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ETHNOPHARMACOLOGICAL RELEVANCE: Flavonoids interact with multiple targets in Central Nervous System resulting in a broad neuroprotection mediated by complementary processes and synergic interactions. Therefore, flavonoid-based therapies may input positive outcomes in the prevention and early management of neurodegenerative diseases. In Brazilian folk medicine Trichilia catigua is used for its neuroactive properties, such as neurostimulant, antioxidant and anti-neuroinflammatory, while Turnera diffusa is traditionally used as a tonic in neurasthenia. Both species are known to be rich in flavonoids. AIM OF THE STUDY: To study aqueous extracts of T. catigua and T. diffusa in terms of their antioxidant and antiglycation effects, inhibition of tyrosinase activity, and interaction with enzymes and pathways engaged in neuroinflammation. Moreover, whenever possible, to establish a relationship between the studied activities and the traditional usage of the species. MATERIALS AND METHODS: The phenolic profiles of the aqueous extracts were validated by HPLC-DAD. The effect of the extracts over mushroom tyrosinase and 5-lipoxygenase activities, as well as their capacity to impair bovine serum albumin glycation, were assessed by in vitro assays. The anti-neuroinflammatory potential of the same extracts was evaluated by their capacity to mitigate the pro-inflammatory stimulus induced in BV-2 microglia cells by interferon-gamma. RESULTS: T. catigua extract, a rich mixture of phenolic acids, catechins and flavonolignans, excels by its ability to decrease lipid peroxidation (EC50â¯=â¯227.18⯱â¯9.04⯵g/mL), and to work as anti-glycation agent, and inhibitor of both tyrosinase and 5-lipoxigenase (IC50â¯=â¯358.84⯱â¯19.05 and 56.25⯱â¯14.53⯵g/mL, respectively). However, only T. diffusa extract, mainly composed by luteolin derivatives, is able to lower NO production by BV-2 microglia cells stimulated with interferon-gamma, despite its lower activities in the other assays. CONCLUSIONS: Overall, this work highlights the value of medicinal plant extracts as sources of bioactive flavonoid-rich extracts with neuroactive effects. Furthermore, these results support their application as alternative strategies to develop functional foods and therapeutics to fight chronic neurodegenerative disorders.
Assuntos
Produtos Finais de Glicação Avançada/antagonistas & inibidores , Meliaceae/química , Monofenol Mono-Oxigenase/antagonistas & inibidores , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Turnera/química , Animais , Antioxidantes/farmacologia , Brasil , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Produtos Finais de Glicação Avançada/efeitos dos fármacos , Inflamação/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Inibidores de Lipoxigenase/farmacologia , Medicina Tradicional , Camundongos , Microglia/efeitos dos fármacos , Óxido Nítrico/metabolismoRESUMO
Cardiovascular benefits for the general population of combined aerobic-resistance exercise training are well-known, but the impact of this exercise training modality on the plasma lipid, inflammatory, and antioxidant status in elderly women that are exposed to a great risk of developing ischemic cardio- and cerebrovascular diseases has not been well investigated. So, we aimed to evaluate the plasma lipids, oxidative stress, and inflammatory cytokines in 27 elderly women (TRAINED group, 69.1 ± 8.1 yrs) that were performing moderate intensity combined aerobic-resistance exercise training (3 times/week for at least 18 months) and in 27 sedentary elderly women (SED group, 72.0 ± 6.4 yrs), not submitted to exercise training for at least 5 yrs. Our results showed that BMI was lower in the TRAINED group than in the SED group (25.1 ± 3.2 vs. 28.7 ± 5.1, p < 0.05). The TRAINED group had lower glycemia (92 ± 3 vs. 118 ± 12, p < 0.05), glycated hemoglobin (5.9 ± 0.1 vs. 6.4 ± 0.2, p < 0.05), and triglycerides (98 (75-122) vs. 139 (109-214), p < 0.01); equal total cholesterol (199 (175-230) vs. 194 (165-220)), LDL-cholesterol (108 (83-133) vs. 109 (98-136)), and non-HDL-cholesterol (54 (30-74) vs. 62 (26-80)); and also higher HDL-cholesterol (64 (52-77) vs. 52 (44-63), p < 0.01) and LDL-C/oxLDL ratio (13378 ± 2570 vs. 11639 ± 3113, p < 0.05) compared to the SED group. Proinflammatory cytokines as IL-1ß (11.31 ± 2.4 vs. 28.01 ± 4.7, p < 0.05), IL-6 (26.25 ± 7.4 vs. 49.41 ± 17.8, p < 0.05), and TNF-α (25.72 ± 2.8 vs. 51.73 ± 4.2, p < 0.05) were lower in the TRAINED group than in the SED group. The TRAINED group had lower total peroxides (26.3 ± 7.4 vs. 49.0 ± 17.8, p < 0.05) and oxidized LDL (1551 ± 50.33 vs. 1773 ± 74, p < 0.02) and higher total antioxidant capacity (26.25 ± 7.4 vs. 49.41 ± 17.8, p < 0.001) compared to the SED group. In conclusion, in TRAINED women, BMI was lower, plasma lipid profile was better, plasma oxidative stress was diminished, and there was less expression of proinflammatory interleukins than in SED, suggesting that combined aerobic-resistance exercise training may promote the protection against the complications of ischemic cardio- and cerebrovascular disease in elderly women.
