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1.
Exp Parasitol ; 188: 79-82, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29625099

RESUMO

The primary choice of drugs to treat Leishmaniasis are the pentavalent antimony-based compounds, nevertheless these drugs presented undesirable side effects. However, safe natural compounds could be used in combination with these drugs to enhance their activity. The aim of this study was to evaluate the sinergism of capsaicin and piperine, isolated from Capsicum frutescens and Piper nigrum, respectively, in combination with meglumine antimoniate against Leishmania infantum promastigote and amastigote forms. Each compound was mixed with the standard drug in several percentage mixtures and tested at various concentrations. Capsaicin and piperine in combination with meglumine antimoniate (25% + 75%) showed better anti-leishmanial activity with EC50 = 4.31 ±â€¯0.44 e 7.25 ±â€¯4.84 µg/mL against promastigote and amastigote forms, respectively. The results point that these spice alkaloids are suitable compounds to be administered in combinations with antileishmanial drugs to improve their action.


Assuntos
Alcaloides/farmacologia , Antiprotozoários/farmacologia , Benzodioxóis/farmacologia , Capsaicina/farmacologia , Leishmania infantum/efeitos dos fármacos , Meglumina/farmacologia , Compostos Organometálicos/farmacologia , Piperidinas/farmacologia , Alcamidas Poli-Insaturadas/farmacologia , Alcaloides/uso terapêutico , Antiprotozoários/uso terapêutico , Benzodioxóis/uso terapêutico , Capsaicina/uso terapêutico , Cromatografia Líquida de Alta Pressão , Sinergismo Farmacológico , Concentração Inibidora 50 , Leishmaniose Visceral/tratamento farmacológico , Espectroscopia de Ressonância Magnética , Meglumina/uso terapêutico , Antimoniato de Meglumina , Compostos Organometálicos/uso terapêutico , Piperidinas/uso terapêutico , Alcamidas Poli-Insaturadas/uso terapêutico , Espectrofotometria Ultravioleta
2.
Pharmaceuticals (Basel) ; 12(3)2019 Jul 26.
Artigo em Inglês | MEDLINE | ID: mdl-31357557

RESUMO

The mosquitoes Aedes aegypti and Aedes albopictus are vectors of arboviruses that cause dengue, zika and chikungunya. Bioactive compounds from plants are environmentally sustainable alternatives to control these vectors and thus the arboviruses transmitted by them. The present study evaluated the larvicidal activity of an acetogenin-rich fraction (ACERF) and its main constituent annonacin obtained from Annona muricata seeds on Ae. aegypti and Ae. albopictus. The larvicidal assays were performed using different concentrations to calculate the LC50 and LC90 values observed 24 h after exposure to the treatment. Annonacin was more active against Ae. aegypti (LC50 2.65 µg·mL-1) in comparison with Ae. albopictus (LC50 8.34 µg·mL-1). In contrast, the acetogenin-rich fraction was more active against Ae. albopictus (LC50 3.41 µg·mL-1) than Ae. aegypti (LC50 12.41 µg·mL-1). ACERF and annonacin treated larvae of Ae. aegypti and Ae. albopictus showed significant differences in the inhibition of their metabolic enzymes when compared to untreated larvae. The results demonstrate the relevant larvicidal action of the acetogenin-rich fraction and annonacin showing the potential to develop new products for the control of Ae. aegypti and Ae. albopictus.

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