RESUMO
Alibertia edulis leaf extract is commonly used in folk medicine, with rutin caffeic and vanillic acids being its major compounds. The Alibertia edulis leaf extract was investigated for its pharmacological effects via platelet aggregation, calcium mobilization, cyclic nucleotides levels, vasodilator-stimulated phosphoprotein Ser157 and Ser239 and protein kinase Cß2 phosphorylation, thromboxane B2, cyclooxygenases 1 and 2, docking and molecular dynamics. Alibertia edulis leaf extract significantly inhibited (100-1000 µg mL-1) platelet aggregation induced by different agonists. Arachidonic acid increased levels of calcium and thromboxane B2, phosphorylation of vasodilator-stimulated phosphoprotein Ser157 and Ser239, and protein kinase Cß, which were significantly reduced by Alibertia edulis leaf extract, rutin, and caffeic acid as well mixtures of rutin/caffeic acid. Cyclooxygenase 1 activity was inhibited for Alibertia edulis leaf extract, rutin and caffeic acid. These inhibitions were firsrtly explored by specific stabilization of rutin and caffeic acid compared to diclofenac at the catalytic site from docking score and free-energy dissociation profiles. Then, simulations detailed the rutin interactions close to the heme group and Tyr385, responsible for catalyzing the conversion of arachidonic acid to its products. Our results reveal the antiplatelet aggregation properties of Alibertia edulis leaf extract, rutin and caffeic acid providing pharmacological information about its origin from cyclooxygenase 1 inhibition and its downstream pathway.
Assuntos
Regulação da Expressão Gênica/efeitos dos fármacos , Extratos Vegetais/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Prostaglandina-Endoperóxido Sintases/metabolismo , Rubiaceae/química , Tromboxanos/antagonistas & inibidores , Ácido 15-Hidroxi-11 alfa,9 alfa-(epoximetano)prosta-5,13-dienoico/administração & dosagem , Ácido 15-Hidroxi-11 alfa,9 alfa-(epoximetano)prosta-5,13-dienoico/farmacologia , Difosfato de Adenosina/administração & dosagem , Difosfato de Adenosina/farmacologia , Animais , Ácido Araquidônico/administração & dosagem , Ácido Araquidônico/farmacologia , Cálcio/metabolismo , Colágeno/administração & dosagem , Colágeno/farmacologia , Inibidores de Ciclo-Oxigenase , Humanos , Extratos Vegetais/química , Folhas de Planta/química , Tromboxanos/genética , Tromboxanos/metabolismo , Peixe-ZebraRESUMO
In vitro activity of the essential oil from Piper diospyrifolium leaves was tested using disk diffusion techniques. The antifungal assay showed significant potencial antifungal activity: the oil was effective against several clinical fungal strains. The majority compounds in the essential oil were identified as sesquiterpenoids by GC-MS and GC-FID techniques.
Assuntos
Antifúngicos , Técnicas In Vitro , Estruturas Vegetais , Piper/crescimento & desenvolvimento , Piper/genética , Piperaceae/genética , Sesquiterpenos/análise , Árvores , Oceano Atlântico , Métodos , Óleos Voláteis , Folhas de Planta , Preparações de Plantas , MétodosRESUMO
In vitro activity of the essential oil from Piper diospyrifolium leaves was tested using disk diffusion techniques. The antifungal assay showed significant potencial antifungal activity: the oil was effective against several clinical fungal strains. The majority compounds in the essential oil were identified as sesquiterpenoids by GC-MS and GC-FID techniques.
