Suppression of arachidonic acid metabolism and nitric oxide formation by kudzu isoflavones in murine macrophages

Inhibitory effect of kudzu isoflavones on arachidonic acid metabolism and nitric oxide (NO) production in lipopolysaccharide activated RAW 264.7 macrophages were investigated. Isoflavone aglycones, such as daidzein, genistein, biochanin A, and formononetin significantly suppressed arachidonic acid release (50 microM). Biochanin A, which displayed the most active inhibition on arachidonic acid release in HT-29 human colon cancer cells, exhibited its most potent suppression in RAW 264.7 cell (by 86%) without showing cytotoxicity. However, isoflavone glucosides, puerarin and daidzin, showed lower inhibitory activities on the release of arachidonic acid and its metabolites. In NO formation, biochanin A showed marked inhibition, by 62% (50 microM), followed by genistein, daidzein, formononetin, and daidzin, 56, 39, 33, and 8%, respectively. 5,7-Dihydroxyl group in the A-ring of isoflavones could be a key functional group responsible for the strong inhibitory activity of biochanin A and genistein on NO production. These activities may contribute to the antiinflammatory and anticarcinogenic properties of kudzu isoflavones.     

红车轴草不同部位中异黄酮含量的测定

采用反相高效液相色谱法对红车轴草不同部位(花、茎和叶)中四种主要异黄酮(鸡豆黄素A、芒柄花黄素、染料木素和大豆黄素)的含量进行了测定,结果表明:以占干物质计,4种异黄酮总量,叶中含量最高(0.856%),茎次之(0.403%),花中含量较低(0.258%)。鸡豆黄素A和芒柄花黄素是红车轴草中两种最主要的异黄酮,主要分布在叶中,其次是茎,花中含量较低。染料木素和大豆黄素,无论是花、茎还是叶,含量均较低。     

Cellular DNA breakage by soy isoflavone genistein and its methylated structural analogue biochanin A

Epidemiological studies have indicated that populations with high isoflavone intake through soy consumption have lower rates of breast, prostate, and colon cancer. The isoflavone polyphenol genistein in soybean is considered to be a potent chemopreventive agent against cancer. In order to explore the chemical basis of chemopreventive activity of genistein, in this paper we have examined the structure–activity relationship between genistein and its structural analogue biochanin A. We show that both genistein and its methylated derivative biochanin A are able to mobilize nuclear copper in human lymphocyte, leading to degradation of cellular DNA. However, the relative rate of DNA breakage was greater in the case of genistein. Further, the cellular DNA degradation was inhibited by copper chelator (neocuproine/bathocuproine) but not by compounds that specifically bind iron and zinc (desferrioxamine mesylate and histidine, respectively). We also compared the antioxidant activity of the two isoflavones against tert‐butylhydroperoxide‐induced oxidative breakage in lymphocytes. Again genistein was found to be more effective than biochanin A in providing protection against oxidative stress induced by tert‐butylhydroperoxide. It would therefore appear that the structural features of isoflavones that are important for antioxidant properties are also the ones that contribute to their pro‐oxidant action through a mechanism that involves redox cycling of chromatin‐bound nuclear copper.     

Plant flavonol quercetin and isoflavone biochanin A differentially induce protection against oxidative stress and inflammation in ARPE-19 cells

In this work, differential ability of plant flavonol quercetin and plant isoflavone biochanin A to modulate oxidative stress and inhibit inflammation-related responses was investigated using human retinal pigment epithelial cells (RPE) at gene expression level. Quercetin protected cells from oxidative stress-induced cell death, whereas biochanin A had no statistically significant protective effects. Quercetin reduced the expression of cytokines IL-6 and IL-1?? in cells treated with H₂O₂, and expression levels of Nrf2 and HO-1 were increased by quercetin treatment suggesting protective function against oxidative stress. Our data indicate that quercetin may protect cells by inhibiting the production of pro-inflammatory factors such as IL-6, and by inducing the expression of ROS-catalyzing phase II proteins such as HO-1. Therefore, plant extracts rich in flavonol quercetin may be an interesting resource for functional food products and other foods targeted for reduced risks of age-related macular degeneration.     