Assuntos
Transtornos Cerebrovasculares , Citocinas/sangue , Exercício Físico , Lipídeos/sangue , Estresse Oxidativo , Idoso , Idoso de 80 Anos ou mais , Transtornos Cerebrovasculares/sangue , Transtornos Cerebrovasculares/prevenção & controle , Feminino , Humanos , Pessoa de Meia-Idade , Oxirredução , Fatores de TempoRESUMO
Cardiovascular benefits for the general population of combined aerobic-resistance exercise training are well-known, but the impact of this exercise training modality on the plasma lipid, inflammatory, and antioxidant status in elderly women that are exposed to a great risk of developing ischemic cardio- and cerebrovascular diseases has not been well investigated. So, we aimed to evaluate the plasma lipids, oxidative stress, and inflammatory cytokines in 27 elderly women (TRAINED group, 69 1±8 1 yrs) that were performing moderate intensity combined aerobic-resistance exercise training (3 times/week for at least 18 months) and in 27 sedentary elderly women (SED group, 72 0±6 4 yrs), not submitted to exercise training for at least 5 yrs. Our results showed that BMI was lower in the TRAINED group than in the SED group (25 1±3 2 vs. 28 7±5 1, p < 0 05). The TRAINED group had lower glycemia (92 ± 3 vs. 118 ± 12, p < 0 05), glycated hemoglobin (5 9±0 1 vs. 6 4±0 2, p < 0 05), and triglycerides (98 (75-122) vs. 139 (109-214), p < 0 01); equal total cholesterol (199 (175-230) vs. 194 (165-220)), LDL-cholesterol (108 (83-133) vs. 109 (98-136)), and non-HDL-cholesterol (54 (30-74) vs. 62 (26-80)); and also higher HDL-cholesterol (64 (52-77) vs. 52 (44-63), p < 0 01) and LDL-C/oxLDL ratio (13378 ± 2570 vs. 11639 ± 3113, p < 0 05) compared to the SED group. Proinflammatory cytokines as IL-1ß (11 31 ± 2 4 vs. 28 01 ± 4 7, p < 0 05), IL-6 (26 25 ± 7 4 vs. 49 41 ± 17 8, p < 0 05), and TNF-α (25 72 ± 2 8 vs. 51 73 ± 4 2, p < 0 05) were lower in the TRAINED group than in the SED group. The TRAINED group had lower total peroxides (26 3±7 4 vs. 49 0 ± 17 8, p < 0 05) and oxidized LDL (1551 ± 50 33 vs. 1773 ± 74, p < 0 02) and higher total antioxidant capacity (26 25 ± 7 4 vs. 49 41 ± 17 8, p < 0 001) compared to the SED group. In conclusion, in TRAINED women, BMI was lower, plasma lipid profile was better, plasma oxidative stress was diminished, and there was less expression of proinflammatory interleukins than in SED, suggesting that combined aerobic-resistance exercise training may promote the protection against the complications of ischemic cardio- and cerebrovascular disease in elderly women.
