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Functional lipids are lipids that are found in food matrices and play an important role in influencing human health as their role goes beyond energy storage and structural components. Ongoing research into functional lipids has highlighted their potential to modulate immune responses and other mechanisms associated with obesity, along with its comorbidities. These lipids represent a new field that may offer new therapeutic and preventive strategies for these diseases by understanding their contribution to health. In this review, we discussed in-depth the potential food sources of functional lipids and their reported potential benefit of the major lipid classification: based on their composition such as simple, compound, and derived lipids, and based on their function such as storage and structural, by investigating the intricate mechanisms through which these lipids interact in the human body. We summarize the key insights into the bioaccessibility and bioavailability of the most studied functional lipids. Furthermore, we review the main immunomodulatory mechanisms reported in the literature in the past years. Finally, we discuss the perspectives and challenges faced in the food industry related to functional lipids.
Functional lipids are immunomodulatory agents in chronic non-communicable diseases.Bioaccessibility and bioavailability depend mainly on the lipid profile and the matrix food.Incorporation of polyunsaturated fat in foods is a current technological challenge.Emerging technologies are good options for extracting functional lipids efficiently.Nanotechnology plays an important role in developing food delivery systems.Food delivery systems improve the bioavailability of functional lipids.
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Skin aging represents a health and aesthetic problem that could result in infections and skin diseases. Bioactive peptides can potentially be used in skin aging regulation. Chickpea (Cicer arietinum L.) selenoproteins were obtained from germination with 2 mg Na2SeO3/100 g of seeds for 2 days. Alcalase, pepsin, and trypsin were used as hydrolyzers, and a membrane < 10 kDa was used to fractionate the hydrolysate. Se content, antioxidant capacity, elastase and collagen inhibition, functional stability, and preventative capacity were analyzed. Significant increases in Se content were found in germinated chickpea flour and protein related to the control. An increase of 38% in protein was observed in the selenized flour related to the control. A band (600-550 cm-1) observed in the selenized hydrolysates suggested the insertion of Se into the protein. Hydrolysates from pepsin and trypsin had the highest antioxidant potential. Se enhanced the stability of total protein and protein hydrolysates through time and increased their antioxidant capacity. Hydrolysates > 10 kDa had higher elastase and collagenase inhibition than the total protein and hydrolysates < 10 kDa. Protein hydrolysates < 10 kDa 6 h before UVA radiation had the highest inhibition of collagen degradation. Selenized protein hydrolysates showed promising antioxidant effects that could be related to skin anti-aging effects.
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Antioxidantes , Cicer , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Cicer/química , Hidrolisados de Proteína/química , Pepsina A/metabolismo , Tripsina/metabolismo , Elastase Pancreática/metabolismoRESUMO
The aim of this study was to explore the effect of capsaicin and particular phenolic compounds profile from cellulase assisted extracts of Habanero (Capsicum chinense) chili pepper seeds (CPS) on the concentration of cytokines (IL-2, IL-6, TNF-α, IL-1ß) in murine macrophages (RAW 264.7) stimulated with lipopolysaccharides (LPS). Capsaicin was quantified by HPLC-DAD, and the phenolic profile was determined by UPLC-MS-QqQ. Anti-inflammatory activity was evaluated by Mouse Cytokine/Chemokine Magnetic Bead Panel 96-well plate assay. Among the 15 different phenolics found in CPS extracts obtained at 120 or 150 min of maceration with 2,500 UI/L at 30 ºC or 45 ºC in a 1:15 (w:v) proportion, the most abundant was vanillic acid (7.97-12.66 µg/g). The extract obtained at 30 ºC and 120 min, showed similar effects than the observed for synthetic anti-inflammatory drugs indomethacin and dexamethasone, and capsaicin standard. Beyond capsaicin, salicylic, protocatechuic and trans-cinnamic acids as well as vanillin in CPS extracts were correlated with the anti-inflammatory effect. On the other hand, capsaicin and chlorogenic acid contents were potential immunostimulants whose concentration varied depending on the cellulase treatment time.