Improving functionality of chocolate: A review on probiotic,prebiotic, and/or synbiotic characteristics

BackgroundChocolate is consumed by people of all ages in all segments of society throughout the world. The popularity of this food is mainly associated with its potential to arouse sensory pleasure and positive emotions. Increasing awareness of the link between healthy eating and well-being is reflected in the current views of the general consumers. Consumers perceive functional foods as a member of the specific food category to which they belong. Also, in developed economies, a key trend at the moment is confectionery products that deliver functional benefits for health and well-being, such as functional chocolate.Scope and approachIn this review, studies related with production of prebiotic, probiotic and synbiotic chocolates as a functional food were investigated and positive and negative aspects of these functional products when compared with standard one were stated, which could shape the following related studies in food area and the production of prebiotic, probiotic and synbiotic chocolates in the food industry.Key findings and conclusionsWhen the studies related with this topic were investigated it could be concluded that the studies associated with chocolate which could play a role in transportation of probiotics and prebiotics might be supported by studies in which bioavailability and bioaccessibility characteristics of them in vivo and in vitro media will be determined. Moreover, in order to improve bioavailability and bioaccessibility properties product quality optimization studies might be required in the future.     

The international scenario of patents concerning isoflavones

BackgroundIsoflavones are a class of phytoestrogens that has been considered important raw material for healthcare products, mainly as dietary supplements for hormone replacement and active ingredients in skin care cosmetics. Because of this, many scientific reviews are found regarding the extraction, analysis methods and biological activities of these compounds. However, it is emphasized that, to date, no studies have been found concerning technological mapping of patents involving isoflavones.Scope and approachThe present study aimed to map patents covering the last 20 years of technology innovation comprising isoflavones. To that, a patent survey was conducted between the years of 1994–2014 in an international patent database (Espacenet) using the title's keywords: isoflavones, genistein, daidzein, glycitein, biochanin A and formononetin.Key findings and conclusionsThe resulting data allowed the identification of the major countries, universities and companies that invest in products containing these compounds. In addition, patents were separated into interest groups. The three clusters discussed in this study were: processes for obtaining enriched isoflavone fractions from different plant materials intended to healthcare products, such as dietary supplements; the use of isoflavones in cosmetic products; and the incorporation of isoflavones in micro and nanostructured systems to mask unpleasant tastes or overcome the low water solubility of bioactive forms. In conclusion, this study, along with other literature reviews, could assist in designing strategic research and worldwide development of new products containing isoflavones.     

Reciprocal interactions between resveratrol and gut microbiota deepen our understanding of molecular mechanisms underlying its health benefits

BackgroundResveratrol is a stilbene-based phytochemical, which possesses multiple pharmacological activities. However, the low bioavalibility of resveratrol mystifies its pharmacology.Scope and approachWe discussed the reciprocal interactions of resveratrol with gut microbiota as investigated by in vitro, animal models as well as humans studies.Key findings and conclusionsThe first part described the current in vitro and in vivo evidence concerning the modulative effect of resveratrol on gut microbiota composition, particularly focusing on the involvement of gut microbiota modulation in the anti-diabetic, anti-obesity, and anti-atherosclerosis effects of resveratrol. The second part summarized the bioconversion of resveratrol by gut microbiota, and the identification of metabolites along with bacterial species as generators of these metabolites. This may not only help reconcile the bioavailability conundrum of resveratrol, but also provide directions to expedite its medical applications.     

Hydrolysis of soybean isoflavone glycosides by a thermostable β-glucosidase from Paecilomycesthermophila

The β-glucosidase from Paecilomyces thermophila J18 was found to be capable of hydrolysing daidzin and genistin in a previous study. This report further evaluated the thermostability and hydrolysis of soybean isoflavone glycosides. The enzyme was found to be very stable at 50 °C, and retained more than 95% of its initial activity after 8 h at 50 °C. It converted isoflavone glycosides, in soybean flour extract and soybean embryo extract, to their aglycones, resulting in more than 93% of hydrolysis of three isoflavone glycosides (namely, daidzin, genistin and glycitin) after 4 h of incubation. Also, addition of the β-glucosidase greatly increased the contents of isoflavone aglycones in the suspended soybean flour and soymilk. The results indicate that the thermostable β-glucosidase may be used to increase the isoflavone aglycones in soy products. This is the first report on the potential application of fungal β-glucosidases for converting isoflavone glycosides to their aglycones in soy products.     

Modified-atmosphere packaging (MAP) does not affect the bioavailability of tocopherols and carotenoids from broccoli in humans: A cross-over study

Aim of the study

Ready-to-eat and pre-packed vegetables are increasingly accepted by consumers but little is known about the effect of these technological approaches on the bioavailability of the nutrients. To assess the effect of modified-atmosphere packaging (MAP) on the bioavailability in humans of carotenoids and tocopherols from broccoli.

