Modeling Mediated Crossover Acute and Subacute Damage to the Pulmonary System During Systemic (Subcutaneous) Administration of Bleomycin in Mice to Test the Potential Therapeutic Effect of Polyphenols / Modelado del Daño Agudo y Subagudo Cruzado Mediado al Sistema Pulmonar Durante la Infección Sistémica (Subcutánea) de Administración de Bleomicina a Ratones para Probar el Posible Efecto Terapéutico de los Polifenoles

SUMMARY: The potential anti-inflammatory and antifibrotic activity of polyphenolic extracts of blueberry and grape was evaluated in a mouse model of lung damage induced by subcutaneous administration of bleomycin. The results of testing the polyphenolic extracts on two different systemic administration variants of bleomycin (intraperitoneal and subcutaneous) were compared. It was found that regardless of the method of bleomycin administration, indirect cross-acute and subacute damage to the pulmonary system was observed. Both patterns exhibited the same prevalence and severity. The administration of polyphenolic extracts of blueberry and grape to mice resulted in a significant decrease in theseverity of acute and subacute patterns of lung damage, suggesting their protective properties for the microcirculatory bed and a pronounced anti-inflammatory effect.

La potencial actividad antiinflamatoria y antifibrótica de los extractos polifenólicos de arándano y uva se evaluó en un modelo de daño pulmonar en ratón inducido por la administración subcutánea de bleomicina. Se compararon los resultados de las pruebas de los extractos polifenólicos en dos variantes diferentes de administración sistémica de bleomicina (intraperitoneal y subcutánea). Se encontró que, independientemente del método de administración de bleomicina, se observaba daño indirecto cruzado, agudo y subagudo al sistema pulmonar. Ambos patrones exhibieron la misma prevalencia y gravedad. La administración de extractos polifenólicos de arándano y uva a ratones dio como resultado una disminución significativa en la gravedad de los patrones agudos y subagudos de daño pulmonar, lo que sugiere sus propiedades protectoras del lecho micro- circulatorio y un efecto antiinflamatorio pronunciado.

Potential antifibrotic effect of blueberry and grape polyphenol extracts in acute and subacute bleomycin-induced lung tissue injury models in mice / Potencial efecto antifibrótico de los extractos de polifenoles de arándano y uva en modelos de lesión tisular pulmonar aguda y subaguda inducida por bleomicina en ratones

SUMMARY: An experimental morphological and morphometric study of the antifibrotic function of blueberry and grape extracts was carried out on a model of lung injury in mice induced by intraperitoneal administration of bleomycin. During intraperitoneal administration of bleomycin to mice, acute and subacute damage to the pulmonary system was noted. Both patterns had the same prevalence and severity. The administration of polyphenolic extracts of blueberry and grape to mice showed a significant reduction in the severity of the acute and subacute pattern of lung injury. Blueberry and grape extracts reduce the acute phase of damage to the microvasculature, enhance phagocytic function, have an anti-inflammatory effect, reducing the degree of lymphohistiocytic infiltration and locoregional foci of residual inflammatory effects.

Se realizó un estudio experimental morfológico y morfométrico de la función antifibrótica de extractos de arándano y uva en un modelo de lesión pulmonar en ratones inducida por la administración intraperitoneal de bleomicina. Durante la administración intraperitoneal de bleomicina a ratones, se observaron daños agudos y subagudos en el sistema pulmonar. Ambos patrones tuvieron la misma prevalencia y severidad. La administración de extractos polifenólicos de arándano y uva a ratones mostró una reducción significativa en la severidad del patrón agudo y subagudo de lesión pulmonar. Los extractos de arándano y uva reducen la fase aguda del daño a la microvasculatura, mejoran la función fagocítica, tienen un efecto antiinflamatorio, reducen el grado de infiltración linfohistiocítica y los focos locorregionales de efectos inflamatorios residuales.

Polyphenol-Rich Beverage Consumption Affecting Parameters of the Lipid Metabolism in Healthy Subjects.

