Bioavailability Of Bioactive Compounds Research Articles

Bioavailability and Bioactivities of Polyphenols Eco Extracts from Coffee Grounds after In Vitro Digestion.

Coffee grounds are a valuable source of bioactive compounds. In Romania, most of the amount obtained is lost through non-recovery; the rest is occasionally used as organic fertilizer. The coffee grounds were selected according to the roasting degree: blonde roasted (BR), medium roasted (MR), and dark roasted (DR). The study aimed to evaluate three extracts, obtained with a mixture of ethanol/water/acetic acid (50/49.5/0.5), depending on the roasting degree. The majority phenolic component, the antioxidant, and anti-inflammatory effect, as well as the role that gastrointestinal transit had on the bioavailability of bioactive compounds were determined. Chlorogenic acid was inversely proportional to the roasting degree. BR showed the best correlation between antioxidant and anti-inflammatory activities in vitro/in vivo. The antiproliferative capacity of the extracts determined an inhibitory effect on the tumor cells. Antimicrobial activities, relevant in the control of type 2 diabetes, were exerted through the inhibition of microbial strains (Escherichia coli). Following gastric digestion, BR demonstrated a maximum loss of 20% in the stomach. The recovery of coffee grounds depended on the pattern of functional compounds and the bioavailability of the main component, chlorogenic acid.

The Human Microbial Metabolism of Quercetin in Different Formulations: An In Vitro Evaluation.

Quercetin is one of the main dietary flavonols, but its beneficial properties in disease prevention may be limited due to its scarce bioavailability. For this purpose, delivery systems have been designed to enhance both stability and bioavailability of bioactive compounds. This study aimed at investigating the human microbial metabolism of quercetin derived from unformulated and phytosome-formulated quercetin through an in vitro model. Both ingredients were firstly characterized for their profile in native (poly)phenols, and then fermented with human fecal microbiota for 24 h. Quantification of microbial metabolites was performed by ultra-high performance liquid chromatography coupled to mass spectrometry (uHPLC-MSn) analyses. Native quercetin, the main compound in both products, appeared less prone to microbial degradation in the phytosome-formulated version compared to the unformulated one during fecal incubation. Quercetin of both products was bioaccessible to colonic microbiota, resulting in the production of phenylpropanoic acid, phenylacetic acid and benzoic acid derivatives. The extent of the microbial metabolism of quercetin was higher in the unformulated ingredient, in a time-dependent manner. This study opened new perspectives to investigate the role of delivery systems on influencing the microbial metabolism of flavonols in the colonic environment, a pivotal step in the presumed bioactivity associated to their intake.

Self-emulsifying formulation of Spinacia oleracea reduces the dose and escalates bioavailability of bioactive compounds to accelerate fracture repair in rats

BackgroundSpinach (Spinacia oleracea) is a rich source of flavonoids and therefore widely used therapeutically as an antioxidant agent in traditional medicine. The present study was undertaken to study the bone regenerating property of dried Spinacia oleracea extract (DSE) and self-emulsifying formulation of the extract (FDSE) on drill-hole model of fracture repair in rats.Methods0.8 mm hole was drilled in the diaphyseal region of femur in adult SD rats. DSE and formulated extract (FDSE) was administered orally and fractured femur was collected after treatment regimen. Micro-CT, transcriptional analysis and measurement of calcein intensity of callus formed at the injured site was performed to study the efficacy of the extract and formulation on bone regeneration. Further, compounds from extract were assessed for in-vitro osteoblast activity.ResultsMicro-architecture of the regenerated bone at injured site exhibited 26% (p < 0.001) and 35% (p < 0.01) increased BV/TV (bone volume /tissue volume) and Tb.N. (trabecular number) for DSE (500 mg.kg− 1). Further, FDSE exhibited similar augmentation in BV/TV (p < 0.01) and Tb. N (p < 0.01) parameters at dose of 250 mg.kg− 1. Analogous results were obtained from transcriptional analysis and calcein intensity at the fractured site. 3-O-Methylpatuletin, one of the compound isolated from the extract stimulated the differentiation and mineralization of primary osteoblast and depicted concentration dependent antagonizing effect of H2O2 in osteoblast apparently, minimizing ROS generation thus affectivity in fracture repair.ConclusionsThe present study showed that bone regenerating property of spinach was augmented by formulating extract to deliverable form and can be further studied to develop as therapeutic agent for fracture repair.Graphical abstract

Updates in bile acid-bioactive molecule conjugates and their applications

Bile acid conjugates are emerging as important chemical resources due to their low cost and wide availability of bile acids, making them privileged molecules in drug carrier systems and building blocks for derivatization and chiral template introduction into bioactive molecules. In recent years, bile acids as scaffolds in supramolecular, medicinal, and material chemistry attracted prime focus of researchers as an area of research to be followed with passion. Due to peculiar physicochemical and biological properties, bile acid exhibited various applications in biomedical and pharmaceutical fields. In this review, the bile acid conjugations with different bioactive compounds have been discussed to understand their influence on the bioavailability of bioactive compounds.

