Blackcurrant press cake by-product: Increased chemical bioaccessibility and reduced antioxidant protection after in vitro simulation of gastrointestinal digestion.

This study describes the bioaccessibility in terms of total phenolic content (TPC) and antioxidant capacity before and after in vitro digestion from blackcurrant press cake extracts (BPC) and the bioactivity in cell culture, human erythrocytes as well as the in silico analysis. Chemical analysis of BPC presented an increase in TPC (270%) and anthocyanins (136%) after in vitro digestion, resulting in an improvement of antioxidant activity (DPPH 112%; FRAP: 153%). This behavior may be related to the highest activity of cyanidin-3-rutinoside, as confirmed by in silico analysis. The digested BPC did not exert cytotoxicity in cells and showed less antioxidant activity against the oxidative damage induced in endothelial cells and human erythrocytes compared to the non-digested extract. The results raise a question about the reliability we should place on results obtained only from crude samples, especially those that will be used to produce foods or nutraceuticals.

Effectiveness of anthocyanin-containing foods and nutraceuticals in mitigating oxidative stress, inflammation, and cardiovascular health-related biomarkers: a systematic review of animal and human interventions.

Cardiovascular diseases (CVDs) are a group of chronic health disorders prevalent worldwide that claim millions of lives yearly. Inflammation and oxidative stress are intricately associated with myocardial tissue damage, endothelial dysfunction, and increased odds of heart failure. Thus, dietary strategies aimed at decreasing the odds of CVDs are paramount. In this regard, the consumption of anthocyanins, natural pigments found in edible flowers, fruits, and vegetables, has attracted attention due to their potential to promote cardiovascular health. The main mechanisms of action linked with their protective effects on antioxidant and anti-inflammatory activities, serum lipid profile modulation, and other cardiovascular health parameters are explained and exemplified. However, little is known about the dose-dependency nature of the effects, which anthocyanin has better efficiency, and whether anthocyanin-containing foods display better in vivo efficacy than nutraceuticals (i.e., concentrated extracts containing higher levels of anthocyanins than foods). Thus, this systematic review focused on determining the effects of anthocyanin-containing foods and nutraceuticals on biomarkers associated with CVDs using animal studies and human interventions supported by in vitro mechanistic insights. Overall, the results showed that the regular consumption of anthocyanin-containing foods and nutraceuticals improved vascular function, lipid profile, and antioxidant and anti-inflammatory effects. The daily dosage, the participants' health status, and the duration of the intervention also significantly influenced the results.

Phenolic-rich extracts from toasted white and tannin sorghum flours have distinct profiles influencing their antioxidant, antiproliferative, anti-adhesive, anti-invasive, and antimalarial activities.

Sorghum is a gluten-free cereal commonly used in foods, and its consumption has been associated with the prevention of human chronic conditions such as obesity and cancer, due to the presence of dietary fiber and phenolic compounds. This study aimed to evaluate, for the first time, the antiproliferative, antioxidant, anti-adhesion, anti-invasion, and antimalarial activities of phenolic extracts from toasted white and tannin sorghum flours to understand how different phenolic profiles contribute to sorghum biological activities. Water and 70 % ethanol/water (v/v), eco-friendly solvents, were used to obtain the phenolic extracts of toasted sorghum flours, and their phenolic profile was analyzed by UPLC-MSE. One hundred forty-five (145) phenolic compounds were identified, with 23 compounds common to all extracts. The solvent type affected the phenolic composition, with aqueous extract of both white sorghum (WSA) and tannin sorghum (TSA) containing mainly phenolic acids. White sorghum (WSE) and tannin sorghum (TSE) ethanolic extracts exhibited a higher abundance of flavonoids. WSE demonstrated the lowest IC50 on EA.hy926 (IC50 = 46.6 µg/mL) and A549 cancer cells (IC50 = 33.1 µg/mL), while TSE showed the lowest IC50 (IC50 = 70.8 µg/mL) on HCT-8 cells (human colon carcinoma). Aqueous extracts also demonstrated interesting results, similar to TSE, showing selectivity for cancer cells at higher IC50 concentrations. All sorghum extracts also reduced the adhesion and invasion of HCT-8 cells, suggesting antimetastatic potential. WSE, rich in phenolic acids and flavonoids, exhibited greater toxicity to both the W2 (chloroquine-resistant) and 3D7 (chloroquine-sensitive) strains of Plasmodium falciparum (IC50 = 8 µg GAE/mL and 22.9 µg GAE/mL, respectively). These findings underscore the potential health benefits of toasted sorghum flours, suggesting diverse applications in the food industry as a functional ingredient or even as an antioxidant supplement. Moreover, it is suggested that, besides the phenolic concentration, the phenolic profile is important to understand the health benefits of sorghum flours.

