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1.
Spectrochim Acta A Mol Biomol Spectrosc ; 284: 121790, 2023 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-36081190

RESUMO

Recently, there has been an increasing demand for developing a reliable method to assess the quality of liquor in the baijiu industry quickly and accurately. The present study sought to establish a strategy for rapid quantitative analysis of the primary flavor components in Nongxiangxing baijiu. Under the experimental conditions, 7 of the 10 major flavor components in Nongxiangxing baijiu could be quantified effectively, such as ethyl butyrate (R2p = 0.9942), ethyl lactate (R2p = 0.9438), n-butanol (R2p = 0.9048), isobutanol (R2p = 0.9696), acetic acid (R2p = 0.9600), butyric acid (R2p = 0.8448), caproic acid (R2p = 0.9971). This result indicates that FT-IR combined with quantitative chemometric modeling could be a potential approach for rapid quality assessment of Nongxiangxing baijiu. Overall, this study provides a theoretical basis for subsequent related studies on Nongxiangxing baijiu.


Assuntos
1-Butanol , Quimiometria , Acetatos , Ácido Butírico , Espectroscopia de Infravermelho com Transformada de Fourier
2.
Food Chem ; 400: 133873, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36087477

RESUMO

To overcome the low production efficiency of Pickering emulsion stabilizers prepared from starch, alcohol precipitation and surface modification were applied in this study. Spherical starch nanoparticles (StNPs) (247.90 ± 1.96 nm) were prepared through nanoprecipitation. The StNPs were surface-esterified to produce starch nanoparticle acetate (StNPAc), and the physicochemical changes of the products were investigated. The contact angle (>89.56° ± 0.56°) of StNPAc (degree of substitution, 0.53) was maintained for over 30 min. The results showed that the hydrophobicity of the StNPs was improved by shielding the surface hydroxyl groups via acetylation. StNPAc was also used to produce emulsions for further evaluation of their feasibility as Pickering emulsifiers. Oil-in-water (3:7, v/v) emulsions containing 1.5 wt% StNPAc were stabilized for over 35 days without creaming. Thus, StNPAc exhibited better emulsifying capacity and storage stability than StNPs. Therefore, hydrophobic starch nanoparticles obtained by acetylation are promising stabilizers for surfactant-free Pickering emulsions.


Assuntos
Nanopartículas , Amido , Acetatos , Emulsões/química , Excipientes , Nanopartículas/química , Tamanho da Partícula , Amido/química , Água/química
3.
J Ethnopharmacol ; 300: 115739, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36126784

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Arnebia euchroma (Royle) I.M.Johnst. (AE) is a Chinese medicinal herb that is traditionally used to treat various circulatory diseases. It exhibits certain effects, such as the promotion of blood circulation and cooling, rash clearance, and detoxification. AIM OF THE STUDY: This study was designed to explore the hepatoprotective and hemostatic effects of the ethyl acetate extract of AE in rats with carbon tetrachloride (CCl4)-induced liver injury. MATERIALS AND METHODS: Wistar rats were treated via oral gavage with different doses of the ethyl acetate extract of AE (3.5, 7, or 14 g kg-1·day-1) for 14 consecutive days, following which hemostatic and liver function tests were conducted. For the hemostatic tests, the platelet count, blood platelet aggregation, blood platelet adhesion to fibrinogen, platelet factor 4 (PF-4) secretion from blood platelets, prothrombin time (PT), activated partial thromboplastin time (aPTT), thrombin time (TT), and fibrinogen levels were measured at the end of the treatment period. For the liver function tests, 0.25 mL/200 g (1.25 mL kg-1·day-1) of olive oil was injected into the abdominal cavity of the control rats, whereas 15% CCl4 plus olive oil (prescription: 7.5 mL CCl4 + 42.5 olive oil) was injected into that of the treated rats at 1 h after extract administration on day 6, 13, and 20. Additionally, food and water were withheld from all the animals. On the following day, the rats were anesthetized and their albumin, aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT), gamma-glutamyl transpeptidase (GGT), lactate dehydrogenase (LDH), reactive oxygen species (ROS), methane dicarboxylic aldehyde (MDA), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) levels were measured. Glutathione S-transferase (GST), glutathione reductase (GR), and glutathione peroxidase (GPx) levels among the groups were determined using a one-way analysis of variance. RESULTS: The platelet count and blood platelet aggregation, blood platelet adhesion to fibrinogen and PF-4 secretion levels were significantly increased in the (3.5 g kg-1 day-1) AE group as compared to those in the control group (all p < 0.001; for the 7 and 14 g kg-1 day-1 AE groups, all p > 0.05, respectively). Although the PT and aPTT were not affected by the AE extract (all p > 0.05), the TT was reduced and the FIB levels were significantly increased in all AE groups (p < 0.05). Liver function tests showed that CCl4 caused significant liver damage, thereby decreasing the albumin, SOD, CAT, GSH, GST, GR, and GPx levels, while increasing the AST, ALT, ALP, SGOT, SGPT, GGT, LDH, ROS, and MDA levels (all p < 0.001). By contrast, treatment with the different doses of AE extract reversed the CCl4 effects on all these parameters. Compared with the levels in the CCl4 group, the GSH and GR levels in the three AE groups (3.5, 7, and 14 g kg-1·day-1) were significantly higher (p < 0.05, p < 0.01, and p < 0.001, respectively), whereas the differences in the other parameters for these three groups were all at the significance levels of p < 0.05, p < 0.05, and p < 0.01, respectively. CONCLUSIONS: AE extracts administered orally exhibited hepatoprotective activity by affecting platelet production and blood coagulation and ameliorating liver function-damaging modifications. Specifically, a dosage of 3.5 g kg-1·day-1 resulted in the most optimal effects.


