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1.
Food Sci Biotechnol ; 33(6): 1351-1358, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38585563

RESUMO

The rising health consciousness of consumers has resulted in multiple studies on the use of animal and vegetable proteins in gluten-free noodle production, but chicken breast meat (CBM) has not been the subject of such studies. Thus, we aimed to create protein-fortified gluten-free noodles using economical and nutritious CBM and compare their quality attributes with commonly used wheat flour noodles (WN). Among the CBM noodles (CN), CN with tapioca starch (CN-T) showed the highest sensory and textural similarity to WN. The color values of cooked noodles were not considerably different. The water absorption capacity and volume expansion ratio of CN-T were not significantly different from those of WN. In CNs, an ungelatinized microstructure was observed, and CN-T displayed well-formed structural bonds related to adhesiveness, similar to WN. The CN-T had a protein content about 2% higher than WN. This finding is informative for the development of gluten-free noodles using CBM.

2.
Mol Nutr Food Res ; 68(3): e2300253, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38054627

RESUMO

SCOPE: Depression is a severe mental condition, common among menopausal women. γ-Oryzanol (ORY) has various biological properties; however, the effect of ORY on menopausal depression and its underlying mechanisms have not been investigated. METHODS AND RESULTS: ORY is orally administered to ovariectomized (OVX) mice for 20 weeks. ORY administration results in lower immobility time in the tail suspension and forced swim test and increases locomotor activity in the open field test. In the primary hippocampal neurons and hippocampi of OVX mice, ORY treatment increases nitric oxide (NO) production and neuronal NO synthase (nNOS) expression. Further, the phosphorylation of extracellular signal-regulated kinase (ERK), cAMP response element-binding protein (CREB), and tropomyosin receptor kinase B, along with the expression of brain-derived neurotrophic factior (BDNF), is upregulated. These stimulatory effects of ORY are diminished by treatment with estrogen receptor ß (ERß) antagonist. ORY similarly interacts with ERß in the molecular docking analysis. Moreover, intracerebroventricular injection of 7-nitroindazole, a nNOS inhibitor, abolishes the antidepressant effects of ORY. CONCLUSIONS: The results indicate that ORY attenuates depressive behavior in OVX mice by upregulating ERß-mediated hippocampal nNOS expression and activating the ERK-CREB-BDNF signaling networks. The findings suggest that ORY is a potential therapeutic agent for attenuating menopausal depression.


Assuntos
Fator Neurotrófico Derivado do Encéfalo , Depressão , Fenilpropionatos , Camundongos , Feminino , Humanos , Animais , Depressão/tratamento farmacológico , Depressão/metabolismo , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Receptor beta de Estrogênio/metabolismo , Simulação de Acoplamento Molecular , Hipocampo/metabolismo , Óxido Nítrico Sintase/metabolismo , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Menopausa , Óxido Nítrico/metabolismo
3.
Antioxidants (Basel) ; 12(10)2023 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-37891920

RESUMO

Sargassum horneri, a brown seaweed, is known for its various health benefits; however, there are no reports on its effects on depression. This study aimed to investigate the antidepressant effects of S. horneri ethanol extract (SHE) in mice injected with corticosterone (CORT) and to elucidate the underlying molecular mechanisms. Behavioral tests were conducted, and corticotropin-releasing hormone (CRH), adrenocorticotropic hormone (ACTH), and CORT levels were measured. A fluorometric monoamine oxidase (MAO) enzyme inhibition assay was performed. Neurotransmitters like serotonin, dopamine, and norepinephrine levels were determined. Moreover, the ERK-CREB-BDNF signaling pathway in the prefrontal cortex and hippocampus was evaluated. Behavioral tests revealed that SHE has antidepressant effects by reducing immobility time and increasing time spent in open arms. Serum CRH, ACTH, and CORT levels decreased in the mice treated with SHE, as did the glucocorticoid-receptor expression in their brain tissues. SHE inhibited MAO-A and MAO-B activities. In addition, SHE increased levels of neurotransmitters. Furthermore, SHE activated the ERK-CREB-BDNF pathway in the prefrontal cortex and hippocampus. These findings suggest that SHE has antidepressant effects in CORT-injected mice, via the regulation of the hypothalamic-pituitary-adrenal axis and monoaminergic pathway, and through activation of the ERK-CREB-BDNF signaling pathway. Thus, our study suggests that SHE may act as a natural antidepressant.