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Capsicum , Celulases , Camundongos , Animais , Capsaicina , Cromatografia Líquida , Frutas/química , Espectrometria de Massas em Tandem , Sementes/química , Anti-Inflamatórios , Extratos Vegetais , Cânfora , Mentol , FenóisRESUMO
Phenolic compounds are abundant in nature and have multiple beneficial effects on human health due to their antioxidant, anti-inflammatory, antithrombotic, antiallergenic, anticancer, and antiatherosclerotic properties. For this reason, phenolics are becoming relevant functional ingredients for several industries, mainly the food industry, derived from food consumer exigencies and regulations. However, the use of their beneficial properties still presents some limitations, such as chemical instability under environmental and processing conditions, which leads to structural changes and compromises their biological activities. They also present poor water solubility and sensitivity to pH changes, decreasing their bioavailability in the organism. The technologies for extraction and stabilization of these compounds have evolved rapidly in the development of different delivery systems to encapsulate sensitive active molecules. Biopolymeric nanoparticles are biodegradable polymer-based colloidal systems with sizes ranging from 1 to 1000 nm, and different techniques can be carried out to develop them. These systems have emerged as a green and effective alternative to improve stability, bioavailability, and biological effects of phenolic compounds. This comprehensive review aims to present an overview of recent advances in encapsulation processes of phenolic compounds within biopolymer nanoparticles as delivery systems and the impact on their physicochemical properties and biological effects after encapsulation. © 2021 Society of Chemical Industry.
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Biopolímeros/química , Sistemas de Liberação de Medicamentos/instrumentação , Nanopartículas/química , Fenóis/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos/métodos , Estabilidade de Medicamentos , Humanos , Fenóis/farmacologiaRESUMO
Cacti are an important source of metabolites but present limitations for their commercial exploitation, like slow growth and a decrease of wild populations. An alternative to obtain their biocompounds without affecting the natural environment are the in vitro culture techniques. We established in vitro cultures from Mammillaria candida Scheidweiler and Turbinicarpus laui Glass and Foster and used different stresses to increase metabolites and antioxidant activity. The cultures were exposed to 1.25% polyethylene glycol to induce a moderate drought stress, 50 g L-1 sucrose to generate an osmotic stress, chitosan (1.25 to 5 mg mL-1) to simulate a biotic attack, or to UV light. Chitosan was the best elicitor improving 1.5 times the concentration of phenolics, 9 to 10 times the content of flavonoids and betalains, and 16% the antioxidant activity in M. candida suspensions. In T. laui suspensions, this elicitor duplicates the flavonoids content and antioxidant activity. The antioxidant levels in elicited suspensions increased 5 to 10 times in relation to plant tubercles. Eleven compounds were identified in M. candida suspensions being digalloyl rhamnoside and epicatequin gallate the most abundant; in the T. laui suspensions, 16 compounds were detected and the most abundant were 17-decarboxi neobetanin and derivatives of luteolin. Thus, cacti in vitro culture is an efficient system to obtain high level of metabolites of biological interest.
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Antioxidantes/química , Cactaceae/química , Antioxidantes/isolamento & purificação , Betalaínas/biossíntese , Cactaceae/crescimento & desenvolvimento , Quitosana , Cromatografia Líquida de Alta Pressão , Meios de Cultura , Flavonoides/biossíntese , Luteolina/biossíntese , Fenóis/química , Fenóis/isolamento & purificação , PolietilenoglicóisRESUMO
Mango (Mangifera indica cv. Ataulfo) peel contains bound phenolics that may be released by alkaline or acid hydrolysis and may be converted into less complex molecules. Free phenolics from mango cv. Ataulfo peel were obtained using a methanolic extraction, and their cellular antioxidant activity (CAA) and permeability were compared to those obtained for bound phenolics released by alkaline or acid hydrolysis. Gallic acid was found as a simple phenolic acid after alkaline hydrolysis along with mangiferin isomers and quercetin as aglycone and glycosides. Only gallic acid, ethyl gallate, mangiferin, and quercetin were identified in the acid fraction. The acid and alkaline fractions showed the highest CAA (60.5% and 51.5%) when tested at 125 µg/mL. The value of the apparent permeability coefficient (Papp) across the Caco-2/HT-29 monolayer of gallic acid from the alkaline fraction was higher (2.61 × 10-6 cm/s) than in the other fractions and similar to that obtained when tested pure (2.48 × 10-6 cm/s). In conclusion, mango peels contain bound phenolic compounds that, after their release, have permeability similar to pure compounds and exert an important CAA. This finding can be applied in the development of nutraceuticals using this important by-product from the mango processing industry.