Assuntos
Boraginaceae , Doença Hepática Induzida por Substâncias e Drogas , Hemostáticos , Plantas Medicinais , Acetatos , Alanina Transaminase , Albuminas/farmacologia , Aldeídos , Fosfatase Alcalina , Animais , Antioxidantes/farmacologia , Aspartato Aminotransferases , Tetracloreto de Carbono/farmacologia , Catalase , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Fibrinogênio , Glutationa/farmacologia , Glutationa Peroxidase , Glutationa Redutase , Glutationa Transferase , Hemostáticos/farmacologia , Lactato Desidrogenases , Fígado , Metano/farmacologia , Azeite de Oliva , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Fator Plaquetário 4/farmacologia , Ratos , Ratos Wistar , Espécies Reativas de Oxigênio , Superóxido Dismutase , gama-Glutamiltransferase
4.
Bioresour Technol ; 367: 128218, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36332870

RESUMO

The culture method using sodium acetate and glucose, widely used as organic carbon sources in the mixotrophy of Haematococcus pluvialis, was compared with its autotrophy. In the 12-day culture, mixotrophy using sodium acetate and glucose increased by 40.4% and 77.1%, respectively, compared to autotrophy, but the mechanisms for the increasing biomass were different. The analysis of the mechanism was divided into autotrophic and heterotrophic metabolism. The mixotrophy with glucose increased the biomass by directly supplying the substrate and ATP to the TCA cycle while inhibiting photosynthesis. Gene expressions related to glycolysis and carbon fixation pathway were confirmed in autotrophy and mixotrophy with glucose and acetate. The metabolism predicted in the mixotrophy with acetate and glucose was proposed via autotrophic and heterotrophic metabolism analysis. The mechanism of Haematococcus pluvialis under mixotrophic conditions with high CO2 concentration was confirmed through this study.


Assuntos
Ciclo do Carbono , Glucose , Glucose/metabolismo , Acetato de Sódio , Biomassa , Carbono/farmacologia , Carbono/metabolismo , Acetatos
5.
Bioresour Technol ; 367: 128301, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36370937

RESUMO

Microalgae cannot meet the bait demand for aquaculture due to light intensity limitation and other disadvantageous conditions. This research selected 6 mixotrophic microalgae, and the optimal strains and organic carbon were screened. The results showed that Thalassiosira pseudonana and Chlorella sp. are suitable for mixotrophic culture. The maximum cell density of Thalassiosira pseudonana was found to be 1.67 times than that of the photoautotrophic group when glycerol was added. The maximum cell density of Chlorella sp. with acetic acid was 1.69 times than that of the photoautotrophic group. When the concentration of acetic acid was 5.0 g·L-1 and the concentration of KNO3 was 0.2 g·L-1, the maximum biomass of Chlorella sp. could reach 3.54 × 107 cells·mL-1; the maximum biomass of Thalassiosira pseudonana was 5.53 × 106 cells·mL-1 with 10.0 g·L-1 glycerol and 0.2 g·L-1 KNO3. Metabolomic analysis further revealed that mixotrophic bait microalgae could promote the accumulation of lipids and amino acids.


Assuntos
Chlorella , Microalgas , Microalgas/metabolismo , Biomassa , Chlorella/metabolismo , Carbono/metabolismo , Glicerol/metabolismo , Nutrientes , Acetatos/metabolismo
6.
Sci Total Environ ; 856(Pt 1): 159100, 2023 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-36174700

