Bioactive compounds in berries relevant to human health

Berries contain powerful antioxidants, potential allergens, and other bioactive compounds. Genetic and environmental factors affect production and storage of such compounds. For this reason breeding and biotechnological approaches are currently used to control or to increase the content of specific health-related compounds in fruits. This work reviews the main bioactive compounds determining the nutritional quality of berries, the major factors affecting their content and activity, and the genetic options currently available to achieve new genotypes able to provide, under controlled cultivation conditions, berries with the proper balance of bioactive compounds for improving consumer health.     

Berries as a Treatment for Obesity-Induced Inflammation: Evidence from Preclinical Models

Inflammation that accompanies obesity is associated with the infiltration of metabolically active tissues by inflammatory immune cells. This propagates a chronic low-grade inflammation associated with increased signaling of common inflammatory pathways such as NF-κB and Toll-like receptor 4 (TLR4). Obesity-associated inflammation is linked to an increased risk of chronic diseases, including type 2 diabetes, cardiovascular disease, and cancer. Preclinical rodent and cell culture studies provide robust evidence that berries and their bioactive components have beneficial effects not only on inflammation, but also on biomarkers of many of these chronic diseases. Berries contain an abundance of bioactive compounds that have been shown to inhibit inflammation and to reduce reactive oxygen species. Therefore, berries represent an intriguing possibility for the treatment of obesity-induced inflammation and associated comorbidities. This review summarizes the anti-inflammatory properties of blackberries, blueberries, strawberries, and raspberries. This review highlights the anti-inflammatory mechanisms of berries and their bioactive components that have been elucidated through the use of preclinical models. The primary mechanisms mediating the anti-inflammatory effects of berries include a reduction in NF-κB signaling that may be secondary to reduced oxidative stress, a down-regulation of TLR4 signaling, and an increase in Nrf2.     

Comparative study of the nutritional and bioactive compounds content of four walnut (Juglans regia L.) cultivars

The proximate and mineral composition, fatty acid profile, total polyphenol, melatonin and serotonin contents were assessed in four walnut (Juglans regia L.) cultivars (cv. Serr, Hartley, Chandler and Howard). The aim was to decide which cultivar is the most suitable from a nutritive, but also commercial, point of view. Proteins and fats accounted for more than 70% of the walnut kernel weight. Due to their content in bioactive compounds such as melatonin, serotonin and total phenols, their high content in magnesium (up to 443 mg 100 g⁻¹ FW) and other minerals, their high contents in polyunsaturated fatty acids (up to 78.0% of total fatty acids) and their favorable n−6/n−3 ratio, among other healthful properties, consumption of all the studied cultivars would be potentially beneficial to health. According to its fatty acid profile, Howard would be the most healthful cultivar, but also it would be theoretically the most sensitive to rancidity, and thus the cultivar with the shortest shelf life. Nonetheless, this cultivar showed the highest content in the antioxidants melatonin and total polyphenols.     

Synthesis, characterization and biological evaluation of some 16β-azolyl-3β-amino-5α-androstane derivatives as potential anticancer agents

A series of new 16β-azolyl-3β-amino-5α-androstane derivatives were synthesized and characterized. The new compounds were screened for their anticancer activity against the human cancer cell lines SW480, A549, HepG2, HeLa and SiHa in vitro using the MTT assay. The results of the in vitro study showed that a number of compounds have shown IC₅₀ values lower than 20 μM against the five cancer cell lines.     

The use of total antioxidant capacity as surrogate marker for food quality and its effect on health is to be discouraged

Attempts have been made to use non-compositional parameters, such as total antioxidant capacity (TAC), determined by assays such as oxygen radical absorbance capacity, ferric-reducing ability of plasma, and trolox-equivalent antioxidant capacity, as surrogate markers for food quality and for monitoring food-related changes in human plasma in dietary intervention studies. Increased TAC of plasma is often indiscriminately, and therefore incorrectly, interpreted as being favorable to human health. Whether or not dietary compounds may indeed exert health effects depends on factors other than mere presence in food or body fluids. Many phytochemicals, for example, are poorly absorbed and rapidly metabolized into molecules with altered physicochemical, and therefore biological, properties. Consequently, the use of TAC assays for the in vitro assessment of antioxidant quality of food, which often is employed as a marketing argument or for the assessment of the “wholesomeness” of food, is to be discouraged.     