Polyphenols are a diverse and widely distributed class of secondary metabolites, which possess numerous beneficial properties including a modulation of glucose and lipid metabolism. This placebo-controlled human intervention study was performed to explore effects of polyphenol-rich beverage (PRB) uptake on lipid metabolism, as well as DNA integrity. In this case, 36 healthy men were randomly divided to consume either 750 mL of a PRB (containing 51% chokeberry, cranberry, and pomegranate) or a placebo drink daily for eight weeks. Only PRB consumption was found to decrease fat and protein intakes significantly compared to the preceding one-week washout period. During the intervention with PRB an increased fat-free mass was shown after four weeks, whereas a significant elevation in body weight and leptin was observed in placebo group. Blood lipids were not significantly altered after PRB consumption, while triglyceride levels increased after placebo drink intake. In platelets, a significant inhibition of phosphodiesterase (PDE) activity was observed, more pronounced in test group. Consuming the PRB decreased total DNA strand breaks in whole blood as well as H2O2-induced breaks in isolated lymphocytes. Overall, our study suggested beneficial effects on lipid metabolism by reduced energy intake, modulation of biomarkers such as PDE activity and improved DNA integrity associated with PRB consumption.

Coordination-Driven Metal-Polyphenolic Nanoparticles toward Effective Anticancer Therapy.

Stabilization of bioactive components, especially for hydrophobic functional factors, is a promising approach for improving their biological activity. Here, a metal-phenolic coordination chemistry that synthesizes biocompatible and biodegradable thin film based on tannic acid and trivalent metal ion (Fe3+ or Al3+ ) is addressed, and the results also demonstrate its use for encapsulating a hydrophobic drug (nobiletin) and triggering drug release for cancer treatment both in vitro and in vivo. This assembled system provides drug-loaded nanoparticles (NPs) with small, but uniform, size (≈200 nm). It displays beneficial potential in enhancing colloidal stability and preventing premature drug leakage. Moreover, the metal-phenolic coating is found to possess high cell biocompatibility as a delivery vector for controlled drug delivery, while the final fabricated drug NPs have effective anti-tumor activity by both inducing higher tumor apoptosis and inhibiting tumor metastasis, which is superior to naked drug formulations. Overall, these findings propose an effective and straightforward way for coating hydrophobic drugs employing interfacial adhesion and assembly, which can be a highly promising vehicle for controlled-release biomedical applications for cancer therapy.

Ingesta de polifenoles y riesgo cardiovascular en el ensayo PREDIMED-Plus. Una comparación de diferentes ecuaciones de riesgo / Polyphenol intake and cardiovascular risk in the PREDIMED-Plus trial. A comparison of different risk equations

Introducción y objetivos: La cuantificación del riesgo cardiovascular se basa en puntuaciones como las de Framingham, Framingham-REGICOR, SCORE o Life's Simple 7 (LS7). Los polifenoles pueden proporcionar beneficios al sistema vascular y reducir la respuesta inflamatoria; sin embargo, los estudios clínico-epidemiológicos muestran resultados discordantes. Nuestro objetivo es evaluar la posible asociación entre la ingesta de diferentes clases de polifenoles y las puntuaciones cardiovasculares. Métodos: Estudio transversal sobre 6.633 participantes del estudio PREDIMED-Plus. El contenido de polifenoles se estimó mediante un cuestionario semicuantitativo de frecuencia alimentaria y se ajustó por la ingesta energética total según el método de residuales. La asociación entre la ingesta de polifenoles y el riesgo cardiovascular se evaluó mediante análisis de regresión lineal. Resultados: La ingesta total de polifenoles y flavonoides se asoció directa y significativamente con la escala LS7. Igualmente, los lignanos se asociaron directa y significativamente con las escalas SCORE y LS7; los estilbenos, con la SCORE y los ácidos fenólicos, con las de Framingham y Framingham-REGICOR. La clase «otros polifenoles» se asoció de manera significativa con las escalas de Framingham, SCORE y LS7. En las mujeres, la ingesta de todas las clases de polifenoles, excepto los ácidos fenólicos, mostró una tendencia directa en los resultados de Framingham y Framingham-REGICOR e indirecta con la escala LS7. Conclusiones: Se encontraron asociaciones inversas entre el consumo de la clase «otros polifenoles» y, especialmente en las mujeres, el riesgo cardiovascular estimado. Los resultados fueron similares con las de Framingham, Framingham-REGICOR y LS7 (después de eliminar el componente de dieta) y diferentes con la SCORE, pero los predictores que se incluyen en este son escasos (AU)