RESUMO

Hydrogen (H2) assisted ex-situ biogas upgrading and liquid chemicals production can augment the fossil fuel-dominated energy market, and alleviate CO2-induced global warming. Recent investigations confirmed that nanoscale zero-valent iron (nZVI) enabled the enhancement of anaerobic digestion for biogas production. However, little is known about the effect of nZVI on the downstream ex-situ biogas upgrading. Herein, different levels (0 mg L-1, 100 mg L-1, 200 mg L-1, 500 mg L-1, 1000 mg L-1, 2000 mg L-1) of nZVI were added for H2-assisted ex-situ biogas upgrading, to study whether nZVI could impact the biomethane purity and acetate yield for the first time. Results showed that all tested nZVI levels were favorable for biogas upgrading in the presence of H2, the highest biomethane content (94.1 %, v/v), the CO2 utilization ratio (95.9 %), and acetate yield (19.4 mmol L-1) were achieved at 500 mg L-1 nZVI, respectively. Further analysis indicated that increased biogas upgrading efficiency was related to an increase in extracellular polymeric substances, which ensures the microbial activity and stability of the ex-situ biogas upgrading. Microbial community characterization showed that the Petrimonas, Romboutsia, Acidaminococcus, and Clostridium predominated the microbiome during biogas upgrading at 500 mg L-1 nZVI with H2 supply. These results suggested that nZVI and H2 contributed jointly to promoting the bioconversion of CO2 in biogas to acetate. The findings could be helpful for paving a new way for efficient simultaneous ex-situ biogas upgrading and liquid chemicals recovery.


Assuntos
Biocombustíveis , Hidrogênio , Metano/química , Ferro , Dióxido de Carbono , Acetatos
7.
Enzyme Microb Technol ; 162: 110145, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36335859

RESUMO

Herein, we describe the impact of the introduction of tertiary amines as additive during the enzymatic kinetic resolution via deacylation of some arylalkyl acetates 1a-8a under promiscuous conditions. Two CAL-B preparations were examined: Novozym®435 and CHIRAZYME® L-2, c.-f. C2, lyo. The influence of the introduction of seven amines is checked: Triethylamine (Et3N), Pyridine, 4-Dimethylaminopyridine (4-DMAP), 1,4-Diazabicyclo[2.2.2]octane (DABCO), Cinchonine, Cinchonidine, Quinine and Quinidine; and that in two organic solvent: diisopropylether (DIPE) and tertiobutylmethyl ether (TBME). Among the examined amines, the use of DABCO as additive recorded the best results in terms of reactivity and selectivity. It was to be highlighted that this additive was reported as an enzyme activator for the first time in the enzymatic kinetic resolution via hydrolysis of racemic acetates under non-aqueous conditions. Both CAL-B preparations showed the same behavior in the presence of the chosen additives during the biodeacylation of the resolved acetates. No direct correlation between the pKa values of several used additives and the CAL-B activation rates has been revealed. An ideal enzymatic kinetic resolution was recorded with the acetate 4a (Conv 50% and E > >200).


Assuntos
Acetatos , Aminas , Estereoisomerismo , Solventes , Hidrólise
8.
Sci Total Environ ; 857(Pt 1): 159267, 2023 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-36208766

RESUMO

With increased understanding of the differences in toxicity between species of haloacetic acids (HAAs) and the possibility of more stringent regulations, the ability to predict individual HAA species formation is important. Nine different haloacetic acids are regulated and their total concentration is referred to as HAA9. A mathematical model to predict concentrations of HAA species was proposed and tested using independent data sets. The amount of HAA9 formed per unit amount of chlorine consumed (µg-HAA9/mg-consumed chlorine) remained constant throughout the reaction times in each sample. Similarly, the fraction of a given HAA species largely remained constant during most of the reaction time. Thus, each HAA species was assumed to have its own yield with respect to consumed chlorine in a given water sample. The parallel second-order (2R) model describing chlorine decay kinetics was then extended to predict HAA species formation kinetics. The combined chlorine and HAA species model closely predicts all tested HAA species and its sum with standard error ≤ 5 µg/L. Within the tested waters having Cl2/N mass ratio ≥ 10.7 (g-Cl2/g-N), ammonia did not impact the mass yield. The mass yield of each HAA species can be calculated from three measurements (e.g. at 0, 4 and 24 h) of HAA species and chlorine. Once the yield is known, HAA species concentrations could be predicted for up to 120 h with only chlorine measurements. The model extends the previous work of predicting the trihalomethane species formation kinetics to HAA species formation kinetics. Further research is needed to understand how the yield varies with source water quality, treatment and in distribution systems.


Assuntos
Desinfetantes , Poluentes Químicos da Água , Purificação da Água , Cloro , Purificação da Água/métodos , Trialometanos/análise , Acetatos , Cloretos , Abastecimento de Água , Poluentes Químicos da Água/análise , Desinfecção/métodos
9.
Bioresour Technol ; 367: 128066, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36202284

RESUMO

Cyanobacteria-derived biofuels can be helpful in achieving a circular bioeconomy. To increase the production of biodiesel/bioethanol from cyanobacterium, Pseudanabaena mucicola GO0704, mixotrophic cultivation using volatile fatty acid (VFA), a cheap organic carbon source, was performed. The treatment of butyric acid or acetic acid enhanced the cell growth, particularly, the dry weight of the butyric acid-treated cells was 2.30-fold higher than the control. The enhancement of the growth led to the increase of metabolite (i.e., lipid and carbohydrate) productions, resulting in high amount of biodiesel and bioethanol to be produced. Butyric acid was more effective compared to acetic acid and the productions of biodiesel (52.2 mg/L) and bioethanol (132.6 mg/L) from the butyric acid-treated P. mucicola GO0704 were 2.34- and 2.17-fold higher compared to the control, respectively. This study will provide a foundation to commercialize the cyanobacteria-based carbon-neutral fuels, and ultimately, achieve a circular bioeconomy.