Thermal stability and bioavailability of bioactive compounds after baking of bread enriched with different onion by-products

This study investigated the effects of the addition of onion waste fractions into gluten-free (GF) bread to promote its health benefits. 5% of the control (C) GF flour blend was replaced with three waste fractions in the form of: fried onion (FO), dried onion (DO) and onion peel (OP). Antioxidant activity, content of flavonols and total polyphenols of breads increased in the following order: C < FO < DO < OP. No differences were observed in sensory analysis. We found that quercetin glycosides, dimers and trimer in OP-bread, determined according to their mass spectra, decomposed during baking and released free quercetin, which points to their thermal instability. Cross-over study revealed that consumption of OP-bread significantly increased (p < 0.05) antioxidant activity of consumers’ blood compared to control bread consumption, indicating good bioavailability of flavonols. Results suggest incorporation of OP into GF bread can increase its biological value with satisfactory sensory acceptance.

Deep eutectic solvents improve the biorefinery of alperujo by extraction of bioactive molecules in combination with industrial thermal treatments

Thermal treatments are the latest developments in the olive oil biorefinery industry to extract bioactive compounds from its by-products, mainly the alperujo. To reach these goals and reduce energy consumption the utilization of deep eutectic solvents has been studied. An initial screening led to define a eutectic mix of choline chloride, glycolic and oxalic acid (DES9) as one of the adequate solvents to increase the solubilization of phenols and sugars, with a temperature reduction from 180 °C to 120 °C. DES9 increased the concentration of acid sugars by six times and the concentration of hydroxytyrosol by 30 times, to up to 85.81 mg/g of dry matter. The activity of DES9 is not due to the activity of each component separately or to the mixture of the two acids, but to the eutectic mixture of all of them. In the future, these solvents could improve the extraction, stability and bioavailability of bioactive compounds and the biorefinery of alperujo.

Development and incorporation of nanoemulsions in food

Currently, nanoencapsulation of bioactive compounds is promising, and is one of the methods that has been proven very effective. The development of food-grade nanoemulsions is in a state of constant innovation due to the interesting features that this method of encapsulation has, such as small droplet size, kinetic stability and appearance. With this technology, it is possible to control some food properties, such as texture, taste and stability. In this article, we present a review of the most commonly used methods in the creation of nanoemulsions, the recent developments of these dispersions, the relevant applications of nanoemulsions in food matrices, the most commonly used food-grade materials and the functionality of nanoemulsions, which are designed primarily to encapsulate compounds with biological activity. Nanoemulsions have been shown to be effective in preventing degradation and improving the bioavailability of bioactive compounds, such as oil-soluble vitamins, antimicrobials, flavours and antioxidants. At the end of this article, facts of interest about acceptance issues and nanotechnology regulatory policies in the food industry are presented.

Agronomic Cultivation, Chemical Composition, Functional Activities and Applications of Pereskia Species – A Mini Review

The exploration of the plant biodiversity as a natural source to obtain sustainable food products and new bioactive pharmaceutical compounds has been growing significantly due to their abundance, safety and economy. Natural pharmaceutical and edible compounds present some advantages when compared to synthetic ones, such as being chemically inert and widely available. In this sense, plants of the genus Pereskia belonging to the Cactaceae family, have been studied. It is an unconventional wild edible plant that contains a large amount of protein and minerals. Studies have demonstrated their biological activities and potential application in different areas such as pharmaceutical, medicinal and food. This review is focused on the chemical composition, functional properties, applications on pharmaceutical, nutraceutical and food areas and formulation techniques to enhance the stability and bioavailability of bioactive compounds from the underutilized wild edible plant known as ora-pro-nobis (Pereskia aculeata or Pereskia grandifolia). The latest studies involving ora-pro-nobis demonstrated its great potential due to its biological activities, which could stimulate further investigations. The utilization of this plant as a natural source to supplement the diet, or to prepare new food products and pharmaceutical formulations is an attractive approach to explore and fully realize the potential of the rich biodiversity found in Brazil and in other countries.