Introduction and objectives: Quantification of cardiovascular risk has been based on scores such as Framingham, Framingham-REGICOR, SCORE or Life's Simple 7 (LS7). In vitro, animal, and randomized clinical studies have shown that polyphenols may provide benefits to the vascular system and reduce the inflammatory response. However, some clinical-epidemiological studies have yielded inconsistent results. Our aim was to assess the possible association between intake of the various polyphenol classes and established cardiovascular scores. Methods: This cross-sectional analysis involved 6633 PREDIMED-Plus study participants. Food polyphenol content was estimated by a semiquantitative food frequency questionnaire, adjusted for total energy intake according to the residual method. The association between polyphenol intake and cardiovascular risk was tested using linear regression analyses. Results: Total polyphenol and flavonoid intake were directly and significantly associated only with the LS7 scale. Intake of lignans was directly and significantly associated with SCORE and LS7 scales, stilbene intake with SCORE, and phenolic acid intake with Framingham and Framingham-REGICOR scores. Other polyphenol classes were associated in a protective and significant manner in Framingham, SCORE and LS7 scores. In women, intake of all the polyphenol classes, except phenolic acids, showed a protective trend in the results of the Framingham, Framingham-REGICOR scores and LS7 scale. Conclusions: An inverse association was found between consumption of the ‘other polyphenols’ class and, especially among women, with estimated cardiovascular risk. The results were similar to those of Framingham, Framingham-REGICOR and LS7 (after eliminating the diet component) and differed from those of SCORE, but the predictors included were limited in the latter case (AU)

Alleviation effects of Rubus coreanus Miquel root extract on skin symptoms and inflammation in chronic atopic dermatitis.

Atopic dermatitis (AD) is an inflammatory skin disease characterized by chronic inflammatory dermatitis with immunological manifestations. The aim of this study was to investigate the effects of polyphenol-containing Rubus coreanus Miquel root extract on skin allergy and AD. The protective effects of R. coreanus root ethanol extract against AD were investigated using the human keratinocyte cell line HaCaT, human mast cell line HMC-1, and the 2,4-dinitrochlorobenzene (DNCB)-induced AD-like skin NC/Nga mouse model. Treatment with R. coreanus root ethanol extracts reduced ß-hexosaminidase and histamine release from HMC-1 cells stimulated with compound 48/80 compared to treatment with R. coreanus fruit ethanol extract. Furthermore, topical application of R. coreanus root ethanol extract dramatically reduced the severity of skin symptoms and the thickening and swelling of the dorsal skin and ear in DNCB-treated NC/Nga mice. The protein and mRNA expression of several cytokines (IL-4, IL-5, IL-12, IFN-γ, TNF-α, and TARC) and IgE was significantly lowered upon application of the R. coreanus root ethanol extract. The promising candidate for the active ingredient of R. coreanus root polyphenols was revealed to be ellagic acid. These findings clearly indicate that the R. coreanus root polyphenols show strong anti-allergic effects and suppress the symptoms of AD. Therefore, polyphenol-containing R. coreanus root ethanol extract could be a novel therapeutic candidate for the treatment of allergy and AD.

Solid Lipid Nanoparticles Administering Antioxidant Grape Seed-Derived Polyphenol Compounds: A Potential Application in Aquaculture.

The supply of nutrients, such as antioxidant agents, to fish cells still represents a challenge in aquaculture. In this context, we investigated solid lipid nanoparticles (SLN) composed of a combination of Gelucire® 50/13 and Precirol® ATO5 to administer a grape seed extract (GSE) mixture containing several antioxidant compounds. The combination of the two lipids for the SLN formation resulted in colloids exhibiting mean particle sizes in the range 139-283 nm and zeta potential values in the range +25.6-43.4 mV. Raman spectra and X-ray diffraction evidenced structural differences between the free GSE and GSE-loaded SLN, leading to the conclusion that GSE alters the structure of the lipid nanocarriers. From a biological viewpoint, cell lines from gilthead seabream and European sea bass were exposed to different concentrations of GSE-SLN for 24 h. In general, at appropriate concentrations, GSE-SLN increased the viability of the fish cells. Furthermore, regarding the gene expression in those cells, the expression of antioxidant genes was upregulated, whereas the expression of hsp70 and other genes related to the cytoskeleton was downregulated. Hence, an SLN formulation containing Gelucire® 50/13/Precirol® ATO5 and GSE may represent a compelling platform for improving the viability and antioxidant properties of fish cells.