Results

Serum lutein increased significantly upon broccoli intake but those of β-carotene, α- and γ-tocopherol did not reach statistical significance. Serum changes were observed regardless of the type of broccoli consumed.

Conclusions

Modified-atmosphere packaging does not affect significantly the in vivo bioavailability of carotenoids and tocopherols from broccoli, supporting its convenience for use by the food industry and consumers.     

Nutrikinetics of Isoflavone Metabolites After Fermented Soybean Product (Cheonggukjang) Ingestion in Ovariectomized Mice

1 Scope

Cheonggukjang (CGJ) is a soybean‐based quick‐fermented food popular in Korea that contains a variety of biologically active compounds including isoflavones and saponins. Isoflavone bioavailability may be important for the bone health of postmenopausal women; therefore, the aim of this study is to evaluate the influence of fermentation on the isoflavone metabolite nutrikinetic profile after single dose CGJ or unfermented soybean administration in ovariectomized (OVX) and sham mice.

2 Methods and results

We identify 34 isoflavone metabolites using UPLC–QTOF‐MS and analyze their nutrikinetics at different time points (0.25, 0.5, 1, 2, 4, 8, 16, and 24 h) to understand their fermentation‐ and OVX‐mediated time‐dependent concentration changes. Nutrikinetics analysis shows that genistein, daidzein, genistein 4′‐sulfate, dihydrodaidzein sulfate, equol 4′‐sulfate, and equol‐7‐glucuronide are present at high concentrations in all groups based on area‐under‐the‐curve analysis. OVX mice appear to show lower isoflavone bioavailability than mice in the sham group. CGJ enhances various isoflavone metabolite bioavailability including genistein, 3‐hydroxygenistein, and equol 7‐glucuronide, compared to the unfermented soybean‐treated group. Among these metabolites, intact isoflavones, 3‐hydroxygenistein, genistein 4′‐sulfate, and equol 7‐glucuronide promote osteoblastogenesis and inhibit osteoclast formation.

3 Conclusions

CGJ has good isoflavone bioavailability and may be beneficial for the bone health of postmenopausal women.     

Enhancing enzymatic hydrolysis of food proteins and production of bioactive peptides using high hydrostatic pressure technology

BackgroundBioactive peptides (BPs) generated by hydrolysis of food proteins exhibit a broad spectrum of biological properties (antihypertensive, hypocholesterolemic, antimicrobial, antioxidant, etc.) in both in vitro and in vivo models. Initially obtained from milk and egg products, BPs have now largely been obtained from food byproducts such as marine, animal and plant biomasses. Amongst the various strategies being developed for BPs production, enzymatic hydrolysis (EH) is the most widely preferred due to its GRAS nature. However, the main challenge of EH is to decrease the time and quantity of enzyme, and improve yield and bioactivity of BPs.Scope and approachConsequently, innovative and efficient food technologies have been developed to satisfy these needs. High hydrostatic pressure (HHP) processing, a non-thermal technology, initially developed to extend food shelf-life, is being considered as a promising tool to improve the efficiency of EH and generate high value-added peptide fractions from various complex biomasses.Findings and conclusionsThis innovative and emerging technology enhances EH by inducing protein unfolding/denaturation, as well as activating the enzymes used while maintaining their nutritional and functional properties. This review discusses the state of the art of HHP technique, its applications in combination with EH, and potential challenges for the production of BPs from food-derived protein sources.     

Evaluation of enzymic potential for biotransformation of isoflavone phytoestrogen in soymilk by Bifidobacterium animalis,Lactobacillus acidophilus and Lactobacillus casei

Three strains of Lactobacillus acidophilus, two of Lactobacillus casei and one of Bifidobacterium were screened for β-glucosidase activity using ρ-nitrophenyl-β-d-glucopyranoside as a substrate and their potential for the breakdown of isoflavone glucosides to the biologically active aglycones in soymilk. Isoflavones quantification with HPLC and β-glucosidase activity were performed after 0, 12, 24, 36, and 48 h of incubation in soymilk at 37 °C. All six micro-organisms produced β-glucosidase, which hydrolysed the predominant isoflavone β-glucosides. There was a significant increase and decrease (P < 0.05) in the concentration of isoflavone aglycones and glucosides, respectively, in fermented soymilk. Based on the concentration of isoflavones during peak β-glucosidase activity, the hydrolytic potential was calculated. L. acidophilus 4461 had the highest aglycone concentration of 76.9% after 24 h of incubation, up from 8% in unfermented soymilk (at 0 h). It also had the best isoflavone hydrolytic index of 2.01, signifying its importance in altering the biological activity of soymilk.     