4.
Foods ; 12(17)2023 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-37685230

RESUMO

Efficient detection methods must be developed for 1,4-dioxane due to its suspected status as a human carcinogen, which is highly mobile in food and environmental resources. In this regard, this experiment has been conducted to develop reliable and selective detection and measurement methods by using static headspace (SH) isolation, followed by gas chromatography-mass spectrometry (GC-MS). A new method was developed for determining the spiked 1,4-dioxane contents in a polyethylene glycol 600 (PEG 600). The optimal condition for SH-GC-MS was discussed. The representative ions of 1,4-dioxane and 1,4-dioxane-d8 in the SIM mode of MS are 88 and 96, respectively, and the peaks of the SIM mode were separated and confirmed. The linear range for the method covers 0.25 to 100 mg/L with a coefficient of determination (R2) ≥ 0.999. The method applicability was demonstrated by spike recovery across a variety of food additives (i.e., chlorine bitartrate, choline chloride, polysorbate 20 and 60, and PEG 1000). All spike recovery from the tested samples was in the range of 89.50-102.68% with a precision of 0.44-11.22%. These findings suggest a new analytical method for food safety inspection, and could be applicable for ensuring the safety of foods and environmental and public health on a broad scale.

5.
Int J Mol Sci ; 24(5)2023 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-36902068

RESUMO

Phloroglucinol is a class of polyphenolic compounds containing aromatic phenyl rings and is known to have various pharmacological activities. Recently, we reported that this compound isolated from Ecklonia cava, a brown alga belonging to the family Laminariaceae, has potent antioxidant activity in human dermal keratinocytes. In this study, we evaluated whether phloroglucinol could protect against hydrogen peroxide (H2O2)-induced oxidative damage in murine-derived C2C12 myoblasts. Our results revealed that phloroglucinol suppressed H2O2-induced cytotoxicity and DNA damage while blocking the production of reactive oxygen species. We also found that phloroglucinol protected cells from the induction of apoptosis associated with mitochondrial impairment caused by H2O2 treatment. Furthermore, phloroglucinol enhanced the phosphorylation of nuclear factor-erythroid-2 related factor 2 (Nrf2) as well as the expression and activity of heme oxygenase-1 (HO-1). However, such anti-apoptotic and cytoprotective effects of phloroglucinol were greatly abolished by the HO-1 inhibitor, suggesting that phloroglucinol could increase the Nrf2-mediated activity of HO-1 to protect C2C12 myoblasts from oxidative stress. Taken together, our results indicate that phloroglucinol has a strong antioxidant activity as an Nrf2 activator and may have therapeutic benefits for oxidative-stress-mediated muscle disease.


Assuntos
Antioxidantes , Estresse Oxidativo , Phaeophyceae , Floroglucinol , Animais , Humanos , Camundongos , Antioxidantes/farmacologia , Apoptose , Linhagem Celular , Heme Oxigenase-1/metabolismo , Peróxido de Hidrogênio/metabolismo , Mioblastos/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Phaeophyceae/metabolismo , Floroglucinol/farmacologia , Espécies Reativas de Oxigênio/metabolismo
6.
Nutrients ; 15(4)2023 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-36839400

RESUMO

Wakefulness is defined as a state in which individuals can react to a change in situations. The number of people staying awake and compensating for lack of sleep has increased in recent years. Caffeine, a representative stimulant, is the most extensively consumed compound globally and is mainly consumed through coffee. Although green tea (Camellia sinensis L.) contains high caffeine content like coffee, its arousal-inducing effects have not yet been studied. In the present study, we aimed to identify the arousal-inducing effect of GT during a chronic administration period (three weeks) using analysis of sleep architecture. Treatment with GT (1500 mg/kg) significantly elevated the sleep latency and wakefulness throughout the treatment period, and chronic administration of GT consistently maintained an increase in wakefulness for up to 3 h. During the treatment period, the arousal-inducing effect of GT (1500 mg/kg) occurred without any change in the tolerance phenomenon or withdrawal symptoms, similar to that observed with caffeine (25 mg/kg). GT (1500 mg/kg) containing 95.6 mg/kg of caffeine did not produce a better arousal-inducing effect than caffeine at 25 mg/kg. These results indicate that the arousal-inducing effect of GT persisted for three weeks without adverse effects and that GT can control the arousal-inducing effects of caffeine due to the hypnotic effects of its other constituents.