Polyphenols extracted from Enteromorpha clathrata alleviates inflammation in lipopolysaccharide-induced RAW 264.7 cells by inhibiting the MAPKs/NF-κB signaling pathways.

ETHNOPHARMACOLOGY RELEVANCE: Enteromorpha has long been recorded in traditional Chinese medicine, with cholesterol-lowering, anti-cancer, anti-inflammatory and antibacterial effects. Recently, we extracted the polyphenol-enriched fraction from Enteromorpha clathrata (E. clathrata) by ethyl acetate (ECPs), and isolated six individual polyphenols from ECPs via high-speed counter-current chromatography (HSCCC) with high-performance liquid chromatography (HPLC). AIM OF THE STUDY: In this study, we explored the anti-inflammatory activity and underlying mechanism of ECPs in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. MATERIALS AND METHODS: ECPs and the six polyphenols were used for nitric oxide (NO) assay to identify the components with potent inflammation inhibitory effect. Enzyme-linked immunosorbent assay (ELISA), quantitative real-time PCR (qPCR), flow cytometry, and Western blot analysis were applied to further investigate their anti-inflammatory effects and underlying mechanism in LPS-stimulated RAW264.7 cells. RESULTS: ECPs and the three individual polyphenols, including (-)-epicatechin, epigallocatechin-3-O-gallate and (-)-epicatechin-3-O-gallate, showed in vitro immunosuppressive activity by altering the cell biology at the gene, protein and functional levels in a dose- and species-dependent manner. Their anti-inflammatory effects were achieved by inhibiting LPS-induced production of nitric oxide and its upstream enzyme inducible nitric oxide synthase (iNOS), the pro-inflammatory cytokines including interleukin-1 beta (IL-1ß), interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α), as well as the phagocytotic capacity, without cytotoxicity. The mechanism study further revealed that these anti-inflammatory properties were, at least partly, attributed to the suppressed activation of nuclear factor-κB (NF-κB) and p38 mitogen-activated protein kinase (MAPK) signaling pathways. CONCLUSIONS: These findings indicated for the first time the correlation between the anti-inflammatory activity of ECPs and NF-κB and MAPK signaling pathways, suggesting that polyphenol-enriched organic fraction of E. clathrata could be potential candidate as therapeutic agent for treating inflammatory diseases.

Grape seed polyphenol extract and cognitive function in healthy young adults: a randomised, placebo-controlled, parallel-groups acute-on-chronic trial.

Grapes are polyphenol-rich, and grape juice intake has shown cognitive benefits in middle-aged females and older adults with mild cognitive impairment. Extracts obtained from grape seeds have similarly been associated with cognitive benefits in older adults. The aim of this research was to investigate whether a highly purified grape seed-derived polyphenol extract was associated with cognitive benefits in healthy young adults following a single acute dose, and chronically following repeated daily dosage over 12 weeks. Following an acute-on-chronic, parallel groups, randomised, double-blind, placebo-controlled design, sixty adults aged 18-30 consumed either a 400 mg grape seed polyphenol extract (GSPE, n = 30) or a placebo (n = 30). Cognitive function was assessed acutely at baseline and 2, 4 and 6 h post consumption, and chronically at 6 and 12 twelve weeks with a computerised battery of multiple cognitive tests. Mood was assessed with the Positive and Negative Affect Schedule. Linear marginal model analysis with baseline included as a covariate did not reveal a consistent pattern of cognitive benefits following the GSPE relative to the placebo either acutely or chronically when considering all outcome measures. GSPE was associated with some improvements in reaction time (acutely) and psychomotor skill (chronically), however the placebo was also associated with some benefits to reaction time and memory. Therefore, a 400 mg GSPE did not consistently improve cognitive function in healthy young adults. These findings suggest that younger, healthy populations are perhaps less sensitive to polyphenol extract doses <400mg relative to older, or cognitively compromised populations.

A Bioactive Extract Rich in Triterpenic Acid and Polyphenols from Olea europaea Promotes Systemic Immunity and Protects Atlantic Salmon Smolts Against Furunculosis.

