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Novel foods especially formulated and targeted for the elderly population should provide sufficient nutrients and bioactive ingredients to counteract the natural age-related deterioration of various organs and tissues. Dietary protein and phenolic compounds achieve this goal; however, older adults have alterations in their gastrointestinal system that may impact their bioavailability and few studies have been aimed at this population. Since phenolic compounds are the subject of multiple biotransformations by host and microbiome enzymes during the digestion process, identification of their bioavailable forms in human plasma or tissues represents a considerable analytical challenge. In this study, UHPLC-ESI-QTOF/MS-MS, chemometrics, and multivariate statistical methods were used to identify the amino acids and phenolic compounds that were increased in the plasma of elderly adults after a 30-day intervention in which they had consumed an especially formulated muffin and beverage containing Brosimum alicastrum Sw. seed flour. A large interindividual variation was observed regarding the amino acids and phenolic metabolites identified in the plasma samples, before and after the intervention. Three phenolic metabolites were significantly increased in the population after the intervention: protocatechuic acid, 5-(methoxy-4'-hydroxyphenyl) valerolactone, and phloretic acid. These metabolites, as well as others that were not significantly increased (although they did increase in several individuals), are probably the product of the microbiota metabolism of the major phenolic compounds present in the B. alicastrum Sw. seed flour and other food ingredients. A significant decrease in 4-ethyl-phenol, a biomarker of stress, was observed in the samples. Results showed that the incorporation of foods rich in phenolic compounds into the regular diet of older adults contributes to the increase in bioactive compounds in plasma, that could substantially benefit their mental, cardiovascular, and digestive health.
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Using stress elicitors in fruits and vegetables is considered a good strategy to increase the content of bioactive compounds in plant foods. However, bioactive compounds can affect the sensory characteristics of food products, and little is known about their shelf-life stability in fresh produce treated with elicitors. In the present work, carotenoids and polyphenols were quantified by spectrophotometric methods in red and green butterhead lettuce treated with elicitors that had previously been demonstrated to increase bioactive compounds: arachidonic acid (AA), methyl jasmonate (MJ), and Harpin protein (HP). The bioactive compounds were determined immediately and during three weeks after harvest. A descriptive sensory analysis was carried out, which included odor, taste, tactile, and visual attributes of control and elicitor-treated lettuce. Carotenoids showed greater shelf-life stability than polyphenols, and both were more stable in red than in green lettuce during the first two weeks of storage. The best elicitor was MJ, which increased phenolic compounds (red and green lettuce), anthocyanins, and carotenoids (red lettuce) through the storage period. Color intensity, crispness, wettability, and bitter taste were some of the primary sensory attributes in butterhead lettuce and were not affected by any treatment. Other organoleptic properties were also not affected by the elicitors. These results suggest that elicitation could improve the content of bioactive compounds, which is stable through the shelf-life of butterhead lettuce, without any adverse effect on the sensory properties.
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Flavonoids are a diverse group of plant-derived compounds that have been shown to have various health benefits, including anti-inflammatory effects. However, their use in the treatment of inflammatory diseases has been limited due to their low bioavailability. The nanoparticle-mediated delivery of flavonoids has been proposed as a potential solution to this issue, as it allows the sustained release of the flavonoids over time. There are several different nanoparticle systems that have been developed for flavonoid delivery, including polymeric nanoparticles, liposomes, and inorganic nanoparticles. This systematic review aims to evaluate the impact of nanoparticle-mediated delivery of flavonoids on pro-inflammatory cytokine production in various diseases. We analyzed the performance of flavonoid-encapsulated nanoparticles in regulating cytokine production in different in vitro and in vivo studies. To this end, we followed the guidelines of the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) to conduct a comprehensive search of the literature and to assess the quality of the included studies. The results showed that flavonoid-encapsulated nanoparticles significantly downregulated pro-inflammatory cytokines, such as TNF-α, IL-1ß, IL-6, and IL-18. In some cases, this effect was significantly greater than that observed with non-encapsulated flavonoids These findings suggest that nanoparticle-mediated delivery of flavonoids may have potential as a therapeutic approach for the treatment of inflammatory diseases.