Assuntos
Cafeína , Camellia sinensis , Camundongos , Animais , Cafeína/farmacologia , Café , Etanol/farmacologia , Sono , Chá , Fármacos do Sistema Nervoso Central , Extratos Vegetais/farmacologia
7.
Food Funct ; 14(2): 1259, 2023 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-36541786

RESUMO

Correction for 'Curcuminoids, a major turmeric component, have a sleep-enhancing effect by targeting the histamine H1 receptor' by Min Young Um et al., Food Funct., 2022, 13, 12697-12706, https://doi.org/10.1039/D2FO02087D.

8.
Antioxidants (Basel) ; 11(12)2022 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-36552561

RESUMO

Phloroglucinol, a phenolic compound, is known to possess a potent antioxidant ability. However, its role in retinal cells susceptible to oxidative stress has not been well elucidated yet. Thus, the objective of this study was to evaluate whether phloroglucinol could protect against oxidative damage in cultured human retinal pigment epithelium ARPE-19 cells. For this purpose, ARPE-19 cells were stimula ted with hydrogen peroxide (H2O2) to mimic oxidative stress. Cell viability, cytotoxicity, apoptosis, reactive oxygen species (ROS) generation, mitochondrial function, DNA damage, and autophagy were then assessed. Our results revealed that phloroglucinol ameliorated cell viability, cytotoxicity, and DNA damage in H2O2-exposued ARPE-19 cells and blocked production of ROS. Phloroglucinol also counteracted H2O2-induced apoptosis by reducing Bax/Bcl-2 ratio, blocking activation of caspase-3, and inhibiting degradation of poly (ADP-ribose) polymerase. H2O2 caused mitochondrial impairment and increased expression levels of mitophagy markers such as PINK1and PARKIN known to be associated with mitochondrial ROS (mtROS) generation and cytosolic release of cytochrome c. However, these changes were significantly attenuated by phloroglucinol. Mito-TEMPO, a selective mitochondrial antioxidant, further enhanced the protective effect of phloroglucinol against dysfunctional mitochondria. Furthermore, H2O2 induced autophagy, but not when ARPE-19 cells were pretreated with phloroglucinol, meaning that autophagy by H2O2 contributed to the pro-survival mechanism and that phloroglucinol protected ARPE-19 cells from apoptosis by blocking autophagy. Taken together, these results suggest that phloroglucinol can inhibit oxidative stress-induced ARPE-19 cell damage and dysfunction by protecting DNA damage, autophagy, and subsequent apoptosis through mitigation of mtROS generation. Thus, phloroglucinol might have therapeutic potential to prevent oxidative stress-mediated damage in RPE cells.

9.
Mar Drugs ; 20(12)2022 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-36547921

RESUMO

Insomnia is a common sleep disorder. Natural sleep aids are gaining worldwide popularity as alternatives to prescription drugs for improving sleep. Recently, numerous studies have investigated the sedative-hypnotic effects of the polyphenols of terrestrial plants. The hypnotic effects of marine polyphenols have also been studied in recent years. Phlorotannins are marine polyphenols that are found only in brown algae. Phlorotannins exert sedative-hypnotic effects via the gamma-aminobutyric acid type A-benzodiazepine receptor. In addition, the brown seaweed Ecklonia cava supplement containing phlorotannins has been approved by the Ministry of Food and Drug Safety as a health-functional ingredient that helps improve sleep quality. Currently, it is meaningful to deal with the sedative-hypnotic effects of phlorotannins as natural sleep aids. The current review comprehensively presents the sedative-hypnotic effects in animal models and human clinical trials as well as their mechanism of action, extraction, purification, and safety.


Assuntos
Phaeophyceae , Alga Marinha , Distúrbios do Início e da Manutenção do Sono , Animais , Humanos , Polifenóis/farmacologia , Polifenóis/uso terapêutico , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico , Hipnóticos e Sedativos/farmacologia , Hipnóticos e Sedativos/uso terapêutico , Sono
10.
Nutrients ; 14(22)2022 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-36432419