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Antioxidantes/farmacologia , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Mangifera/química , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Antioxidantes/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Humanos , Permeabilidade , Fenóis/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/químicaRESUMO
Isorhamnetin glycosides are representative compounds of Opuntia ficus-indica that possess different biological activities. There is slight information about the changes in bioaccessibility induced by the glycosylation pattern of flavonoids, particularly for isorhamnetin. In this study, the bioaccessibility and permeability of isorhamnetin glycosides extracted from O. ficus-indica were contrasted with an isorhamnetin standard. Also, the plasma stability of these isorhamnetin glycosides after intravenous administration in rats was evaluated. Recoveries of isorhamnetin after oral and gastric digestion were lower than that observed for its glycosides. After intestinal digestion, isorhamnetin glycosides recoveries were reduced to less than 81.0%. The apparent permeability coefficient from apical (AP) to basolateral (BL) direction (Papp(AP-BL)) of isorhamnetin was 2.6 to 4.6-fold higher than those obtained for its glycosides. Isorhamnetin diglycosides showed higher Papp(AP-BL) values than triglycosides. Sugar substituents affected the Papp(AP-BL) of the triglycosides. Isorhamnetin glycosides were better retained in the circulatory system than the aglycone. After intravenous dose of the isorhamnetin standard, the elimination half-life was 0.64 h but increased to 1.08 h when the O. ficus-indica extract was administered. These results suggest that isorhamnetin glycosides naturally found in O. ficus-indica could be a controlled delivery system to maintain a constant plasmatic concentration of this important flavonoid to exert its biological effects in vivo.
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Glicosídeos/farmacocinética , Mucosa Intestinal/metabolismo , Opuntia/química , Extratos Vegetais/farmacocinética , Quercetina/análogos & derivados , Animais , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão , Glicosídeos/química , Humanos , Estrutura Molecular , Permeabilidade , Extratos Vegetais/química , Quercetina/química , Quercetina/farmacocinética , Ratos , Reprodutibilidade dos TestesRESUMO
BACKGROUND: Mango bark is an important agro-industrial residue from mango pruning. In traditional medicine, the aqueous extract from mango bark (MBE) has been used in ethnomedicine for the treatment of many diseases. However, there is scarce information using cellular models to evaluate the potential use of this plant material for human consumption. In this study, the phenolic content from the MBE from four varieties (Kent, Keitt, Ataulfo and Tommy Atkins) was analyzed by high-performance liquid chromatography coupled to photodiode array detector (HPLC-DAD) and liquid chromatography coupled with time-of-flight mass spectrometry (LC/MS-TOF). Additionally, the cellular antioxidant activity of the MBE from the four mango varieties were compared. Finally, the intestinal permeability of the main polyphenols found in the MBE (mangiferin and gallic acid) was evaluated. RESULTS: Mangiferin and gallic acid were the main constituents in the MBE from the four mango varieties. Furthermore, the Ataulfo variety showed the highest cellular antioxidant activity (67%) at the concentration of 100 µg mL−1 . The intestinal permeability of mangiferin present in the bark extracts was 3- to 4.8-fold higher than those of mangiferin as standard, whereas the intestinal permeability of gallic acid varied among the tested extracts. CONCLUSION: MBE has the potential to exert antioxidant activity at the cellular level and can have an impact on human health. It may also be a good source for the extraction of polyphenols mainly mangiferin.
