In situ extraction/encapsulation of olive leaves antioxidants in zein for improved oxidative stability of edible oils.

This study presents a sustainable and cost-effective method for preserving the bioactivity of phenolic compounds in olive leaves (OLE) during their application. The extraction and nanoencapsulation of OLE were performed in a single-step process using a rotor-stator system with zein as the encapsulating agent. The nanoprecipitation step was carried out using an aqueous sodium caseinate solution, resulting in spherical particles with an average diameter of about 640 nm, as confirmed by Transmission Electron Microscopy. Thermal characterization showed that the produced nanoparticles were more thermally stable than free OLE until 250 °C, and FTIR spectra indicated effective interaction between the phenolic compounds and zein. Antioxidant activity was evaluated using TBARS, DPPH, ABTS, and FRAP assays, with results showing that encapsulated OLE had lower antioxidant activity than free OLE. The best antioxidant capacity results were determined by TBARS assay, with IC50 results equal to 43 and 103 µgOLE/mL for free and encapsulated OLE, respectively. No anti-inflammatory potential was detected for both samples using the RAW 264.7 model, and only free OLE showed cytotoxic activity against lung cancer and gastric carcinoma. Encapsulated and free OLE were used as antioxidants in soy, palm, and palm kernel oils and compared to BHT using Rancimat. The Schaal Oven Test was also performed, and the PARAFAC chemometric method analyzed the UV-Vis spectra, which revealed high stability of the oil when 300 mg or the nanoparticles were added per kg oil. Results suggested that zein-encapsulated olive leaf antioxidants can improve the oxidative stability of edible oils.

Bioactive Activities of the Phenolic Extract from Sterile Bracts of Araucaria angustifolia.

Sterile bracts can represent 80% of Araucaria angustifolia pinecone and are a rich source of phenolic compounds. This study aimed to optimize the extraction of the phenolic compounds from Araucaria angustifolia bracts using response surface methodology; the bioactivity properties were also investigated. The effects of the ethanol concentration, solute/solvent ratio, and temperature in relation to the phenolic composition and antioxidant activity were evaluated. The quantification and identification of the individual phenolic compounds (using high-performance liquid chromatography) and their bioactivity were evaluated. The optimized extraction conditions, which detected gallic acid, catechin, epicatechin, quercetin, and kaempferol, were obtained using 60% ethanol at a ratio of 1:38 (w/v) and a temperature of 80 °C. The extract showed high levels of phenolic classes and antioxidant activity. The extract also showed an inhibitory activity for pathogenic (approximately 80%, 10,000 µg/mL) and lactic acid (27.9%, 15,000 µg/mL) bacteria strains. The α-glucosidase inhibitory activity was approximately ten times greater than acarbose, demonstrating its high antiglycemic potential. No antioxidant and anti-inflammatory cellular activity were determined; however, a high cytotoxicity for non-tumor cells and the antiproliferative activity against the tumor cells were observed. Overall, the phenolic extract showed promising action in relation to the fight against the diseases related to oxidative stress and, hopefully, the application of the safe concentrations of the extract, based on bioavailability assays, can be verified.

Low-cost alternative for the bioproduction of bioactive phenolic compounds of callus cultures from Cereus hildmannianus (K.) Schum.

The aim of this study was to establish a sustainable alternative callus culture of Cereus hildmannianus for the production and bioactive determination of phenolic compounds from this species. The conventional callus was cultivated using agar and Murashige and Skoog (MS) medium, while for the alternative culture the agar was replaced with a cotton support covered with filter paper and MS medium (incubated at 32 °C with photoperiod of 16 h), and the morphological characteristics and growth index were assessed (8 weeks). Extracts were obtained by maceration followed by partition, characterized by nuclear magnetic resonance - NMR and ultra-high performance liquid chromatography - UHPLC, quantified (phenolic compounds) by UV-Vis methods, and their antioxidant, antitumor activities, as well as cytotoxicity, were evaluated. The establishment of an alternative callus culture was carried out successfully. Characteristic signals of phenolic compounds were determined by NMR, and 46 compounds with fragment ions were identified using UHPLC analysis. The highest concentrations of phenolic compounds, and greatest antioxidant and antitumor activities, were obtained with the dichloromethane fractions of both callus tissue cultures, which were not cytotoxic. The callus culture from C. hildmannianus has shown promise as a source for the sustainable production of phenolic compounds with antioxidant and antiproliferative activities and thus, has potential use as a natural antitumor product.

Cytotoxicity and anti-inflammatory activities of Gallesia integrifolia (Phytolaccaceae) fruit essential oil.

