ArticleBritish journal of pharmacology2010
Novel ruthenium complexes as potential drugs for Chagas's disease: enzyme inhibition and in vitro/in vivo trypanocidal activity.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 84 citations in OpenAlex.
- Advances and challenges in the search for new treatments for Chagas disease.Memorias do Instituto Oswaldo Cruz · 2026Review
- TrypPROTACs Unlocking New Therapeutic Strategies for Chagas Disease.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Exploring glycolytic enzymes in disease: potential biomarkers and therapeutic targets in neurodegeneration, cancer and parasitic infections.Open biology · 2025Review
- Optimization of the 2-arylquinazoline-4(3RSC medicinal chemistry · 2023Article
- New nitrosyl ruthenium complexes with combined activities for multiple cardiovascular disorders.Dalton transactions (Cambridge, England : 2003) · 2023Article
- Article
- Ruthenium Complexes in the Fight against Pathogenic Microorganisms. An Extensive Review.Pharmaceutics · 2021Review
- Review on Experimental Treatment Strategies AgainstJournal of experimental pharmacology · 2021Review
- A divergent mode of activation of a nitrosyl iron complex with unusual antiangiogenic activity.Journal of inorganic biochemistry · 2020Article
- An unusual bidentate methionine ruthenium(II) complex: photo-uncaging and antimicrobial activity.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020Article
- New metallophamaceutic reduced renal injury induced by non-steroidal anti-inflammatory.Acta cirurgica brasileira · 2020Article
- [Ru(bpy)Frontiers in pharmacology · 2019Article
- Thiol-Activated HNO Release from a Ruthenium Antiangiogenesis Complex and HIF-1α Inhibition for Cancer Therapy.ACS chemical biology · 2016Article
- Antileishmanial Activity and Inducible Nitric Oxide Synthase Activation by RuNO Complex.Mediators of inflammation · 2016Article
- Preventing the transmission of American trypanosomiasis and its spread into non-endemic countries.Infectious diseases of poverty · 2015Review
- Article
- Glyceraldehyde 3-phosphate dehydrogenase-telomere association correlates with redox status in Trypanosoma cruzi.PloS one · 2015Article
- Ruthenium complex with benznidazole and nitric oxide as a new candidate for the treatment of chagas disease.PLoS neglected tropical diseases · 2014Article
- Nitro/nitrosyl-ruthenium complexes are potent and selective anti-Trypanosoma cruzi agents causing autophagy and necrotic parasite death.Antimicrobial agents and chemotherapy · 2014Article
- Challenges and perspectives of Chagas disease: a review.The journal of venomous animals and toxins including tropical diseases · 2013Article
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe discovery of the pharmacological functions of nitric oxide has led to the development of NO donor compounds as therapeutic agents. A new generation of ruthenium NO donors, cis-[Ru(NO)(bpy)(2)L]X(n), has been developed, and our aim was to show that these complexes are able to lyse Trypanosoma cruzi in vitro and in vivo. EXPERIMENTAL APPROACH: NO donors were incubated with T. cruzi and their anti-T. cruzi activities evaluated as the percentage of lysed parasites compared to the negative control. In vivo, trypanocidal activity was evaluated by observing the levels of parasitaemia, survival rate and elimination of amastigotes in mouse myocardial tissue. The inhibition of GAPDH was monitored by the biochemical reduction of NAD(+) to NADH. KEY
resultsThe NO donors cis-[Ru(NO)(bpy)(2)L]X(n) presented inhibitory effects on T. cruzi GAPDH (IC(50) ranging from 89 to 153 microM). The crystal structure of the enzyme shows that the inhibitory mechanism is compatible with S-nitrosylation of the active cysteine (cys166) site. Compounds cis-[Ru(NO)(bpy)(2)imN](PF(6))(3) and cis-[Ru(NO)(bpy)(2)SO(3)]PF(6), at a dose of 385 nmol.kg(-1), yielded survival rates of 80 and 60%, respectively, in infected mice, and eradicated any amastigotes from their myocardial tissue. CONCLUSIONS AND IMPLICATIONS: The ruthenium compounds exhibited potent in vitro and in vivo trypanocidal activities at doses up to 1000-fold lower than the clinical dose for benznidazole. Furthermore, one mechanism of action of these compounds is via the S-nitrosylation of Cys166 of T. cruzi GAPDH. Thus, these compounds show huge potential as candidates for the development of new drugs for the treatment of Chagas's disease.
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