Assuntos
Cianobactérias , Microalgas , Biocombustíveis , Biomassa , Ácido Butírico/metabolismo , Ácidos Graxos Voláteis/metabolismo , Carbono/metabolismo , Carboidratos , Acetatos/metabolismo , Microalgas/metabolismo
10.
Food Chem ; 400: 134051, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36067692

RESUMO

This pioneering investigation involved the application of accentuated cut edges (ACE) technique to Sauvignon blanc winemaking. The concentration of varietal thiol precursors in juice was significantly higher for ACE treatment compared to conventional crushing, with two-way or three-way interactions of the experimental factors, which included yeast strain and malolactic fermentation, being determined from the wine data. ACE yielded higher concentrations of 4-methyl-4-sulfanylpentan-2-one (4-MSP) and enantiomers of 3-sulfanylhexanol (3-SH) and 3-sulfanylhexyl acetate (3-SHA) in wines that were more abundant in phenolic compounds. Compared to Sauvy yeast strain, VIN13 produced greater amounts of 3-SH and 3-SHA but less 4-MSP with wines exhibiting lower intensity 'floral' and 'fruity' notes. MLF increased 3-SH and 4-MSP concentrations and led to wines that exhibited more non-fruity sensory attributes. The study revealed the potential of ACE for increasing varietal thiol concentrations in Sauvignon blanc wine and altering overall sensory profiles, with interactions involving yeast strain and MLF.


Assuntos
Vitis , Vinho , Acetatos , Fermentação , Saccharomyces cerevisiae , Compostos de Sulfidrila/análise , Vitis/química , Vinho/análise
11.
J Am Chem Soc ; 144(46): 21232-21243, 2022 Nov 23.
Artigo em Inglês | MEDLINE | ID: mdl-36350298

RESUMO

Serpentinizing hydrothermal systems generate H2 as a reductant and harbor catalysts conducive to geochemical CO2 conversion into reduced carbon compounds that form the core of microbial autotrophic metabolism. This study characterizes mineral catalysts at hydrothermal vents by investigating the interactions between catalytically active cobalt sites and silica-based support materials on H2-dependent CO2 reduction. Heteroatom incorporated (Mg, Al, Ca, Ti, and Zr), ordered mesoporous silicas are applied as model support systems for the cobalt-based catalysts. It is demonstrated that all catalysts surveyed convert CO2 to methane, methanol, carbon monoxide, and low-molecular-weight hydrocarbons at 180 °C and 20 bar, but with different activity and selectivity depending on the support modification. The additional analysis of the condensed product phase reveals the formation of oxygenates such as formate and acetate, which are key intermediates in the ancient acetyl-coenzyme A pathway of carbon metabolism. The Ti-incorporated catalyst yielded the highest concentrations of formate (3.6 mM) and acetate (1.2 mM) in the liquid phase. Chemisorption experiments including H2 temperature-programmed reduction (TPR) and CO2 temperature-programmed desorption (TPD) in agreement with density functional theory (DFT) calculations of the adsorption energy of CO2 suggest metallic cobalt as the preferential adsorption site for CO2 compared to hardly reducible cobalt-metal oxide interface species. The ratios of the respective cobalt species vary depending on the interaction strength with the support materials. The findings reveal robust and biologically relevant catalytic activities of silica-based transition metal minerals in H2-rich CO2 fixation, in line with the idea that autotrophic metabolism emerged at hydrothermal vents.


Assuntos
Dióxido de Carbono , Dióxido de Silício , Dióxido de Carbono/química , Titânio , Cobalto/química , Formiatos , Acetatos
12.
Drugs ; 82(15): 1549-1556, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36331779

RESUMO

An oral fixed-dose combination of relugolix/estradiol/norethisterone (also known as norethindrone) acetate (Ryeqo®; Myfembree®) has been approved for the management of heavy menstrual bleeding associated with uterine fibroids in the USA and management of moderate to severe symptoms of uterine fibroids in the EU. Relugolix is a gonadotropin releasing hormone (GnRH) receptor antagonist that decreases serum estradiol and progesterone concentrations to postmenopausal levels. The addition of estradiol/norethisterone acetate to relugolix ameliorates relugolix-induced bone loss and hot flush. In the two phase 3 LIBERTY trials, relugolix + estradiol/norethisterone substantially decreased menstrual bleeding and improved a range of other uterine fibroid symptoms in women with uterine fibroids-associated heavy menstrual bleeding. The combination was generally well tolerated, with vasomotor symptoms being the most common adverse reaction. Treatment with this combination for over up to 2 years did not induce a clinically meaningful bone loss in the majority of women. Relugolix/estradiol/norethisterone acetate, with its convenient once-daily administration, is a useful addition to current pharmacological treatment options for premenopausal women with symptomatic uterine fibroids.


