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1.
Daily Consumption of Chocolate Rich in Flavonoids Decreases Cellular Genotoxicity and Improves Biochemical Parameters of Lipid and Glucose Metabolism.
Leyva-Soto, A, Chavez-Santoscoy, RA, Lara-Jacobo, LR, Chavez-Santoscoy, AV, Gonzalez-Cobian, LN
Molecules (Basel, Switzerland). 2018;(9)
Abstract
In recent years, the incidence of atherosclerotic cardiovascular disease, obesity, and diabetes has increased largely worldwide. In the present work, we evaluated the genoprotective effect of the consumption of flavonoids-rich chocolate on 84 young volunteers. Biochemical indicators related to the prevention and treatment of cardiovascular risk and metabolic syndrome were also determined. A randomized, placebo-controlled, double-blind study was performed in the Autonomous University of Baja California. The treatments comprised the daily consumption of either 2 g of dark chocolate containing 70% cocoa, or 2 g of milk chocolate, for 6 months. The total amount of phenolic compounds and flavonoids was determined in both types of chocolate. Anthropometrical and Biochemical parameters were recorded prior to and after the study. The evaluation of the genotoxicity in buccal epithelial cells was performed throughout the duration of the study. Flavonoids from cocoa in dark chocolate significantly prevented DNA damage, and improved the nucleus integrity of cells. This effect could be related to the antioxidant capacity of the dark chocolate that decreased cellular stress. Biochemical parameters (total cholesterol, triglycerides, and LDL-cholesterol level in blood) and anthropometrical parameters (waist circumference) were improved after six months of daily intake of 2 g of dark chocolate with a 70% of cocoa.
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2.
Experimental and computational modeling of interaction of kolaviron-kolaflavanone with aldehyde dehydrogenase.
Kolawole, AN, Akinladejo, VT, Elekofehinti, OO, Akinmoladun, AC, Kolawole, AO
Bioorganic chemistry. 2018;:68-79
Abstract
Aldehyde dehydrogenases (ALDHs) are a diverse family of enzymes that catalyze the NAD(P)+-dependent detoxification of toxic aldehyde compounds. ALDHs are also involved in non-enzymatic ligand binding to endobiotics and xenobiotics. Here, the enzyme crucial non-canonical and non-catalytic interaction with kolaflavanone, a component of kolaviron, and a major bioflavonoid isolated from Garcinia kola (Bitter kola) was characterized by various spectroscopic and in silico approaches under simulated physiological condition. Kolaflavanone quenched the intrinsic fluorescence of ALDH in a concentration dependent manner with an effective quenching constant (Ksv) of 1.14 × 103 L.mol-1 at 25 °C. The enzyme has one binding site for kolaflavanone with a binding constant (Ka) of 2.57 × 104 L.mol-1 and effective Forster resonance energy transfer (FRET) of 4.87 nm. The bonding process was enthalpically driven. The reaction was not spontaneous and was predominantly characterized by Van der Waals forces and hydrogen bond. The flavonoid bonding slightly perturbed the secondary and tertiary structures of ALDH that was 'tryptophan-gated'. The interaction was regulated by both diffusion and ionic strength. Molecular docking showed the binding of kolaflavanone was at the active site of ALDH and the participation of some amino acid residues in the complex formation with -9.6 kcal mol-1 binding energy. The profiles of atomic fluctuations indicated the rigidity of the ligand-binding site during the simulation. With these, ALDH as a subtle nano-particle determinant of kolaviron bioavailability and efficacy is hereby proposed.
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3.
Comparison of Flavonoids and Centella asiatica for the treatment of chronic anal fissure. A randomized clinical trial.
