Introduction:Maytenus guianensis is a member of the Celastraceae family that is used in traditional medicine, particularly for its anti-parasitic and anti-cancer effects. To explore the ethnopharmacological potential of this plant, the present study was designed to screen the in vitro antileishmanial activities of extracts and compounds isolated from M. guianensis. Methods: Maytenus guianensis stems and leaves were extracted in acetone, followed by the preparation of eluates and isolation of secondary metabolites using chromatography on a glass column with silica gel as the fixed phase. The chemical components were identified using spectroscopic methods, including one-and two-dimensional nuclear magnetic resonance of hydrogen-1 and carbon-13, mass spectroscopy, and infrared spectroscopy. The anti-Leishmania amazonensis activities of these eluates and compounds were evaluated by direct promastigote counting and viability assays. Results: It was found that the hexane bark eluate produced the strongest anti-L. amazonensis effect, with 90-100% inhibition of the promastigote form. The isolated metabolite that produced the best result was tingenone B, followed by a compound formed by the union of tingenone and tingenone B (80-90% inhibition). Conclusions: Maytenus guianensis shows anti-parasite activity that warrants further investigation to determine the mechanisms underlying this antileishmanial effect and to evaluate the pharmacological potential of these eluates and isolated secondary metabolites, while minimizing any adverse effects.
Introduction: Malaria and leishmaniasis are prevalent in tropical regions, which have environmental characteristics that are highly favorable to protozoa and vectors of these diseases; the transmission of these infections in sub-tropical regions, although recognized, represents only a small fraction of cases. Plants are constantly being used in the search for and acquisition of new drugs, and many compounds derived from them have been used to combat various diseases. In this study, we evaluated the action of the dichloromethanolic extract of Myrciaria dubia leaves against the protozoa Plasmodium falciparum, Leishmania amazonensis, Leishmania braziliensis, and Leishmania chagasi through bioassays. Methods: The extract from M. dubia was tested for its anti-P. falciparum activity in an anti-histidine-rich protein II immunosorbent assay. The antileishmanial assays were performed using the resazurin method, while cytotoxicity against human hepatoma (HepG2) strain was determined using the colorimetric MTT [3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-2H tetrazolium bromide] method. Results: The M. dubia extract presented a half-maximal inhibitory concentration equal to 2.35 (1.05)μg/mL for P. falciparum, 190.73 (6.41) μg/mL for L. amazonensis, and greater than equal to 200µg/mL for L. chagasi and L. braziliensis strains. The cytotoxic concentration for 50% of the cells was above 500μg/mL for HepG2, indicating no toxicity and greater selectivity against parasites. Conclusions:The results obtained indicate the presence of antiplasmodial and leishmanicidal bioactive compounds in the dichloromethanolic extracts of M. dubia leaves, and point towards future studies to elucidate the mechanism of action for each physiological effect.
Introduction: This study assessed the activity of compounds from Piper tuberculatum against Plasmodium falciparum and Leishmania guyanensis. Methods: The effects of compounds from P. tuberculatum fruits on P. falciparum and L. guyanensis promastigote growth in vitro were determined. Hemolytic action and cytotoxicity in HepG2 and J774 cells were measured. Results: Three compounds showed strong antiplasmodial activity and one compound showed strong antileishmanial activity. Two compounds were non-toxic to HepG2 cells and all were toxic to J774 cells. The compounds showed no hemolytic activity. Conclusions: The tested compounds from P. tuberculatum exhibited antiparasitic and cytotoxic effects.
Introdução: A resistência bacteriana aos antimicrobianos é um grave problema de saúde pública. Este fato associado à formação de biofilmes dificulta o tratamento de infecções provocadas por estes microrganismos. Entre os candidatos mais promissores frente a resistência bacteriana estão os peptídeos e proteínas bioativas, em especial as serpentes pertencentes ao gênero Bothrops. O veneno de serpente constitui uma ampla fonte de moléculas bioativas, contendo proteínas, peptídeos e enzimas. Dentre estes componentes, destacam-se as fosfolipases A2 (PLA2), a qual possui uma grande variedade de atividades biológicas. Objetivo: Prospecção in vitro dos peptídeos miméticos PLAS-VP e PLAS-AK de venenos de serpentes do gênero Bothrops contra bactérias formadoras de biofilme. Materiais e Métodos: A técnica de poço-difusão foi realizada em placas de petri com a adição dos peptídeos e semeadura das cepas bacterianas Gram-negativas (Escherichia coli ATCC e Pseudomonas aeruginosa ATCC) em dupla camada de meio Mueller Hinton (MH). Os testes para determinação da concentração inibitória mínima (CIM) foi realizado em placas de 96 poços a 37 ºC por 24 horas em triplicata, nas concentrações de 200 a 1,56 µg/mL, tendo o imipenem como controle positivo. Resultados: Os peptídeos PLAS-VP e PLAS-AK, não apresentaram halos de inibição nas concentrações testadas. Entretanto os resultados de ambos os peptídeos apresentaram crescimento microbiano nas concentrações utilizadas quando comparados ao controle positivo. Discussão: Dentre as perspectivas iniciais do projeto, consideramos a hipótese de uma ação antagônica quando comparado a inibição microbiana. Devido à presença de bioativos ainda não elucidados que proporcionaram o crescimento das unidades formadoras de colônia bacteriana. Conclusão: Os peptídeos não demostraram atividades antimicrobiana, entretanto, os resultados demonstram expressivo desenvolvimento microbiológico, prospectando assim um potencial bioativo como insumo para a ação proliferativa de bactérias relacionado a biotecnologia médica.
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