Uterine fibroids are a common type of noncancerous tumours that grow in the uterus. In some women, these tumours cause debilitating symptoms, such as heavy menstrual bleeding, pelvic pain and passing of blood clots. Hysterectomy is the only definitive treatment for this condition, but is associated with some disadvantages. Less invasive procedures and medical treatments are now available to treat these symptoms. Recently, a fixed-dose tablet comprising relugolix, estradiol and norethisterone acetate (Ryeqo®; Myfembree®) has been approved to treat symptoms of uterine fibroids. This combination works by suppressing ovarian hormone levels. In clinical trials, relugolix + estradiol/norethisterone substantially reduced menstrual bleeding and improved several other symptoms in women with uterine fibroids-associated heavy menstrual bleeding. The combination was generally well tolerated and had a minimal impact on bone loss, a known adverse effect of such therapies. With its convenient once-daily administration, relugolix/estradiol/norethisterone acetate is a useful addition to current medical treatment options for premenopausal women with symptomatic uterine fibroids.


Assuntos
Leiomioma , Menorragia , Neoplasias Uterinas , Feminino , Humanos , Acetato de Noretindrona , Menorragia/complicações , Menorragia/tratamento farmacológico , Neoplasias Uterinas/complicações , Neoplasias Uterinas/tratamento farmacológico , Leiomioma/tratamento farmacológico , Noretindrona/efeitos adversos , Estradiol/uso terapêutico , Acetatos/uso terapêutico
13.
Pharmacol Res ; 186: 106536, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36332810

RESUMO

Adrenergic ß2-agonists represent a mainstay in asthma management. Their chronic use has been associated with decreased bronchoprotection and rebound hyperresponsiveness. Here we investigate on the possible therapeutic advantage of a pharmacological association of ß2-agonists with montelukast, a highly selective leukotriene receptor antagonist, in modulating bronchial reactivity and controlling asthma features. The study has been conducted in vitro and in vivo and also takes advantage of the synthesis of a salt that gave us the possibility to simultaneously administer in vivo formoterol and montelukast (MFS). In vitro studies demonstrate that montelukast (1) preserves ß2-agonist response in isolated bronchi by preventing homologous ß2-adrenoceptor desensitization; (2) reduces desensitization by modulating ß2-receptor translocation in bronchial epithelial cells. In vivo studies demonstrate that sensitized mice receiving formoterol or montelukast display a significant reduction in airway hyperresponsiveness, but the ß2-agonist relaxing response is still impaired. Allergen challenge causes ß2 heterologous desensitization that is further increased by treatment in vivo with formoterol. Conversely MFS not only inhibits airway hyperresponsiveness but it rescues the ß2-agonist response. Histological analysis confirms the functional data, demonstrating an enhanced therapeutic efficiency of MSF in controlling also pulmonary metaplasia and lung inflammation. MFS is efficacious also when sensitized mice received the drug by local administration. In conclusion, the data obtained evidenced a therapeutic advantage in the association of ß2-agonists with montelukast in the control of asthma-like features and a better rescue bronchodilation response to ß2-agonists.


Assuntos
Agonistas Adrenérgicos beta , Asma , Camundongos , Animais , Fumarato de Formoterol/farmacologia , Fumarato de Formoterol/uso terapêutico , Agonistas Adrenérgicos beta/uso terapêutico , Asma/tratamento farmacológico , Acetatos/farmacologia , Acetatos/uso terapêutico
14.
Epilepsy Behav ; 137(Pt A): 108964, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36343532