Assuntos
Feminino , Triglicerídeos , Exercício Físico , Colesterol , Citocinas , Aterosclerose , LipídeosRESUMO
Inflammation is a natural defense mechanism of the immune system; however, when unregulated, it can lead to chronic illness. Glucocorticoids are the most commonly used agents to effectively treat inflammatory conditions, including autoimmune diseases, however these substances can trigger a number of side effects. Thus, viable alternatives to the use of these drugs would be advantageous. In this study, we have analyzed the anti-inflammatory profile of three synthetic peptides first identified in skin secretion of the tree frog Hypsiboas raniceps. Structural characterization was performed using NMR spectroscopy and Mass Spectrometry, and the peptides were tested in vitro in RAW 264.7 cells and in vivo in Balb/c mice for their functional properties. The samples did not show a significant antimicrobial profile. NMR spectroscopy indicated that AC12 (ACFLTRLGTYVC) has a disulfide bond between C2 and C11 and a ß-sheet-turn-ß-sheet conformation in aqueous solution. This peptide showed no cytotoxic effect in mammalian cells and it was the most effective in reducing anti-inflammatory markers, such as NO, TNF-α and IL-12. Peptide DK16 (DKERPICSNTFRGRKC) demonstrated anti-inflammatory properties in vitro, while RC11 (RCFRRRGKLTC) significantly altered the cell viability in RAW 264.7 but was shown to be safe in Balb/c erythrocytes. Our results indicate that, of the three peptides studied, AC12 is the most efficient in reducing anti-inflammatory markers, and it could be a potential agent for the treatment of inflammatory diseases.
Assuntos
Anti-Inflamatórios/farmacologia , Anuros/metabolismo , Inflamação/tratamento farmacológico , Peptídeos/farmacologia , Pele/metabolismo , Proteínas de Anfíbios/química , Proteínas de Anfíbios/metabolismo , Proteínas de Anfíbios/farmacologia , Animais , Anti-Infecciosos/farmacologia , Biomarcadores , Interleucina-12 , Espectroscopia de Ressonância Magnética , Masculino , Espectrometria de Massas , Camundongos , Camundongos Endogâmicos BALB C , Peptídeos/química , Peptídeos/metabolismo , Conformação Proteica , Células RAW 264.7 , Pele/química , Fator de Necrose Tumoral alfaRESUMO
BACKGROUND: We have recently demonstrated that palmitoleic acid (16:1n7) increases lipolysis, glucose uptake and glucose utilization for energy production in white adipose cells. In the present study, we tested the hypothesis that palmitoleic acid modulates bioenergetic activity in white adipocytes. METHODS: For this, 3 T3-L1 pre-adipocytes were differentiated into mature adipocytes in the presence (or absence) of palmitic (16:0) or palmitoleic (16:1n7) acid at 100 or 200 µM. The following parameters were evaluated: lipolysis, lipogenesis, fatty acid (FA) oxidation, ATP content, oxygen consumption, mitochondrial mass, citrate synthase activity and protein content of mitochondrial oxidative phosphorylation (OXPHOS) complexes. RESULTS: Treatment with 16:1n7 during 9 days raised basal and isoproterenol-stimulated lipolysis, FA incorporation into triacylglycerol (TAG), FA oxidation, oxygen consumption, protein expression of subunits representing OXPHOS complex II, III, and V and intracellular ATP content. These effects were not observed in adipocytes treated with 16:0. CONCLUSIONS: Palmitoleic acid, by concerted action on lipolysis, FA esterification, mitochondrial FA oxidation, oxygen consumption and ATP content, does enhance white adipocyte energy expenditure and may act as local hormone.
Assuntos
Trifosfato de Adenosina/metabolismo , Adipócitos Brancos/efeitos dos fármacos , Adipócitos Brancos/metabolismo , Ácidos Graxos Monoinsaturados/farmacologia , Ácidos Graxos/metabolismo , Consumo de Oxigênio/efeitos dos fármacos , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Lipólise/efeitos dos fármacos , Camundongos , Oxirredução/efeitos dos fármacos , Triglicerídeos/metabolismoRESUMO
It is widely accepted that the consumption of ω-3 polyunsaturated fatty acids has beneficial effects on human health. In this work, ten brown macroalgae species collected along the Portuguese west coast were studied for their fatty acids composition by GC-MS after alkaline hydrolysis and derivatization. The results of this survey showed that different macroalgae from the same region display distinct fatty acids profile. Concerning ω-3 polyunsaturated fatty acids, eicosapentaenoic acid was found in all but one species. Additionally, some species contained docosahexaenoic acid. Linoleic acid, an essential fatty acid of the ω-6 series, was present in all studied macroalgae. Fucus spiralis L. exhibited the highest amounts of monounsaturated fatty acids and of polyunsaturated fatty acids of the ω-3 and ω-6 series. The ω-6/ω-3 ratio in half of the studied species was lower than 1. This information reinforces the potential application of some brown macroalgae as dietary sources of polyunsaturated fatty acids.
