Antimalarial and antioxidant activities of novel artesunate-ellagic acid hybrid compound in vitro and in vivo .

Autor:	Ishola AA; Department of Biochemistry, University of Ilorin, Ilorin, Nigeria., Adebayo JO; Department of Biochemistry, University of Ilorin, Ilorin, Nigeria., Ceravolo IP; Malária Experimentale Humana, Instituto René Rachou, Fundacao Oswaldo Cruz, Belo Horizonte, Mato Grosso, Brazil., Tijjani H; Department of Biochemistry, Bauchi State University, Gadau, Nigeria., Bento ES; Instituto de Quimica e Biotecnologia, Universidade Federal de Alagoas (UFAL), Maceio, Alagoas, Brazil., Goulart HF; Laboratório de Pesquisa Em Recursos Naturais (LPqRN), Campus de Engenharias Ciencias Agrárias, Rio Largo, Brazil., Crispim AC; Instituto de Quimica e Biotecnologia, Universidade Federal de Alagoas (UFAL), Maceio, Alagoas, Brazil., Balogun EA; Department of Biochemistry, University of Ilorin, Ilorin, Nigeria., Santana AEG; Laboratório de Pesquisa Em Recursos Naturais (LPqRN), Campus de Engenharias Ciencias Agrárias, Rio Largo, Brazil., Krettli AU; Malária Experimentale Humana, Instituto René Rachou, Fundacao Oswaldo Cruz, Belo Horizonte, Mato Grosso, Brazil.
Jazyk:	angličtina
Zdroj:	Frontiers in pharmacology [Front Pharmacol] 2024 Jun 18; Vol. 15, pp. 1192659. Date of Electronic Publication: 2024 Jun 18 (Print Publication: 2024).
DOI:	10.3389/fphar.2024.1192659
Abstrakt:	Introduction: Emergence of drug resistant strains of Plasmodium species has necessitated the search for novel antimalarials with unique mechanisms of action. Synthesis of hybrid compounds has been one approach to tackling this challenge. In this study, the synthesis of artesunate-ellagic acid hybrid compound (EA31) from ellagic acid and artesunate and its evaluation for antimalarial and antioxidant activities using in vitro and in vivo models were carried out. Method: EA31 was synthesized from artesunate and ellagic acid. The activities of the hybrid compound against Plasmodium falciparum W2 and P. berghei NK65 were evaluated, and its antioxidant activities were also determined. Results: The results revealed that EA31 was more active against P. falciparum W2 (chloroquine resistant) clone and less cytotoxic to buffalo green monkey kidney cell line compared to artesunate. EA31 was also active against Plasmodium berghei NK65 in vivo . The results revealed inhibition of β-hematin formation as one of the mechanisms of action of EA31. EA31 also exhibited antioxidant activities. Conclusion: The results revealed that EA31 may exert dual action of killing malaria parasite and mopping the reactive oxygen species that mediate the secondary complications of malaria. Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. (Copyright © 2024 Ishola, Adebayo, Ceravolo, Tijjani, Bento, Goulart, Crispim, Balogun, Santana and Krettli.)
Databáze:	MEDLINE
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