The chemical composition of Gallesia integrifolia fruits essential oil was obtained by hydrodistillation using a modified Clevenger apparatus was investigated by gas chromatography coupled to mass spectrometry (GC/MS). In addition, the cytotoxicity activity against human tumor cell lines MCF-7 (breast adenocarcinoma), NCI-H460 (large cell lung carcinoma), HeLa (cervical carcinoma), and HepG2 (hepatocellular carcinoma), and non-tumor PLP2 (porcine liver primary cells) as well as the anti-inflammatory action was proposal. The compounds were predominantly organosulfates (2,8-dithianonane, dimethyl trisulfide, and lenthionine). Anti-inflammatory activity that provides 50% inhibition of nitric oxide production (55 µg/mL) of essential oil of the fruits. It also presents cytotoxic activity against MCF-7 (GI50 = 66 µg/mL), NCI-H-460 (GI50 = 147 µg/mL), HeLa (GI50 = 182 µg/mL) and HepG2 (GI50 = 240 µg/mL). The essential oil is more active in tumor cells than in non-tumor cells and the GI50 values for essential oil reported in our work support future studies.

Nutritional value, physicochemical characterization and bioactive properties of the Brazilian quinoa BRS Piabiru.

Chenopodium quinoa Willd. is an ancient food crop that has provided nutrition to Andean populations for thousands of years. BRS Piabiru is a quinoa genotype developed and adapted to tropical climate by the Brazilian Agricultural Research Corporation. In this work, BRS Piabiru quinoa was evaluated concerning its nutritional, physicochemical and phenolic composition and also its bioactive properties. This variety showed high carbohydrate and protein contents and a low-fat level, composed of 86% of unsaturated fatty acids, 60% of which are polyunsaturated fatty acids. Four organic acids were detected, with quinic acid as the most abundant, while α- and γ-tocopherols were the vitamin E isoforms found. Quercetin and kaempferol glycosides were the main phenolic compounds in the quinoa extract, which also revealed relevant antioxidant and antimicrobial activities, with no toxic effect. These results support the potential of BRS Piabiru quinoa as a nutritious food crop and a source of bioactive compounds.

Characterization and Application of Pomegranate Epicarp Extracts as Functional Ingredients in a Typical Brazilian Pastry Product.

Currently, there is a clear tendency to incorporate natural ingredients into food and pharmaceutical formulations. Besides being well-accepted by consumers, these ingredients have less adverse side effects than their artificial counterparts. The pomegranate processing industry produces large quantities of by-products that are discarded as bio-residues, despite containing bioactive compounds. Accordingly, the epicarp of two pomegranate varieties (Mollar de Elche and Purple Queen) was tested as a potential source of bioactive compounds with food application. The phenolic profile was identified by HPLC-DAD-ESI/MS, revealing fourteen phenolic compounds in both varieties (Purple Queen showed also three anthocyanins), with punicalagin isomers as the major compounds. Nonetheless, Mollar de Elche presented greater antioxidant and antibacterial activities. Despite this result, Purple Queen was selected to be tested as a new natural colouring and functionalizing ingredient in a Brazilian pastry product. The incorporation of the selected extract maintained the nutritional profile and provided a higher antioxidant activity compared to the traditional product. In this way, this work confirmed the possible use of pomegranate epicarp as a natural ingredient in the food industry, conferring dyeing and functionalizing effects, and anticipating a possible valorisation of this bio-residue.

Jabuticaba residues (Myrciaria jaboticaba (Vell.) Berg) are rich sources of valuable compounds with bioactive properties.

Jabuticaba (Myrciaria jaboticaba (Vell.) Berg) is a Brazilian berry, very appreciated for in natura consumption. However, its epicarp is not normally consumed due to its stiffness and astringent taste, and in manufacture of products from jabuticaba fruit, it is responsible for the generation of large amounts of residues. The exploration of by-products is becoming important for the obtainment of valuable bioactive compounds for food and pharmaceutical industries. In this context, jabuticaba epicarp was studied regarding its chemical composition, namely in terms of phenolic compounds, tocopherols, and organic acids, and its bioactive properties, such as antioxidant, anti-proliferate, anti-inflammatory, and antimicrobial activities. A total of sixteen phenolic compounds, four tocopherols and six organic acids were identified in jabuticaba epicarp. Regarding bioactive properties, it showed high antioxidant activity, also presenting moderate anti-inflammatory, anti-proliferative, and antimicrobial activities. The extract did not present hepatotoxicity, confirming the possibility of its applications without toxicity issues.

Chemical composition and bioactive properties of byproducts from two different kiwi varieties.