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Flavonoides , Nanopartículas , Flavonoides/farmacología , Citocinas , Factor de Necrosis Tumoral alfa , LiposomasRESUMEN
The beneficial health effect of red wine depends on its phenolic content and the phenolic content in red wines is affected by ecological, agricultural, and enological practices. Enriched wines have been proposed as an alternative to increase the phenolic content in wines. Nevertheless, phenolic compounds are related to the sensory characteristics of red wines, so enrichment of red wines requires a balance between phenolic content and sensory characteristics. In the present study, a Merlot red wine was enriched with a phenolic extract obtained from Cabernet Sauvignon grape pomace. Two levels of enrichment were evaluated: 4 and 8 g/L of total phenolic content (gallic acid equivalents, GAE). Wines were evaluated by a trained panel to determine their sensory profile (olfactive, visual, taste, and mouthfeel phases). The bioaccessibility of phenolic compounds from enriched red wines was evaluated using an in vitro digestive model and phenolic compounds were quantified by High Performance Liquid Chromatography coupled to tandem mass spectrometry (HPLC-MS/MS). Enrichment increased mainly flavonols and procyanidins. Such an increase impacted astringency and sweetness perceived by judges. This study proposes an alternative to increase the phenolic content in wines without modifying other main sensory characteristics and offers a potential beneficial effect on the health of consumers.
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Tree nuts are rich in polar (phenolic compounds) and non-polar (tocols) antioxidants, with recognized effects in the prevention of diseases such as cancer. These biomolecules possess antiproliferative activity on cancer cells; however, the combined effect of both types of compounds has been scarcely studied, and this approach could give valuable information on the real anticancer potential of tree nuts. In the present study, the antiproliferative activity of pure tocols and phenolic compounds, tocol- and phenolic-rich extracts (TRE and PRE, respectively) from tree nuts and the extracts combinations, was evaluated in four cancer (HeLa, MCF7, PC3, A549) and one control (ARPE) cell lines. The most sensible cell lines were HeLa and MCF7. TRE and PRE from nuts were chemically characterized; γ and δ tocopherols, total tocols, total tocopherols and total phenolic compounds were negatively correlated with cell viability in MCF7 cells. In HeLa cells, only δ and total tocopherols were negatively correlated with cell viability. TRE and PRE had a low effect in reducing cell viability of the cancer cell lines, the most effective extracts were those of emory oak acorn (EOA), pecan nut (PEC) and walnut (WAL), and these were further studied for their pharmacological interactions, using the combination index and the isobologram methods. Combinations of both extracts showed a synergistic and strongly synergistic behavior in the three nuts (EOA, PEC and WAL), with combination indexes between 0.12 and 0.55. These results highlight the need to understand the interactions among components found in complex natural extracts or food products in order to fully understand their bioactivities.
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Neoplasias , Nueces , Células HeLa , Humanos , Nueces/química , Fenoles/análisis , Fenoles/farmacología , Extractos Vegetales/análisis , Extractos Vegetales/farmacología , Tocoferoles/análisisRESUMEN
Physiological changes in elderly individuals (EI) can contribute to nutritional deterioration and comorbidities that reduce their quality of life. Factors such as diet can modulate some of these effects. The aim was to evaluate the functionality of foods added with Brosimum alicastrum Sw. seed flour in EI. EI (n = 23) living in nursing home conditions agreed to participate. A control stage was carried out (30 days) and subsequently, an intervention stage (30 days) was realized in which a muffin and a beverage, designed for EI, were added to the participants' their usual diet. In both stages, anthropometric parameters, body composition, nutritional status, dietary intake, sarcopenic status, cognitive and affective states, biometric parameters, and total phenolic compounds (TPC), and antioxidant capacity in foods and plasma of EI were determined. The results showed that the consumption of the foods improved the energy intake and preserved the muscle reserves of the EI. The EI gained body weight (+1.1 kg), increased their protein (+18.6 g/day; 1.5 g/kg BW/day), dietary fiber (+13.4 g/day), iron (+4.4 mg/day), zinc (+1.8 mg/day), folic acid (+83.4 µg/day) consumption while reducing their cholesterol (-66 mg/day) and sodium (-319.5 mg/day) consumption. LDL-C lipoproteins reduced (14.8%) and urea (33.1%) and BUN (33.3%) increased. The TPC increased (7.8%) in the plasma, particularly in women (10.7%). The foods improve the EI nutritional status, and this has a cardiovascular protective effect that can benefit the health of the EI.
