Prospecção de propriedades bioativas e metabólicas associadas às sementes de Triplaris gardneriana Wedd. (Polygonaceae) e seus constituintes fenólicos

Abstract

Triplaris gardneriana Wedd. is a plant species from Brazilian semiarid region with ethnotherapeutic applications related to the presence of secondary metabolites, especially phenolic compounds. Knowledge of the medicinal properties associated with the metabolism of these chemical entities after oral administration of plant extracts provides valuable information about stability during digestion and absorption by the gastrointestinal tract. Moreover, this knowledge can estimate rational and sufficient dosage regimes for the expected biological events to occur. Considering the antioxidant effect as the reason for many of the bioactivities of T. gardneriana described in the literature and the limited number of studies that analyze the behavior of herbal preparations in human body, the present work aimed to characterize the extract of T. gardneriana seeds (EETg) and its phenolic constituents in terms of anti-inflammatory action, metabolism and prebiotic potential, integrating in silico, in vitro and in vivo strategies. In general, EETg at 10 and 20 μg/mL, was able to modulate the pro-inflammatory functions of human neutrophils, such as degranulation and respiratory burst. In addition, its main phenolic components showed high binding affinity in silico to neutrophil myeloperoxidase. A kinetics study showed that 40% of total content of these phytochemicals were released from the extract causing increased antioxidant capacity after 180 min of gastrointestinal simulation. After computational analysis, 7 of the 9 main phenolic compounds of EETg showed good pharmacokinetic parameters, such as intestinal absorption and bioavailability score. In addition, EETg showed a protective effect against oxidative stress induced by copper and H2O2 in Drosophila melanogaster and Saccharomyces cerevisiae, respectively. Finally, the prebiotic score of EETg was comparable to that of inulin (standard), considering their respective growth ratios for Lactobacillus acidophilus and S. cerevisiae as well as those of the enteric pathogens Escherichia coli and Candida albicans. These findings suggest that oral administration of EETg may provide phenolic compounds partially absorbable by the human intestine and capable of promoting health benefits associated with the inhibition of oxidative stress and modulation of the growth of gut microorganisms.