High-throughput synchronous erythrocyte cellular antioxidant activity and protection screening of phenolic-rich extracts: Protocol validation and applications.

Oxidative/nitrosative damage takes part in chronic disease development, which generates an urgent need for intervention and better therapies to manage them. The scientific community has demanded easy-to-run, cheap, and reliable methods for cellular antioxidant activity assays. This work standardised and validated an erythrocyte cellular antioxidant activity and membrane protection/injury (HERYCA-P) protocol to study food-derive extracts. The method measures intracellular reactive oxygen species (ROS) generation, lipoperoxidation, and haemolysis induced by 2,2'-azobis(2-amidinopropane) dihydrochloride. Quercetin decreased ROS generation by 50.4% and haemolysis by 2.2%, while ascorbic acid inhibited lipid peroxidation by 40.1%. Total phenolic contents of teas were correlated with decreased ROS generation (r = -0.924), lipoperoxidation (r = -0.951), and haemolysis (r = -0.869). The erythrocyte ROS generation and lipoperoxidation were also associated with CUPRAC (r = -0.925; r = -0.951) and hydroxyl radical scavenging activity (r = -0.936; r = -0.949). The precision rates of antioxidant standards and tea samples were below 15%. HERYCA-P is feasible as a complementary antioxidant assay for food matrices.

Sustainable and effective approach to recover antioxidant compounds from purple tea (Camellia sinensis var. assamica cv. Zijuan) leaves.

Camellia sinensis var. assamica cv. Zijuan (purple tea) is known for its content of anthocyanins, flavan-3-ols, and bioactivities. This study aimed to verify the influence of solvent polarity, in a solid-liquid extraction, on the content of phenolic compounds and chlorophylls, instrumental color, and antioxidant activity. Different proportions of water and ethanol (0:100, 25:75, 50:50, 75:25, and 100:0 v/v) were used for extraction. The results showed that the hydroalcoholic extract (75 % ethanol + 25 % water) had the highest contents of total flavonoids, total anthocyanins, chlorophyll A, and total carotenoids, as well as presenting the highest color intensity, proportion of yellow pigments, and antioxidant activity (total reducing capacity and scavenging of the DPPH free radical). Twenty-two compounds were identified, with chlorogenic acid, hesperidin, (-)-epicatechin, (-)-epigallocatechin gallate, and isoquercitrin being the main phenolics. This phenolic-rich extract inhibited lipoperoxidation induced in egg yolk homogenate (IC50 = 455 mg/L), showed no hemolytic behavior when human erythrocytes were subjected to osmotic stress, and exerted in vitro cytotoxic effects against cancer and hybrid cells. The extract obtained with the mixture of non-toxic solvents presented critical bioactivities, as well as a comprehensive identification of phenolic compounds in the cultivar, and has potential to be used in technological applications.

Enzyme-assisted extraction of anthocyanins and other phenolic compounds from blackcurrant (Ribes nigrum L.) press cake: From processing to bioactivities.

The effects of commercial enzymes (pectinases, cellulases, beta-1-3-glucanases, and pectin lyases) on the recovery of anthocyanins and polyphenols from blackcurrant press cake were studied considering two solid:solvent ratios (1:10 and 1:4 w/v). ß-glucanase enabled the recovery of the highest total phenolic content - 1142 mg/100 g, and the extraction of anthocyanins was similar using all enzymes (∼400 mg/100 g). The use of cellulases and pectinases enhanced the extraction of antioxidants (DPPH - 1080 mg/100 g; CUPRAC - 3697 mg/100 g). The freeze-dried extracts presented antioxidant potential (CUPRAC, DPPH), which was associated with their biological effects in different systems: antiviral activity against both non-enveloped viruses (enterovirus coxsackievirus A-9) and enveloped coronaviruses (HCoV-OC43), and cytotoxicity towards cancer cells (A549 and HCT8). No cytotoxic effects on normal human lung fibroblast (IMR90) were observed, and no anti-inflammatory activity was detected in lipopolysaccharides-treated murine immortalised microglial cells.