Chiaretti, M, Fegatelli, DA, Ceccarelli, G, Carru, GA, Pappalardo, G, Chiaretti, AI
Annali italiani di chirurgia. 2018;:330-336
Abstract
AIMS: We aim to test and compare the effects of Flavonoids (Fs) and Centella asiatica (Ca), and the traditional treatment to find out which best deals with healing time, bleeding and pain in the treatment of chronic Anal Fissure (AF). Materials of Study: 98 outpatients were divided randomly into treated (either Fs or Ca) and control group. The control group (Group C, n=32) received the traditional treatment along with the other two subgroups which were treated, additionally, with Fs (Group A, n=30) or Ca (Group B, n=36). Patients were observed once weekly over 8 consecutive weeks. RESULTS The median time to stop bleeding in the group A was 1 week, in the Group B was 3 weeks and in the group C was 4 weeks. There were significant differences between Groups in terms of time to end bleeding (A vs B: p-value= 0.022; A vs C: p-value<0.001; B vs C: p-value=0.070). As for pain score from baseline to the 2nd week were statistically different between Groups A and B on the one hand and Group C on the other hand (A vs C: p-value=0.004; B vs C: p-value 0.035). All patients healed within 8th week. DISCUSSION Either patients treated with Fs or Ca experienced early pain disappearance. Fs and Ca did not show side effects CONCLUSIONS The treatment with Fs is the most effective for bleeding. Patients additionally treated with either Fs or Ca experienced an earlier healing and disappearance of pain in comparison with patients underwent to the traditional treatment. KEY WORDS Anal bleeding, Anal fissure, Defecation pain.
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4.
Curcumin and fisetin internalization into Saccharomyces cerevisiae cells via osmoporation: impact of multiple osmotic treatments on the process efficiency.
Medeiros, FGM, Correia, RTP, Dupont, S, Beney, L, Pedrini, MRS
Letters in applied microbiology. 2018;(4):363-369
Abstract
UNLABELLED Cell osmoporation is a simple and straightforward procedure of creating food-grade biocapsules. This study proposes a new protocol of sequential cell osmoporation stages and evaluates its impact on the efficiency of curcumin and fisetin internalization into Saccharomyces cerevisiae cells. To the best of our knowledge, this is the first report in the literature regarding the subject. To assess how multiple osmoporation stages influence the encapsulation efficiency (% EE), encapsulated amount of curcumin (IC) and fisetin (IF) into S. cerevisiae cells and cell viability, the residual supernatant was used for the subsequent encapsulation stages and viability was assessed by the CFU method. Quantification was carried through direct extraction, using an ultrasonic bath and UV-Vis spectrophotometry. Experimental data demonstrated that the addition of a second osmoporation stage increases both the EE (% EE) and the amount of encapsulated curcumin and fisetin (IC and IF). As a result, the EE was considerably improved and the obtained microcapsules contained a higher amount of the targeted bioactive compounds in its internal structure. However, adding a third osmoporation stage proved to less beneficial to the process efficiency due to its lower yield and the significant negative impact to cell viability. SIGNIFICANCE AND IMPACT OF THE STUDY For the first time in the literature, a protocol of serial osmoporation stages to enhance the encapsulation efficiency of hydrophobic low molecular weight molecules (curcumin and fisetin) into Saccharomyces cerevisiae cells was determined. By increasing overall efficiency, this protocol empowers the encapsulation process and creates a rational way to reduce waste for future industrial osmoporation applications.
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5.
Flavonoids in the Treatment of Alzheimer's and Other Neurodegenerative Diseases.
Airoldi, C, La Ferla, B, D Orazio, G, Ciaramelli, C, Palmioli, A
Current medicinal chemistry. 2018;(27):3228-3246
Abstract
Flavonoids are phytochemicals present in almost all terrestrial plants and, as a consequence, in plant-based foods, and thus consumed by humans through diet. Recent evidences suggest that several flavonoids have positive effects against dementia and Alzheimer's disease, reversing age-related declines in neurocognitive performances. In this review, we provide a general classification of natural and synthetic flavonoids, a description of their physico-chemical properties, in particular their redox properties and stability, and an extensive overview about their biological activities and structure-activity relationship in the field of neurodegenerative diseases. In addition, a section will be dedicated to the synthetic strategies for the preparation of bioactive derivatives. This information will be essential for the design and development of new drugs that can improve brain functions.
