Bioavailability Of Polyphenols Research Articles

Ultra‐Long‐Term Anti‐Inflammatory Polyphenol Capsule to Remodel the Microenvironment for Accelerating Osteoarthritis Healing by Single Dosage

AbstractOsteoarthritis (OA) is a common chronic inflammatory disease that leads to disability and death. Existing therapeutic agents often require frequent use, which can lead to drug resistance and long‐term side effects. Polyphenols have anti‐inflammatory and antioxidant potential. However, they are limited by their short half‐life and low bioavailability. This work presents a novel pure polyphenol capsule for sustained release of polyphenols, which is self‐assembled via hydrophobic and hydrogen bonds. The capsule enhances cellular uptake, scavenges reactive oxygen and nitrogen species, reduces inflammatory markers, and remodels the OA microenvironment by inhibiting the p38 MAPK pathway. The capsule overcomes the limitations of short half‐life and low bioavailability of polyphenols and achieves single‐dose cure in mouse and dog OA models, providing an optimal therapeutic window for OA repair. Taking advantage of simple manufacturing, convenient administration, and pure polyphenol composition, these capsules show great potential for clinical treatment of osteoarthritis and chronic inflammatory diseases.

Role of red beetroot in bread for reducing mycotoxin risks: Bioavailability of beetroot polyphenols and betalains with ochratoxin a, aflatoxin B1 and zearalenone in Caco-2 cells

Role of red beetroot in bread for reducing mycotoxin risks: Bioavailability of beetroot polyphenols and betalains with ochratoxin a, aflatoxin B1 and zearalenone in Caco-2 cells

Design strategies of polysaccharide, protein and lipid-based nano-delivery systems in improving the bioavailability of polyphenols and regulating gut homeostasis.

Polyphenols are plant secondary metabolites that have attracted much attention due to their anti-inflammatory, antioxidant, and gut homeostasis promoting effects. However, food matrix interaction, poor solubility, and strong digestion and metabolism of polyphenols cause barriers to their absorption in the gastrointestinal tract, which further reduces bioavailability and limits polyphenols' application in the food industry. Nano-delivery systems composed of biocompatible macromolecules (polysaccharides, proteins and lipids) are an effective way to improve the bioavailability of polyphenols. Therefore, this review introduces the construction of biopolymer-based nano-delivery systems and their application in polyphenols, with emphasis on improving the solubility, stability, sustained release and intestinal targeting of polyphenols. In addition, there are possible positive effects of polyphenol-loaded nano-delivery systems on modulating gut microbiota and gut homeostasis, with particular emphasis on modulating intestinal inflammation, metabolic syndrome, and gut-brain axis. It is worth noting that the safety of bio-based nano-delivery systems still need to be further studied. In summary, the application of the bio-based nano-delivery system to deliver polyphenols provides insights for improving the bioavailability of polyphenols and for the treatment of potential diseases in the future.

Influence of varied processing methods on the antioxidant capacity, antibacterial activity, and bioavailability of Iranian black, oolong, and green leafy teas

In this study, the impact of various tea preparation techniques on the content of bioactive compounds, antioxidant capacity, antibacterial properties, and polyphenol bioavailability in green, black, and oolong tea infusions was examined. The findings demonstrated that the fermentation process significantly influences the levels of bioactive compounds, with green tea infusions exhibiting the highest, and black tea the lowest, content of phenolic compounds. A positive correlation was observed between the content of the phenolic compound and both antioxidant and antibacterial activities. Additionally, the microwave brewing method was identified as the most effective preparation technique for maximizing the bioactive compound content and bioavailability. The inclusion of skim milk powder was found to further enhance the bioavailability of phenolic compounds during digestive process. The research suggests that green tea infusions prepared using the microwave brewing method and supplemented with the skim milk powder, could serve as a functional beverage offering enhanced health benefits.

Does Encapsulation Improve the Bioavailability of Polyphenols in Humans? A Concise Review Based on In Vivo Human Studies.