In the present study, the modulation of the transcriptional immune response (microarray analysis) in the head kidney (HK) of the anadromous fish Atlantic salmon (Salmo salar) fed a diet supplemented with an olive fruit extract (AQUOLIVE®) was evaluated. At the end of the trial (133 days), in order to investigate the immunomodulatory properties of the phytogenic tested against a bacterial infection, an in vivo challenge with Aeromonas salmonicida was performed. A total number of 1,027 differentially expressed genes (DEGs) (805 up- and 222 downregulated) were found when comparing the transcriptomic profiling of the HK from fish fed the control and AQUOLIVE® diets. The HK transcripteractome revealed an expression profile that mainly favored biological processes related to immunity. Particularly, the signaling of i-kappa B kinase/NF-kappa and the activation of leukocytes, such as granulocytes and neutrophils degranulation, were suggested to be the primary actors of the innate immune response promoted by the tested functional feed additive in the HK. Moreover, the bacterial challenge with A. salmonicida that lasted 12 days showed that the cumulative survival was higher in fish fed the AQUOLIVE® diet (96.9 ± 6.4%) than the control group (60.7 ± 13.5%). These results indicate that the dietary supplementation of AQUOLIVE® at the level of 0.15% enhanced the systemic immune response and reduced the A. salmonicida cumulative mortality in Atlantic salmon smolts.

Catechins, theaflavins and ginger freeze-dried extract based functional drink significantly mitigate the hepatic, diabetic and lipid abnormalities in rat model.

The Current study was planned to explore the therapeutic potential of green tea, black tea and ginger based nutraceuticals (catechins, theaflavins and ginger freeze dried extract) against obesity, diabetes and renal malfunctioning. Bioevaluation study was carried out by involving 250 male Sprague Dawley rats. Accordingly, three types of studies were conducted on the basis of different diets i.e. study I (Hyperglycemic rats), study II (obese rats), study III (liver malfunctional rats) each study comprised of five groups of rats ten in each (Sample size according to power analysis) were provided the five types of drinks i.e. control, theaflavin enriched, catechins enriched, ginger extract supplemented and combination of catechins, theaflavins and ginger extract were given to the representative groups. Results showed that the body weight of rats effected significantly with functional drinks in all studies. However, catechin enriched drink (T1) resulted maximum reduction in weight during the entire study. Similarly, T2 exerted maximum decline in cholesterol level during study I, II and III by 11.03 & 10.63, 7.62 & 8.05 and 5.99 & 6.01% whereas LDL by 14.25 & 15.10, 10.45 & 12.10 and 7.25 & 8.01%, respectively (trial 1 & 2). The attenuation in serum glucose and enhancement in insulin level of rats are the indicators for the positive impact of black tea functional drinks. In this context, Catechins+theaflavins+GFD enriched drink (T4) Showed better performance than rest and caused 8.82 & 9.77, 11.03 & 12.23 and 5.83 & 5.96% reduction in glucose. Moreover, the T4 significantly improved the liver and antioxidant enzymes. Accordingly, T4 was proved effective for glutathione enhancement whilst T2 alleviated TBARS efficiently during the investigation. The normal ranges of renal function tests and hematological aspects proved the safety of resultant drinks. From the current exploration, it is concluded that drinks supplemented with theaflavin and catechins & GFD are effectual to mitigate lifestyle related malfunctioning.

Polyphenol rich extracts of Geranium L. species as potential natural antioxidant and antimicrobial agents.