Kiwis are an example of fruits with excellent bioactive properties worldwide appreciated and consumed generating tons of waste. Thus, the objective of this work was to compare two varieties of kiwi: Actinidia deliciosa cv. "Hayward" (green) and Actinidia spp. (red) regarding the nutritional value of their pulps, chemical composition and bioactivities of each pulp and peel. The results revealed that pulps have a high water content and low amount of other macronutrients. Both parts of red kiwi presented the highest tocopherols content and red kiwi pulp presented the highest content in ascorbic acid. In general, the peels exhibited the highest antioxidant activity and green kiwi peels showed cytotoxicity and anti-inflammatory activity, which could be related to its higher content in phenolic compounds, especially B-type (epi)catechin dimer. Therefore, kiwi components currently underutilized may be indicated as a source of natural functionalizing ingredients with several benefits for human health.

Phytochemical Composition and Bioactive Effects of Salvia africana, Salvia officinalis 'Icterina' and Salvia mexicana Aqueous Extracts.

In the present study, aqueous extracts of Salvia africana, Salvia officinalis 'Icterina' and Savia mexicana origin were screened for their phenolic composition and for antibacterial, antioxidant, anti-inflammatory and cytotoxic properties. The three aqueous extracts contained distinct phenolic compounds, with S. africana presenting the highest total levels (231.6 ± 7.5 µg/mg). Rosmarinic acid was the dominant phenolic compound in all extracts, yet that of S. africana origin was characterized by the present of yunnaneic acid isomers, which overall accounted for about 40% of total phenolics. In turn, S. officinalis 'Icterina' extract presented glycosidic forms of apigenin, luteolin and scuttelarein, and the one obtained from S. mexicana contained several simple caffeic acid derivatives. S. africana aqueous extract exhibited high antioxidant potential in four methods, namely the DPPH• (2,2-diphenyl-1-picrylhydrazyl) scavenging ability, iron-reducing power, inhibition of ß-carotene bleaching and of thiobarbituric acid reactive substances (TBARS), for which EC50 values were equal or only 1.3-3.1 higher than those of the standard compounds. Moreover, this extract was able to lower the levels of nitric oxide (NO) production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages (EC50 = 47.8 ± 2.1 µg/mL). In addition, the three sage aqueous extracts showed promising cytotoxic effect towards hepatocellular HepG2, cervical HeLa, and breast carcinoma cells MCF-7. Overall this study highlights the potential of three little-exploited Salvia species, with commercial value for applications in food or pharmaceutical industries.

A new variety of purple tomato as a rich source of bioactive carotenoids and its potential health benefits.

Carotenoid-rich fractions (CRF) from pulp and peel of a new variety of purple tomato were investigated in comparison to a Red Cherry variety regarding carotenoids characterization, antioxidant capacity, and inhibition of proliferation of four tumor cell lines. CRF from peel of Purple tomato contains lutein, lycopene, and ß-carotene up to 6, 1.5, and 2.5 times more than that of Red Cherry and it exhibited the highest antioxidant activity at 400 µg/mL, reaching 82% and 97% in DPPH and ABTS•+ assays, respectively. Besides that, the Purple peel showed the highest scavenging lipoperoxides capacity as well as displayed the highest ferric reducing antioxidant power compared to the other CRF. In turn, the Red Cherry pulp CRF showed the highest antiproliferative activity against four tumor cell lines (MCF-7, NCI-H460, HeLa, and HepG2) at non-toxic concentrations. High concentration of neurosporene, and lycopene in Red Cherry pulp CRF show to be related to the good antiproliferative activity found on it. Therefore, this new variety of nutrient-rich purple tomato could be explored as well as the commercial variety Red Cherry, since both are good sources of dietary carotenoids with health-promoting properties.

Nutritional composition and bioactivity of Umbilicus rupestris (Salisb.) Dandy: An underexploited edible wild plant.

The inclusion of edible wild plants in human diet has been receiving an increasing attention, as they represent an easily accessible source of nutrients, vitamins and antioxidants. In this work, the leaves of Umbelicus rupestris (Salisb.) Dandy, an edible species for which only scarce data is available in literature, were thoroughly evaluated for its nutritional profile, chemical characterization and bioactive properties. Being considered a succulent plant, the leaves revealed a very high content of moisture, with several beneficial compounds, including omega-3 polyunsaturated fatty acids, tocopherols and different polyphenols. A total of twelve flavonoids, three phenolic acids and one phenylpropanoid glucoside were identified in the decoction and/or hydroethanolic extracts, with most of them being described for the first time in this plant. Both extracts showed antioxidant activity and potential to inhibit some of the assayed bacteria, while not presenting cytotoxic effects on a non-tumour primary cell culture.