From the forest to the plate - Hemicelluloses, galactoglucomannan, glucuronoxylan, and phenolic-rich extracts from unconventional sources as functional food ingredients.

This study aimed to characterise pressurised hot water (PHW) extracts from nonconventional sources of functional carbohydrates and phenolic compounds in terms of antioxidant capacity, antiviral activity, toxicity, and human erythrocytes' protection antidiabetic potential. PHW extracts of Norway spruce bark (E1 + E2) and Birch sawdust (E3 + E4) contained mostly galactoglucomannan and glucuronoxylan. In contrast, samples E5 to E9 PHW extracted from Norway spruce, and Scots pine bark are rich sources of phenolic compounds. Overall, phenolic-rich extracts presented the highest inhibition of α-amylase and α-glucosidase and protection against stable non-enveloped enteroviruses. Additionally, all extracts protected human erythrocytes from hemolysis. Cell-based experiments using human cell lines (IMR90 and A549) showed extracts' non-toxicin vitroprofile. Considering the relative toxicological safety of extracts from these unconventional sources, functional carbohydrates and polyphenol-rich extracts can be obtained and further used in food models.

Black tea kombucha: Physicochemical, microbiological and comprehensive phenolic profile changes during fermentation, and antimalarial activity.

This study shows the changes in physicochemical and microbiological composition, and in the phenolic profile of black tea kombucha during fermentation. In addition, the antimalarial potential of the kombucha was evaluated. Ultra-performance liquid chromatography-mass spectrometry multiplex analysis (UPLC-MSE) results revealed a 1.7 log2 fold-change increase in phenolics with the fermentation time, with emphasis on the increase of phenolic acids (0.3 log2 fold-change). Over time there was degradation of flavonoids such as nepetin, hesperidin and catechin 5-O-gallate, to the detriment of the increase in phenolic acids such as gallic acid and cinnamic acid. In addition, black tea kombucha presented antiplasmodic activity against the 3D7 (sensitive chloroquine) and W2 (resistant to chloroquine) strains. Therefore, important changes in the black tea kombucha phenolic profile take place during fermentation, which may help in the development of kombuchas with higher bioactive potential and contribute to a better understanding of the kombucha fermentation process.

Purple tea (Camellia sinensis var. assamica) leaves as a potential functional ingredient: From extraction of phenolic compounds to cell-based antioxidant/biological activities.

A statistical optimization study was used to maximize the extraction of bioactive compounds and antioxidant activity from green tea derived from purple leaves of Camellia sinensis var. assamica. Simultaneous optimization was applied, and a combination of 60 °C, 15 min, and a mass-solvent ratio of 1 g of dehydrated purple leaves to 62.3 mL of an ethanol/citric acid solution, were determined as the ideal extraction conditions. The optimized extract of purple tea leaves (OEPL) contained showed stability in relation to variations in pH, and lyophilized OEPL exerted cytotoxic and antiproliferative effects against cancerous cells (A549 and HCT8), demonstrated antimicrobial activity towards Listeria monocytogenes (ATCC 7644), Staphylococcus aureus (ATCC 13565) and Staphylococcus epidermidis (ATCC 12288), inhibition of α-amylase and α-glycosidase enzymes and reduced the release of pro-inflammatory cytokines (TNF-α, CXCL2/MIP-2, and IL-6) in lipopolysaccharides-stimulated RAW 264.7 macrophages. Thus, our results provide a broad assessment of the bioactivity of "green" extracts obtained by a simple and low-cost process using non-toxic solvents, and they have the potential to be used for technological applications.

Antioxidant/pro-oxidant and antiproliferative activities of phenolic-rich foods and extracts: A cell-based point of view.