Ethnopharmacology, phytochemistry and biological activity of Erodium species: A review.

Erodium spp. is a genus that can be found in all continents that has been traditionally used in folk medicine to treat many diseases such as hemorrhage, dermatological disorders, indigestion, and inflammatory diseases. Moreover, Erodium leaves have been used for the preparation of salads, omelets, sandwiches, sauces and soups, among other food products. The objective of this review was to show the recent and relevant studies about extraction of bioactive compounds, the phytochemical characterization, the potential biological activities and toxicological evidence reported in both in vitro and in vivo studies from Erodium spp. In addition, the use of Erodium spp. as natural compounds against the development of diseases were also showed. This review highlights the traditional use of Erodium species in several countries as a therapeutic agent to treat several diseases (such as constipation, dermatological disorders, diabetes, indigestion, urinary inflammations, and as carminative agent), the factors influencing the extraction of bioactive compounds (mainly species and solvent composition on phenolic compounds) and phytochemical profile (presence of essential oils and alkaloids), the scientific evidence about its anti-inflammatory, antimicrobial (against both spoilage and pathogenic microorganisms), antiviral and other health-related activities (anti-protozoal and anti-viral activity) as well as the toxicological evidence. Erodium spp. is a relevant source of compounds with antioxidant, antimicrobial, and biological activity, which support its potential exploration in pharmacological and food area. Major efforts are necessary to advance the knowledge about Erodium genus regarding the relation between traditional use and scientific evidence, optimization of extraction conditions, the influence on biological mechanisms at animal and clinical levels, and bioaccessibility and bioavailability of bioactive compounds.

Effects of Gut Microbiota on the Bioavailability of Bioactive Compounds from Ginkgo Leaf Extracts.

Ginkgo leaf extract (GLE) is a popular herbal medicine and dietary supplement for the treatment of various diseases, including cardiovascular disease. GLE contains a variety of secondary plant metabolites, such as flavonoids and terpenoids, as active components. Some of these phytochemicals have been known to be metabolized by gut microbial enzymes. The aim of this study was to investigate the effects of the gut microbiota on the pharmacokinetics of the main constituents of GLE using antibacterial-treated mice. The bilobalide, ginkgolide A, ginkgolide B, ginkgolide C, isorhamnetin, kaempferol, and quercetin pharmacokinetic profiles of orally administered GLE (600 mg/kg), with or without ciprofloxacin pretreatment (150 mg/kg/day for 3 days), were determined. In the antibacterial-treated mice, the maximum plasma concentration (Cmax) and area under the curve (AUC) of isorhamnetin were significantly (p < 0.05) increased when compared with the control group. The Cmax and AUC of kaempferol and quercetin (other flavonol glycosides) were slightly higher than those of the control group, but the difference was not statistically significant, while both parameters for terpenoids of GLE showed no significant difference between the antibacterial-treated and control groups. These results showed that antibacterial consumption may increase the bioavailability of isorhamnetin by suppressing gut microbial metabolic activities.

THERAPEUTIC MICROEMULSION OF CURCUMIN FOR THE MANAGEMENT OF OSTEOARTHRITIS

Curcumin (diferuloylmethane) is a natural polyphenolic compound with potent anti-inflammatory, anticancer and antioxidant activities. However, its bioavailability is low as it is poorly absorbed in the gastrointestinal tract. Microemulsions offer the potential to improve the solubility and bioavailability of bioactive compounds; the present work investigated the topical delivery potential of microemulsion gel loaded with curcumas. Curcumin microemulsion was prepared by spontaneous emul­sification method using oil (Oleic acid), surfactant:cosurfactant (Smix) (Ethanol and Tween 80, Span 80 and n Butanol) and water. The optimized formulations of microemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in microemulsion, zeta potential and vesicle size measurement and then microemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Tween 80, Span 80 was selected as surfactant, ethanol, n Butanol as co surfactant and Oleic acid as oil component based on solubility study. The optimized formulation contained Curcumin (10 mg). The in vitro drug release from curcumin microemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of microemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of curcumin can be increased by formulating into microemulsion gel.&#x0D; Keyword: Curcumin, Microemulsion, In-vitro diffusion, Spreadability, Zeta potential, Stability, span 40

Okara residue as source of antioxidants against lipid oxidation in milk enriched with omega-3 and bioavailability of bioactive compounds after in vitro gastrointestinal digestion.