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Two of the most important Mexican plant-foods are tomato (Solanum lycopersicum L.) and husk tomato (Physalis ixocarpa Brot.). In this study three objectives were followed: i) to evaluate the bioaccessible phenolic compounds (PC) in T and HT during upper gastrointestinal digestion, ii) to in vitro ferment the indigestible fractions of the samples to evaluate the short-chain fatty acids (SCFA) production, iii) the microbial metabolites, bioconverted PC and volatile organic compounds (VOCs) generated during the fermentation. Vanillic acid was the most bioaccessible PC and after 48 h, 3-hydroxyphenylacetic acid was the most abundant microbial metabolite identified in both samples. The identification of VOCs belonging to terpenes (and derivatives) group in T and HT can be product of the microbial metabolism of carotenoids. The study shows new knowledge of the in vitro intestinal digestion and fermentation of T and HT final compounds with biological potential which should be evaluated in further studies.
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Colon/microbiología , Ácidos Grasos Volátiles/metabolismo , Fermentación , Frutas/química , Microbioma Gastrointestinal , Fenoles/metabolismo , Disponibilidad Biológica , Carotenoides/metabolismo , Digestión , Solanum lycopersicum , Fenilacetatos/metabolismo , Physalis , Ácido Vanílico/metabolismo , Compuestos Orgánicos Volátiles/metabolismoRESUMEN
'Kerman' pistachios (KP; Pistacia vera L.) are an important crop for several countries but their commercial value is diminished by their shell dehiscence status and prolonged storage in popular marketplaces. The aim was to evaluate the independent/synergistic effect of prolonged storage (1-4 year) and dehiscence status (split/unsplit) on KP's morphometry and chemical composition. Whole nut's and kernel's length, width, thickness, surface area, and volume were more affected by dehiscence (split > unsplit; p ≤ 0.01) than storage time; Kernel's mass, macronutrient composition and tocopherols (T)/tocotrienols (T3) were not much affected by dehiscence but time-trend correlations were observed with macronutrient composition (split/unsplit; ρ = - 0.57-0.42) and T + T3 (unsplit; ρ = 0.81). Specific/total fatty acids were affected by a complex dehiscence × storage time interaction, and they linearly correlated with certain morphometric characteristics (r ≥ 0.6). Shell dehiscence status more than prolonged storage substantially modifies KP's quality.
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Several studies have related moderate consumption of red wine with prevention of cardiovascular diseases (CVD). According to epidemiological studies, those regions with high consumption of red wine and a Mediterranean diet show a low prevalence of CVD. Such an effect has been attributed to phenolic compounds present in red wines. On the other hand, by-products obtained during winemaking are also a significant source of phenolic compounds but have been otherwise overlooked. The cardioprotective effect of red wine and its byproducts is related to their ability to prevent platelet aggregation, modify the lipid profile, and promote vasorelaxation. Phenolic content and profile seem to play an important role in these beneficial effects. Inhibition of platelet aggregation is dose-dependent and more efficient against ADP. The antioxidant capacity of phenolic compounds from red wine and its by-products, is involved in preventing the generation of ROS and the modification of the lipid profile, to prevent LDL oxidation. Phenolic compounds can also, modulate the activity of specific enzymes to promote NO production and vasorelaxation. Specific phenolic compounds like resveratrol are related to promote NO, and quercetin to inhibit platelet aggregation. Nevertheless, concentration that causes those effects is far from that in red wines. Synergic and additive effects of a mix of phenolic compounds could explain the cardioprotective effects of red wine and its byproducts.
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Vitis , Vino , Antioxidantes , Fenoles/análisis , Resveratrol , Vino/análisisRESUMEN
The ultimate health benefits of peanuts and tree nuts partially depend on the effective gastrointestinal delivery of their phytochemicals. The chemical composition and in vitro bioaccessibility of tocopherols, tocotrienols and phenolic compounds from peanuts and seven tree nuts were evaluated by analytical and chemometric methods. Total fat and dietary fiber (g 100 g-1) ranged from 34.2 (Emory oak acorn) to 72.5 (pink pine nut; PPN) and from 1.2 (PPN) to 22.5 (pistachio). Samples were rich in oleic and linoleic acids (56-87 g 100 g-1 oil). Tocopherols and tocotrienols (mg·kg-1) ranged from 48.1 (peanut) to 156.3 (almond) and 0 (almond, pecan) to 22.1 (PPN) and hydrophilic phenolics from 533 (PPN) to 12,896 (Emory oak acorn); flavonoids and condensed tannins (mg CE.100 g-1) ranged from 142 (white pine nut) to 1833 (Emory oak acorn) and 14 (PPN) to 460 (Emory oak acorn). Three principal components explained 90% of the variance associated with the diversity of antioxidant phytochemicals in samples. In vitro bioaccessibility of tocopherols, tocotrienols, hydrophilic phenolics, flavonoids, and condensed tannins ranged from 11-51%, 16-79%, 25-55%, 0-100%, and 0-94%, respectively. Multiple regression analyses revealed a potential influence of dietary fiber, fats and/or unsaturated fatty acids on phytochemical bioaccessibility, in a structure-specific manner.