Phenolic compounds have demonstrated several in vitro beneficial properties by acting as antioxidant and pro-oxidant agents. This chapter approaches the relationship among oxidative stress, cancer, phenolic compounds and antiproliferative activity. Moreover, it discusses in vitro techniques and their biological applications, regarding cell viability and intracellular measure of reactive oxygen assays. The in vitro methods are important tools for screening and understanding the pathways involved on antiproliferative and antioxidant/pro-oxidant effects of phenolic compounds. These findings open avenues for the development of innovative food, chemical structures, technological applications and future perspectives in this research field.

Chemical Composition, Antioxidant, Antimicrobial and Cytotoxic/Cytoprotective Activity of Non-Polar Extracts of Grape (Vitis labrusca cv. Bordeaux) and Blackberry (Rubus fruticosus) Seeds.

The aim of this study was to compare the influence of the extraction method, chemical composition, antimicrobial effects, antioxidant activity, and cytotoxicity on human cells of the non-polar extracts of grape (Vitis labrusca) and blackberry (Rubus fruticosus) seeds. The Soxhlet (Sox), Bligh-Dyer (BD), and ultrasound (US) methods were used for extractions. For blackberry non-polar seed extract, extraction via the BD method showed the highest mean values of total phenolic content (TPC), expressed in milligrams of gallic acid equivalent per 100 mL of non-polar seed extracts (102.37 mg GAE/100 mL), and higher antioxidant activity in relation to the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical, expressed in milligrams of gallic acid equivalent per 100 mL of non-polar seed extracts (11.50 mg AAE/100 mL), if compared with the Sox and US extractions. Similar results were obtained for the non-polar grape seed extracts, where BD extraction obtained the highest values for TPC (28.61 mg GAE/100 mL) and DPPH (35.36 mg AAE/100 mL). The type of extraction method had an impact on the composition of fatty acids. Only the non-polar blackberry and grape seed extracts obtained via the Sox method showed some in vitro inhibitory effect against Escherichia coli (IAL 2064) and Staphylococcus aureus (ATCC 13565). Regardless of the extraction method used, the non-polar blackberry and grape seed extracts did not decrease the cell viability (IC50 >1000 µg/mL) of cancer and normal cell lines, thus indicating the relative safety of the extracts. All the seed extracts decreased the generation of reactive oxygen species in the cell lines. Blackberry and grape seed lipid fractions can be utilized as antioxidants, and the extraction methods used cause significant changes in relation to their bioactivity and chemical composition.

Toxicological and bioactivity evaluation of blackcurrant press cake, sea buckthorn leaves and bark from Scots pine and Norway spruce extracts under a green integrated approach.

Aqueous extracts from blackcurrant press cake (BC), Norway spruce bark (NS), Scots pine bark (SP), and sea buckthorn leaves (SB) were obtained using maceration and pressurized hot water and tested for their bioactivities. Maceration provided the extraction of higher dry matter contents, including total phenolics (TPC), anthocyanins, and condensed tannins, which also impacted higher antioxidant activity. NS and SB extracts presented the highest mean values of TPC and antioxidant activity. Individually, NS extract presented high contents of proanthocyanidins, resveratrol, and some phenolic acids. In contrast, SB contained a high concentration of ellagitannins, ellagic acid, and quercetin, explaining the antioxidant activity and antibacterial effects. SP and BC extracts had the lowest TPC and antioxidant activity. However, BC had strong antiviral efficacy, whereas SP can be considered a potential ingredient to inhibit α-amylase. Except for BC, the other extracts decreased reactive oxygen species (ROS) generation in HCT8 and A549 cells. Extracts did not inhibit the production of TNF-alpha in lipopolysaccharide-stimulated THP-1 macrophages but inhibited the ROS generation during the THP-1 cell respiratory burst. The recovery of antioxidant compounds from these by-products is incentivized for high value-added applications.

Ellagitannins from jabuticaba (Myrciaria jaboticaba) seeds attenuated inflammation, oxidative stress, aberrant crypt foci, and modulated gut microbiota in rats with 1,2 dimethyl hydrazine-induced colon carcinogenesis.