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6.
LC-ESI-MS/MS profiling of phenolics in the leaves of Eleutherococcus senticosus cultivated in the West Europe and anti-hyaluronidase and anti-acetylcholinestarase activities.
Kuźniewski, R, Załuski, D, Olech, M, Banaszczak, P, Nowak, R
Natural product research. 2018;(4):448-452
Abstract
Neither secondary metabolites of the spring leaves nor the autumn leaves of Eleutherococcus senticosus species cultivated in Poland, or the bioactivity are known. The richest in polyphenols was the autumn leaves (171.1 mg/g DE), while in flavonoids the spring leaves (107.9 mg/g DE). Using LC-ESI-MS/MS, protocatechuic acid has been identified as the most abundant compound in the spring and autumn leaves (200 and 70 μg/g DE, respectively). Amongst flavonoids, naringenin 7-O-glucoside occurred in the largest amount (20 and 10 mg/g DE in the spring and autumn leaves, respectively). The autumn leaves inhibited Hyal the strongest (74.3%), comparing to the spring leaves (33%). A weak inhibition was found towards AChE (0.64 and 5.8% for the autumn and spring leaves, respectively). To our best knowledge, no information was available on the phytochemical composition and activity of the leaves of E. senticosus cultivated in Poland.
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7.
[Flavonoids in the treatment of hypertension in geriatric patients].
Gutiérrez-Venegas, G
Revista medica del Instituto Mexicano del Seguro Social. 2018;(Suppl 1):S94-S101
Abstract
BACKGROUND Geriatric patients belong to a group over 65 years old. In general these patients present multiple chronic diseases and impairments with disability, body mass diminished and generalized fatigue. On the other hand, a high percentage of these patients have cardiovascular diseases. For this reason, several studies suggest that associated with drugs treatment consumption of natural products such as flavonoids, contribute to improve the quality of life of geriatric patients. The aim of this work is to review in literature the effect of flavonoids in vascular protection of older adults. RESULTS Literature review indicates that the intake of flavonoids significantly reduces the risk of hypertension and cardiovascular disease. Likewise, its consumption is associated with an improvement in endothelial function, since they act regulating different kinases like protein kinase B, nitric oxide synthase and the consequent synthesis of nitric oxide (NO), which leads to improve vasodilation. Finally, flavonoids also act to regulate the functioning of other kinases, phophodiesterases, ion channels diminishing vascular inflammation. CONCLUSION Foods enriched in polyphenols improve endothelial function by promoting vascular dilation and lowering blood pressure.
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8.
Impact of short-term flavanol supplementation on fasting plasma trimethylamine N-oxide concentrations in obese adults.
Angiletta, CJ, Griffin, LE, Steele, CN, Baer, DJ, Novotny, JA, Davy, KP, Neilson, AP
Food & function. 2018;(10):5350-5361
Abstract
The gut microbiome metabolizes choline and carnitine to release trimethylamine (TMA), which subsequently undergoes hepatic conversion to trimethylamine N-oxide (TMAO). Elevated TMAO levels are associated with cardiovascular disease and all-cause mortality risk. Dietary flavanols modulate the composition and function of the gut microbiome. Therefore, the possibility exists that these compounds could reduce intestinal TMA production and lower circulating TMAO. However, this hypothesis has never been tested in humans. A secondary analysis was performed on blood samples from a clinical study in which obese subjects at risk for insulin resistance consumed tea or cocoa flavanols in a randomized crossover design while consuming a controlled diet. These subjects generally had elevated TMAO levels (∼5 μM) compared to levels previously measured in healthy subjects (∼1 μM). None of the interventions significantly altered TMAO levels. Individual variability for choline and carnitine was relatively low. However, TMAO exhibited somewhat greater inter-individual variability. No differences in mean TMAO concentrations observed across interventions were seen based on separating subjects by glycemic status, body mass index (BMI), race, age, or gender. However, subject minimum and maximum values observed across the interventions appeared to be more strongly associated with glycemic status and age than mean values across interventions, suggesting that average TMAO values over time may be less useful than maximum or minimum values as markers of disease risk. Traditional physiological characteristics do not appear to predict TMAO responsiveness to flavanol interventions. However, African-American subjects appeared less responsive compared to non-Hispanic white subjects for both green tea and high cocoa treatments, and female subjects appeared less responsive than males for the high cocoa treatment. The present results suggest that a short-term flavanol intervention does not generally reduce fasting TMAO levels in subjects with elevated circulating TMAO.
