Abstract：
:Trypanosomatidae is a family of unicellular parasites belonging to the phylum Euglenozoa, which are causative agents in high impact human diseases such as Leishmaniasis, Chagas disease and African sleeping sickness. The impact on human health and local economies, together with a lack of satisfactory chemotherapeutic treatments and effective vaccines, justifies stringent research efforts to search for new disease therapies. Here, we present in vitro trypanocidal activity data and mode of action data, repositioning leishmanicidal [1,2,3]Triazolo[1,5-a]pyridinium salts against Trypanosoma cruzi, the aetiological agent of Chagas disease. This disease is one of the most neglected tropical diseases and is a major public health issue in Central and South America. The disease affects approximately 6-7 million people and is widespread due to increased migratory movements. We screened a suite of leishmanicidal [1,2,3]Triazolo[1,5-a]pyridinium salt compounds, of which compounds 13, 20 and 21 were identified as trypanocidal drugs. These compounds caused cell death in a mitochondrion-dependent manner through a bioenergetic collapse. Moreover, compounds 13 and 20 showed a remarkable inhibition of iron superoxide dismutase activity of T. cruzi, a key enzyme in the protection from the damage produced by oxidative stress.
journal_name
Parasitol Resjournal_title
Parasitology researchauthors
Martín-Escolano R,Martín-Escolano J,Ballesteros-Garrido R,Cirauqui N,Abarca B,Rosales MJ,Sánchez-Moreno M,Ballesteros R,Marín Cdoi
10.1007/s00436-020-06779-0subject
Has Abstractpub_date
2020-09-01 00:00:00pages
2943-2954issue
9eissn
0932-0113issn
1432-1955pii
10.1007/s00436-020-06779-0journal_volume
119pub_type
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