RESUMO

In the previous study, it was reported that green kiwifruit peel ethanol extract (GKPEE) increases sleep duration and decreases sleep latency in pentobarbital-treated mice. The pentobarbital-induced sleep test can be used to verify sleep quantity, which includes factors such as sleep duration and latency, but not sleep quality. In the present study, the sleep-promoting effects of GKPEE were investigated by the analysis of electroencephalogram (EEG) and electromyogram in mice and were compared with the results of diazepam (DZP), a representative sedative-hypnotic agent. The acute administration of GKPEE (250, 500 and 1000 mg/kg) increased the amount of non-rapid eye movement sleep (NREMS) and decreased sleep latency in a dose-dependent manner. The effect of GKPEE at 1000 mg/kg produced persistently significantly different results until the second hour of time-course changes. In particular, GKPEE did not produce any change in delta activity compared to DZP. Furthermore, sub-chronic administration (15 days) of GKPEE (500 mg/kg) continued sleep-promoting effects, whilst the EEG power density of NREMS did not show significant differences, indicating that there were no tolerance phenomena. Our findings suggest that GKPEE may be a promising natural sleep aid for treating sleep disorders. In addition, considering the number of by-products discarded each year by the food industry, the application of GKPEE here contributes to the utilization of processed kiwifruit by-products and can help to solve environmental problems.


Assuntos
Pentobarbital , Sono , Camundongos , Animais , Eletromiografia , Pentobarbital/farmacologia , Eletroencefalografia , Extratos Vegetais/farmacologia , Diazepam/farmacologia
11.
Food Funct ; 13(24): 12697-12706, 2022 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-36408594

RESUMO

Turmeric (Curcuma longa) had been considered as a universal panacea in functional foods and traditional medicines. In recent, the sedative-hypnotic effect of turmeric extract (TE) was reported. However, sleep-promoting compounds in TE have been not yet demonstrated. Curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin) are the major constituents of turmeric being responsible for its various biological activities. Therefore, they can be first assumed to be sedative-hypnotic compounds of TE. In the present study, we aimed to investigate the effects and underlying mechanisms of curcuminoids and each constituent on the sleep-wake cycle of mice. Molecular docking studies, histamine H1 receptor (H1R) binding assays, and H1R knockout animal studies were used to investigate the molecular mechanisms underlying the sleep-promoting effects. Curcuminoids and their constituents reduced sleep latency and increased sleep duration in the pentobarbital-induced sleep test in mice. In addition, curcuminoids significantly increased the duration of NREMS and reduced sleep latency without altering the REMS and delta activity. Curcumin, demethoxycurcumin, and bisdemethoxycurcumin were predicted to interact with H1R in the molecular model. In the binding affinity assay, we found that curcuminoids, as well as their constituents, significantly bind to H1R with the Ki value of 1.49 µg mL-1. Furthermore, sleep latency was reduced and NREMS frequency was increased following curcuminoid administration in wild-type mice but not in H1R knockout mice. Therefore, we conclude that curcuminoids reduce sleep latency and enhance the quantity of NREMS by acting as modulators of H1R, indicating their usefulness in treating insomnia.


Assuntos
Curcuma , Curcumina , Diarileptanoides , Receptores Histamínicos H1 , Medicamentos Indutores do Sono , Latência do Sono , Sono REM , Animais , Camundongos , Curcuma/química , Curcumina/química , Curcumina/farmacologia , Diarileptanoides/farmacologia , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Receptores Histamínicos H1/genética , Receptores Histamínicos H1/metabolismo , Latência do Sono/efeitos dos fármacos , Sono REM/efeitos dos fármacos , Medicamentos Indutores do Sono/química , Medicamentos Indutores do Sono/farmacologia
12.
Nutrients ; 14(11)2022 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-35684048

RESUMO

Sleep is one of the most essential factors required to maintain good health. However, the global prevalence of insomnia is increasing, and caffeine intake is a major trigger. The objective of this study was to investigate the inhibitory effect of black pepper, Piper nigrum extract (PE), on caffeine-induced sleep disruption and excitation in mice. Caffeine significantly decreased sleep duration in the pentobarbital-induced sleep test. It also resulted in a significant increase in sleep onset and a decrease in non-rapid eye movement sleep. Moreover, in an open-field test, caffeine-treated mice exhibited a significantly increased time in the center zone and total distance traveled. However, the co-administration of caffeine and PE did not result in similar arousal activities. Thus, our results suggest that PE can be used as a potential therapeutic agent to treat sleep problems and excitatory status associated with caffeine intake.