RESUMO

INTRODUCTION: Acetate has been shown to have neuroprotective and anti-inflammatory effects. It is oxidized by astrocytes and can thus provide auxiliary energy to the brain in addition to glucose. Therefore, we hypothesized that it may protect against seizures, which is investigated here by feeding glyceryl triacetate (GTA), to provide high amounts of acetate without raising sodium or acid levels. METHOD: CD1 male mice were fed controlled diets with or without GTA for up to three weeks. Body weights, blood glucose levels, plasma short-chain fatty acid levels, and other hematological parameters were monitored. Seizure thresholds were determined in 6 Hz and maximal electroshock seizure threshold (MEST) tests. Antioxidant capacities were evaluated in the cerebral cortex and plasma using a ferric reducing antioxidant power (FRAP) assay and Trolox equivalent antioxidant capacity assay. RESULTS: Body weight gain was similar with both diets with and without GTA in two experiments. Glyceryl triacetate-fed groups showed 2-3- and 1.6-fold increased acetate and propionate levels in plasma, respectively. Glucose levels were unaltered in blood collected from the tail tip but increased in trunk blood. No differences were found in the activity of cerebral cortex acetyl-CoA synthetase. In the 6 Hz threshold test, seizure thresholds were lower by 3 mA and 2.4 mA after 8 and 14 days, respectively, in the GTA compared to the control diet-fed group, but showed no difference on day 16, showing that GTA has small, but inconsistent proconvulsant effects in this model. In MEST tests, a slightly increased seizure threshold (1 mA) was found on day 19 in the GTA-fed group, but not in another experiment on day 21. There were no differences in antioxidant capacity in plasma or cortex between the two groups. CONCLUSION: Glyceryl triacetate feeding showed no antioxidant effects nor beneficial changes in acute electrical seizure threshold mouse models, despite its ability to increase plasma acetate levels.


Assuntos
Anticonvulsivantes , Convulsões , Animais , Camundongos , Masculino , Anticonvulsivantes/farmacologia , Anticonvulsivantes/uso terapêutico , Relação Dose-Resposta a Droga , Convulsões/tratamento farmacológico , Eletrochoque , Modelos Animais de Doenças , Acetatos/uso terapêutico , Glucose
15.
J Phys Chem A ; 126(46): 8562-8576, 2022 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-36378081

RESUMO

We studied the steps in the formation of active palladium catalyst species from palladium acetate dimer employing density functional theory calculations. We explored the possible pathways with an automated reaction search and studied the kinetics with stochastic simulation analysis. The dimeric form of palladium acetate is considered a resting state of the catalyst. Our reaction search starting from the dimeric form by sequential ligand addition resulted in experimentally observed monomeric species. We analyzed the bonding in the palladium acetate dimer and the role of Pd in the stability of the dimeric species. We implemented the Gillespie stochastic simulation algorithm to gain more insights into multichannel reaction paths and applied it to the degradation pathways. The analysis of the thermodynamic and kinetic data for these degradation pathways suggests that the dimeric form of the catalyst can be a potential catalytic precursor in the palladium acetate-catalyzed coupling reactions under the experimental reaction conditions.


Assuntos
Acetatos , Paládio , Catálise , Cinética , Ligantes
16.
Molecules ; 27(21)2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36364335

RESUMO

We have developed a simple and convenient method for the synthesis of 3-aryl- and 3-hetaryl-1,2,4-oxadiazin-5-ones bearing an easily functionalizable (methoxycarbonyl)methyl group at position 6 via the reaction of aryl or hetaryl amidoximes with maleates or fumarates. The conditions for this reaction were optimized. Different products can be synthesized selectively in good yields depending on the base used and the ratio of reactants: substituted (1,2,4-oxadiazin-6-yl)acetic acids, corresponding methyl esters, or hybrid 3-(aryl)-6-((3-(aryl)-1,2,4-oxadiazol-5-yl)methyl)-4H-1,2,4-oxadiazin-5(6H)-ones. The reaction is tolerant to substituents' electronic and steric effects in amidoximes. As a result, a series of 2-(5-oxo-3-(p-tolyl)-5,6-dihydro-4H-1,2,4-oxadiazin-6-yl)acetic acids, their methyl esters, and 1,2,4-oxadiazoles based on them were prepared and characterized by HRMS, 1H, and 13C NMR spectroscopy. The structures of three of them were elucidated with X-ray diffraction.


Assuntos
Ésteres , Oxidiazóis , Oxidiazóis/química , Oximas , Acetatos
17.
Theranostics ; 12(17): 7319-7334, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36438501