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Antioxidantes/farmacocinética , Nueces/química , Fitoquímicos/farmacocinética , Disponibilidad Biológica , Flavonoides/farmacocinética , Humanos , Hidroxibenzoatos/farmacocinética , Análisis de Componente Principal , Proantocianidinas/farmacocinética , Análisis de Regresión , Tocoferoles/farmacocinética , Tocotrienoles/farmacocinéticaRESUMEN
Legume seeds are rich sources of protein, fiber, and minerals. In addition, their phenolic compounds as secondary metabolites render health benefits beyond basic nutrition. Lowering apolipoprotein B secretion from HepG2 cells and decreasing the level of low-density lipoprotein (LDL)-cholesterol oxidation are mechanisms related to the prevention of cardiovascular diseases (CVD). Likewise, low-level chronic inflammation and related disorders of the immune system are clinical predictors of cardiovascular pathology. Furthermore, DNA-damage signaling and repair are crucial pathways to the etiology of human cancers. Along CVD and cancer, the prevalence of obesity and diabetes is constantly increasing. Screening the ability of polyphenols in inactivating digestive enzymes is a good option in pre-clinical studies. In addition, in vivo studies support the role of polyphenols in the prevention and/or management of diabetes and obesity. Soybean, a well-recognized source of phenolic isoflavones, exerts health benefits by decreasing oxidative stress and inflammation related to the above-mentioned chronic ailments. Similar to soybeans, chickpeas are good sources of nutrients and phenolic compounds, especially isoflavones. This review summarizes the potential of chickpea as a substitute for soybean in terms of health beneficial outcomes. Therefore, this contribution may guide the industry in manufacturing functional foods and/or ingredients by using an undervalued feedstock.
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Antiinflamatorios/análisis , Antioxidantes/análisis , Cicer/química , Glycine max/química , Isoflavonas/análisis , Fitoquímicos/análisis , Animales , Antiinflamatorios/química , Antiinflamatorios/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Humanos , Isoflavonas/química , Isoflavonas/farmacología , Fitoquímicos/química , Fitoquímicos/farmacologíaRESUMEN
BACKGROUND: Serum lipoproteins are in dynamic equilibrium, partially controlled by the apolipoprotein A1 to apolipoprotein B ratio (APOA1/APOB). Freeze-dried mango pulp (FDM) is a rich source of phenolic compounds (MP) and dietary fiber (MF), although their effects on lipoprotein metabolism have not yet been studied. RESULTS: Thirty male Wistar rats were fed with four different isocaloric diets (3.4 kcal g-1 ) for 12 weeks: control diet, high cholesterol (8 g kg-1 ) + sodium cholate (2 g kg-1 ) diet either alone or supplemented with MF (60 g kg-1 ), MP (1 g kg-1 ) or FDM (50 g kg-1 ). MP and FDM reduced food intake, whereas MF and MP tended to increase serum APOA1/APOB ratio, independently of their hepatic gene expression. This suggests that lipoprotein metabolism was favorably altered by mango bioactives, MP also mitigated the non-alcoholic steatohepatitis that resulted from the intake of this diet. CONCLUSION: We propose that phenolics are the most bioactive components of mango pulp, acting as anti-atherogenic and hepatoprotective agents, with a mechanism of action tentatively based on changes to the main protein components of lipoproteins. © 2018 Society of Chemical Industry.