Assuntos
Piper nigrum , Animais , Cafeína/farmacologia , Camundongos , Pentobarbital/farmacologia , Extratos Vegetais/farmacologia , Sono
13.
Foods ; 11(10)2022 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-35626951

RESUMO

Recently, many manufacturers have been developing or producing imitation crab sticks (ICSs) that are highly similar to real snow crab leg meat (RC). This study evaluated the similarities between commercial ICSs and RC based on the analysis of physicochemical and sensory properties. Normal ICS (NS) and premium ICSs either with real crab leg meat (PS-RC) or without it (PS) were compared with RC. The sensory evaluation results showed that PS and NS had the highest and lowest levels of similarity to RC, respectively. The carbohydrate contents of ICSs (10-23%) were higher than that of RC (0.5%). Among ICSs, PS showed more similarity with RC than NS and PS-RC in terms of gel strength and texture profiles. PS-RC and PS showed a microstructural pattern that slightly imitated the muscle fiber arrangement of RC. The electric tongue analysis of taste compounds, such as sugars, free amino acids, and nucleotides, showed that the taste profile of ICSs is distinctly different from that of RC. The electronic nose analysis identified 32 volatile compounds, while the principal component analysis using electronic nose data successfully distinguished three clusters: PS-RC and PS, RC, and NS. Our results could provide useful information for the development of ICSs with higher similarity to RC.

14.
Nutrients ; 13(8)2021 Aug 19.
Artigo em Inglês | MEDLINE | ID: mdl-34445005

RESUMO

Caffeine, a natural stimulant, is known to be effective for weight loss. On this basis, we screened the arousal-inducing effect of five dietary supplements with a weight loss effect (Garcinia cambogia, Coleus forskohlii, Camellia sinensis L., Irvingia gabonensis, and Malus pumila M.), of which the G. cambogia peel extract (GC) showed a significant arousal-inducing effect in the pentobarbital-induced sleep test in mice. This characteristic of GC was further evaluated by analysis of electroencephalogram and electromyogram in C57L/6N mice, and it was compared to that of the positive control, caffeine. Administration of GC (1500 mg/kg) significantly increased wakefulness and decreased non-rapid eye movement sleep, similar to that of caffeine (25 mg/kg), with GC and caffeine showing a significant increase in wakefulness at 2 and 6 h, respectively. Compared to that of caffeine, the shorter duration of efficacy of GC could be advantageous because of the lower possibility of sleep disturbance. Furthermore, the arousal-inducing effects of GC (1500 mg/kg) and caffeine (25 mg/kg) persisted throughout the chronic (3 weeks) administration study. This study, for the first time, revealed the arousal-inducing effect of GC. Our findings suggest that GC might be a promising natural stimulant with no side effects. In addition, it is preferential to take GC as a dietary supplement for weight loss during the daytime to avoid sleep disturbances owing to its arousal-inducing effect.


Assuntos
Nível de Alerta/efeitos dos fármacos , Ondas Encefálicas/efeitos dos fármacos , Encéfalo/efeitos dos fármacos , Estimulantes do Sistema Nervoso Central/farmacologia , Eletroencefalografia , Garcinia cambogia , Extratos Vegetais/farmacologia , Animais , Fármacos Antiobesidade/farmacologia , Encéfalo/fisiologia , Cafeína/farmacologia , Estimulantes do Sistema Nervoso Central/isolamento & purificação , Frutas , Garcinia cambogia/química , Hipnóticos e Sedativos/farmacologia , Masculino , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos ICR , Pentobarbital/farmacologia , Extratos Vegetais/isolamento & purificação , Sono/efeitos dos fármacos
15.
Mol Nutr Food Res ; 65(14): e2100100, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-34003596

RESUMO

SCOPE: Turmeric has a broad spectrum of biological properties; however, the sleep-promoting effects of turmeric have not yet been reported. Thus, this study aims to investigate the effect of turmeric on sleep and the molecular mechanism underlying this effect. METHODS AND RESULTS: Pentobarbital-induce sleep test and sleep-wake profile assessment using recorded electroencephalography are used to evaluate the hypnotic effects of the turmeric extract (TE) compared to diazepam on sleep in mice. Additionally, the molecular mechanism of TE's sleep effect is investigated using ex vivo electrophysiological recordings from brain slices in histamine H1 receptor (H1 R) knockout mice. Oral administration of TE and diazepam significantly reduce sleep latency and increase non-rapid eye movement sleep (NREMS) duration without delta activity in mice. Like doxepin, TE inhibits the H1 R agonist (2-pyridylethylamine dihydrochloride)-induced increase in action potentials in the hypothalamic neurons. In animal tests using neurotransmitter agonists or antagonists, TE effect mimick H1 R antagonistic effect of doxepin. Additionally, both reduce sleep latency and increase NREMS in wild-type mice, although these effects are not observed in H1 R knockout mice. CONCLUSION: TE has a sleep-promoting effect owing to reduction in sleep latency and enhancement of NREMS via H1 R blockade; therefore, it could be useful in insomnia.