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Antioxidantes/metabolismo , Mucosa Intestinal/metabolismo , Mangifera/química , Fenóis/metabolismo , Casca de Planta/química , Extratos Vegetais/metabolismo , Antioxidantes/química , Células CACO-2 , Ácido Gálico/análise , Ácido Gálico/metabolismo , Humanos , Mangifera/classificação , Fenóis/química , Extratos Vegetais/química , Xantonas/análise , Xantonas/metabolismoRESUMO
(OFI) contains health-promoting compounds like flavonoids, being the isorhamnetin glycosides the most abundant. We evaluated the effect of OFI extracts with different isorhamnetin glycosides against two different human colon cancer cells (HT-29 and Caco2). The extracts were obtained by alkaline hydrolysis with NaOH at 40 °C during 15, 30 or 60 min. Tri and diglycosides were the most abundant isorhamnetin glycosides, therefore these compounds were isolated to compare their cytotoxic effect with the obtained from the extracts. The OFI extracts and purified isorhamnetin glycosides were more cytotoxic against HT-29 cells than Caco2 cells. OFI-30 exhibited the lowest IC50 value against HT-29 (4.9 ± 0.5 µg/mL) and against Caco2 (8.2 ± 0.3 µg/mL). Isorhamnetin diglycosides IG5 and IG6 were more cytotoxic than pure isorhamnetin aglycone or triglycosides when they were tested in HT-29 cells. Bioluminescent analysis revealed increased activity of caspase 3/7 in OFI extracts-treated cells, particularly for the extract with the highest concentration of isorhamnetin triglycosides. Flow cytometry analysis confirmed that OFI extract and isorhamnetin glycosides induced a higher percentage of apoptosis in HT-29 than in Caco2, while isorhamnetin was more apoptotic in Caco2. This research demonstrated that glycosilation affected antiproliferative effect of pure isorhamnetin glycosides or when they are mixed with other phytochemicals in an extract obtained from OFI.
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Adenocarcinoma/tratamento farmacológico , Apoptose/efeitos dos fármacos , Neoplasias do Colo/tratamento farmacológico , Glicosídeos/uso terapêutico , Opuntia/química , Fitoterapia , Quercetina/análogos & derivados , Adenocarcinoma/metabolismo , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Células CACO-2 , Caspases/metabolismo , Linhagem Celular Tumoral , Proliferação de Células , Colo/efeitos dos fármacos , Neoplasias do Colo/metabolismo , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Glicosídeos/farmacologia , Células HT29 , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Quercetina/farmacologia , Quercetina/uso terapêuticoRESUMO
The study investigated Chenopodium berlandieri to analyze its oleanolic acid (OA) content. Response surface methodology with central composite design was used to improve saponin extraction, varying temperature, ethanol, and sample-to-solvent ratio. Best conditions (65 °C, 50% ethanol, 1:10 ratio) yielded 53.45 ± 0.63 mg/g of extract from Huauzontle seeds. Temperature linearly impacted extract yield, while temperature and ethanol influenced total saponin content. Hydrolyzing saponin-rich extracts produced OA-rich extracts. Characterization via HPLC-ELSD and LC-MS identified OA4 as the most concentrated OA saponin (5.54 ± 0.16 mg/g). OA alone reached 2.02 ± 0.12 mg/g. Acid hydrolysis increased OA content by up to 3.27×, highlighting the potential of hydrolyzed Huauzontle extracts as a natural ingredient for various industries due to enhanced OA content.
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Chenopodium , Ácido Oleanólico , Extratos Vegetais , Saponinas , Ácido Oleanólico/química , Ácido Oleanólico/análise , Saponinas/química , Hidrólise , Extratos Vegetais/química , Chenopodium/química , Cromatografia Líquida de Alta Pressão , Sementes/químicaRESUMO
A supercritical CO2 method was optimized to recover naringenin-rich extract from Mexican oregano (Lippia graveolens), a flavanone with high antioxidant and anti-inflammatory activity. The effect of the extraction parameters like pressure, temperature, and co-solvent on naringenin concentration was evaluated. We used response surface methodology to optimize the naringenin extraction from oregano; the chemical composition by UPLC-MS of the optimized extract and the effect of simulated gastrointestinal digestion on its antioxidant capacity and total phenolic content were also evaluated. The optimum conditions were 58.4 °C and 12.46% co-solvent (ethanol), with a pressure of 166 bar, obtaining a naringenin content of 46.59 mg/g extract. Also, supercritical optimized extracts yielded high quantities of cirsimaritin, quercetin, phloridzin, apigenin, and luteolin. The results indicated that the naringenin-rich extract obtained at optimized conditions had higher total phenolic content, antioxidant capacity by TEAC and ORAC, and flavonoid content, compared with the methanolic extract, and the simulated gastrointestinal digestion reduced all these values.
