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Platinum(II) metal complexes as potential anti-Trypanosoma cruzi agents
- Source :
- JOURNAL OF INORGANIC BIOCHEMISTRY, Artículos CONICYT, CONICYT Chile, instacron:CONICYT
- Publication Year :
- 2008
- Publisher :
- Elsevier BV, 2008.
-
Abstract
- In the search for new therapeutic tools against Chagas' disease (American Trypanosomiasis) two series of new platinum(II) complexes with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands were synthesized, characterized and in vitro evaluated. Most of the complexes showed IC50 values in the muM range against two different strains of Trypanosoma cruzi, causative agent of the disease, being as active as the anti-trypanosomal drug Nifurtimox. In particular, the coordination of L3 (4-ethyl-1-(5-nitrofurfurylidene)thiosemicarbazide) to Pt(II) forming [Pt(L3)2] lead to almost a five-fold activity increase in respect to the free ligand. Trying to get an insight into the trypanocidal mechanism of action of these compounds, DNA and redox metabolism (intra-parasite free radical production) were evaluated as potential parasite targets. Results suggest that the complexes could inhibit parasite growth through a dual mechanism of action involving production of toxic free radicals by bioreduction and DNA interaction.
- Subjects :
- Thiosemicarbazones
Chagas disease
Free Radicals
Organoplatinum Compounds
Spectrophotometry, Infrared
Stereochemistry
Trypanosoma cruzi
Radical
Spectrum Analysis, Raman
Biochemistry
Inorganic Chemistry
chemistry.chemical_compound
medicine
Animals
Nifurtimox
Nuclear Magnetic Resonance, Biomolecular
biology
Chemistry
Ligand
DNA
biology.organism_classification
medicine.disease
Trypanocidal Agents
In vitro
Mechanism of action
medicine.symptom
medicine.drug
Subjects
Details
- ISSN :
- 01620134
- Volume :
- 102
- Database :
- OpenAIRE
- Journal :
- Journal of Inorganic Biochemistry
- Accession number :
- edsair.doi.dedup.....02bf39f6df28272f300d4cd7ff4f67f6