Since dietary factors are thought to be responsible for high colon cancer risk, we investigated the chemopreventive effect of jabuticaba seed extract (LJE) by administering yogurt with or without LJE against 1,2 dimethyl hydrazine (DMH)-induced colon carcinogenesis in rats. Results showed that LJE contained a total phenolic content of 57.16 g/100 g of seed extract in which 7.67 and 10.09 g/100 g represented total flavonoids and ellagitannins, respectively. LJE protected DNA and human LDL against induced in vitro oxidation, which was associated with the ellagitannin content and with the free-radical scavenging and reducing capacities. LJE alone had a non-clastogenicity/aneugenicity property, but in combination with cisplatin, it enhanced the chromosome aberrations in cancer cells. In colon cancer-induced rats, yogurt with or without LJE caused a reduction in pro-inflammatory parameters, decreased the RNA expression of antiapoptotic cytokines and increased the expression of proapoptotic cytokines. Moreover, LJE attenuated colon cancer initiation and progression by decreasing aberrant crypt foci and LJE recovered the gut microbiome. Together, this evidence suggests that LJE provides chemopreventive protection against colon cancer development by reducing inflammation and increasing proapoptotic pathways.

Extraction optimization of bioactive compounds from ora-pro-nobis (Pereskia aculeata Miller) leaves and their in vitro antioxidant and antihemolytic activities.

Ora-pro-nobis (Pereskia aculeata Miller) is a non-conventional food plant common in Brazil. The objective of this study was to optimize the extraction of bioactive phenolic compounds from ora-pro-nobis leaves by employing solvent mixtures. Ten extracts were obtained with water, ethanol, acetone, and their binary and ternary mixtures, evaluating the chemical composition, antioxidant activity and bioactivities in vitro. The response surface methodology was applied to model the results and calculate the optimal solvent composition, which is 60% water, 40% ethanol and 0% acetone. The optimized extract is rich in phenolic compounds (64 mg GAE/g) and proteins (823 mg/g) and presents antioxidant activity (in intracellular media as well) and inhibits lipid peroxidation (32%) along with hypotonic hemolysis (H50 = 0.339%), it does not present toxicity in vitro against cancer and normal cells. This is the first report of chicoric, caffeoyl-hexaric and coumaroyl-hexaric acids and some glycosylate derivatives of flavonols in ora-pro-nobis leaves.

Polyphenols of jabuticaba [Myrciaria jaboticaba (Vell.) O.Berg] seeds incorporated in a yogurt model exert antioxidant activity and modulate gut microbiota of 1,2-dimethylhydrazine-induced colon cancer in rats.

The chemical composition, antioxidant activity (AA), cytotoxic activity, antihemolytic effects, and enzyme inhibition (EI) of lyophilized jabuticaba (Myrciaria jaboticaba) seed extract (LJE) was studied. The main compounds found were castalagin, vescalagin, procyanidin A2, and ellagic acid. LJE was more toxic to cancer cells than to normal cells, meaning relative toxicological safety. This cytotoxic effect can be attributed to the pro-oxidant effect observed in the reactive oxygen species (ROS) generation assay. LJE inhibited α-amylase, α-glucosidase, and ACE-I activities and protected human erythrocytes from hemolysis. LJE was incorporated into yogurts at different concentrations and the total phenolic content, AA, and EI increased in a dose-dependent manner. LJE-containing yogurt presented 86% sensory acceptance. The yogurt was administered to Wistar rats bearing cancer and it modulated the gut bacterial microbiota, having a prebiotic effect. LJE is a potential functional ingredient for food companies looking for TPC, AA, and prebiotic effect in vivo.

Optimizing the extraction of bioactive compounds from pu-erh tea (Camellia sinensis var. assamica) and evaluation of antioxidant, cytotoxic, antimicrobial, antihemolytic, and inhibition of α-amylase and α-glucosidase activities.