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Apolipoproteína A-I/sangre , Apolipoproteínas B/sangre , Colesterol/metabolismo , Mangifera/metabolismo , Enfermedad del Hígado Graso no Alcohólico/dietoterapia , Fenol/metabolismo , Extractos Vegetales/administración & dosificación , Extractos Vegetales/metabolismo , Colato de Sodio/metabolismo , Animales , Humanos , Hígado/metabolismo , Masculino , Mangifera/química , Enfermedad del Hígado Graso no Alcohólico/metabolismo , Fenol/análisis , Extractos Vegetales/análisis , Ratas , Ratas WistarRESUMEN
BACKGROUND: Globally, snake envenomation is a well-known cause of death and morbidity. In many cases of snakebite, myonecrosis, dermonecrosis, hemorrhage and neurotoxicity are present. Some of these symptoms may be provoked by the envenomation itself, but others are secondary effects of the produced oxidative stress that enhances the damage produced by the venom toxins. The only oxidative stress effect known in blood is the change in oxidation number of Fe (from ferrous to ferric) in hemoglobin, generating methemoglobin but not in other macromolecules. Currently, the effects of the overproduction of methemoglobin derived from snake venom are not extensively recorded. Therefore, the present study aims to describe the oxidative stress induced by Crotalus molossus nigrescens venom using erythrocytes. METHODS: Human erythrocytes were washed and incubated with different Crotalus molossus nigrescens venom concentrations (0-640 µg/mL). After 24 h, the hemolytic activity was measured followed by attenuated total reflectance-Fourier transform infrared spectroscopy, non-denaturing PAGE, conjugated diene and thiobarbituric acid reactive substances determination. RESULTS: Low concentrations of venom (<10 µg/mL) generates oxyhemoglobin release by hemolysis, whereas higher concentrations produced a hemoglobin shift of valence, producing methemoglobin (>40 µg/mL). This substance is not degraded by proteases present in the venom. By infrared spectroscopy, starting in 80 µg/mL, we observed changes in bands that are associated with protein damage (1660 and 1540 cm-1) and lipid peroxidation (2960, 2920 and 1740 cm-1). Lipid peroxidation was confirmed by conjugated diene and thiobarbituric acid reactive substance determination, in which differences were observed between the control and erythrocytes treated with venom. CONCLUSIONS: Crotalus molossus nigrescens venom provokes hemolysis and oxidative stress, which induces methemoglobin formation, loss of protein structure and lipid peroxidation.
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The inhibitory activity and binding characteristics of caffeic acid, p-coumaric acid, quercetin and capsaicin, four phenolic compounds found in hot pepper, against porcine pancreatic lipase activity were studied and compared to hot pepper extract. Quercetin was the strongest inhibitor (IC50=(6.1±2.4) µM), followed by p-coumaric acid ((170.2±20.6) µM) and caffeic acid ((401.5±32.1) µM), while capsaicin and a hot pepper extract had very low inhibitory activity. All polyphenolic compounds showed a mixed-type inhibition. Fluorescence spectroscopy studies showed that polyphenolic compounds had the ability to quench the intrinsic fluorescence of pancreatic lipase by a static mechanism. The sequence of Stern-Volmer constant was quercetin, followed by caffeic and p-coumaric acids. Molecular docking studies showed that caffeic acid, quercetin and p-coumaric acid bound near the active site, while capsaicin bound far away from the active site. Hydrogen bonds and π-stacking hydrophobic interactions are the main pancreatic lipase-polyphenolic compound interactions observed.
