https://www.mdpi.com/2304-6740/10/1/4oxidovanadium(IV) phenantrholine chrysinvanadium cellular uptakeanticanceralbumin interaction |
| spellingShingle | Agustin Actis Dato Luciana G. Naso Marilin Rey Pablo J. Gonzalez Evelina G. Ferrer Patricia A. M. Williams Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System Inorganics oxidovanadium(IV) phenantrholine chrysin vanadium cellular uptake anticancer albumin interaction |
| title | Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System |
| title_full | Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System |
| title_fullStr | Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System |
| title_full_unstemmed | Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System |
| title_short | Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System |
| title_sort | phenanthroline complexation enhances the cytotoxic activity of the vo chrysin system |
| topic | oxidovanadium(IV) phenantrholine chrysin vanadium cellular uptake anticancer albumin interaction |
| url | https://www.mdpi.com/2304-6740/10/1/4 |
| work_keys_str_mv | AT agustinactisdato phenanthrolinecomplexationenhancesthecytotoxicactivityofthevochrysinsystem AT lucianagnaso phenanthrolinecomplexationenhancesthecytotoxicactivityofthevochrysinsystem AT marilinrey phenanthrolinecomplexationenhancesthecytotoxicactivityofthevochrysinsystem AT pablojgonzalez phenanthrolinecomplexationenhancesthecytotoxicactivityofthevochrysinsystem AT evelinagferrer phenanthrolinecomplexationenhancesthecytotoxicactivityofthevochrysinsystem AT patriciaamwilliams phenanthrolinecomplexationenhancesthecytotoxicactivityofthevochrysinsystem |