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• W293942008 abstract "Malaria is one of the most important parasitic infections of humans due to the high morbidity and mortality attributed to this disease, which threatens to over two billion people living in areas with high incidence. Plasmodium falciparum, a causative agent of malaria, has a high capacity to adapt by mutation and may be resistant to various antimalarial drugs already available, such as chloroquine, which makes it important to search for new antimalarials. The Brazilian semi-arid region cover about 11.5% of the country, and the biome has been less studied in relation to flora and fauna, and one who has suffered further degradation and predation by the inordinate use in the last 400 years. Given the pharmacological potential of natural products, the aim of this study was to evaluate the antimalarial activity of pure compounds extracted from native or endemic plant species of arid and semi-synthetic derivatives. From a library of 160 substances screened for antimalarial activity, we selected two classes of compounds for evaluation in vitro and in vivo: The betulinic acid and derivatives, as well as lapachol and derivatives. It was also selected a third class of molecules, physalins using the method of Similarity Ensemble Approach (SEA), who predicted the antimalarial action of these substances. Among the tested derivatives of betulinic acid, betulinic acid acetate showed the highest pharmacological potency in vitro when compared with other derivatives, and was active in vivo. The antimalarial activity of physalins was confirmed in vitro assays. When analyzed in vivo the physalins F and D had the opposite results (exacerbation and protection against infection, respectively), possibly due to the immunosuppressive activity of physalin F and absent in physalin D. The analysis of lapachol and its derivatives was initiated through studies in silico by Quantitative Structure-Activity Relationship (QSAR), which indicated that the isolacet the derivative with greater activity, which was confirmed by in vitro assays. The antimalarial activity of isolacet was confirmed in vivo, and further studies of this molecule by Docking with falcipain 2 P. falciparum, which indicated that this cysteine protease is a possible isolacet target. Our results indicate the potential antimalarial compounds isolated from plants of the semi-arid and demonstrate the importance of the combination of various approaches to understanding the mechanisms of action of molecules with pharmacological activity." @default.
• W293942008 created "2016-06-24" @default.
• W293942008 creator A5067369815 @default.
• W293942008 date "2011-01-01" @default.
• W293942008 modified "2023-10-14" @default.
• W293942008 title "Avaliação da atividade antimalárica de substâncias obtidas de espécies vegetais nativas ou endêmicas do semi-árido brasileiro e derivados sintéticos" @default.
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