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Background Globally, snake envenomation is a well-known cause of death and morbidity. In many cases of snakebite, myonecrosis, dermonecrosis, hemorrhage and neurotoxicity are present. Some of these symptoms may be provoked by the envenomation itself, but others are secondary effects of the produced oxidative stress that enhances the damage produced by the venom toxins. The only oxidative stress effect known in blood is the change in oxidation number of Fe (from ferrous to ferric) in hemoglobin, generating methemoglobin but not in other macromolecules. Currently, the effects of the overproduction of methemoglobin derived from snake venom are not extensively recorded. Therefore, the present study aims to describe the oxidative stress induced by Crotalus molossus nigrescens venom using erythrocytes. Methods Human erythrocytes were washed and incubated with different Crotalus molossus nigrescens venom concentrations (0-640 μg/mL). After 24 h, the hemolytic activity was measured followed by attenuated total reflectance-Fourier transform infrared spectroscopy, non-denaturing PAGE, conjugated diene and thiobarbituric acid reactive substances determination. Results Low concentrations of venom (<10 μg/mL) generates oxyhemoglobin release by hemolysis, whereas higher concentrations produced a hemoglobin shift of valence, producing methemoglobin (>40 μg/mL). This substance is not degraded by proteases present in the venom. By infrared spectroscopy, starting in 80 μg/mL, we observed changes in bands that are associated with protein damage (1660 and 1540 cm−1) and lipid peroxidation (2960, 2920 and 1740 cm−1). Lipid peroxidation was confirmed by conjugated diene and thiobarbituric acid reactive substance determination, in which differences were observed between the control and erythrocytes treated with venom. Conclusions Crotalus molossus nigrescens venom provokes hemolysis and oxidative stress, which induces methemoglobin formation, loss of protein structure and lipid peroxidation.(AU)
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Animales , Venenos de Crotálidos , Estrés Oxidativo , Eritrocitos , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Espectroscopía Infrarroja por Transformada de Fourier/veterinaria , Metahemoglobina , Peroxidación de LípidoRESUMEN
Background Globally, snake envenomation is a well-known cause of death and morbidity. In many cases of snakebite, myonecrosis, dermonecrosis, hemorrhage and neurotoxicity are present. Some of these symptoms may be provoked by the envenomation itself, but others are secondary effects of the produced oxidative stress that enhances the damage produced by the venom toxins. The only oxidative stress effect known in blood is the change in oxidation number of Fe (from ferrous to ferric) in hemoglobin, generating methemoglobin but not in other macromolecules. Currently, the effects of the overproduction of methemoglobin derived from snake venom are not extensively recorded. Therefore, the present study aims to describe the oxidative stress induced by Crotalus molossus nigrescens venom using erythrocytes. Methods Human erythrocytes were washed and incubated with different Crotalus molossus nigrescens venom concentrations (0-640 μg/mL). After 24 h, the hemolytic activity was measured followed by attenuated total reflectance-Fourier transform infrared spectroscopy, non-denaturing PAGE, conjugated diene and thiobarbituric acid reactive substances determination. Results Low concentrations of venom (<10 μg/mL) generates oxyhemoglobin release by hemolysis, whereas higher concentrations produced a hemoglobin shift of valence, producing methemoglobin (>40 μg/mL). This substance is not degraded by proteases present in the venom. By infrared spectroscopy, starting in 80 μg/mL, we observed changes in bands that are associated with protein damage (1660 and 1540 cm−1) and lipid peroxidation (2960, 2920 and 1740 cm−1). Lipid peroxidation was confirmed by conjugated diene and thiobarbituric acid reactive substance determination, in which differences were observed between the control and erythrocytes treated with venom. Conclusions Crotalus molossus nigrescens venom provokes hemolysis and oxidative stress, which induces methemoglobin formation, loss of protein structure and lipid peroxidation.(AU)
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Animales , Venenos de Serpiente , Análisis Espectral , Metahemoglobina , Oxihemoglobinas , Crotalus , Estrés Oxidativo , Eritrocitos , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
Abstract Background Globally, snake envenomation is a well-known cause of death and morbidity. In many cases of snakebite, myonecrosis, dermonecrosis, hemorrhage and neurotoxicity are present. Some of these symptoms may be provoked by the envenomation itself, but others are secondary effects of the produced oxidative stress that enhances the damage produced by the venom toxins. The only oxidative stress effect known in blood is the change in oxidation number of Fe (from ferrous to ferric) in hemoglobin, generating methemoglobin but not in other macromolecules. Currently, the effects of the overproduction of methemoglobin derived from snake venom are not extensively recorded. Therefore, the present study aims to describe the oxidative stress induced by Crotalus molossus nigrescens venom using erythrocytes. Methods Human erythrocytes were washed and incubated with different Crotalus molossus nigrescens venom concentrations (0640 g/mL). After 24 h, the hemolytic activity was measured followed by attenuated total reflectance-Fourier transform infrared spectroscopy, non-denaturing PAGE, conjugated diene and thiobarbituric acid reactive substances determination. Results Low concentrations of venom ( 10 g/mL) generates oxyhemoglobin release by hemolysis, whereas higher concentrations produced a hemoglobin shift of valence, producing methemoglobin (>40 g/mL). This substance is not degraded by proteases present in the venom. By infrared spectroscopy, starting in 80 g/mL, we observed changes in bands that are associated with protein damage (1660 and 1540 cm1) and lipid peroxidation (2960, 2920 and 1740 cm1). Lipid peroxidation was confirmed by conjugated diene and thiobarbituric acid reactive substance determination, in which differences were observed between the control and erythrocytes treated with venom. Conclusions Crotalus molossus nigrescens venom provokes hemolysis and oxidative stress, which induces methemoglobin formation, loss of protein structure and lipid peroxidation.