Assuntos
Antagonistas dos Receptores Histamínicos H1/farmacologia , Extratos Vegetais/farmacologia , Sono/efeitos dos fármacos , Animais , Curcuma , Diazepam , Doxepina , Eletroencefalografia , Hipnóticos e Sedativos/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos ICR , Camundongos Knockout , Polissonografia , Receptores Histamínicos H1/genética , Latência do Sono/efeitos dos fármacos , Sono de Ondas Lentas
16.
J Enzyme Inhib Med Chem ; 36(1): 831-846, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33752569

RESUMO

Small molecule modulators of mitochondrial function have been attracted much attention in recent years due to their potential therapeutic applications for neurodegenerative diseases. The mitochondrial translocator protein (TSPO) is a promising target for such compounds, given its involvement in the formation of the mitochondrial permeability transition pore in response to mitochondrial stress. In this study, we performed a ligand-based pharmacophore design and virtual screening, and identified a potent hit compound, 7 (VH34) as a TSPO ligand. After validating its biological activity against amyloid-ß (Aß) induced mitochondrial dysfunction and in acute and transgenic Alzheimer's disease (AD) model mice, we developed a library of analogs, and we found two most active compounds, 31 and 44, which restored the mitochondrial membrane potential, ATP production, and cell viability under Aß-induced mitochondrial toxicity. These compounds recovered learning and memory function in acute AD model mice with improved pharmacokinetic properties.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Mitocôndrias/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Agregação Patológica de Proteínas/tratamento farmacológico , Bibliotecas de Moléculas Pequenas/farmacologia , Doença de Alzheimer/metabolismo , Doença de Alzheimer/patologia , Peptídeos beta-Amiloides/antagonistas & inibidores , Peptídeos beta-Amiloides/metabolismo , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Humanos , Ligantes , Camundongos , Mitocôndrias/metabolismo , Estrutura Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Agregação Patológica de Proteínas/metabolismo , Agregação Patológica de Proteínas/patologia , Bibliotecas de Moléculas Pequenas/síntese química , Bibliotecas de Moléculas Pequenas/química , Regulador Transcricional ERG/antagonistas & inibidores , Regulador Transcricional ERG/metabolismo
17.
Nutr Neurosci ; 24(11): 835-842, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31650903

RESUMO

Phlorotannin supplement (PS) is a natural hypnotic substrate that modulates γ-aminobutyric acid type A (GABAA)-benzodiazepine (BZD) receptors. However, there is a lack of functional data assessing the role of individual components of PS, such as Dieckol, as allosteric activators of GABAA receptors (GABAAR). Using the whole cell patch clamp technique, we demonstrated that PS functionally enhanced the activity of GABAA-BZD receptors in a heterologous system and in primary cultured neurons. Application of diazepam (DZP) or Dieckol (1) increased GABAAR-mediated inward current in HEK293T cells containing the α1 subunit in a dose-dependent manner, (2) which was blocked by co-treatment with the selective benzodiazepine site antagonist, flumazenil (FLZ); it also (3) increased the amplitude of GABAA-BZD receptors in primary cultured neurons, which was blocked by FLZ and (4) attenuated spontaneous activity in cultured neurons. These results indicate that PS and Dieckol act as positive allosteric activators of GABAA-BZD receptors, which might be the underlying mechanism of the sedative-hypnotic effect of PS. To our knowledge, this is the first study to directly link Dieckol-induced GABAAR activation via the BZD site binding and suppression of spontaneous neuronal activity in vitro.


