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.

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.

Phenolic composition by UHPLC-Q-TOF-MS/MS and stability of anthocyanins from Clitoria ternatea L. (butterfly pea) blue petals.

The aim of the present study was to evaluate the phenolic composition of crude lyophilized extracts (CLE) and partially purified (PPE) extracts of C. ternatea blue petals as well as the anthocyanin stability against pH, temperature and light in the presence and absence of fructooligosaccharides. Twelve compounds were tentatively identified by UHPLC-Q-TOF-MS/MS in CLE and PPE extracts. In direct/reverse spectrophotometric titration, anthocyanins showed colour changes between pH 2.25 to 10.20, and colour reversibility, maintaining antioxidant activity against the DPPH radical. The aqueous extracts at pH 3.6 and 5.4 exhibited thermal stability with the presence and absence of fructooligosaccharides with activation energy higher than 99 kJ/mol. The addition of fructooligosaccharides in the extracts at pH 5.4 exposed to light provided a protective effect against anthocyanin photodegradation. The data show the technological potential of aqueous extract of C. ternatea blue petals as a natural colourant in a functional beverage model system.

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.

Clitoria ternatea L. petal bioactive compounds display antioxidant, antihemolytic and antihypertensive effects, inhibit α-amylase and α-glucosidase activities and reduce human LDL cholesterol and DNA induced oxidation.

The purpose of this study was to use a statistical approach to optimise the experimental conditions regarding the extraction of bioactive compounds, and to analyse the in vitro functional properties of crude lyophilized extracts (CLE) and partially purified (PPE) extracts of Clitoria ternatea petals. The results showed that the factors of temperature and time influenced the extraction of phenolic compounds, antioxidant activity and the physicochemical parameters. Simultaneous optimisation showed that the same levels of bioactive compounds were extracted when using temperatures from 11.7 to 68.3 °C and times from 8.47 to 51.12 min. Principal component analysis revealed the experimental conditions that provided the extraction producing the highest level of phenolic content (40 °C/30 min). The CLE showed antimicrobial activity; protective effect against hemolysis of erythrocytes; inhibition of α-amylase, α-glucosidase and angiotensin-I-converting (ACE-I) enzymes; and inhibition of lipid peroxidation. The CLE and PPE demonstrated oxygen radical absorption capacity; inhibition of DNA strand scission; inhibition of LDL cholesterol oxidation; intracellular antioxidant activity against reactive oxygen species (>100 µg/mL); and no cytotoxicity (IC50, GI50 and LC50 > 900 µg/mL) against A549, HCT8 and IMR90 cell lines.

Red Chicory (Cichorium intybus) Extract Rich in Anthocyanins: Chemical Stability, Antioxidant Activity, and Antiproliferative Activity In Vitro.

Red chicory leaves are appreciated sensorially and their constituents contain bioactive properties. The objectives of this study were as follows: to use an experimental design to extract anthocyanins from red chicory in aqueous solution at pH 2.5; to determine the stability of the extracts in relation to temperature and pH; and to evaluate the antioxidant activity and in vitro cytotoxic effect of the lyophilized and purified extracts. The best extraction conditions for the bioactive compounds from red chicory were a temperature of 64.2 °C for 25 min; the anthocyanin content was 73.53 ± 0.13 mg per 100 g fresh weight basis sample. The EC50 (Half maximal effective concentration) value for the antioxidant activity assay in relation to DPPH (2,2-diphenyl-1-picrylhydrazyl) with optimized extract was 0.363, which corresponds to a concentration of 39.171 µmol/L of anthocyanins. The activation energy for the degradation reaction of the anthocyanins from the red chicory extract was 84.88 kJ/mol. The optimized extract, which was rich in anthocyanins, showed chemical and biological antioxidant activity (protection against erythrocyte hemolysis) and inhibited lipid peroxidation in vitro. The Cichorium intybus L. extracts interfered on the levels of reactive oxygen species generation and the crude extract did not present procarcinogenic effect. PRACTICAL APPLICATION: Red chicory is basically consumed as a part of traditional dishes worldwide. Here, we developed a process to extract and purify the anthocyanins from Cichorium intybus leaves and test the extracts in terms of the chemical composition, thermal stability, antioxidant activity, and antiproliferative effects. The anthocyanin-rich extract presented antioxidant activity in chemical and biological assays and low cytotoxicity and cytoprotective effects in relation to HepG2, HCT8, and Caco-2 cell lines. Additionally, the red chicory extract protected human erythrocytes against hemolysis. This extract may be used as a natural colorant/antioxidant in foods.

In vitro antioxidant and antihypertensive compounds from camu-camu (Myrciaria dubia McVaugh, Myrtaceae) seed coat: A multivariate structure-activity study.

Camu-camu (Myrciaria dubia) pulp, seeds, and skin are widely known because of their nutritional properties. However, the seed coat has never been studied as a source of bioactive compounds. Herein, we characterized the phenolic composition, the antioxidant activity, and inhibition of angiotensin-converting enzyme (ACE) of three different extracts (water, propanone, and ethanol) from this residue and assessed the structure-activity using bivariate and multivariate statistical approaches. Phenolic acids and flavonoids were quantified by high-performance liquid chromatography while the ferric reducing antioxidant power (FRAP), inhibition of lipid peroxidation using egg yolk and Wistar rat brain, scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH•) radical, Folin-Ciocalteu reducing capacity (FCRC), and the inhibition of angiotensin-converting enzyme (ACE) by the extracts were also analyzed. t-Resveratrol was found in camu-camu seed coat for the first time. The aqueous extract had the highest total phenolic content, FRAP, DPPH•, FCRC, and inhibition of lipid oxidation using both chemical and biological assays, while the propanone extract showed the opposite behavior but it presented higher in vitro antihypertensive activity. The ethanolic extract exhibited intermediate values for the responses. The association between chemical composition and the functional properties of the camu-camu seed coat extracts were revealed using correlation analysis and principal component analysis.

Chemical study, antioxidant, anti-hypertensive, and cytotoxic/cytoprotective activities of Centaurea cyanus L. petals aqueous extract.

This study aimed to optimise the experimental conditions of extraction of the phytochemical compounds and functional properties of Centaurea cyanus petals. The following parameters were determined: the chemical composition (LC-ESI-MS/MS), the effects of pH on the stability and antioxidant activity of anthocyanins, the inhibition of lipid peroxidation, antioxidant activity, anti-hemolytic activity, antimicrobial, anti-hypertensive, and cytotoxic/cytoprotective effect, and the measurements of intracellular reactive oxygen species. Results showed that the temperature and time influenced (p ≤ 0.05) the content of flavonoids, anthocyanins, and FRAP. Only the temperature influenced the total phenolic content, non-anthocyanin flavonoids, and antioxidant activity (DPPH). The statistical approach made it possible to obtain the optimised experimental extraction conditions to increase the level of bioactive compounds. Chlorogenic, caffeic, ferulic, and p-coumaric acids, isoquercitrin, and coumarin were identified as the major compounds in the optimised extract. The optimised extract presented anti-hemolytic and anti-hypertensive activity in vitro, in addition to showing stability and reversibility of anthocyanins and antioxidant activity with pH variation. The C. cyanus petals aqueous extract exhibited high IC50 and GI50 (>900 µg/mL) values for all cell lines, meaning low cytotoxicity. Based on the stress oxidative assay, the extract exhibited pro-oxidant action (10-100 µg/mL) but did not cause damage or cell death.