OBJECTIVE: Plants and plant extracts are of great scientific interest due to the chemical diversity and pharmacological properties of present bioactive molecules. The Geranium L. species are widely used in ethnomedicine. In the current study, the total phenolic and tannin content, antioxidant and antimicrobial activity of methanol extracts of eight Geranium species were investigated. MATERIALS AND METHODS: The total phenolic and tannin content were determined by the FC method. Antioxidant capacity was evaluated in FRAP, DPPH, and biochemical assays, while antimicrobial activity was examined using the broth microdilution method. RESULTS: The high total phenolic (170.64-636.32 mg GAE/g dry extract) and tannin content (37.80-414.02 mg GAE/g DE), along with significant total antioxidant (FRAP values 1.13-8.80 mmol Fe2+/g) and DPPH radical scavenging activity (SC50 values 4.24-34.52 µg/mL) were observed. The prominent antioxidant capacity was confirmed in biochemical assays (OS values -1.47 - -13.02). The extracts exhibited significant antimicrobial activity against ATTC strains (MICs dominantly in the range of 12.5-200 µg/mL) as well as against clinical isolates of E. coli (MICs mostly 50 and 100 µg/mL). The pronounced antioxidant and antimicrobial activity can be due to the high phenolic content, particularly due to the presence of hydrolyzable tannins. CONCLUSIONS: Based on the high content of polyphenols, pronounced antioxidant and antimicrobial activities, the examined extracts are promising natural antioxidant and antimicrobial agents with the potential medicinal purpose and use as a functional food.

Polyphenol containing Sargassum horneri attenuated Th2 differentiation in splenocytes of ovalbumin-sensitised mice: involvement of the transcription factors GATA3/STAT5/NLRP3 in Th2 polarization.

CONTEXT: Sargassum horneri (Turner) C. Agardh (Sargassaceae) is a brown marine alga used in oriental medicine to treat allergic conditions. OBJECTIVE: This study clarifies the effect of polyphenol-containing S. horneri ethanol extract (SHE) on T-helper type-2 (Th2) polarisation. MATERIALS AND METHODS: All mice (BALB/c mice, n = 12) except in the healthy control group were first sensitised with an intraperitoneal injection of ovalbumin (OVA; 20 µg) and alum (2 mg) on Day 0 and Day 14. Similarly, phosphate-buffered saline (PBS) was injected according to the same schedule into the healthy control mice. After the final administration, splenocytes were obtained. OVA sensitised mice were challenged with OVA (100 µg/mL) in the absence or presence (62.5 and 125 µg/mL) of SHE while healthy control group remained untreated. RESULTS: SHE (0-1000 µg/mL) was not cytotoxic to splenocytes and demonstrated IC50 values of 3.27 and 3.92 mg/mL, respectively, at 24 and 48 h of incubation. SHE suppressed cell proliferation at concentrations ≥62.5 µg/mL. SHE treatment (125 µg/mL) subdued (by 1.8-fold) the population expansion of CD3+CD4+ helper T cells induced by OVA challenge. SHE attenuated the OVA-induced activation of respective transcription factors GATA3 and NLRP3. Simultaneously, highly elevated levels of cytokines interleukin (IL)-4 and IL-5 caused by OVA stimulation were removed completely and IL-13 suppressed by 1.5-fold. CONCLUSIONS: SHE exhibits Th2 immune suppression under OVA stimulation via GATA3- and NLRP3-dependent IL-4, IL-5, and IL-13 suppression. Therefore, SHE could be therapeutically useful for alleviating the symptoms of allergen-mediated immune diseases.

Circulating Structurally Related (-)-Epicatechin Metabolite Species and Levels after Sustained Intake of a Cocoa Powder High in Polyphenols Are Comparable to Those Achieved after a Single Dose.

BACKGROUND: While the bioavailability of cocoa polyphenols, particularly of the monomer (-)-epicatechin, has been investigated after a single-dose intake, the effect of sustained cocoa consumption on the metabolic profile of the structurally related (-)-epicatechin metabolites (SREMs) has not been investigated. METHODS: A randomized, controlled crossover clinical trial in healthy young adults (18-40 year) was conducted to evaluate SREMs after consumption of a single-dose and after daily consumption of 1.3 g of polyphenol-rich cocoa powder for 28 days. The circulating SREMs were measured by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). RESULTS: Twenty subjects (eleven males and nine females) were enrolled. The SREMs concentrations increased to 1741 ± 337 nM after a single-dose and to 1445 ± 270 nM after sustained supplementation. Sulfate conjugates showed higher levels in females (p < 0.05). The epicatechin-3'-glucuronide (E3'G) and epicatechin-3'-sulfate (E3'S) were the most abundant metabolites in all subjects. A high intra-individual correlation (r = 0.72, p < 0.001) between SREMs concentrations after single-dose and sustained supplementation was observed. The antioxidant capacity of plasma did not change in response to the intervention and was not correlated with any of the SREMs. CONCLUSION: The individual SREMs profile and concentrations after a 28-day supplementation are comparable to those after a single dose.