Colonic metabolites of berry polyphenols: the missing link to biological activity?

The absorption of dietary phenols, polyphenols and tannins (PPT) is an essential step for biological activity and effects on health. Although a proportion of these dietary bioactive compounds are absorbed intact, depending on their chemical structure and the nature of any attached moiety (e.g. sugar, organic acid), substantial amounts of lower molecular weight catabolites are absorbed after biotransformation by the colon microflora. The main products in the colon are (a) benzoic acids (C6-C1), especially benzoic acid and protocatechuic acid; (b) phenylacetic acids (C6-C2), especially phenylacetic acid per se; (c) phenylpropionic acids (C6-C3), where the latter are almost entirely in the dihydro form, notably dihydrocaffeic acid, dihydroferulic acid, phenylpropionic acid and 3-(3'-hydroxyphenyl)-propionic acid. As a result of this biotransformation, some of these compounds can each reach mm concentrations in faecal water. Many of these catabolites are efficiently absorbed in the colon, appear in the blood and are ultimately excreted in the urine. In the case of certain polyphenols, such as anthocyanins, these catabolites are major products in vivo; protocatechuic acid is reported to represent a substantial amount of the ingested dose of cyanidin-3-O-glucoside. The major catabolites of berries, and especially blackcurrants, are predicted based on compositional data for polyphenols from berries and other sources. Since microbial catabolites may be present at many sites of the body in higher concentration than the parent compound, it is proposed that at least a part of the biological activities ascribed to berry polyphenols and other PPT are due to their colonic catabolites.     

Comprehensive analysis of phenolic compounds and abscisic acid profiles of twelve native Canadian berries

Wild berries, integral parts of North American Natives’ traditional nutrition, are a rich source of phytochemicals involved in the prevention of metabolic syndrome. Although phenolic compounds are generally considered to be the functional components in fruits, the identification of specific compounds in relation to this beneficial activity remains to be uncovered. With the long-term goal of establishing the contribution of phytochemical compounds to their beneficial health effects, we investigated in a comprehensive manner the composition of twelve native Canadian berries: Saskatoon berry, alpine bearberry, chokeberry, black crowberry, honeysuckle, chokecherry, cloudberry, elderberry, lowbush blueberry, alpine blueberry, lingonberry and highbush cranberry. All harvested in the province of Quebec, these fruits were analyzed for their phenolic composition (anthocyanins, flavonols, flavan-3-ols, phenolic acids, proanthocyanidins and ellagitannins) and their content in abscisic acid derivatives (cis- and trans-ABA, abscisic acid-glucose ester, 7′-hydroxy-abscisic acid, neo-phaseic acid, phaseic acid and dihydrophaseic acid). Over 60 different phenolic compounds were identified and quantified in berries. Along with the characterization of abscisic acid, this study reports for the first time a complete characterization of proanthocyanidins in these fruits, highbush cranberry presenting the highest content of this class of compounds.     

Olive tree (Olea europaea) leaves: potential beneficial effects on human health

Olive tree ( Olea europaea L.) leaves have been widely used in traditional remedies in European and Mediterranean countries such as Greece, Spain, Italy, France, Turkey, Israel, Morocco, and Tunisia. They have been used in the human diet as an extract, an herbal tea, and a powder, and they contain many potentially bioactive compounds that may have antioxidant, antihypertensive, antiatherogenic, anti-inflammatory, hypoglycemic, and hypocholesterolemic properties. One of these potentially bioactive compounds is the secoiridoid oleuropein, which can constitute up to 6–9% of dry matter in the leaves. Other bioactive components found in olive leaves include related secoiridoids, flavonoids, and triterpenes. The evidence supporting the potentially beneficial effects of olive leaves on human health are presented in this brief review.     