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Flavanonas , Lippia , Origanum , Antioxidantes/química , Lippia/química , Origanum/química , Dióxido de Carbono , Cromatografia Líquida , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectrometria de Massas em Tandem , Fenóis , Solventes/química , DigestãoRESUMO
It has been reported that pineapple (Ananas comosus) contains healthy nutrients and phytochemicals associated with antioxidant and anti-inflammatory capacities. However, a substantial amount of pineapple residue is produced due to a lack of valorization applications at the industrial scale, resulting in the loss of valuable nutrients. Solid-state fermentation (SSF) is proposed as an innovative strategy to enhance the release of bound phenolics from pineapple residues. In this work, the effects of SSF of pineapple peels with Lactobacillus plantarum, Lactobacillus rhamnosus, and Aspergillus oryzae on the release of phenolic compounds and their antioxidant and anti-inflammatory activities were evaluated, respectively. Pineapple peel extracts after SSF showed an increase in the release of phenolic compounds (248.11% with L. plantarum, 182% with A. oryzae, and 180.10% with L. rhamnosus), which led to an increase in the cellular antioxidant (81.94% with L. rhamnosus) and anti-inflammatory potential (nitric oxide inhibition of 62% with L. rhamnosus) compared to non-fermented extracts. Therefore, SSF of pineapple peels with L. plantarum, L. rhamnosus, and A. oryzae thrives as a new approach for the production of secondary metabolites with remarkable biological benefits, which can be the precursors for novel biofortified and nutraceutical-enriched foods that meet the needs of the most demanding and health-conscious consumers.
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The world faces threats that the United Nations has classified into 17 categories with different objectives as solutions for each challenge that are enclosed in the Sustainable Development Goals (SDGs). These actions involved the widespread use of science and technology as pathways to ensure their implementation. In this regard, sustainability science seeks the research community's contribution to addressing sustainable development challenges. Specifically, nanotechnology has been recognized as a key tool to provide disruptive and effective strategies to reach the SDGs. This review proposes the application of bimetallic nanoparticle substances capable of providing possible solutions to achieve target SDG 3: good health and well-being, SDG 6: clean water and sanitation, and SDG 12: responsible consumption and production. Furthermore, the term green nanotechnology is introduced in each section to exemplify how green synthesized bimetallic nanoparticles have been used to resolve each target SDG. This review also outlines the current scenario regarding the utilization of metallic nanomaterials in the market, together with the upscaling challenges and the lack of understanding of the long-term effects and hazards to the environment regarding bimetallic nanoparticles.
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The genus Opuntia spp. includes plants capable of growing in arid, temperate and tropical climates. The vast majority of wild species grow in Mexico, but O. ficus-indica (prickly pear or nopal) is cultivated around the world and it is one of the most studied. This review shows the currently available knowledge concerning the action of O. ficus-indica and other Opuntia species (Opuntia vulgaris, Opuntia robusta, Opuntia streptacantha, Opuntia microdasys, Opuntia dillenii and Opuntia dejecta) on liver health. The available data demonstrate the positive effects of extracts, vinegar, juices or seed oil of the Opuntia genus on the alterations induced in the liver by inadequate feeding patterns or the administration of chemicals. In this regard, the potential beneficial effects of nopal are related to the attenuation of triglyceride accumulation, oxidative stress and/or inflammation. Nevertheless, there is no information concerning the bioactive compound's characterisation in most of these studies; consequently, it is not possible to link the therapeutic effects of these plants to the presence of specific compounds in the nopal extracts. Therefore, further research is needed to confirm if the positive effects observed in animal models are also found in humans, in order to determine whether Opuntia can represent an effective tool to prevent and/or manage hepatic alterations.
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Ultrasound-assisted extraction (UAE) is an efficient and sustainable method for extracting bioactive compounds from agro-industrial by-products. Moreover, it has been reported that ultraviolet A (UVA) radiation can induce the biosynthesis and accumulation of bioactive phenolic compounds. This study optimized the efficiency of ultrasound-assisted extraction (UAE) for recovering ultraviolet A (UVA)-induced phenolic compounds in strawberry by-products (RF-N). The impact of three factors (solid-liquid ratio, ethanol concentration, and ultrasound power) on total phenolic compound (TPC) kinetics using Peleg's model was investigated. The developed model showed a suitable fit for both RF-N and strawberry by-products treated with UVA (RF-E). The optimal UAE conditions obtained were of a 1:30 ratio, 46% ethanol, and 100% ultrasound power, resulting in an average yield of 13 g total phenolics kg-1. The bioaccessibility of phenolic compounds during in-vitro digestion was 36.5%, with agrimoniin being the predominant compound. UAE combined with UVA treatment increased the bioactivity of RF extracts, displaying significant anti-proliferative effects on HT29 and Caco-2 cancer cell lines, as well as anti-inflammatory potential and cellular antioxidant activity. The ultrasound proved to be a sustainable and effective technique for extracting phenolic compounds from RF, contributing to the valorization of strawberry agro-industrial by-products, and maximizing their nutraceutical potential.