Polyphenols offer an array of health benefits that can contribute to well-being. Nevertheless, their bioactivity can be compromised due to their low bioavailability. Encapsulation has been explored as a strategy to enhance the stability and bioavailability of polyphenols. During encapsulation, polyphenols are protected from degradation by a wall material that acts as a protective coating. This coating shields the polyphenols from the harsh physiological conditions of digestion, ensuring their delivery to the intestine. However, the majority of evidence, particularly regarding bioavailability after digestion, is derived from in vitro studies. While these studies provide valuable preliminary insights, they cannot definitively confirm the effects in vivo due to their inability to accurately replicate physiological conditions and the complex gut microbial ecosystem. Consequently, this review seeks to evaluate the current evidence from in vivo human studies to elucidate the efficacy of encapsulation in improving polyphenols' bioavailability. Current clinical evidence on the impact of encapsulation on polyphenol bioavailability is primarily focused on polyphenols derived from grape pomace, cocoa, and bilberries, as well as individual polyphenols such as fisetin, hesperidin, and curcumin. Encapsulation has been an effective technique in improving the bioavailability of individual polyphenols like hesperidin, fisetin, and curcumin. However, this approach has not yielded consistent results when applied to groups of polyphenols, such as bilberry anthocyanins or cocoa phenolic acids. Encapsulation by micellization has shown promising results in improving the bioavailability of curcumin in a nutraceutical context. Further studies are needed to explore the bioavailability of encapsulated polyphenols, especially in the functional food context.

Dietary Polyphenols, Food Processing and Gut Microbiome: Recent Findings on Bioavailability, Bioactivity, and Gut Microbiome Interplay.

Polyphenols are organic chemical compounds naturally present in plants, renowned for their anti-inflammatory, antioxidant, immunomodulatory, anticancer, and cardiovascular protective properties. Their bioactivity and bioavailability can vary widely depending on the methods of food processing and interactions with the gut microbiome. These factors can induce changes in polyphenols, affecting their ability to achieve their intended health benefits. Thus, it is essential to develop and apply food processing methods that optimize polyphenol content while maintaining their bioactivity and bioavailability. This review aims to explore how various food processing techniques affect the quantity, bioactivity, and bioavailability of polyphenols, as well as their interactions with the gut microbiome, which may ultimately determine their health effects.

Structural modification and functional improvement of lactoferrin through non-covalent and covalent binding to coffee polyphenol

Studies have suggested that milk may enhance or neutralize the bioavailability of coffee polyphenols, possibly due to reversible and irreversible interactions between coffee polyphenols and milk proteins. The effects of non-covalent and covalent binding of lactoferrin (BLF) to caffeic acid (CAA) on protein structure and function were investigated. SDS-PAGE analysis confirmed the covalent interaction between BLF and CAA. Multispectral experiments characterized the BLF-CAA complexes and conjugates, revealing alterations in the tertiary structure of the proteins in the BLF-CAA conjugates. Molecular docking and kinetics results demonstrated that hydrogen bonding, electrostatic interaction, and hydrophobic forces were the primary internal forces between CAA and BLF. When combined with CAA, the covalent conjugates exhibited superior functional properties including solubility, oxidation resistance, thermal stability, emulsification and foamability, bioaccessibility, and antimicrobial properties. This study offers a theoretical foundation and technical benchmark for the preparation of protein-based delivery vectors with synergistic effects.

The bioavailability of polyphenols following acute consumption of pigmented barley and wheat.

Polyphenols from pigmented cereal grains exert health-promoting effects but data on their bioavailability are limited. This study investigated the acute bioavailability of polyphenols from the consumption of pigmented whole grain cereal porridges, including purple barley (PB), purple wheat (PW), and blue wheat (BW), compared to a non-pigmented regular wheat (RW). A secondary objective was to assess their effects on plasma antioxidant and inflammatory status postprandially. Phenolic characterisation and antioxidant profiling were performed on extracts from the cooked cereals. Three healthy individuals consumed 200 g of a cereal in a 4-way crossover trial with a one-week washout in between meals. Blood samples were collected at fasting baseline, 30 minutes, 1 hour, 2 hours and 4 hours postprandially. Urine samples were collected at fasting baseline and the 4-hour time point. Pigmented grains exhibited significantly higher phenolic content and antioxidant capacity (p < 0.001) compared to RW. This suggests that pigmented grains may be a better source of polyphenols and potentially offer greater health benefits. However, polyphenol bioavailability following pigmented grain consumption was reduced (less than 6%), suggesting that a substantial fraction remained unabsorbed. The bioavailable phenolic compounds detected included phenolic acids (protocatechuic and caffeic acid), hippuric acid and other phenolic metabolites. Interpersonal variability and the type of grain consumed had an impact on the absorption and excretion of phenolic acids. Only PW consumption resulted in significant (p < 0.01) increases in plasma antioxidant status but no short-term impact on the inflammatory status. This study provides valuable insights into the complex dynamics of polyphenol bioavailability from pigmented cereal consumption and warrants further investigation.