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9.
Effect of fisetin supplementation on inflammatory factors and matrix metalloproteinase enzymes in colorectal cancer patients.
Farsad-Naeimi, A, Alizadeh, M, Esfahani, A, Darvish Aminabad, E
Food & function. 2018;(4):2025-2031
Abstract
A growing body of evidence indicates that inflammation is associated with tumorigenesis, metastasis and chemotherapeutic resistance in patients with colorectal cancer (CRC). Natural flavonoids are promising agents for inflammation-related tumor progression in patients with CRC. This study aimed to assess the efficacy of flavonoid fisetin supplementation on the inflammatory status and matrix metalloproteinase (MMP) levels in these patients. In this double-blind, randomized placebo-controlled clinical trial, 37 CRC patients undergoing chemotherapy were assigned to receive either 100 mg fisetin (n = 18) or placebo (n = 19) for seven consecutive weeks. The supplementation began one week before chemotherapy and continued until the end of the second chemotherapy cycle. Levels of interleukin (IL)-8, IL-10, high-sensitivity C-reactive protein (hs-CRP), MMP-7, and MMP-9 were measured in plasma using ELISA, before and after the intervention. The trial was registered at http://www.irct.ir (code: IRCT2015110511288N9). The participants were 55.59 ± 15.46 years old with 62.16% being male. After the intervention, the plasma levels of IL-8 and hs-CRP reduced significantly in the fisetin group (p < 0.04 and p < 0.01, respectively). Additionally, fisetin supplementation suppressed the values of MMP-7 levels (p < 0.02). However, significant changes were observed only in IL-8 concentrations in the fisetin group when compared with the placebo group (p < 0.03). The changes in the levels of other metabolic factors were not statistically significant. According to the results, fisetin could improve the inflammatory status in CRC patients, suggesting it as a novel complementary antitumor agent for these patients and warranting further studies.
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10.
Rice Protein Matrix Enhances Circulating Levels of Xanthohumol Following Acute Oral Intake of Spent Hops in Humans.
O'Connor, A, Konda, V, Reed, RL, Christensen, JM, Stevens, JF, Contractor, N
Molecular nutrition & food research. 2018;(6):e1700692
Abstract
SCOPE Xanthohumol (XN), a prenylated flavonoid found in hops, exhibits anti-inflammatory and antioxidant properties. However, poor bioavailability may limit therapeutic applications. As food components are known to modulate polyphenol absorption, the objective is to determine whether a protein matrix could enhance the bioavailability of XN post oral consumption in humans. METHODS AND RESULTS This is a randomized, double-blind, crossover study in healthy participants (n = 6) evaluating XN and its major metabolites (isoxanthohumol [IX], 6- and 8-prenylnaringenin [6-PN, 8-PN]) for 6 h following consumption of 12.4 mg of XN delivered via a spent hops-rice protein matrix preparation or a control spent hops preparation. Plasma XN and metabolites are measured by LC-MS/MS. Cmax , Tmax , and area-under-the-curve (AUC) values were determined. Circulating XN and metabolite response to each treatment was not bioequivalent. Plasma concentrations of XN and XN + metabolites (AUC) are greater with consumption of the spent hops-rice protein matrix preparation. CONCLUSION Compared to a standard spent hops powder, a protein-rich spent hops matrix demonstrates enhanced plasma levels of XN and metabolites following acute oral intake.