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The health-related compounds present in kale are vulnerable to the digestive process or storage conditions. Encapsulation has become an alternative for their protection and takes advantage of their biological activity. In this study, 7-day-old Red Russian kale sprouts grown in the presence of selenium (Se) and sulfur (S) were spray-dried with maltodextrin to assess their capacity to protect kale sprout phytochemicals from degradation during the digestion process. Analyses were conducted on the encapsulation efficiency, particle morphology, and storage stability. Mouse macrophages (Raw 264.7) and human intestinal cells (Caco-2) were used to assess the effect of the intestinal-digested fraction of the encapsulated kale sprout extracts on the cellular antioxidant capacity, the production of nitric oxide (NOx), and the concentrations of different cytokines as indicators of the immunological response. The highest encapsulation efficiency was observed in capsules with a 50:50 proportion of the hydroalcoholic extract of kale and maltodextrin. Gastrointestinal digestion affected compounds' content in encapsulated and non-encapsulated kale sprouts. Spray-dried encapsulation reduced the phytochemicals' degradation during storage, and the kale sprouts germinated with S and Se showed less degradation of lutein (35.6%, 28.2%), glucosinolates (15.4%, 18.9%), and phenolic compounds (20.3%, 25.7%), compared to non-encapsulated ones, respectively. S-encapsulates exerted the highest cellular antioxidant activity (94.2%) and immunomodulatory activity by stimulating IL-10 production (88.9%) and COX-2 (84.1%) and NOx (92.2%) inhibition. Thus, encapsulation is an effective method to improve kale sprout phytochemicals' stability and bioactivity during storage and metabolism.
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Plants of the Phoradendron genus have been traditionally used for their lipid- and glucose-lowering effects. However, the compounds responsible for these effects and the overall chemical profile of these plants have not been thoroughly investigated. We aimed to characterize the metabolome of leaves, stems, and aerial parts of the Phoradendron brachystachyum plant. We used mass spectrometry and colorimetric screening techniques (with various solvents) to identify and characterize the metabolites present. We also evaluated the antioxidant (FRAP, ORAC, TEAC, and DPPH assays) and inhibitory effects on pancreatic lipase and α-glucosidase enzymes of hydrophilic extracts. Furthermore, we compared the molecular fingerprints between the identified metabolites and FDA-approved drugs to gain insights into the metabolites that might be responsible for the observed effects on enzymes. Our findings revealed the presence of 59 putative metabolites, primarily flavonoids. However, we also hint at the presence of peptide and carbohydrate derivatives. The leaf extracts demonstrated the most promising metrics across all assays, exhibiting strong antioxidant and enzyme inhibitory effects as well as high levels of phenolic compounds, flavonoids, and tannins. Fingerprint analysis suggested potential peptide and carbohydrate metabolites as pancreatic lipase and α-glucosidase inhibitors. Overall, our study provides evidence on specific metabolites in Phoradendron brachystachyum that could be responsible for the therapeutic effects noted in obese and type 2 diabetes subjects.
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Bioactive peptides have gained the attention and interest of researchers and the industry for their therapeutic effects and high specificity, thus reducing the risks of side effects and making them an attractive alternatives in developing new biopharmaceuticals or cosmeceuticals. Nevertheless, their incorporation into formulations and administration presents challenges such as low stability under different storage conditions and gastrointestinal degradation after oral delivery. Likewise, the parenteral route is an invasive method that is painful and therefore reduces patient compliance. Topical delivery of bioactive peptides is a painless noninvasive alternative to reduce peptide degradation, exert local effects in the applied area, and improve patient compliance. In this review, we discuss the physicochemical properties of peptides and the mechanisms involved in their degradation. In addition, the most important aspects of skin structure and skin permeation routes, and the requirements for topical and transdermal drug delivery are also discussed in this article. Finally, nanocarrier development advances for the topical delivery of peptides (water-in-oil-in-water emulsions, microemulsions, nanoparticles, solid lipid nanoparticles, liposomes, niosomes, and microneedles) and other strategies, such as metal complexation, cell-penetrating peptides, and synthetic modification, are also reviewed. All these topics consider the perspective of their effect to improve skin permeability to peptides and their stability over time during storage.