The aims of this study were to quantify and optimize the extraction of total phenolic content (TPC), total flavonoids (TF) and antioxidant activity (AA) of aqueous pu-erh (Camellia sinensis var. assamica) extracts, as well as to compare the optimized pu-erh tea extract (OPT) with toasted mate (Ilex paraguariensis), black and green (Camellia sinensis) teas. The optimization process increased the TPC and the ferric reducing antioxidant power (FRAP). The results showed that the green tea extract presented the highest values for TPC and antioxidant capacity. The pasteurized OPT showed lower TPC and TF, and higher FRAP, DPPH and Cu2+ chelating ability compared to the non-pasteurized OPT. The lyophilized OPT showed inhibition of lipid peroxidation in Wistar rat brain homogenate and displayed antibiofilm activity against Enterococcus faecalis ATCC 25212 and 19433, and Staphylococcus aureus ATCC 25923. Additionally, lyophilized OPT presented cytotoxic and antiproliferative effects against tumor cell lines (Caco-2, A549 and HepG2), inhibited the production of reactive oxygen species in A549 and IMR90 cells, and presented antihemolytic activity in human erythrocytes. The lyophilized OPT inhibited α-glucosidase (IC50 = 47.0 µg/mL) and α-amylase at 30.0 mg/mL. The main compounds detected in OPT were gallic acid, caffeine and theobromine.

Camu-camu (Myrciaria dubia) seeds as a novel source of bioactive compounds with promising antimalarial and antischistosomicidal properties.

Parasitic diseases have attracted worldwide attention of their consequent impact on mortality and morbidity. Accordingly, several plants have been screened for antiparasitic activity aiming to create new alternatives for treatment. These diseases have been neglected and have not attracted worldwide attention (nowadays), the health concerns are focused in chronic diseases, but it is necessary to focus on parasitic diseases and look for prophylactic alternatives, such as plant extracts. Although camu-camu (Myrciaria dubia) seeds are a rich source of antioxidant antimutagenic, cytotoxic, anti-inflammatory, antimicrobial, antihypertensive and neuroprotective compounds, nothing is known about their antiparasitic effects. Thus, in the present study we aimed to evaluate five extracts of camu-camu seeds (100% water, 100% ethyl alcohol, 50% water + 50% ethyl alcohol, 25% water + 75% ethyl alcohol, and 75% water + 25% ethyl alcohol) in relation to their in vitro antimalarial, antischistosomicidal, leishmanicidal and anti-hemolytic effects. The extracts exhibited antischistosomicidal (ED50 values from 418.4 to >1000.0 µg/mL) and antimalarial activities (IC50 values from 24.2 to 240.8 µg/mL) for both W2 and 3D7 strains in all intra-erythrocytic stages. Correlation analysis showed that the toxic effects may mainly be attributed to methylvescalagin (r = -0.548 to -0.951, p < 0.05) and 2,4-dihydroxybenzoic acid (r = -0.612 to -0.917, p < 0.05) contents. Moreover, the anti-hemolytic effect was associated to methylvescalagin (r = -0.597, p < 0.05). No toxic effects were observed for leishmaniasis and IMR90 normal cells. Herein, methylvescalagin was the bioactive compound of greatest interest once it presented simultaneous relation with antiparasitic and anti-hemolytic activities.

Response surface optimization of phenolic compounds extraction from camu-camu (Myrciaria dubia) seed coat based on chemical properties and bioactivity.