Phytochemical profile and biological activities of 'Ora-pro-nobis' leaves (Pereskia aculeata Miller), an underexploited superfood from the Brazilian Atlantic Forest.

Pereskia aculeata Miller, known worldwide as ora-pro-nobis, is a highly nutritive species of the Cactaceae family from the Brazilian Atlantic Forest. In this work, we report inedited information on the phenolic profile of P. aculeata leaves, besides a broad study of their antioxidant potential using a set of five different methods. A total of ten phenolic compounds were identified, such as two phenolic acids (caffeic acid derivatives) and eight flavonoids (quercetin, kaempferol and isorhamnetin glycoside derivatives). Caftaric acid was the extract's major phenolic constituent, accounting for more than 49% of the phenolic content, followed by quercetin-3-O-rutinoside (14.99%) and isorhamnetin-O-pentoside-O-rutinoside (9.56%). Overall, the ora-pro-nobis leaf extract showed relevant values of antioxidant capacity, with higher activities than the Trolox in the DPPH and ABTS trials. The antimicrobial activity exhibited by the extract against both Gram-positive and Gram-negative bacteria suggests the presence of a broad spectrum of phytochemicals with antibiotic activity.

The nanoencapsulation of curcuminoids extracted from Curcuma longa L. and an evaluation of their cytotoxic, enzymatic, antioxidant and anti-inflammatory activities.

Curcumin, bisdemethoxycurcumin and demethoxycurcumin are the main curcuminoids present in Curcuma longa L. and are known for their bioactivity. However, their low water solubility results in poor bioavailability and therapeutic efficacy. This work aimed to investigate the in vitro modulation capacity on the enzymes acetylcholinesterase (AChE) and glutathione S-transferase (GST), as well as the in vitro antioxidant (OxHLIA and TBARS) and anti-inflammatory activities (RAW 264.7 test) of nanoencapsulated curcuminoids. Cytotoxicity on tumor and non-tumor cell lines was also investigated. Curcuminoid nanoparticles significantly inhibited the in vitro activity of AChE (12% inhibition at 50 µM) and GST (30% inhibition at 5 µM). They presented antioxidant activity and toxic effects against breast adenocarcinoma, lung, cervical and hepatocellular carcinoma cells when dispersed in water. Encapsulated curcuminoids exhibited bioactive properties in aqueous medium (no hydrophobic solvent added), exerting antioxidant and cytotoxic effects and acting on the cholinergic and endogenous antioxidant systems.

Effects of in vitro gastrointestinal digestion and colonic fermentation on a rosemary (Rosmarinus officinalis L) extract rich in rosmarinic acid.

The potential phytochemical losses occurring throughout the sequential steps of in-vitro gastrointestinal digestion and colonic fermentation of a rosemary aqueous extract were investigated. Crude (CE), digested (DE) and fermented (FE) extracts were characterized in terms of their phenolic profile and biological activities. Rosmarinic acid was the phytochemical that underwent the most significate transformation during digestion and fermentation, which amounted to 60% compared to the 26% degradation of the total phenolics. Overall, the simulated digestion step decreased the antioxidant activity estimated by DPPH, ABTS, FRAP, ORAC and TBARS assays. Both CE and DE did not present antiproliferative potential, however, FE exhibited a pronounced cytotoxic activity (GI50 = 116 µg/mL) against HeLa cells. CE and DE showed to be moderate inhibitors of methicillin-resistant Staphylococcus aureus (MRSA), methicillin-susceptible S. aureus (MSSA), S. aureus, Listeria monocytogenes, whilst the FE acted as a moderate inhibitor of MRSA and MSSA.

Bioactive properties and phytochemical assessment of Bacupari-anão (Garcinia brasiliensis Mart.) leaves native to Rondônia, Brazil.

Leaf fractions of Garcinia brasiliensis were evaluated concerning their antioxidant, antimicrobial, anti-inflammatory and cytotoxic properties, and the most active fraction was then fully characterized regarding its phenolic composition using HPLC-DAD-ESI/MSn. The ethyl acetate fraction from partitioning of the methanolic leaf extract revealed a strong antioxidant activity that was comparable to Trolox, the positive control. This fraction was also able to show a significant antimicrobial activity against Gram-positive and Gram-negative bacteria and the fungus Candida albicans. However, the dichloromethane fraction was found to present the highest anti-inflammatory (83 ± 9 µg mL-1) and cytotoxic activities, thus presenting slight toxicity using a non-tumor cell line. Regarding the phenolic profile, the ethyl acetate fraction presented twelve flavonoids, with morelloflavone-7''-O-glucoside (52.1 ± 0.4 mg g-1) and gardinia biflavonoid 2a glucoside (27.5 ± 0.2 mg g-1) being the major compounds identified. These results indicate that leaves of G. brasiliensis might be a potential source of natural biomolecules for pharmaceutical and medicinal applications.

