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Abstract Title:

Cardamonin Presents in Vivo Activity against Schistosoma mansoni and Inhibits Potato Apyrase.

Abstract Source:

Chem Biodivers. 2021 Nov ;18(11):e2100604. Epub 2021 Oct 27. PMID: 34608744

Abstract Author(s):

Lara Soares Aleixo de Carvalho, Lívia Mara Silva, Vinícius Carius de Souza, Marcos Paulo Nascimento da Silva, Priscila V S Z Capriles, Priscila de Faria Pinto, Josué de Moraes, Ademar Alves Da Silva Filho

Article Affiliation:

Lara Soares Aleixo de Carvalho

Abstract:

Schistosomiasis, a neglected tropical disease caused by Schistosoma species, harms over 250 million people in several countries. The treatment is achieved with only one drug, praziquantel. Cardamonin, a natural chalcone with in vitro schistosomicidal activity, has not been in vivo evaluated against Schistosoma. In this work, we evaluated the in vivo schistosomicidal activities ofcardamonin against Schistosoma mansoni worms and conducted enzymatic apyrase inhibition assay, as well as molecular docking analysis of cardamonin against potato apyrase, S. mansoni NTPDase 1 and S. mansoni NTPDase 2. In a mouse model of schistosomiasis, the oral treatment with cardamonin (400 mg/kg) showed efficacy against S. mansoni, decreasing the total worm load in 46.8 % and reducing in 54.5 % the number of eggs in mice. Cardamonin achieved a significant inhibition of the apyrase activity and the three-dimensional structure of the potato apyrase, obtained by homology modeling, showed that cardamonin may interact mainly through hydrogen bonds. Molecular docking studies corroborate with the action of cardamonin in binding and inhibiting both potato apyrase and S. mansoni NTPDases.

Study Type : In Vitro Study

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