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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Urquiza, Nora M. Islas, María S. Ariza, Santiago T. Jori, Nadir Martínez Medina, Juan J. Lavecchia, Martín J. López Tévez, Leonor L. Lezama, Luis Rojo, Teófilo Williams, Patricia A. M. Ferrer, Evelina G. |
| Description | Country affiliation: Argentina Author Affiliation: Urquiza NM ( Cátedra de Química Analítica, Instituto de Química Analítica, Facultad de Bioquímica, Química y Farmacia, Universidad Nacional de Tucumán, Ayacucho 471, 4000 San Miguel de Tucumán, Argentina.); Islas MS ( Centro de Química Inorgánica (CEQUINOR/CONICET, UNLP), Facultad de Ciencias Exactas, UNLP, C. Correo 962, 1900 La Plata, Argentina.); Ariza ST ( Centro de Química Inorgánica (CEQUINOR/CONICET, UNLP), Facultad de Ciencias Exactas, UNLP, C. Correo 962, 1900 La Plata, Argentina.); Jori N ( Centro de Química Inorgánica (CEQUINOR/CONICET, UNLP), Facultad de Ciencias Exactas, UNLP, C. Correo 962, 1900 La Plata, Argentina.); Martínez Medina JJ ( Universidad Nacional del Chaco Austral, Cte. Fernández 755, 3700 Roque Sáenz Peña, Chaco, Argentina.); Lavecchia MJ ( Instituto de Investigación Biomedicina de Buenos Aires (IBioBA)-CONICET-Partner Institute of the Max Planck Society, Godoy Cruz 2390, C1425FQA Buenos Aires, Argentina.); López Tévez LL ( Universidad Nacional del Chaco Austral, Cte. Fernández 755, 3700 Roque Sáenz Peña, Chaco, Argentina.); Lezama L ( Departamento de Química Inorgánica, Facultad de Ciencia y Tecnología, Universidad del País Vasco, Apdo 644, 48080 Bilbao, Spain.); Rojo T ( Departamento de Química Inorgánica, Facultad de Ciencia y Tecnología, Universidad del País Vasco, Apdo 644, 48080 Bilbao, Spain.); Williams PA ( Centro de Química Inorgánica (CEQUINOR/CONICET, UNLP), Facultad de Ciencias Exactas, UNLP, C. Correo 962, 1900 La Plata, Argentina.); Ferrer EG ( Centro de Química Inorgánica (CEQUINOR/CONICET, UNLP), Facultad de Ciencias Exactas, UNLP, C. Correo 962, 1900 La Plata, Argentina. Electronic address: evelina@quimica.unlp.edu.ar.) |
| Abstract | It has been reported that various metal coordination compounds have improved some biological properties. A high activity of acid phosphatase (AcP) is associated to several diseases (osteoporosis, Alzheimer's, prostate cancer, among others) and makes it a target for the development of new potential inhibitors. Anti-thyroid agents have disadvantageous side effects and the scarcity of medicines in this area motivated many researchers to synthesize new ones. Several copper(II) complexes have shown antifungal activities. In this work we presented for a first time the inhibition of AcP and the anti-thyroid activity produced by methimazole-Cu(II) complexes. Cu-Met ([Cu(MeimzH)2(H2O)2](NO3)2·H2O) produces a weak inhibition action while Cu-Met-phen ([Cu(MeimzH)2(phen)(H2O)2]Cl2) shows a strong inhibition effect (IC50 = 300 µM) being more effective than the reported behavior of vanadium complexes. Cu-Met-phen also presented a fairly good anti-thyroid activity with a formation constant value, Kc=1.02 × 10(10)M(-1) being 10(6) times more active than methimazole (Kc = 4.16 × 10(4)M(-1)) in opposition to Cu-Met which presented activity (Kc=9.54 × 10(3)M(-1)) but in a lesser extent than that of the free ligand. None of the complexes show antifungal activity except Cu-phen (MIC = 11.71 µgmL(-1) on Candidaalbicans) which was tested for comparison. Besides, albumin interaction experiments denoted high affinity toward the complexes and the calculated binding constants indicate reversible binding to the protein. |
| File Format | HTM / HTML |
| ISSN | 00092797 |
| Volume Number | 229 |
| e-ISSN | 18727786 |
| Journal | Chemico-Biological Interactions |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2015-03-05 |
| Publisher Place | Ireland |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Biochemistry Discipline Pharmacology Acid Phosphatase Antagonists & Inhibitors Antifungal Agents Pharmacology Antithyroid Agents Coordination Complexes Copper Methimazole Serum Albumin, Bovine Metabolism Animals Chemistry Candida Drug Effects Candidiasis Drug Therapy Cattle Humans Protein Conformation Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Toxicology |
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