Development of egg yolk lipoprotein hydrolysate for nano-delivery of curcumin: Structure-function relationship

Curcumin is a lipophilic polyphenol extracted from the rhizomes of the turmeric plant, exhibiting versatile biological activities. However, its poor solubility, stability, and bioaccessibility present barriers to its effective use in foods or nutraceutical supplements. Egg yolk lipoprotein is a class of natural protein-lecithin composite found in egg yolks with a strong affinity for different hydrophobic active ingredients. In this study, egg yolk lipoprotein hydrolysate was employed to encapsulate hydrophobic curcumin, thereby increasing its solubility, stability, and bioaccessibility. The resulting curcumin-loaded nanoparticles had an average size of 680.9 nm, a zeta potential of around −30 mV, and an encapsulation rate of up to 68.4 %. The solubility of curcumin in water increased by 80 times while maintaining excellent thermal and storage stability. Fluorescence and infrared spectroscopy analysis demonstrated that the assembly process was driven by hydrophobic interactions and hydrogen bonds. The bioavailability of curcumin in nanoparticles has been improved to 30 %, a tenfold increase. These results suggested that egg yolk lipoprotein hydrolysate, a novel peptide-lecithin complex nanoparticle, can improve the stability and bioavailability of hydrophobic polyphenols.

R-Q@P-D nanoparticle for improving the oral bioavailability and therapeutic efficacy: A novel reversible dual-target-mild-inhibition intestinal metabolic enzymes strategy for resveratrol delivery

The low bioavailability of polyphenols, such as resveratrol (RES), is typically caused by the poor solubility and first-pass effect. To improve bioavailability and reduce adverse effects, an oral reversible UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs) dual-target-mild-inhibition strategy was designed, and a proof-of-concept was studied. This R-Q@P-D nanoparticle for the codelivery of RES and quercetin (QUE) was constructed using pea protein isolate and dipotassium glycyrrhizinate (DG) as nanocarriers. These nanoparticle ingredients were all plant extracts approved by the FDA, and the fabrication process was a simple but novel pH-ultrasonic-shifting method in water conditions. R-Q@P-D exhibited high encapsulation efficiency of RES (97.25 ± 1.13 %) and QUE (94.21 ± 0.62 %), with a uniform nanosize (147.73 ± 1.85 nm). Characterizations implied that RES and QUE could be successfully encapsulated in nanoparticles in amorphous states, and the self-assembly binding between them was non-covalent bonds. Moreover, the in-silicon simulation and experimental results verified interactions between RES and DG, while there was no interaction between QUE and DG. In vivo evaluations showed that R-Q@P-D increased the bioavailability of RES by mildly and reversibly inhibiting intestinal UGTs and SULTs, but without inhibiting hepatic UGTs and SULTs. Moreover, molecular simulations showed that QUE and RES are competitively bound to SULTs but not UGTs. R-Q@P-D had significant therapeutic efficacy and excellent safety performance for its oral application. The tremendous safety and simple fabrication benefited the clinical translation. Together, R-Q@P-D based on reversible UGTs and SULTs dual-target-mild-inhibition strategy might be a promising nano-platform for improving the bioavailability and efficacy of hydrophobic polyphenols.

Interaction of zein/HP-β-CD nanoparticles with digestive enzymes: Enhancing curcumin bioavailability

The low bioavailability of polyphenolic compounds due to poor solubility and stability is a major challenge. Encapsulation of polyphenols in zein-based composite nanoparticles can improve the water dispersion, stability, targeted delivery, and controlled release of polyphenols in the gastrointestinal tract. In this study, we investigated the fluorescence properties, bioactivity, and microstructural characteristics of polyphenols during digestion, revealing that zein nanoparticles protect polyphenols from gastric degradation and promote their sustained release in the small intestine. The effects of different ionic species and salt ion concentrations on the digestive properties of polyphenol complex delivery systems have also been explored. In addition, the formation of “protein corona” structures during digestion may affect bioavailability. These findings highlight the potential of nanoparticle formulations to improve polyphenol stability and absorption. The results of this study may provide new insights and references for the study of polyphenol bioavailability enhancement.