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Urease is a nickel-dependent amidohydrolase that catalyses the decomposition of urea into carbamate and ammonia, a reaction that constitutes an important source of nitrogen for bacteria, fungi and plants. It is recognized as a potential antimicrobial target with an impact on medicine, agriculture, and the environment. The list of possible urease inhibitors is continuously increasing, with a special interest in those that interact with and block the flexible active site flap. We show that disulfiram inhibits urease in Citrullus vulgaris (CVU), following a non-competitive mechanism, and may be one of this kind of inhibitors. Disulfiram is a well-known thiol reagent that has been approved by the FDA for treatment of chronic alcoholism. We also found that other thiol reactive compounds (l-captopril and Bithionol) and quercetin inhibits CVU. These inhibitors protect the enzyme against its full inactivation by the thiol-specific reagent Aldrithiol (2,2'-dipyridyl disulphide, DPS), suggesting that the three drugs bind to the same subsite. Enzyme kinetics, competing inhibition experiments, auto-fluorescence binding experiments, and docking suggest that the disulfiram reactive site is Cys592, which has been proposed as a "hinge" located in the flexible active site flap. This study presents the basis for the use of disulfiram as one potential inhibitor to control urease activity.
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Disulfiram/farmacología , Inhibidores Enzimáticos/farmacología , Reactivos de Sulfhidrilo/farmacología , Ureasa/antagonistas & inhibidores , Aprobación de Drogas/legislación & jurisprudencia , Cinética , Estados Unidos , United States Food and Drug AdministrationRESUMEN
Anthocyanins (ACNs) are plant secondary metabolites from the flavonoid family. Red to blue fruits are major dietary sources of ACNs (up to 1 g/100 g FW), being cyanidin-3-O-glucoside (Cy3G) one of the most widely distributed. Cy3G confers a red hue to fruits, but its content in raspberries and strawberries is low. It has a good radical scavenging capacity (RSC) against superoxide but not hydroxyl radicals, and its oxidative potential is pH-dependent (58 mV/pH unit). After intake, Cy3G can be metabolized (phases I, II) by oral epithelial cells, absorbed by the gastric epithelium (1%-10%) and it is gut-transformed (phase II & microbial metabolism), reaching the bloodstream (<1%) and urine (about 0.02%) in low amounts. In humans and Caco-2 cells, Cy3G's major metabolites are protocatechuic acid and phloroglucinaldehyde which are also subjected to entero-hepatic recycling, although caffeic acid and peonidin-3-glucoside seem to be strictly produced in the large bowel and renal tissues. Solid evidence supports Cy3G's bioactivity as DNA-RSC, gastro protective, anti-inflammatory, anti-thrombotic chemo-preventive and as an epigenetic factor, exerting protection against Helicobacter pylori infection, age-related diseases, type 2 diabetes, cardiovascular disease, metabolic syndrome and oral cancer. Most relevant mechanisms include RSC, epigenetic action, competitive protein-binding and enzyme inhibition. These and other novel aspects on Cy3G's physical-chemistry, foodomics, and health effects are discussed.
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Peroxisome proliferator-activated receptors (PPAR) are transcription factors that modulate energy metabolism in liver, adipose tissue and muscle. High fat diets (HFD) can negatively impact PPAR expression or activity, favoring obesity, dyslipidemia, insulin resistance and other conditions. However, polyphenols (PP) found in vegetable foodstuffs are capable of positively modulating this pathway. We therefore focused this review on the possible effects that PP can have on PPAR when administered together with HFD. We found that PP from diverse sources, such as coffee, olives, rice, berries and others, are capable of inducing the expression of genes involved in a decrease of adipose mass, liver and serum lipids and lipid biosynthesis in animal and cell models of HFD. Since cells or gut bacteria can transform PP into different metabolites, it is possible that a synergistic or antagonistic effect ultimately occurs. PP molecules from vegetable sources are an interesting option to maintain or return to a state of energy homeostasis, possibly due to an adequate PPAR expression and activity.