Green tea and bone metabolism

Osteoporosis is a major health problem in both elderly women and men. Epidemiological evidence has shown an association between tea consumption and the prevention of age-related bone loss in elderly women and men. Ingestion of green tea and green tea bioactive compounds may be beneficial in mitigating bone loss of this population and decreasing their risk of osteoporotic fractures. This review describes the effect of green tea or its bioactive components on bone health, with an emphasis on (i) the prevalence and etiology of osteoporosis; (ii) the role of oxidative stress and antioxidants in osteoporosis; (iii) green tea composition and bioavailability; (iv) the effects of green tea and its active components on osteogenesis, osteoblastogenesis, and osteoclastogenesis from human epidemiological, animal, as well as cell culture studies; (v) possible mechanisms explaining the osteoprotective effects of green tea bioactive compounds; (vi) other bioactive components in tea that benefit bone health; and (vii) a summary and future direction of green tea and bone health research and the translational aspects. In general, tea and its bioactive components might decrease the risk of fracture by improving bone mineral density and supporting osteoblastic activities while suppressing osteoclastic activities.     

Postprandial metabolic events and fruit-derived phenolics: a review of the science

There is increasing evidence that the postprandial state is an important contributing factor to chronic disease. The role of fruit phenolic compounds to protect health and lower disease risk through their actions in mitigating fed-state metabolic and oxidative stressors is of interest and the topic of the present paper. Two main questions are posed: first, what is the role of plant foods, specifically fruits rich in complex and simple phenolic compounds in postprandial metabolic management; and second, does the evidence support consuming these fruits with meals as a practical strategy to preserve health and lower risk for disease? This review provides an overview of the postprandial literature, specifically on the effect of fruits and their inherent phenolic compounds in human subjects on postprandial lipaemia, glycaemia/insulinaemia and associated events, such as oxidative stress and inflammation. Among the identified well-controlled human trials using a postprandial paradigm, >50?% of the trials used wine or wine components and the remaining used various berries. Notwithstanding the need for more research, the collected data suggest that consuming phenolic-rich fruits increases the antioxidant capacity of the blood, and when they are consumed with high fat and carbohydrate 'pro-oxidant and pro-inflammatory' meals, they may counterbalance their negative effects. Given the content and availability of fat and carbohydrate in the Western diet, regular consumption of phenolic-rich foods, particularly in conjunction with meals, appears to be a prudent strategy to maintain oxidative balance and health.     

Design, synthesis and biological evaluation of substituted 11H-benzo[a]carbazole-5-carboxamides as novel antitumor agents

A series of novel 11H-benzo[a]carbazole-5-carboxamide derivatives were designed, synthesized and evaluated for their antitumor activity against human cancer A549 and HCT-116 cell lines. Most of the compounds showed potent antitumor activities, and compound 8 displayed remarkable in vitro and in vivo anticancer activity comparable to that of amonafide.     