Synthesis of plyphenol-containing cationic linear and dendrimeric peptides with anti-oxidant activity

Natural polyphenols are of great interest from the point of view of their use for the pharmacological control of oxidative stress and many diseases. However, the low bioavailability and rapid metabolism of polyphenols in the form of glycosides or aglycones stimulates the search for effective means of delivery into systemic circulation. Conjugation of polyphenols with cationic amphiphilic peptides can result in compounds with strong antioxidant activity and the ability to cross biological barriers. Such compounds may be in demand as drugs for antioxidant therapy, including for the treatment of viral, oncological and neurodegenerative diseases due to the diverse range of biological activities inherent in polyphenols and peptides. In this work, cationic linear and dendrimer amphiphilic cationic peptides were synthesized by the solid phase method, and a number of peptides were conjugated to gallic acid (Ga). Ga is a non-toxic natural phenolic acid and an important functional element of many flavonoids with high antioxidant activity. It was shown that the resulting Ga-peptide conjugates exhibited antioxidant (antiradical) activity that was 2-3 times higher than that of ascorbic acid. Other tests indicated that the addition of Ga did not affect the toxicity and hemolytic activity of the conjugates. Ga-modified peptides stimulated the transmembrane transfer of the pGL3 plasmid encoding the luciferase reporter gene; however, the addition of Ga to the N-terminus of the peptide reduced its transfection activity. Some of the resulting compounds had noticeable inhibitory activity against theE. сoli-Dh5α strain.

Bacterial Degradation of Antinutrients in Foods: The Genomic Insight.

Antinutrients, also known as anti-nutritional factors (ANFs), are compounds found in many plant-based foods that can limit the bioavailability of nutrients or can act as precursors to toxic substances. ANFs have controversial effects on human health, depending mainly on their concentration. While the positive effects of these compounds are well documented, the dangers they pose and the approaches to avoid them have not been discussed to the same extent. There is no dispute that many ANFs negatively alter the absorption of vitamins, minerals, and proteins in addition to inhibiting some enzyme activities, thus negatively affecting the bioavailability of nutrients in the human body. This review discusses the chemical properties, plant bioavailability, and deleterious effects of anti-minerals (phytates and oxalates), glycosides (cyanogenic glycosides and saponins), polyphenols (tannins), and proteinaceous ANFs (enzyme inhibitors and lectins). The focus of this study is on the possibility of controlling the amount of ANF in food through fermentation. An overview of the most common biochemical pathways for their microbial reduction is provided, showing the genetic basis of these phenomena, including the active enzymes, the optimal conditions of action, and some data on the regulation of their synthesis.

Antioxidant, Anti-Inflammatory, Anti-Diabetic, and Pro-Osteogenic Activities of Polyphenols for the Treatment of Two Different Chronic Diseases: Type 2 Diabetes Mellitus and Osteoporosis.

Polyphenols are natural bioactives occurring in medicinal and aromatic plants and food and beverages of plant origin. Compared with conventional therapies, plant-derived phytochemicals are more affordable and accessible and have no toxic side effects. Thus, pharmaceutical research is increasingly inclined to discover and study new and innovative natural molecules for the treatment of several chronic human diseases, like type 2 diabetes mellitus (T2DM) and osteoporosis. These pathological conditions are characterized by a chronic inflammatory state and persistent oxidative stress, which are interconnected and lead to the development and worsening of these two health disorders. Oral nano delivery strategies have been used to improve the bioavailability of polyphenols and to allow these natural molecules to exert their antioxidant, anti-inflammatory, anti-diabetic, and pro-osteogenic biological activities in in vivo experimental models and in patients. Polyphenols are commonly used in the formulations of nutraceuticals, which can counteract the detrimental effects of T2DM and osteoporosis pathologies. This review describes the polyphenols that can exert protective effects against T2DM and osteoporosis through the modulation of specific molecular markers and pathways. These bioactives could be used as adjuvants, in combination with synthetic drugs, in the future to develop innovative therapeutic strategies for the treatment of T2DM and osteoporosis.