Cordyceps Militaris improves neurite outgrowth in Neuro2A cells and reverses memory impairment in rats

The aim of this study was to evaluate the effect of Cordyceps militaris (CM) on neurite outgrowth in Neuro2A mouse neuroblastoma cells and scopolamineinduced learning and memory deficits in rats. Pretreatment with CM (5–20 μg/mL) for 1 h was sufficient to stimulate primary neurite sprouting and extension of Neuro2A cells after 24 h cultivation in a dose-dependent manner. The CM also increased choline acetyltransferase expression in differentiated Neuro2A cells. Administration of CM significantly reversed the scopolamine-induced deficit in memory, and it alleviated decrease in cholinergic immunoreactivity in the hippocampus. Our results demonstrated that in vitro neuritogenesis of Neuro2A cell lines by CM constitutes a potential clue that could help to explain in vivo improvement of memory functions using the behavioral tasks. These results suggest that CM is strongly effective in protecting against memory-related neuronal degeneration in the brain and retarding the progression of memory deficits associated with various neurodegenerative diseases.     

Radioprotection by quercetin-3-O-rutinoside,a flavonoid glycoside – A cellular and mechanistic approach

The present study was aimed to evaluate the in vivo radioprotective efficacy of quercetin-3-O-rutinoside (PMC-1), the key bioactive constituent flavonoid glycoside isolated from the whole plant of Pilea microphylla was evaluated. In vivo survival studies established the optimum effective dose of PMC-1 at 25 mg/kg/i.p. At the optimum dose, PMC-1 prevented the depletion of endogenous antioxidants in the liver of irradiated mice. In vivo protection towards gastrointestinal tract and haematopoietic system was confirmed by the restoration of radiation-induced reduction in villi height, number of crypt cells and spleen index. PMC-1 also attenuated the radiation-induced apoptosis in spleenocytes significantly. Single cell gel electrophoresis of peripheral blood leukocytes showed inhibition of radiation-induced DNA damage by PMC-1. PMC-1 pretreatment significantly reversed the changes by increasing pro-survival (ERK) and decreasing pro-apoptotic (BAX) gene expressions compared to radiation control. Thus, PMC-1 exhibits protective effects against γ-radiation and the probable mechanism of action involves maintenance of antioxidant enzymes, prophylactic action and inhibition of apoptosis.     

Antioxidant phenolics and their microbial production by submerged and solid state fermentation process: A review

BackgroundBioactive phenolic compounds have recently received great attention in the food and clinical sectors due to their antioxidant potential. Extensive studies have been carried out to explore antioxidant potential of different phenolics from various natural sources in order to replace the use of health hazard synthetic antioxidants in food products.Scope and approachThe present review aims to provide an update of existing state-of-art and future prospect of both submerged fermentation (SmF) and solid-state fermentation (SSF) processes for the production/extraction of bioactive phenolics utilizing various substrates and microorganisms. Studies on enhancement of antioxidant potentials by increasing phenolics content of food materials including cereals and legumes by mainly SSF are reviewed and discussed thoroughly.Key findings and conclusionsMicrobial fermentation processes have been established as a potent tool for the production of antioxidant phenolic compounds due to their cost-effectiveness and environmental advantages. Extraction of phenolics through fermentation process is by far a more efficient process considering that conventional extraction methods using organic solvents do not allow complete release of bound phenolics from plant materials. During fermentation process, antioxidant phenolics are either produced by microorganisms through secondary metabolic pathway or released from the matrix of the substrate by extracellular enzymatic action. Fermentation technology is no doubt proving to be a boon for the food industry; however, extensive in vivo and toxicological researches are essential before the application of antioxidant-rich fermented foods for human health benefits.     