Steroid hormone receptors and dietary ligands: a selected review

Members of the nuclear steroid hormone superfamily mediate essential physiological functions. Steroid hormone receptors (SHR) act directly on DNA, regulate the synthesis of their target genes and are usually activated by ligand binding. Both endogenous and exogenous compounds and their metabolites may act as activators of SHR and disruptors of endocrine, cellular and lipid homeostasis. The endogenous ligands are generally steroids such as 17beta-oestradiol, androgens, progesterone and pregnenolone. The exogenous compounds are usually delivered through the diet and include non-steroidal ligands. Examples of such ligands include isoflavanoids or phytooestrogens, and food contaminants such as exogenous oestrogens from hormone-treated cattle, pesticides, polychlorinated biphenyls and plasticisers. Certain drugs are also ligands; so nuclear receptors are also important drug targets for intervention in disease processes. The present review summarises recent reports on ligand-activated SHR that describe the selective regulation of a tightly-controlled cross-talking network involving exchange of ligands, and the control of major classes of cytochrome P450 (CYP) isoforms which metabolise many bioactive exogenous compounds. Many CYP have broad substrate activity and appear to be integrated into a coordinated metabolic pathway, such that whilst some receptors are ligand specific, other sensors may have a broader specificity and low ligand affinity to monitor aggregate levels of inducers. They can then trigger production of metabolising enzymes to defend against possible toxic nutrients and xenobiotic compounds. The influence of dietary intakes of nutrients and non-nutrients on the human oestrogen receptors (alpha and beta), the aryl hydrocarbon receptor, the pregnane X receptor, the constitutive androstane receptor, and the peroxisome proliferator-activated receptors (alpha and gamma), can be examined by utilising computer-generated molecular models of the ligand-receptor interaction, based on information generated from crystallographic data and sequence homology. In relation to experimental and observed data, molecular modelling can provide a scientifically sound perspective on the potential risk and benefits to human health from dietary exposure to hormone-mimicking chemicals, providing a useful tool in drug development and in a situation of considerable public concern.     

Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE

Central heteroaryl ring analogues belonging to a series of potent hydroxamate TACE inhibitors were synthesized. The TACE inhibitory activities of these compounds were evaluated by in vitro WBA and in silico molecular modeling studies using crystal structure of human TACE. Compound 14 showed very good in vitro inhibition, supported by the in silico docking studies.     

The effect of fruit size and fruit colour on chemical composition in ‘Kordia’ sweet cherry (Prunus avium L.)

The effect of fruit size (<26 mm, 26–28 mm, >28 mm) and fruit colour (Ctifl 4 and Ctifl 6) of ‘Kordia’ sweet cherry on composition of nutritive (sugars, organic acids) and bioactive (phenolics) compounds, on content of vitamin C, total phenolic content (TPC) and total antioxidant activity (TAA) was evaluated. The compositional data analysis was used for comparing relative contents of chemical compounds. The differences in average composition were examined on the basis of multivariate analysis of variance and further analysis of variance for each isometric log-ratio transformed variable. Five compounds have been identified for the first time: dicaffeoylquinic acid ([M−H]⁻ at m/z 515), procyanidin trimer ([M−H]⁻ at m/z 865), quercetin-3-(2G-glucosyl-rutinoside) ([M−H]⁻ at m/z 771), quercetin-3-galactoside ([M−H]⁻ at m/z 463) and kaempferol-3-glucoside ([M−H]⁻ at m/z 447). In the composition of sweet cherry ‘Kordia’ fruit bioactive compounds represented from 0.6% to 0.8%. The fruit colour modifies the chemical composition of phytochemicals more than fruit size; the two variables were correlated. More coloured fruit were larger, with better pomological traits and changed composition of nutritive compounds and phenolics.     

Fermentation of Vaccinium floribundum Berries with Lactiplantibacillus plantarum Reduces Oxidative Stress in Endothelial Cells and Modulates Macrophages Function