RESUMO
Ficus carica L., Moraceae, is one of the first plants that were cultivated by humans, being the fruit an important crop worldwide for dry and fresh consumption. In this work, phenolics and antioxidant potential of dried fruits of seventeen Tunisian F. carica varieties, from green, red and black phenotypes, were assessed for the first time. HPLC-DAD analysis was performed. All samples presented a similar qualitative profile. The phenolics content ranged between 29.18 and 55.56 mg/kg (in black and red phenotypes, respectively) and quercetin-3-O-rutinoside was always the major compound. The antioxidant potential against DPPH, superoxide and nitric oxide radicals of three varieties representing each phenotype was checked. All samples exhibited activity against the first two radicals in a concentration-dependent way, "Bayoudi" variety being the most effective one (IC25 values of 10.32 and 2.89 µg/ mL, respectively). Nevertheless, only "Hammouri" variety presented some capacity to scavenge nitric oxide radical. Our results reveal nice perspectives for these typical fruits, as they present an interesting phenolic composition and good antiradical activity and may encourage their consumption for health protection.
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In this study, the carotenoid profile of the echinoderm Marthasterias glacialis L. was established using HPLC-DAD-APCI-MS/MS equipped with a C(30) column. This approach rendered the identification of 20 compounds, eight of them reported for the first time in this marine organism. Differentiation of carotenoid isomers was also achieved.
Assuntos
Carotenoides/análise , Equinodermos/química , Animais , Carotenoides/química , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas em TandemRESUMO
Coreopsis tinctoria Nutt., Asteraceae, flowering tops infusion has been traditionally used in many countries to control hyperglycaemia. In this work we report for the first time fatty acids and volatile compounds in this species. Fifteen fatty acids and sixteen volatile compounds were determined by GC-ITMS, being saturated fatty acids and monoterpenes the main compounds. The antioxidant and antibacterial potential of this matrix was checked for the first time by several in vitro assays. A concentration-dependent activity was noticed against DPPH, nitric oxide and superoxide radicals. Antibacterial capacity was assessed against Gram-positive and Gram-negative bacteria, being more effective against the first. Additionally, acetylcholinesterase and butyrylcholinesterase inhibitory activity was also evaluated, but no effect was found. Our results provide evidence of a wide diversity of compounds with several biological properties, improving the knowledge on this poorly studied matrix, which can lead to an increment of the use of C. tinctoria flowering tops, namely in food and pharmaceutical applications.
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Capsella bursa-pastoris (L.) Medik. (Brassicaceae) is a wild herb with high nutritional value that can be eaten raw or cooked. A metabolomic study was performed with different extracts of its aerial parts that were tested concerning their antiradical, acetylcholinesterase inhibitory and antibacterial activities. Phenolic compounds were identified and quantified by HPLC-DAD, organic acids and amino acids were determined by HPLC-UV, while free fatty acids and sterols were analysed by GC-ITMS. The vegetal material was rich in kaempferol-3-O-rutinoside (mean value 2247.09 mg/kg of dry plant), quinic acid (95628.00 mg/kg of dry plant), arginine (mean value of 1.18 mg/kg of dry plant), palmitic acid (284.48 mg/kg) and β-sitosterol (28 percent). The extracts presented a concentration-dependent antiradical activity (against DPPH, O2- and LOO), being most effective against NO (EC25 0.20 µg/mL). In addition, the extracts were also acetylcholinesterase inhibitors and antibacterial active, revealing that, besides the plant's good nutritional value, it presents important biological properties as well.
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We describe here a regulated and highly active K+ uptake pathway in potato (Solanum tuberosum), tomato (Lycopersicon esculentum), and maize (Zea mays) mitochondria. K+ transport was not inhibited by ATP, NADH, or thiol reagents, which regulate ATP-sensitive K+ channels previously described in plant and mammalian mitochondria. However, K+ uptake was completely prevented by quinine, a broad spectrum K+ channel inhibitor. Increased K+ uptake in plants leads to mitochondrial swelling, respiratory stimulation, heat release, and the prevention of reactive oxygen species formation. This newly described ATP-insensitive K+ import pathway is potentially involved in metabolism regulation and prevention of oxidative stress.