RESUMO

Background: The gut microbiota plays a vital role in maintaining tissue homeostasis and regulating disease pathophysiology; however, the underlying mechanisms remain to be elucidated. We previously showed that mice depleted of gut microbiota with antibiotics (ABX mice) were more prone to cardiac rupture after infarction, suggesting that the gut microbiota impacts cardiac structural remodeling following injury. Here, we aimed to determine whether the gut microbiota is required for adaptive cardiac remodeling in response to pressure overload stress. Methods: Transverse aortic constriction (TAC) surgery was performed and cardiac function was evaluated by echocardiography and catheterization, followed by mechanical tests and extracellular matrix (ECM) studies. Germ-free mice with cecal microbiota transplantation were used for validation. 16S ribosomal DNA sequencing and PICRUSt2 analysis were applied to predict the key metabolic pathways. ABX mice were supplemented with the derived metabolic products and their efficacy was tested. To elucidate the underlying mechanism, we isolated mouse primary cardiac fibroblasts and treated them with the metabolites. Lastly, G-coupled protein receptor 41 (GPR41) and GPR43 double knockdown cardiac fibroblasts were generated and the anti-fibrogenic effect of metabolites was determined. Results: Cardiac hypertrophy and dysfunction were more severe in ABX-TAC mice compared to the controls. Moreover, TAC-induced fibrosis was more profound in ABX hearts, which was accompanied by disrupted ECM structure making the heart tissues mechanically weaker and more brittle. Reconstruction of healthy gut microbiota in germ-free mice successfully restored cardiac function and prevented excessive fibrosis and ECM disarray under stress. Furthermore, functional prediction identified acetate and propionate as critical mediators in the gut microbiota-modulated cardiac mechanics. Supplementation of acetate and propionate improved heart function, attenuated fibrosis, and reversed ECM disarray after TAC. In addition, treating primary cardiac fibroblasts with acetate and propionate attenuated cell contraction, inhibited myofibroblast formation, and reduced collagen formation after TGF-ß1 stimulus. Finally, knocking down GPR41 and GPR43 receptors in cardiac fibroblasts blunted the inhibitory effects of acetate and propionate. Conclusions: The gut microbiota is a potential therapeutic target for cardiac ECM remodeling and heart structural integrity. By establishing a healthy gut microbiome or replenishing the derived metabolites, we could improve cardiac health under dysbiosis after pressure-overload stress.


Assuntos
Microbioma Gastrointestinal , Camundongos , Animais , Propionatos/farmacologia , Coração , Fibrose , Acetatos
18.
Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi ; 38(11): 1011-1017, 2022 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-36328432

RESUMO

Objective To observe the role of connective tissue growth factor (CTGF) and collagen synthesis in anti-pulmonary fibrosis (PF) by Kiwi fruit essence(unsaturated fatty acid of actinidia chinesis planch seed oil)in rats. Methods Sixty male SD rats were randomly divided into control group, model group, Kiwi fruit essence (60, 120, 240 mg/kg) treatment groups, and 5 mg/kg prednisone acetate group, with 10 animals in each group. Rats in control group were intratracheally administered with 9 g/L sodium chloride solution, and animals in other groups were intratracheally administered with bleomycin A5 to establish PF model. From the second day on, rats in the latter 4 groups were intragastrically treated with Kiwi fruit essence of 60, 120 and 240 mg/kg and prednisone acetate of 5 mg/kg, respectively. Rats in control and model groups were treated with 9 g/L sodium chloride solution once a day. All rats were sacrificed on day 28, and then pulmonary tissues were removed. The extent of PF lesions were evaluated using HE and Masson staining. The contents of hydroxyproline (HYP) were measured by a commercial kit. The mRNA expressions of CTGF and α-smooth muscle actin (α-SMA) in pulmonary tissues was detected by quantitative real-time PCR. The protein expressions of CTGF, α-SMA, collagen type 1 (Col1) and Col3 were measured by Western blotting. The protein levels of CTGF were analyzed using immunohistochemical staining. Results Compared with the model group, the alveolitis and PF extent in 60, 120, 240 mg/kg Kiwi fruit essence treatment groups as well as 5 mg/kg prednisone acetate group were significantly alleviated, and the content of HYP and the expression of CTGF, α-SMA, Col1 and Col3 decreased. The changes of above indicators were dose-dependent among the (60, 120, 240) mg/kg Kiwi fruit essence treatment groups. Moreover, the above indicators were found higher in (60, 120) mg/kg Kiwi fruit essence treatment groups than those in 5 mg/kg prednisone acetate group, which, however, showed no significantly difference between 240 mg/kg Kiwi fruit essence treatment group and 5 mg/kg prednisone acetate group. Conclusion Kiwi fruit essence down-regulates CTGF expression and decreases the levels of α-SMA, leading to inhibition of Col1 and Col3 synthesis and alleviation of PF.


Assuntos
Actinidia , Óleos Voláteis , Fibrose Pulmonar , Ratos , Masculino , Animais , Actinidia/metabolismo , Fator de Crescimento do Tecido Conjuntivo/genética , Fator de Crescimento do Tecido Conjuntivo/metabolismo , Prednisona , Cloreto de Sódio , Ratos Sprague-Dawley , Fibrose Pulmonar/tratamento farmacológico , Fibrose Pulmonar/prevenção & controle , Fibrose Pulmonar/genética , Colágeno Tipo I/genética , Colágeno Tipo I/metabolismo , Ácidos Graxos Insaturados , Óleos Vegetais/farmacologia , Acetatos
19.
Respir Res ; 23(1): 279, 2022 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-36217131