Accumulating evidence suggests that high consumption of natural antioxidants promotes health by reducing oxidative stress and, thus, the risk of developing cardiovascular diseases. Similarly, fermentation of natural compounds with lactic acid bacteria (LAB), such as Lactiplantibacillus plantarum, enhances their beneficial properties as regulators of the immune, digestive, and cardiovascular system. We investigated the effects of fermentation with Lactiplantibacillus plantarum on the antioxidant and immunomodulatory effects of Pushgay berries (Vaccinium floribundum, Ericaceae family) in human umbilical vein endothelial cells (HUVECs) and macrophage cell line RAW264.7. Polyphenol content was assayed by Folin–Ciocalteu and HPLC-MS/MS analysis. The effects of berries solutions on cell viability or proliferation were assessed by WST8 (2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium, monosodium salt and Lactate dehydrogenase (LDH) release, Trypan blue exclusion test, and Alamar blue assay. Antioxidant activity was evaluated by a cell-based chemiluminescent probe for the detection of intracellular H₂O₂ production in HUVECs. Heme oxygenase-1 (HO-1) expression levels were investigated by RT-qPCR. Glutathione reductase (GR), glutathione peroxidase (Gpx), superoxide dismutase (SOD), and catalase (CAT) activities, as markers of intracellular antioxidant defense, were evaluated by spectrophotometric analysis. The immunomodulatory activity was examined in RAW 264.7 by quantification of inducible nitric oxide synthase (iNOS) and Tumor Necrosis Factor—alpha (TNFα) by RT-qPCR. Data showed that fermentation of Pushgay berries (i) enhances the content of quercetin aglycone, and (ii) increases their intracellular antioxidant activity, as indicated by the reduction in H₂O₂-induced cell death and the decrease in H₂O₂-induced HO-1 gene expression in HUVECs treated for 24 h with fermented berries solution (10 µg/mL). Moreover, treatment with Pushgay berries for 72 h (10 µg/mL) promotes cells growth in RAW 264.7, and only fermented Pushgay berries increase the expression of iNOS in the same cell line. Taken together, our results show that LAB fermentation of Pushgay berries enhances their antioxidant and immunomodulatory properties.     

Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds

The synthesis of several series of imidazo[2,1-a]isoindol-5-ol derivatives and the results of their evaluation against Plasmodium falciparum are presented and discussed. The effects of electron-withdrawing or-donating substituents on different parts of the molecule, as well as those produced by the incorporation of an additional fused ring, were analyzed. Several compounds showed significant antimalarial activity in vitro with IC₅₀ values as low as 60 nM and a certain efficacy in vivo by reducing parasitemia in Plasmodium berghei mouse models.     

Daily polyphenol intake from fresh fruits in Portugal: contribution from berry fruits

Abstract

Fresh fruits, particularly berries, are rich in polyphenols. These bioactive compounds are important in the prevention of chronic inflammatory diseases. The present study aimed to assess polyphenol intake from fresh fruit in Portugal and the relative contribution of berries to overall intake, using an online semi quantitative food frequency questionnaire. Consumption of processed berry products was also studied. Mean fresh fruit consumption was 365.6?±?8.2?g/day. Berries accounted for 9% of total fresh fruit intake, from which 80% were due to strawberries. Total polyphenol intake from fresh fruits was 783.9?±?31.7?mg of Gallic Acid Equivalents (GAE) per day, from which 14% were from berries. Within berries, strawberries accounted for 11% of total polyphenol intake, with the other consumed berries accounting for 3% of the total polyphenol intake per day. Main reasons reported for relative low consumption of berries were market availability and price. The most consumed processed berry product was yogurt.     

Krill for human consumption: nutritional value and potential health benefits

The marine crustacean krill (order Euphausiacea) has not been a traditional food in the human diet. Public acceptance of krill for human consumption will depend partly on its nutritive value. The aim of this article is to assess the nutritive value and potential health benefits of krill, an abundant food source with high nutritional value and a variety of compounds relevant to human health. Krill is a rich source of high-quality protein, with the advantage over other animal proteins of being low in fat and a rich source of omega-3 fatty acids. Antioxidant levels in krill are higher than in fish, suggesting benefits against oxidative damage. Finally, the waste generated by the processing of krill into edible products can be developed into value-added products.     

Supervision of community peer counsellors for infant feeding in South Africa: an exploratory qualitative study

Background  

Recent years have seen a re-emergence of community health worker (CHW) interventions, especially in relation to HIV care, and in increasing coverage of child health interventions. Such programmes can be particularly appealing in the face of human resource shortages and fragmented health systems. However, do we know enough about how these interventions function in order to support the investment? While research based on strong quantitative study designs such as randomised controlled trials increasingly document their impact, there has been less empirical analysis of the internal mechanisms through which CHW interventions succeed or fail. Qualitative process evaluations can help fill this gap.