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Article

Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity

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Faculdade de Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, R. José Lourenço Kelmer s/n, Campus Universitário, Juiz de Fora 36036-900, MG, Brazil
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Programa de Pós-Graduação em Modelagem Computacional, Departamento de Ciência da Computação, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora 36036-900, MG, Brazil
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Núcleo de Pesquisa em Doenças Negligenciadas, Universidade Guarulhos, Guarulhos 07023-070, SP, Brazil
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Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora 36036-900, MG, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Juan José Torrado
Pharmaceutics 2022, 14(5), 1071; https://doi.org/10.3390/pharmaceutics14051071
Received: 8 April 2022 / Revised: 10 May 2022 / Accepted: 12 May 2022 / Published: 17 May 2022
Schistosomiasis, caused by parasites of the genus Schistosoma, is a neglected disease with high global prevalence, affecting more than 240 million people in several countries. Praziquantel (PZQ) is the only drug currently available for the treatment. S. mansoni NTPDases (known as SmNTPDases, ATP diphosphohydrolases or ecto-apyrases) are potential drug targets for the discovery of new antischistosomal drugs. In this study, we screen NTPDases inhibitors from Centella erecta (Apiaceae) using an ultrafiltration combined UHPLC-QTOF-MS method and potato apyrase, identifying asiaticoside as one of the apyrase-binding compounds. After isolation of asiaticoside from C. erecta extract, we assessed its in vivo antischistosomal activities against Schistosoma mansoni worms and its in vitro enzymatic apyrase inhibition. Also, molecular docking analysis of asiaticoside against potato apyrase, S. mansoni NTPDases 1 and 2 were performed. Asiaticoside showed a significant in vitro apyrase inhibition and molecular docking studies corroborate with its possible actions in potato apyrase and S. mansoni NTPDases. In mice harboring a patent S. mansoni infection, a single oral dose of asiaticoside (400 mg/kg. p.o.) showed significantly in vivo antischistosomal efficacy, markedly decreasing the total worm load and egg burden, giving support for further exploration of apyrase inhibitors as antischistosomal agents. View Full-Text
Keywords: Schistosoma mansoni; natural products; asiaticoside Schistosoma mansoni; natural products; asiaticoside
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MDPI and ACS Style

de Carvalho, L.S.A.; de Souza, V.C.; Rodrigues, V.C.; Ribeiro, A.C.; Nascimento, J.W.L.; Capriles, P.V.S.Z.; Pinto, P.d.F.; de Moraes, J.; da Silva Filho, A.A. Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity. Pharmaceutics 2022, 14, 1071. https://doi.org/10.3390/pharmaceutics14051071

AMA Style

de Carvalho LSA, de Souza VC, Rodrigues VC, Ribeiro AC, Nascimento JWL, Capriles PVSZ, Pinto PdF, de Moraes J, da Silva Filho AA. Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity. Pharmaceutics. 2022; 14(5):1071. https://doi.org/10.3390/pharmaceutics14051071

Chicago/Turabian Style

de Carvalho, Lara S.A., Vinícius C. de Souza, Vinícius C. Rodrigues, Aline C. Ribeiro, Jorge W.L. Nascimento, Priscila V.S.Z. Capriles, Priscila d.F. Pinto, Josué de Moraes, and Ademar A. da Silva Filho. 2022. "Identification of Asiaticoside from Centella erecta (Apiaceae) as Potential Apyrase Inhibitor by UF-UHPLC-MS and Its In Vivo Antischistosomal Activity" Pharmaceutics 14, no. 5: 1071. https://doi.org/10.3390/pharmaceutics14051071

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