The residue from soy processing (okara) was evaluated for phenolic compounds, flavonoids, radical scavenging activity and reducing power ability. The ability of okara to decelerate the oxidation of omega-3 fatty acids caused by light exposure in a milk matrix, as well as its bioavailability after in vitro digestion, were investigated. Okara contained phenolic compounds (106.7mg gallic acid equivalents (GAE)/100g) and flavonoids (32.7mg quercetin equivalents/100g) and showed antioxidant activity. The addition of okara to omega-3 fatty acids-enriched milk inhibited the production of conjugated dienes and malonaldehyde during 8days of storage compared to the control (without okara), particularly at the higher (3g/L) than lower inclusion concentrations studied (1 and 2g/L). The bioavailability assay demonstrated that polyphenols (41mg GAE/100g) were still present after in vitro digestion and had antioxidant activity. Okara, which is considered a residue and is discarded, can potentially be used as an antioxidant ingredient for the enrichment of foods.

Phenolic acids prolife and antioxidant properties of bread enriched with sprouted wheat flour

The influence of addition of sprouted flour (SF), obtained from elicited wheat seeds, on phenolic acids profile and antioxidant properties of wheat bread was examined. The sensorial properties of bread were also studied. Bread was obtained from white flour replaced with (SF) at 5, 10, 15, and 20% levels. The addition of SF significantly enriched wheat bread with phenolic acids, especially vanillic, syringic, p-coumaric, t-ferulic, and t-sinapic acids. Significant decrease of caffeic, cis-ferulic, t-sinapic, and cis-sinapic acids was observed in the samples obtained from bread with high level of SF. Bread with SF was the good source of antiradical and chelating compounds as well as phytochemicals able to prevent lipids against oxidation. Far weaker results were obtained while considering the reducing power. In addition, bioactive compounds contained in SF were potentially bioaccessible. Replacement of wheat flour with SF by up to 10% had little influence on the overall acceptability. Practical applications Flour from elicited wheat seedlings is a potential additive for functional food production. Both elicitation and sprouting affected the phenolic acids profile and the antioxidant potential of wholemeal wheat flour. Antioxidant potential of functional products was determined in light of potential bioaccessibility and bioavailability of bioactive compounds. Bread with sprouted flour is the good source of antiradical and chelating compounds as well as phytochemicals, which are able to prevent lipids against oxidation. In addition, bioactive compounds are thermostable and potentially bioaccessible.

Effect of addition of Agaricus blazei mushroom residue to milk enriched with Omega‐3 on the prevention of lipid oxidation and bioavailability of bioactive compounds after in vitro gastrointestinal digestion

SummaryThe residue from a hydroalcoholic extract of the mushroom Agaricus blazei (MAR) was evaluated for phenolic compounds, flavonoids and antioxidant activity. The ability of MAR to slow the oxidation of Omega‐3 resulting from light exposure in milk matrix, and its bioavailability after in vitro digestion was investigated. MAR presented phenolic compounds and flavonoids and showed antioxidant activity. At each concentration, addition of MAR to Omega‐3‐supplemented milk inhibited the production of conjugated dienes and malonaldehyde compared with samples without MAR. The bioavailability assay showed that polyphenols were still present after in vitro digestion and had antioxidant activity.

Cruciferin coating improves the stability of chitosan nanoparticles at low pH.

Encapsulation is an emerging technique to improve the solubility, permeability and bioavailability of bioactive compounds. Cruciferin, a major canola protein, has the potential to protect chitosan-based delivery systems under the gastric conditions due to its resistance to gastric digestion. Positively charged spherical nanoparticles with an average size of 165 nm were prepared. Two water-soluble and -insoluble model compounds (brilliant blue and β-carotene) were encapsulated. The characteristic studies of the particles showed that the chitosan-based core was coated by a cruciferin layer mainly through hydrogen bonding based on FTIR, DSC, surface hydrophobicity, dissociating and intrinsic fluorescence studies. The particles did not show toxicity to Caco-2 cells and their cellular uptake was observed using confocal microscopy. Release studies showed that the particles were resistant to simulated gastric and intestinal fluids and released less than 20% of the encapsulated compounds. Our results suggested that the particles are promising carriers for encapsulation of heat, pH and protease-degradable hydrophilic and hydrophobic bioactive compounds.

