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Brazilian native fruits are a rich source of polyphenolic compounds that can act as anti-inflammatory and antioxidant agents. Here, we determined the polyphenolic composition, anti-inflammatory mechanism of action, antioxidant activity and systemic toxicity in Galleria mellonella larvae of Eugenia selloi B.D.Jacks. (synonym Eugenia neonitida Sobral) extract (Ese) and its polyphenol-rich fraction (F3) obtained through bioassay-guided fractionation. Phenolic compounds present in Ese and F3 were identified by LC-ESI-QTOF-MS. The anti-inflammatory activity of Ese and F3 was tested in vitro and in vivo through NF-κB activation, cytokine release and neutrophil migration assays. The samples were tested for their effects against reactive species (ROO•, O2•-, HOCl and NO•) and for their toxicity in Galleria mellonella larvae model. The presence of hydroxybenzoic acid, ellagitannins and flavonoids was identified. Ese and F3 reduced NF-κB activation, cytokine release and neutrophil migration, with F3 being three-fold more potent. Overall, F3 exhibited strong antioxidant effects against biologically relevant radicals, and neither Ese nor F3 were toxic to G. mellonella larvae. In conclusion, Ese and F3 revealed the presence of phenolic compounds that decreased the inflammatory parameters evaluated and inhibited reactive oxygen/nitrogen species. E. selloi is a novel source of bioactive compounds that may provide benefits for human health., Competing Interests: The authors have declared that no competing interests exist.

The anti-inflammatory and antibiofilm activities as well as toxicity and chemical profile of Eugenia brasiliensis pulp extract (EBE), were evaluated. EBE chemical profile and phenolic content were determined by LC-MS/MS. EBE was tested for its in vitro and in vivo anti-inflammatory activity, including TNF-α release, NF-кB activation, neutrophil migration and paw edema. The MIC/MBC and antibiofilm activities were tested against methicillin sensitive and resistant Staphylococcus aureus, Escherichia coli, Pseudomona aeruginosa, Streptococcus mutans, and Lactobacillus acidophilus. EBE acute toxicity was evaluated in Galleria mellonella and RAW 264.7 macrophage. EBE total phenolic content was 389.88 ± 3.48 mg GAE/g with identified polyphenols. EBE decreased TNF-α release in vivo and in vitro, NF-кB activation, neutrophil influx into peritoneal cavity, and it showed maximal inhibition of paw edema after 2 h. MIC of EBE ranged from 62.5-500 μg/mL while MBC values were >500 μg/mL, with a decrease in L. acidophilus biofilm formation. EBE showed negligible toxicity in larvae and macrophage cells. Our findings open new perspectives concerning EBE application as source of anti-inflammatory and antibiofilm molecules as a functional food, pharmaceutical lead or agribusiness commodity., (Copyright © 2018 Elsevier Masson SAS. All rights reserved.)

Brazilian endemic fruit species have aroused attention due to their highly valuable, yet unexplored, agro-industrial, food and therapeutic potential. Herein, we describe the antifungal activity of four Eugenia spp. against Candida albicans biofilms, and further demonstrate insights into their potential mode(s) of action and toxicity in vitro and in vivo. Extracts from different parts (seeds, pulps, leaves) of E. leitonii (EL), E. brasiliensis (EB), E. myrcianthes (EM) and E. involucrata (EI) were obtained (S23°23',W45°39') and chemically characterized by GC/MS. The active extracts were tested against C. albicans biofilm viability and architecture, as well as mode of action, and toxicology using RAW 264.7 macrophages and Galleria mellonella larvae. The MIC values ranged from 15.62 to >2000 μg/mL. The most active extracts were EL (seed, 15.62 μg/mL) and EB (leaf and seeds, 31.25 and 15.62 μg/mL, respectively). Treatment with these extracts at 10xMIC reduced biofilm viability by 54-55% (P < 0.0001) as compared to 42% by nystatin. At 10xMIC, all extracts caused damages to biofilm architecture and integrity, and fewer hyphae remained attached to treated biofilms. None of them was found to interfere with cell wall biosynthesis or complexation with ergosterol. The extracts had low toxicity against macrophages in vitro (P > 0.05) and G. mellonella larvae, with mean in vivo LD 50 of 1500 mg/kg (EL, seeds); 2500 mg/kg (EB, seeds); and 1250 mg/kg (EB, leaf). The phenolic compounds epicatechin and gallic acid were the major constituents in the extracts. Our findings may open avenues for the application of these yet unexplored native fruits in the food and pharmaceutical industry., (Copyright © 2017 Elsevier Ltd. All rights reserved.)

Brazilian native fruits are unmatched in their variety, but a poorly explored resource for the development of food and pharmaceutical products. The aim of this study was to evaluate the phenolic composition as well as the antioxidant and anti-inflammatory activities of the extracts of leaves, seeds, and pulp of four Brazilian native fruits (Eugenia leitonii, Eugenia involucrata, Eugenia brasiliensis, and Eugenia myrcianthes). GC-MS analyses of the ethanolic extracts showed the presence of epicatechin and gallic acid as the major compounds in these fruits. Antioxidant activity was measured using synthetic DPPH free-radical scavenging, β-carotene bleaching assay, and reactive oxygen species (ROO·, O2·-, and HOCl). The fruit extracts also exhibited antioxidant effect against biologically relevant radicals such as peroxyl, superoxide, and hypochlorous acid. In general, the pulps were the fruit fractions that exhibited the lowest antioxidant activities, whereas the leaves showed the highest ones. The anti-inflammatory activity was assessed in an in vivo model using the carrageenan-induced neutrophil migration assay, which evaluates the inflammatory response in the acute phase. The pulp, seeds, and leaves of these fruits reduced the neutrophil influx by 40% to 64%. Based on these results, we suggest that the anti-inflammatory activity of these native fruits is related to the modulation of neutrophil migration, through the inhibition of cytokines, chemokines, and adhesion molecules, as well as to the antioxidant action of their ethanolic extracts in scavenging the free-radicals released by neutrophils. Therefore, these native fruits can be useful to produce food additives and functional foods.