Antiproliferative Activity of Neem Leaf Extracts Obtained by a Sequential Pressurized Liquid Extraction.

Azadirachta indica A. Juss (neem) extracts have been used in pharmaceutical applications as antitumor agents, due to their terpenes and phenolic compounds. To obtain extracts from neem leaves with potential antiproliferative effect, a sequential process of pressurized liquid extraction was carried out in a fixed bed extractor at 25 °C and 100 bar, using hexane (SH), ethyl acetate (SEA), and ethanol (SE) as solvents. Extractions using only ethanol (EE) was also conducted to compare the characteristics of the fractionated extracts. The results obtained by liquid chromatography-electrospray ionization mass spectrometry suggested a higher concentration of terpenes in the SEA extract in comparison to SH, SE, and EE extracts. Therefore, antiproliferative activity showed that SEA extracts were the most efficient inhibitor to human tumor cells MCF-7, NCI-H460, HeLa, and HepG2. Hepatocellular cells were more resistant to SH, SEA, SE, and EE compared to breast, lung, hepatocellular, and cervical malignant cells. Neem fractioned extracts obtained in the present study seem to be more selective for malignant cells compared to the non-tumor cells.

The influence of electron beam radiation in the nutritional value, chemical composition and bioactivities of edible flowers of Bauhinia variegata L. var. candida alba Buch.-Ham from Brazil.

As edible flowers are highly perishable, irradiation technology can be applied to increase their shelf life, as also for phytosanitary purposes. Herein, flowers of Bauhinia variegata L. var. candida alba Buch.-Ham were submitted to electron beam irradiation at the doses of 0.5, 0.8 and 1kGy, to study the effects in the nutritional and chemical profiles, and also in antioxidant, cytotoxic and anti-inflammatory activities. The petals of white flowers revealed interesting bioactive properties being kaempferol derivatives the most abundant compounds, especially kaempferol-3-O-rutinoside. The applied irradiation doses did not highly affect the nutritional profile. No changes were produced in cytotoxicity, but the anti-inflammatory activity slightly decreased. However, the antioxidant activity was increased, especially in the dose of 0.5kGy, in agreement with the higher content in phenolic compounds found at this dose.

Multifunctions of Pleurotus sajor-caju (Fr.) Singer: A highly nutritious food and a source for bioactive compounds.

A study with Pleurotus sajor-caju was conducted to: evaluate the nutritional and chemical composition of the fruiting bodies; optimize the preparation of bioactive phenolic extracts; and characterize the optimized extract in terms of bioactive compounds and properties. P. sajor-caju revealed an equilibrated nutritional composition with the presence of hydrophilic (sugars and organic acids) and lipophilic (tocopherols and PUFA) compounds. p-Hydroxybenzoic, p-coumaric and cinnamic acids were identified in the extract obtained with ethanol (30g/l ratio) at 55°C for 85min. This extract showed antioxidant properties (mainly reducing power and lipid peroxidation inhibition), antibacterial activity against MRSA and MSSA and cytotoxicity against NCI-H460, MCF-7 and HeLa. Furthermore, as the extract showed capacity to inhibit NO production in Raw 264.7 macrophages, molecular docking studies were performed to provide insights into the anti-inflammatory mechanism of action, through COX-2 inhibition by the phenolic acids identified.

Bioactive formulations prepared from fruiting bodies and submerged culture mycelia of the Brazilian edible mushroom Pleurotus ostreatoroseus Singer.

Pleurotus ostreatoroseus is a Brazilian edible mushroom whose chemical characterization and bioactivity still remain underexplored. In this study, the hydrophilic and lipophilic compounds as well as the antioxidant, anti-inflammatory and antimicrobial activities of formulations (ethanol extracts) prepared with its fruiting bodies and submerged culture mycelia were compared. The bioactive formulations contain at least five free sugars, four organic acids, four phenolic compounds and two tocopherols. The fruiting body-based formulation revealed higher reducing power, DPPH scavenging activity, ß-carotene bleaching inhibition and lipid peroxidation inhibition in brain homogenates than the mycelium-based preparation, as well as higher anti-inflammatory and antimicrobial activities. The absence of hepatotoxicity was confirmed in porcine liver primary cells. These functional responses can be related to the levels of bioactive components including phenolic acids, organic acids and tocopherols.