In silico toxicologic profile and in vivo trypanocidal activity of estafietin, a sesquiterpene lactone isolated from Stevia alpina Griseb

Chagas disease is an infection caused by the protozoan affecting 6-8 million people worldwide. Only two drugs are available for its treatment, having a limited efficacy and adverse side-effects. Estafietin is a sesquiterpene lactone isolated from with activity against and low cytotoxicity against ma...

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Bibliographic Details
Published in:Natural product research 2024-02, Vol.38 (4), p.690-695
Main Authors: Elso, Orlando G, Cerny, Natacha, Laurella, Laura C, Bivona, Augusto E, Sánchez Alberti, Andrés, Morales, Celina, Catalán, Cesar A N, Malchiodi, Emilio L, Sülsen, Valeria P
Format: Article
Language:English
Subjects:
Animal models
Biocompatibility
Chagas disease
Chronic infection
Cytotoxicity
In vivo methods and tests
Inflammation
Mammalian cells
Myocytes
Parasitemia
Side effects
Stevia
Toxic diseases
Toxicity
Vector-borne diseases
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Summary:Chagas disease is an infection caused by the protozoan affecting 6-8 million people worldwide. Only two drugs are available for its treatment, having a limited efficacy and adverse side-effects. Estafietin is a sesquiterpene lactone isolated from with activity against and low cytotoxicity against mammalian cells. The aim of this work was to predict the toxicologic profile of estafietin by methods and assess its activity on a murine model of Chagas disease. Estafietin showed low toxicity according to pkCSM web tool and passed the PAINS filter from PAINS-remover web server. The treatment of infected mice with 1 mg/Kg/day of estafietin for five consecutive days administrated by intraperitoneal route significatively decreased parasitemia levels and reduced inflammatory infiltrates and myocyte damage on muscle tissue. These results suggest that estafietin had effect both on acute and chronic stages of the infection.
ISSN:1478-6419
1478-6427
DOI:10.1080/14786419.2023.2188208