Aquatic photochemistry of isoflavone phytoestrogens: degradation kinetics and pathways

Isoflavones are plant-derived chemicals that are potential endocrine disruptors. Although some recent studies have detected isoflavones in natural waters, little is known about their aquatic fates. The photochemical behaviors of the isoflavones daidzein, formononetin, biochanin A, genistein, and equol were studied under simulated solar light and natural sunlight. All of these phytoestrogens were found to be photolabile under certain conditions. Daidzein and formononetin degraded primarily by direct photolysis. Their expected near-surface summer half-lives in pH 7 water at 47° latitude are expected to be 10 and 4.6 h, respectively. Biochanin A, genistein, and equol degraded relatively slowly by direct photolysis at environmentally realistic pH values, though they showed significant degradation rate enhancements in the presence of natural organic matter (NOM). The indirect photolysis rates for these compounds scaled with NOM concentration, and NOM from microbial origin was found to be a more potent photosensitizer than NOM from terrestrial sources. Mechanistic studies were performed to determine the indirect photolysis pathways responsible for the rate enhancements. Results of these studies implicate reaction with both singlet oxygen and excited state triplet NOM. Environmental half-lives for biochanin A, genistein, and equol are expected to vary on the basis of pH as well as NOM source and concentration.     

In vitro and in vivo antioxidant properties of ferulic acid: A comparative study with other natural oxidation inhibitors

Ferulic acid exhibits a wide range of therapeutic effects that are attributed to its potent antioxidant capacity. However, in vitro antioxidant properties of ferulic acid have not been elucidated in detail. Evidence that polyphenols, including ferulic acid, act as antioxidants in vivo is also limited. In order to elucidate in more detail the scientific background of antioxidant activities of ferulic acid, we carried out in vitro and in vivo experiments. We focused on superoxide anion scavenging activity, xanthine oxidase inhibition activity, and chain-breaking activity. The combined antioxidant activity from radical scavenging and xanthine oxidase inhibition of ferulic acid was much weaker than that of (−)-epigallocatechin gallate (EGCG) and ascorbic acid. On the other hand, EGCG, ascorbic acid and ferulic acid exhibited chain-breaking activity and prevented ischaemia-reperfusion-associated intestinal injury. Chain-breaking activity may play a contributory role in the protective effect of ferulic acid on oxidative injury in humans and in in vivo studies.     

Edible halophytes of the Mediterranean basin: Potential candidates for novel food products

BackgroundRecent trends in the food science industry and consumers’ preferences for diversified diets suggest the consumption of wild greens not only as diet complements but also as healthy and functional foods for targeted conditions, rendering its commercial cultivation of major importance in order to avoid irrational gathering and genetic erosion threats. The Mediterranean basin abounds in wild edible species which have been used for food and medicinal purposes by human throughout the centuries. Many of these species can be found near coastal areas and usually grow under saline conditions, while others can adapt in various harsh conditions including high salinity.Scope and approachThe aim of this review focuses on listing and describing the most important halophyte species that traditionally have been gathered by rural communities of the Mediterranean basin, while special interest will be given on their chemical composition and health promoting components. Cases of commercially cultivated halophytes will be also presented to highlight their potential as alternative cash crops, while results from in vitro and in vivo health effects will be presented.Key findings and conclusionsThe recent literature has provided useful information regarding the potential of wild halophytes as promising ingredients in functional food products and/or as sources of bioactive compounds. However, further research is needed regarding the chemical characterization of these species under commercial cultivation practices, while further clinical and model trials have to be conducted to assess their long term bioactivity and elucidate potential toxic effects and regulations of safe consumption.     

Promising interaction between nanoencapsulated lutein with low molecular weight chitosan: Characterization and bioavailability of lutein in vitro and in vivo

This study aims to develop water-soluble low molecular weight chitosan (LMWC) nanoencapsules with lutein to improve its bioavailability. Lutein-LMWC nanoencapsules were prepared, characterized and bioavailability was studied in vitro and in vivo with lutein in mixed micelles (control). The particle size ranged between 80–600 nm, which was confirmed by Atomic Force Microscope. The interaction between LMWC and lutein in nanocencapsules by ¹H and ¹³C NMR showed the essentiality of water molecules to hold the lutein between LMWC chains of nanoparticle with a reversible weak bond. Bioavailability of lutein (200 μM) in vitro showed that lutein-LMWC nanoencapsules was significantly higher (27.7%) than control. Postprandial lutein level in the plasma (54.5%), liver (53.9%) and eyes (62.8%) of mice fed on nanoencapsulated lutein were higher than the control. LMWC may serve as novel carrier for enhancing the lutein bioavailability and can be suggested as the better dietary compound in food and pharmaceutical applications.