Changes and biotransformation mechanism of main functional compounds during kombucha fermentation by the pure cultured tea fungus

Kombucha was fermented by the pure cultured tea fungus, and the changes of functional compounds and their transformation were explored. After fermentation, the contents of total polyphenols, total flavonoids, quercetin, kaempferol and catechins respectively enhanced by 77.14%, 69.23%, 89.11%, 70.32% and 45.77% compared with the control, while flavonol glycosides reduced by 38.98%. The bioavailability of polyphenols and flavonoids respectively increased by 29.52% and 740.6%, and DPPH and ABTS respectively increased by 43.81% and 35.08% compared with the control. Correlation analysis showed that microorganisms and the antioxidant activity were highly positive correlation with total polyphenols, total flavonoids, EGC, EC, EGCG, ECG, quercetin and kaempferol, and negative correlation with kaempferol-3-glucoside. The constructed models confirmed that organic acids were more likely to damage the structure of tea leaves, and enzymes (polygalacturonidase and tannase) and solvents (acids, alcohols and esters) had a synergistic effect on the biotransformation of functional compounds.

Microencapsulation of green tea polyphenols: Utilizing oat oil and starch-based double emulsions for improved delivery

The stability and bioavailability of green tea polyphenols, crucial for their health benefits, are compromised by environmental sensitivity, limiting their use in functional foods and supplements. This study introduces a novel water-in-oil-in-water double emulsion technique with microwave-assisted extraction, significantly enhancing the stability and bioavailability of these compounds. The primary objective of this study was to assess the effectiveness of several encapsulating agents, such as gum Arabic as control and native and modified starches, in improving encapsulated substances' stability and release control. Native and modified starches were chosen for their outstanding film-forming properties, improving encapsulation efficiency and protecting bioactive compounds from oxidative degradation. The combination of maltodextrin and tapioca starch improved phenolic content retention, giving 46.25 ± 2.63 mg/g in tapioca starch microcapsules (GTTA) and 41.73 ± 3.24 mg/g in gum arabic microcapsules (GTGA). Besides the control, modified starches also had the most potent antioxidant activity, with a 45 % inhibition (inh%) in the DPPH analysis. Oat oil was utilized for its superior viscosity and nutritional profile, boosting emulsion stability and providing the integrity of the encapsulated polyphenols, as indicated by the microcapsules' narrow span index (1.30 ± 0.002). The microcapsules' thermal behavior and structural integrity were confirmed using advanced methods such as Differential Scanning Calorimetry (DSC) and Fourier-Transform Infrared Spectroscopy (FT-IR). This study highlights the critical role of choosing appropriate wall materials and extraction techniques. It sets a new standard for microencapsulation applications in the food industry, paving the way for future innovations.

Whey Protein Sodium-Caseinate as a Deliverable Vector for EGCG: In Vitro Optimization of Its Bioaccessibility, Bioavailability, and Bioactivity Mode of Actions.

Epigallocatechin gallate (EGCG), the principal catechin in green tea, exhibits diverse therapeutic properties. However, its clinical efficacy is hindered by poor stability and low bioavailability. This study investigated solid particle-in-oil-in-water (S/O/W) emulsions stabilized by whey protein isolate (WPI) and sodium caseinate (NaCas) as carriers to enhance the bioavailability and intestinal absorption of EGCG. Molecular docking revealed binding interactions between EGCG and these macromolecules. The WPI- and NaCas-stabilized emulsions exhibited high encapsulation efficiencies (>80%) and significantly enhanced the bioaccessibility of EGCG by 64% compared to free EGCG after simulated gastrointestinal digestion. Notably, the NaCas emulsion facilitated higher intestinal permeability of EGCG across Caco-2 monolayers, attributed to the strong intermolecular interactions between caseins and EGCG. Furthermore, the emulsions protected Caco-2 cells against oxidative stress by suppressing intracellular reactive oxygen species generation. These findings demonstrate the potential of WPI- and NaCas-stabilized emulsions as effective delivery systems to improve the bioavailability, stability, and bioactivity of polyphenols like EGCG, enabling their applications in functional foods and nutraceuticals.