Assuntos
Neurônios , Receptores de GABA-A , Benzofuranos , Células HEK293 , Humanos , Neurônios/metabolismo , Receptores de GABA-A/metabolismo , Ácido gama-Aminobutírico/farmacologia
18.
Nutr Res Pract ; 14(6): 568-579, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33282120

RESUMO

BACKGROUD/OBJECTIVES: Hepatic steatosis is the most common liver disorder, particularly in postmenopausal women. This study investigated the protective effects of standardized rice bran extract (RBS) on ovariectomized (OVX)-induced hepatic steatosis in rats. MATERIALS/METHODS: HepG2 cells were incubated with 200 µM oleic acid to induce lipid accumulation with or without RBS and γ-oryzanol. OVX rats were separated into three groups and fed a normal diet (ND) or the ND containing 17ß-estradiol (E2; 10 µg/kg) and RBS (500 mg/kg) for 16 weeks. RESULTS: RBS supplementation improved serum triglyceride and free fatty acid levels in OVX rats. Histological analysis showed that RBS significantly attenuated hepatic fat accumulation and decreased hepatic lipid, total cholesterol, and triglyceride levels. Additionally, RBS suppressed the estrogen deficiency-induced upregulation of lipogenic genes, such as sterol regulatory element-binding protein 1 (SREBP1), acetyl-CoA carboxylase 1, fatty acid synthase, glycerol-3-phosphate acyltransferase, and stearoyl-CoA desaturase 1. CONCLUSIONS: RBS and γ-oryzanol effectively reduced lipid accumulation in a HepG2 cell hepatic steatosis model. RBS improves OVX-induced hepatic steatosis by regulating the SREBP1-mediated activation of lipogenic genes, suggesting the benefits of RBS in preventing fatty liver in postmenopausal women.

19.
Front Pharmacol ; 11: 494, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32362829

RESUMO

We had previously demonstrated that phlorotannins, which are marine polyphenols, enhance sleep in mice via the GABAA-benzodiazepine (BZD) receptor. Among the constituents of phlorotannin, dieckol is a major marine polyphenol from the brown alga Ecklonia cava. Although phlorotannins are known to exert hypnotic effects, the sleep-enhancing effect of dieckol has not yet been determined. We evaluated the effect of dieckol on sleep-wake state of mice by analyzing electroencephalograms (EEGs) and electromyograms. Flumazenil, a GABAA-BZD antagonist, was used to investigate the molecular mechanism underlying the effects of dieckol on sleep. The polygraphic recordings and corresponding hypnograms revealed that dieckol accelerated the initiation of non-rapid eye movement sleep (NREMS); it shortened sleep latency and increased NREMS duration. According to the change in time-course, dieckol showed sleep-enhancing effects by increasing the amount of NREMS and decreasing wakefulness during the same hours. Additionally, sleep quality was evaluated by analyzing the EEG power density, and dieckol was found to not affect sleep intensity while zolpidem was found to reduce it. Finally, we treated mice with zolpidem or dieckol in combination with flumazenil and found the latter to inhibit the sleep-enhancing effect of dieckol and zolpidem, thereby indicating that dieckol exerts sleep-enhancing effects by activating the GABAA-BZD receptor, similar to zolpidem. These results implied that dieckol can be used as a promising herbal sleep aid with minimal side effects, unlike the existing hypnotics.

20.
Foods ; 9(2)2020 Feb 12.
Artigo em Inglês | MEDLINE | ID: mdl-32059391

RESUMO

Until now, most studies using calcium alginate gel (CAG) have been conducted primarily at room temperature (20 °C) without considering gelation temperature. Moreover, the effects of gelation temperature on the physical properties of CAG beads have not been studied in detail. We aimed to study the effect of gelation temperature on the physical properties (diameter, sphericity, and rupture strength) of CAG beads. Response surface methodology was used in this study. The independent variables were sodium alginate concentration (X1, 1.2%-3.6%, w/v), calcium lactate concentration (X2, 0.5%-4.5%, w/v), gelation temperature (X3, 5-85 °C), and gelation time (X4, 6-30 min). Diameter (Y1, mm), sphericity (Y2, %), and rupture strength (Y3, kPa) were selected as the dependent variables. A decrease in gelation temperature increased the diameter, sphericity and rupture strength of the CAG beads. Additionally, the CAG beads prepared at 5 °C exhibited the highest rupture strength (3976 kPa), lowest calcium content (1.670 mg/g wet), and a regular internal structure. These results indicate that decreasing the gelation temperature slows the calcium diffusion rate in CAG beads, yielding a more regular internal structure and increasing the rupture strength of the beads.

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