RESUMO

BACKGROUND: Whether cysteinyl-leukotriene receptor antagonists (LTRAs) have a similar antitussive effect to inhaled corticosteroids and long-acting ß2-agonist (ICS/LABA), and that LTRA plus ICS/LABA is superior to LTRAs alone or ICS/LABA alone in treating cough variant asthma (CVA) remain unclear. This study aimed to investigate and compare the efficacy of montelukast alone, budesonide/formoterol alone and the combination of both in the treatment of CVA. METHODS: Ninety-nine CVA patients were assigned randomly in a 1:1:1 ratio to receive montelukast (M group: 10 mg, once daily), budesonide/formoterol (BF group: 160/4.5 µg, one puff, twice daily), or montelukast plus budesonide/formoterol (MBF group) for 8 weeks. The primary outcomes were changes in the cough visual analogue scale (VAS) score, daytime cough symptom score (CSS) and night-time CSS, and the secondary outcomes comprised changes in cough reflex sensitivity (CRS), the percentage of sputum eosinophils (sputum Eos%) and fractional exhaled nitric oxide (FeNO). CRS was presented with the lowest concentration of capsaicin that induced at least 5 coughs (C5). The repeated measure was used in data analysis. RESULTS: The median cough VAS score (median from 6.0 to 2.0 in the M group, 5.0 to 1.0 in the BF group and 6.0 to 1.0 in the MBF group, all p < 0.001), daytime CSS (all p < 0.01) and night-time CSS (all p < 0.001) decreased significantly in all three groups after treatment for 8 weeks. Meanwhile, the LogC5 and sputum Eos% improved significantly in all three groups after 8 weeks treatment (all p < 0.05). No significant differences were found in the changes of the VAS score, daytime and night-time CSSs, LogC5 and sputum Eos% among the three groups from baseline to week 8 (all p > 0.05). The BF and MBF groups also showed significant decreases in FeNO after 8 weeks treatment (p = 0.001 and p = 0.008, respectively), while no significant change was found in the M group (p = 0.457). Treatment with MBF for 8 weeks significantly improved the FEV1/FVC as well as the MMEF% pred and decreased the blood Eos% (all p < 0.05). CONCLUSIONS: Montelukast alone, budesonide/formoterol alone and a combination of both were effective in improving cough symptom, decreasing cough reflex sensitivity and alleviating eosinophilic airway inflammation in patients with CVA, and the antitussive effect and anti-eosinophilic airway inflammation were similar. Trial registration ClinicalTrials.gov, number NCT01404013.


Assuntos
Antitussígenos , Asma , Acetatos , Administração por Inalação , Corticosteroides/uso terapêutico , Antitussígenos/uso terapêutico , Asma/diagnóstico , Asma/tratamento farmacológico , Budesonida/uso terapêutico , Combinação Budesonida e Fumarato de Formoterol/uso terapêutico , Capsaicina , Tosse/diagnóstico , Tosse/tratamento farmacológico , Ciclopropanos , Fumarato de Formoterol/uso terapêutico , Humanos , Inflamação , Antagonistas de Leucotrienos , Quinolinas , Sulfetos
20.
Artigo em Inglês | MEDLINE | ID: mdl-36232220

RESUMO

Microglial activation has been found to play a crucial role in various neurological disorders. Proinflammatory substances overproduced by activated microglia, such as cytokines, chemokines, reactive oxygen species, and nitric oxide (NO), can result in neuroinflammation that further exacerbates the course of the diseases. This study aimed to explore the anti-inflammatory effect of the ethyl acetate extract of Pueraria mirifica on microglial activation. Lipopolysaccharide (LPS)-induced inflammation was used as a model to investigate the effects of P. mirifica on HAPI (highly aggressive proliferating immortalized), a rat microglial cell line. Administration of ethyl acetate extract from the tuberous roots of P. mirifica to HAPI cells dose-dependently reduced NO production and iNOS expression induced by LPS. Attenuation of IRF-1 (interferon regulatory factor-1) induction, one of the transcription factors governing iNOS expression, suggested that the inhibitory effect on NO production by the plant extract was at least partially mediated through this transcription factor. In addition, LPS-stimulated mRNA expression of MCP-1 (monocyte chemoattractant protein-1), IL-6 (interleukin-6), and TNF-α (tumor necrosis factor-α) was also suppressed with P. mirifica extract pretreatment. This study indicates that the ethyl acetate extract of P. mirifica could potentially serve as an anti-inflammatory mediator and may be useful in relieving the severity of neurological diseases where microglia play a role.


Assuntos
Lipopolissacarídeos , Pueraria , Acetatos , Animais , Anti-Inflamatórios/farmacologia , Quimiocina CCL2 , Quimiocinas/metabolismo , Citocinas/metabolismo , Fator Regulador 1 de Interferon/metabolismo , Interleucina-6/metabolismo , Lipopolissacarídeos/toxicidade , Microglia , Óxido Nítrico/metabolismo , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia , Pueraria/genética , Pueraria/metabolismo , RNA Mensageiro/metabolismo , Ratos , Espécies Reativas de Oxigênio/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
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