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Peptídeos Penetradores de Células , Nanopartículas , Administração Cutânea , Sistemas de Liberação de Medicamentos , Humanos , Lipossomos , PeleRESUMO
Capsaicinoids are the main bioactive compounds extracted from chili pepper seeds (CPSs) but other bioactive compounds such as phenolic compounds may be found. Enzyme-assisted extraction (EAE) improves the extraction of bioactive compounds from fruits and seeds. The aim of this study was to establish the cellulase-assisted extraction conditions of capsaicinoids and phenolic compounds from Habanero CPSs (Capsicum chinense) and to evaluate the anti-inflammatory activity of the obtained extracts on murine macrophages. EAE was performed using different temperatures (T1 = 30°C, T2 = 45°C and T3 = 60°C), enzyme concentrations (E1 = 2,500 UI/L and E2 = 250 UI/L), and extraction time periods (0-150 min). Total phenolic compounds were quantified using the Folin-Ciocalteu assay, capsaicin (CAP) and dihydrocapsaicin (DHC) contents were evaluated by HPLC, and anti-inflammatory activity was performed with Griess assay on murine macrophage RAW 264.7 cell culture. The highest phenolic compound content (337.96 mg GAE/L) was achieved at 30°C, 2,500 UI/L, and 150 min of extraction. The highest CAP content (310.23 µg/ml) was obtained at 45°C with 250 UI/L for 150 min, while for DHC (167.72 µg/ml), the conditions were 60°C, 2,500 UI/L, and 120 min. The highest anti-inflammatory response was obtained when 60°C, E2, and 150 min were used for the extraction, and nitric oxide (NO) production was reduced to 22.56%. Based on the results obtained in this research, EAE allowed the recovery of compounds with anti-inflammatory activity from CPS using water as a solvent. There was a correlation between the extraction of CAP and DHC. But although a moderate direct correlation between the concentration of capsaicinoids and total phenolic compounds (TPCs) and an inverse correlation of the presence of the bioactive compounds (TPC, CAP, and DHC) with the NO synthesis, these were not statistically significant. We demonstrated that Habanero seeds are an important raw material to recover anti-inflammatory compounds beyond capsaicinoids using water in EAE.
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Background: The revalorization of agro-industrial by-products by applying ultraviolet A (UVA) radiation to biofortify with phenolic compounds has been studied in recent times, showing improvements in the individual and total phenolic content and their bioactivity. Therefore, the main aim of this work was to optimize the biofortification process of phenolic compounds by UVA radiation to strawberry agro-industrial by-products (RF). Moreover, the effect of UVA radiation on the potential biological activity of the phenolics accumulated in RF due to the treatment was also determined. Methods: The assays followed a factorial design with three variables at three levels: UVA dose (LOW, MEDIUM, and HIGH), storage temperature (5, 10, and 15°C), and storage time (0, 24, 48, and 72 h). At each experimental condition, phenylalanine ammonia-lyase (PAL) and polyphenol oxidase (PPO) enzymatic activities, total phenolic compound content (TPC), phenolics profile (TPCHPLC), and agrimoniin content (AGN) were evaluated; and the optimal UVA dose, storage time, and temperature were determined. In vitro bioaccessibility of the accumulated phenolic compound was studied on RF tissue treated with UVA at optimal process conditions. The digested extracts were tested for antiproliferative activity in colorectal cancer cells, cellular antioxidant capacity, and anti-inflammatory activity. Results: The results showed that applying UVA-HIGH (86.4 KJ/m2) treatment and storing the tissue for 46 h at 15°C increased PAL activity (260%), phenolic content (240%), and AGN (300%). The biofortification process improves the bioaccessibility of the main phenolic compound of RF by 9.8 to 25%. The digested optimum extract showed an IC50 for HT29 and Caco-2 cells of 2.73 and 5.43 µg/mL, respectively, and presented 60% cellular antioxidant capacity and 30% inhibition of NOX production. Conclusion: The RF treated with UVA is an excellent source of phenolic compounds; specifically, ellagitannins and the UVA radiation proved to be efficient in biofortify RF, significantly improving the phenolic compounds content and their bioactive properties with adequate bioaccessibility, adding value to the strawberry agro-industrial by-products.