Food companies should comply with the requirements of a zero-waste concept to adapt to the circular economy requirements. In fruit companies, usually seeds are discarded without proper utilization and extraction of the bioactive compounds. Fruit seeds are sources of chemical compounds that can be extracted, studied, and applied in high value-added products. Thus, in this work the experimental conditions for the water extraction of phenolic compounds from camu-camu (Myrciaria dubia) seed coat were optimized using a central composite design and the desirability function. Total phenolic content (TPC), and condensed tannins (CT), DPPH radical scavenging activity, ferric reducing antioxidant capacity (FRAP), Folin-Ciocalteu reducing capacity (FCRC), and Cu2+ chelating ability were assessed. Seed coat extracted for 51.1 min using a 1:34.1 solid:liquid ratio was the optimal condition to extract 6,242 mg gallic acid equivalent (GAE)/100 g of TPC and 695 mg catechin equivalent (CE)/100 g of CT. The optimized extract displayed free-radical scavenging activity, reducing properties and ability to chelate Cu2+ , and inhibited the growth of Listeria monocytogenes, Pseudomonas aeruginosa, Salmonella Typhimurium, Salmonella Enteritidis, Bacillus cereus, and Staphylococcus aureus. Additionally, the lyophilized water extract inhibited the in vitro activity of α-amylase, α-glucosidase, and angiotensin converting enzyme and showed cytotoxic effects towards Caco-2, A549, and HepG2 cancer cells, but no cytotoxicity towards IMR90 cells. Vescalagin, castalagin, and 3,4-dihydroxybenzoic acid were the major phenolic compounds identified in the optimized extract. In conclusion, the optimized camu-camu seed coat water extract is a rich source of phenolic compounds with antioxidant, antidiabetic, antihypertensive, and antiproliferative effects. PRACTICAL APPLICATION: Camu-camu fruit pulp and seeds have been studied for their phenolic composition and bioactivity. However, seeds are usually discarded and represent an environmental problem in South American countries. We presented a methodological overview on the extraction optimization of the phenolic compounds from camu-camu seed coat and studied the bioactivity of the optimized extract using chemical, enzymatic, and cell-based experiments. Results can be used by camu-camu processors to obtain a phenolic-rich extract for industrial applications, without any further processing.

Response surface optimization of phenolic compounds from jabuticaba (Myrciaria cauliflora [Mart.] O.Berg) seeds: Antioxidant, antimicrobial, antihyperglycemic, antihypertensive and cytotoxic assessments.

The aim of this study was to evaluate the effects of different solvents and maximize the extraction of bioactive compounds from jabuticaba (Myrciaria cauliflora) seeds. In general, the solvent system composed of water and propanone (52:48 v/v) modified the extract polarity and increased extraction yield of bioactive compounds. The optimized extract presented antioxidant capacity measured by different chemical and biological assays. The optimized extract exerted antiproliferative and cytotoxic effects against A549 and HCT8 cells, antimicrobial and antihemolytic effects, inhibited α-amylase/α-glucosidase activities and presented in vitro antihypertensive effect. Nonetheless, the optimized extract showed no cytotoxicity in a human cell model (IMR90). Vescalagin, castalagin and ellagic acid were the major phenolic compounds in the optimized extract. Our results show that jabuticaba seed may be a potential ingredient for the development of potentially functional foods.

A new analytical concept based on chemistry and toxicology for herbal extracts analysis: From phenolic composition to bioactivity.

Studies regarding the bioactivity of teas are mainly based on the phenolic composition and in vitro antioxidant activity of the herbal species used in their preparation. The aim of this study was to compare the in vitro and ex vivo antioxidant activity, cytotoxic/antiproliferative activity against cancer cells, the inhibitory activity of α-amylase, α-glucosidase and angiotensin I-converting enzymes, as well as the inhibition of DNA-induced fission of the peroxyl radical, in relation to aqueous extracts of Camellia sinensis var. sinensis (CS), Ilex paraguariensis (IP), Aspalathus linearis (AL) and an optimised extract (OT) containing the three herb species. A bivariate and multivariate statistical approach was employed to associate functional activities with individual phenolic composition. The CS and OT extracts showed the highest levels of hesperidin, quercetin-3-rutinoside, (-)-epigallocatechin-3-gallate and isoquercitrin. The CS and OT extracts showed the highest antioxidant activity, greater ability to inhibit α-amylase and proliferation of HCT8 cells, and greater ability to reduce Folin-Ciocalteu reagent. The AL extract, which is the major source of quercetin-3-rutinoside, hesperidin and isoquercitrin, showed the highest ability to inhibit α-glucosidase, the inhibition of LDL oxidation and protection of human erythrocytes. The IP extract showed the highest inhibition of lipoperoxidation in brain homogenate of Wistar rats, antihypertensive activity, and A549 cell proliferation; chlorogenic acid was its major phenolic compound. In general, the in vitro functionality of each extract was dependent on its chemical composition and the OT extract presented the most varied phenolic composition, and biological activity similar to the CS sample. In conclusion, the mixture of CS, AL, and IP represents a chemical and functional-based strategy to develop functional teas.