The Zebrafish Embryo as a Model to Test Protective Effects of Food Antioxidant Compounds.

The antioxidant activity of food compounds is one of the properties generating the most interest, due to its health benefits and correlation with the prevention of chronic disease. This activity is usually measured using in vitro assays, which cannot predict in vivo effects or mechanisms of action. The objective of this study was to evaluate the in vivo protective effects of six phenolic compounds (naringenin, apigenin, rutin, oleuropein, chlorogenic acid, and curcumin) and three carotenoids (lycopene B, ß-carotene, and astaxanthin) naturally present in foods using a zebrafish embryo model. The zebrafish embryo was pretreated with each of the nine antioxidant compounds and then exposed to tert-butyl hydroperoxide (tBOOH), a known inducer of oxidative stress in zebrafish. Significant differences were determined by comparing the concentration-response of the tBOOH induced lethality and dysmorphogenesis against the pretreated embryos with the antioxidant compounds. A protective effect of each compound, except ß-carotene, against oxidative-stress-induced lethality was found. Furthermore, apigenin, rutin, and curcumin also showed protective effects against dysmorphogenesis. On the other hand, ß-carotene exhibited increased lethality and dysmorphogenesis compared to the tBOOH treatment alone.

Cissus subtetragona Planch. Ameliorates Inflammatory Responses in LPS-induced Macrophages, HCl/EtOH-induced Gastritis, and LPS-induced Lung Injury via Attenuation of Src and TAK1.

Several Cissus species have been used and reported to possess medicinal benefits. However, the anti-inflammatory mechanisms of Cissus subtetragona have not been described. In this study, we examined the potential anti-inflammatory effects of C. subtetragona ethanol extract (Cs-EE) in vitro and in vivo, and investigated its molecular mechanism as well as its flavonoid content. Lipopolysaccharide (LPS)-induced macrophage-like RAW264.7 cells and primary macrophages as well as LPS-induced acute lung injury (ALI) and HCl/EtOH-induced acute gastritis mouse models were utilized. Luciferase assays, immunoblotting analyses, overexpression strategies, and cellular thermal shift assay (CETSA) were performed to identify the molecular mechanisms and targets of Cs-EE. Cs-EE concentration-dependently reduced the secretion of NO and PGE2, inhibited the expression of inflammation-related cytokines in LPS-induced RAW264.7 cells, and decreased NF-κB- and AP-1-luciferase activity. Subsequently, we determined that Cs-EE decreased the phosphorylation events of NF-κB and AP-1 pathways. Cs-EE treatment also significantly ameliorated the inflammatory symptoms of HCl/EtOH-induced acute gastritis and LPS-induced ALI mouse models. Overexpression of HA-Src and HA-TAK1 along with CETSA experiments validated that inhibited inflammatory responses are the outcome of attenuation of Src and TAK1 activation. Taken together, these findings suggest that Cs-EE could be utilized as an anti-inflammatory remedy especially targeting against gastritis and acute lung injury by attenuating the activities of Src and TAK1.

Regular, but not acute, green tea supplementation increases total antioxidant status and reduces exercise-induced oxidative stress: a systematic review.

This systematic review aims to investigate the effects of green tea supplementation on exercise-induced oxidative stress. Four electronic databases were searched from inception to December 2020: SPORTDiscuss, PubMed, Scopus, and Web of Science. The search strategy was established in the following manner: (green tea) (Title/Abstract) AND (exercise OR training) (Title/Abstract) AND (oxidative stress OR antioxidant OR oxidation) (Title). After the application of inclusion and exclusion criteria 11, randomized or non-randomized control trials were included, 6 with a parallel design and 5 with a crossover design. Study methodological quality was assessed with the PEDro scale, and all studies were considered of moderate quality. Overall, acute green tea ingestion does not appear to influence antioxidant status or reduce exercise-induced oxidative stress. In contrast, green tea supplementation before exercise, for periods of more than 1 week, in a dose range of 400 to 800 mg of catechins per day, appears to be efficacious to increase total antioxidant status and protect cells against exercise-induced oxidative stress. Future investigations should focus on beginning green tea supplementation more than 7 days before exercise and completing it 2 or 3 days after while monitoring the change of markers of oxidative stress up to 48-72 h after exercise.