Artichoke extract and human bifidobacteria to attain symbiotic sheep milk cheeses

There is a growing interest for healthy non-bovine functional dairy products. Therefore, in the present study, an aqueous polyphenol-rich artichoke extract (AE) and two Bifidobacterium strains of human origin (B. pseudolongum INIA P2 and B. longum INIA P132) were added, alone or in combination with AE, for the manufacture of six sheep milk cheeses. In general, addition of 1.25 g of lyophilized AE per 100 g of curd did not affect cheese pH, dry matter, lactoccci starter counts or organic acid levels during ripening. Bifidobacterial strains showed good viability in cheeses with AE during ripening and after simulated major gastrointestinal conditions. Cheeses with AE showed improved functional properties, with significantly (P < 0.01) higher total polyphenol content and, especially, antioxidant activity The cheese with AE and strain INIA P2 fulfil the definition of a symbiotic cheese. It contains prebiotic compounds and Bifidobacterium at adequate levels to sustain a therapeutic effect, which are able to survive major gastrointestinal conditions. This cheese could confer beneficial effects on consumers’ health by contributing to the host antioxidant capacity and increasing polyphenol bioavailability.

Encapsulated polyphenols in functional food production

Polyphenols are present as nutrient components in many functional food formulations. However, their bioavailability is quite low, and they tend to degrade under extreme technological conditions, e.g., heating, pH, etc. Moreover, polyphenols are known for their specific bitter taste. As a result, a large amount of polyphenols spoils the sensory properties of the finished product. Encapsulation seems a prospective solution to this problem. This article provides a comprehensive review of scientific publications on various methods of polyphenol encapsulation.&#x0D; The review covered publications registered in PubMed, Google Scholar, ResearchGate, Elsevier, eLIBRARY.RU, and Cyberleninka in 2002–2023 with a focus on original research articles published after 2012. The search involved such keywords as polyphenols, encapsulation, flavonoids, delivery systems, and functional products. &#x0D; Encapsulating materials are made of organic or inorganic substances, as well as of their combinations. Mineral salts delay the contact between polyphenols and taste buds. However, they are not resistant enough to gastric juice. In this respect, organic matrices are more effective. Carbohydrates protect active molecules from degradation in the stomach. Liposomes increase the bioavailability of polyphenols. Milk or whey proteins also proved quite effective for a number of reasons. First, they mask the astringent taste, which makes it possible to include more polyphenols in functional food formulations. Second, the resulting product is fortified with valuable proteins and essential amino acids. Third, high concentrations of polyphenols possess enough antioxidant properties to increase the shelf-life.&#x0D; Polyphenol encapsulation is an effective method of functional product design, especially in the sphere of foods made for dietary nutrition, sports, preventive diets, etc.

Dietary Polyphenols: Review on Chemistry/Sources, Bioavailability/Metabolism, Antioxidant Effects, and Their Role in Disease Management.

Polyphenols, as secondary metabolites ubiquitous in plant sources, have emerged as pivotal bioactive compounds with far-reaching implications for human health. Plant polyphenols exhibit direct or indirect associations with biomolecules capable of modulating diverse physiological pathways. Due to their inherent abundance and structural diversity, polyphenols have garnered substantial attention from both the scientific and clinical communities. The review begins by providing an in-depth analysis of the chemical intricacies of polyphenols, shedding light on their structural diversity and the implications of such diversity on their biological activities. Subsequently, an exploration of the dietary origins of polyphenols elucidates the natural plant-based sources that contribute to their global availability. The discussion extends to the bioavailability and metabolism of polyphenols within the human body, unraveling the complex journey from ingestion to systemic effects. A central focus of the review is dedicated to unravelling the antioxidant effects of polyphenols, highlighting their role in combating oxidative stress and associated health conditions. The comprehensive analysis encompasses their impact on diverse health concerns such as hypertension, allergies, aging, and chronic diseases like heart stroke and diabetes. Insights into the global beneficial effects of polyphenols further underscore their potential as preventive and therapeutic agents. This review article critically examines the multifaceted aspects of dietary polyphenols, encompassing their chemistry, dietary origins, bioavailability/metabolism dynamics, and profound antioxidant effects. The synthesis of information presented herein aims to provide a valuable resource for researchers, clinicians, and health enthusiasts, fostering a deeper understanding of the intricate relationship between polyphenols and human health.