Optimization Processing Parameters for Curcuma xanthorriza Oleoresin Yield and its Antioxidant Activity

Processing is a critical aspect of herbal based products, and processing method is known to affect the content, activity and bioavailability of bioactive compounds. Extraction of oleoresin from Curcuma xanthorriza is effected by several processing parameters. Appropriate solvent selection such as polar solvent result in better extraction yield while lower polarity solvent end up with extracts having higher concentration of active compounds. In this study, different processing parameters were carried out including blanching treatment (boiled, steamed) at range of time (24 hours, 48 hours and 72 hours), solvent of extraction (methanol, ethanol and acetone). The curcuminoid content and antioxidant activity were determined in Curcuma xanthorriza oleoresin. The result obtained was proved that ethanol was the most effective solvent. Blanching treatment affects the yield of oleoresin and promotes the release of curcuminoids content

Recent developments in nanoformulations of lipophilic functional foods

Recently, nutraceuticals have great attention due to their excellent functional properties for health promotion and disease prevention. Especially, lipophilic materials could give various health benefits such as antioxidant, anti-inflammatory, wound healing, and even anti-cancer effects. However, there are some limitations to apply them into food system and oral administration due to their poor water solubility, low oral absorption, and poor bioavailability which are pivotal issues to overcome for lipophilic nutraceuticals. In this review, various nanoformulations have been introduced with their advantages and disadvantages, including those that can enhance solubility and bioavailability of bioactive compounds.

Challenges in providing credible scientific evidence of health benefits of dietary polyphenols

► Credible scientific evidence of health benefits of dietary polyphenols is needed. ► Bioavailability of bioactive compounds must be known. ► Bioavailability includes absorption, distribution, metabolism, and excretion. ► Metabolites must be included in vitro and in vivo studies. ► Physiological concentrations of bioactive compounds must be used.

Cocoa consumption reduces NF-κB activation in peripheral blood mononuclear cells in humans

Background and aimsEpidemiological studies have demonstrated an association between high-polyphenol intake and reduced incidence of atherosclerosis. The healthy effects of cocoa-polyphenols may be due to their antioxidant and anti-inflammatory actions, although the exact mechanisms are unknown and depend on the matrix in which cocoa-polyphenols are delivered. Nuclear factor κB (NF-κB) is a key molecule in the pathophysiology of atherosclerosis involved in the regulation of adhesion molecules(AM) and cytokine expression and its activation is the first step in triggering the inflammatory process. The aim of this study was to evaluate the effect of acute cocoa consumption in different matrices related to the bioavailability of cocoa-polyphenols in NF-κB activation and the expression of AM. Methods and resultsEighteen healthy volunteers randomly received 3 interventions: 40g of cocoa powder with milk (CM), with water (CW), and only milk (M). NF-κB activation in leukocytes and AM (sICAM, sVCAM, E-selectin) were measured before and 6h after each intervention. Consumption of CW significantly decreased NF-κB activation compared to baseline and to CM (P < 0.05, both), did not change after CM intervention, and significantly increased after M intervention (P = 0.014). sICAM-1 concentrations significantly decreased after 6h of CW and CM interventions (P ≤ 0.026; both) and E-selectin only decreased after CW intervention (P = 0.028). No significant changes were observed in sVCAM-1 concentrations. ConclusionsThe anti-inflammatory effect of cocoa intake may depend on the bioavailability of bioactive compounds and may be mediated at least in part by the modulation of NF-κB activation and downstream molecules reinforcing the link between cocoa intake and health.

Optimization of Extraction Conditions of Antioxidant Activity from Zingiber zerumbet Oleoresin

The health promoting capacity of natural antioxidant from phytochemicals has increase attention from researchers and public. However, processing is affecting the activity and the bioavailability of bioactive compounds. Therefore, the optimization of extraction condition of antioxidant activity from Zingiber zerumbet oleoresin was investigated. A Box-Behnken design technique was employed to study the effect of different range parameters of soxhlet extraction. Analysis of variance and response surface methodology were applied to identify the optimal processing parameter. Independent variables were extraction time (8, 10 and 12), type of solvent used (hexane, acetone, ethanol) and blanching treatment (steam treated, boil treated, untreated). The response and variables were fitted well to each other by multiple regressions. All the independent parameters affected oleoresin yield and antioxidant activity significantly. The optimal processing parameter that fulfilled the requirement for yield of oleoresin and antioxidant activity were found to be 12 h extraction time, ethanol as the solvent used and untreated sample. While, the optimal yield of oleoresin was 13.05% w/w and antioxidant activity was 16.01% w/w.