Effect of Decaffeinated Green Tea Polyphenols on Body Fat and Precocious Puberty in Obese Girls: A Randomized Controlled Trial.

Background: Obesity has been reported to be an important contributing factor for precocious puberty, especially in girls. The effect of green tea polyphenols on weight reduction in adult population has been shown, but few related studies have been conducted in children. This study was performed to examine the effectiveness and safety of decaffeinated green tea polyphenols (DGTP) on ameliorating obesity and early sexual development in girls with obesity. Design: This is a double-blinded randomized controlled trial. Girls with obesity aged 6-10 years old were randomly assigned to receive 400 mg/day DGTP or isodose placebo orally for 12 weeks. During this period, all participants received the same instruction on diet and exercise from trained dietitians. Anthropometric measurements, secondary sexual characteristics, B-scan ultrasonography of uterus, ovaries and breast tissues, and related biochemical parameters were examined and assessed pre- and post-treatment. Results: Between August 2018 and January 2020, 62 girls with obesity (DGTP group n = 31, control group n = 31) completed the intervention and were included in analysis. After the intervention, body mass index, waist circumference, and waist-to-hip ratio significantly decreased in both groups, but the percentage of body fat (PBF), serum uric acid (UA), and the volumes of ovaries decreased significantly only within the DGTP group. After controlling confounders, DGTP showed a significantly decreased effect on the change of PBF (ß = 2.932, 95% CI: 0.214 to 5.650), serum UA (ß = 52.601, 95% CI: 2.520 to 102.681), and ovarian volumes (right: ß = 1.881, 95% CI: 0.062 to 3.699, left: ß = 0.971, 95% CI: 0.019 to 1.923) in girls with obesity. No side effect was reported in both groups during the whole period. Conclusion: DGTP have shown beneficial effects of ameliorated obesity and postponed early sexual development in girls with obesity without any adverse effects. Clinical Trial Registration: [https://clinicaltrials.gov/ct2/show/NCT03628937], identifier [NCT03628937].

The Health Effects of Chocolate and Cocoa: A Systematic Review.

Chocolate has a history of human consumption tracing back to 400 AD and is rich in polyphenols such as catechins, anthocyanidins, and pro anthocyanidins. As chocolate and cocoa product consumption, along with interest in them as functional foods, increases worldwide, there is a need to systematically and critically appraise the available clinical evidence on their health effects. A systematic search was conducted on electronic databases such as MEDLINE, EMBASE, and Cochrane Central Register of Controlled Trials (CENTRAL) using a search strategy and keywords. Among the many health effects assessed on several outcomes (including skin, cardiovascular, anthropometric, cognitive, and quality of life), we found that compared to controls, chocolate or cocoa product consumption significantly improved lipid profiles (triglycerides), while the effects of chocolate on all other outcome parameters were not significantly different. In conclusion, low-to-moderate-quality evidence with short duration of research (majority 4-6 weeks) showed no significant difference between the effects of chocolate and control groups on parameters related to skin, blood pressure, lipid profile, cognitive function, anthropometry, blood glucose, and quality of life regardless of form, dose, and duration among healthy individuals. It was generally well accepted by study subjects, with gastrointestinal disturbances and unpalatability being the most reported concerns.

Fungi and Algae as Sources of Medicinal and Other Biologically Active Compounds: A Review.

Many species of fungi including lichenized fungi (lichens) and algae have the ability to biosynthesize biologically active compounds. They produce, among others, polysaccharides with anticancer and immunostimulatory properties: (1) Background: This paper presents the characteristics of the most important bioactive compounds produced by fungi and algae; (2) Methods: Based on the example of the selected species of mushrooms, lichens and algae, the therapeutic properties of the secondary metabolites that they produce and the possibilities of their use are presented; (3) Results: The importance of fungi, especially large-fruited mushrooms, lichens and algae, in nature and human life is discussed, in particular, with regard to their use in the pharmaceutical industry and their nutritional value; (4) Conclusions: The natural organisms, such as fungi, lichenized fungi and algae, could be used as supplementary medicine, in the form of pharmaceutical preparations and food sources. Further advanced studies are required on the pharmacological properties and bioactive compounds of these organisms.