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1.
Pharmacol Res ; 176: 106083, 2022 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-35033647

RESUMO

The pathogenic hyper-inflammatory response has been revealed as the major cause of the severity and death of the Corona Virus Disease 2019 (COVID-19). Xuanfei Baidu Decoction (XFBD) as one of the "three medicines and three prescriptions" for the clinically effective treatment of COVID-19 in China, shows unique advantages in the control of symptomatic transition from moderate to severe disease states. However, the roles of XFBD to against hyper-inflammatory response and its mechanism remain unclear. Here, we established acute lung injury (ALI) model induced by lipopolysaccharide (LPS), presenting a hyperinflammatory process to explore the pharmacodynamic effect and molecular mechanism of XFBD on ALI. The in vitro experiments demonstrated that XFBD inhibited the secretion of IL-6 and TNF-α and iNOS activity in LPS-stimulated RAW264.7 macrophages. In vivo, we confirmed that XFBD improved pulmonary injury via down-regulating the expression of proinflammatory cytokines such as IL-6, TNF-α and IL1-ß as well as macrophages and neutrophils infiltration in LPS-induced ALI mice. Mechanically, we revealed that XFBD treated LPS-induced acute lung injury through PD-1/IL17A pathway which regulates the infiltration of neutrophils and macrophages. Additionally, one major compound from XFBD, i.e. glycyrrhizic acid, shows a high binding affinity with IL17A. In conclusion, we demonstrated the therapeutic effects of XFBD, which provides the immune foundations of XFBD and fatherly support its clinical applications.

2.
Int J Gen Med ; 15: 555-565, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35046713

RESUMO

Objective: This study aims at exploring the relationship between necroptosis-related miRNAs and colon cancer prognosis. Methods: We downloaded the miRNA sequencing data from the TCGA, and eight differentially expressed necroptosis-related miRNAs were screened. Then, we used Cox regression analysis to establish a prediction model of necroptosis-related miRNA. Finally, the prognosis related miRNAs were used to predict the target genes, and functional analysis was used to explore the potential mechanism of these target genes. Results: The miRNA-seq data of 444 COAD cases were downloaded from TCGA. We identified 8 differentially expressed miRNAs (has-miR-16-5p, has-miR-141-3p, has-miR-148a-3p, has-miR-425-5p, has-miR-7-5p, has-miR-223-3p, has-miR-200a-5p, and has-miR-500a-3p), then Cox analysis was performed for determining eight-miRNA signature prognostic biomarkers with obviously different OS. The area under the curve (AUC) of receiver operating characteristic (ROC) curve for predicting 1-, 3-, and 5-year survival were 0.663, 0.653 and 0.639, respectively. The multivariate analysis also implied that the risk score was an independent prognostic factor considering other confounding factors (HR = 1.847, 95% CI = 1.197-2.848, P = 0.006). According to the Kaplan-Meier analysis, the expression of hsa-miR-500a-3p (P = 0.003), hsa-miR-16-5p (P = 0.004) and hsa-miR-148a-3p (P = 0.035) significantly affected OS outcomes. We predicted the target genes of these three miRNAs and then screened 10 hub genes (CCND1, SMAD3, SMAD2, CDK1, TGFB2, CDC25A, CHEK1, VEGFA, CCNE1, WEE1). In addition, CHEK1 was associated with the survival prognosis. Conclusion: Our study demonstrated that necroptosis is closely associated with colon cancer, and the model of eight necroptosis-related miRNAs are potentially useful prognostic biomarkers and therapeutic targets for colon cancer.

3.
J Colloid Interface Sci ; 611: 255-264, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34953458

RESUMO

Carbon dots (CDs) have been widely used in recent years because of their excellent water solubility and abundant surface functional groups. However, compared with quantum dots or biological probes, the quantum yield of CDs is lower, and the fluorescence mainly concentrated in the blue-green range, which significantly limits the biological applications of CDs. Heteroatoms doping is the most common method to improve the luminescence of CDs. In this work, nitrogen and sulfur co-doped luminescent CDs were successfully synthesized by microwave assisted method using glutathione (GSH) and p-phenylenediamine (PPD) as raw materials. It can emit bright green fluorescence in ethanol solution, and the maximum emission wavelength is 535 nm when excited at 374 nm, and the absolute quantum yield is as high as 63%. Iron ion (Fe3+) can interact with the functional groups on the surface of the CDs to form CDs/Fe3+, which is a non-fluorescence complex, and Fe3+ can be reduced to ferrous ion (Fe2+). In other words, the reaction mechanism of CDs and Fe3+ is a combination of dynamic quenching and static quenching. The fluorescence of CDs quenched by Fe3+ can be restored by thiol, because there is a stronger binding force between sulfhydryl (-SH) on the surface of thiol and Fe3+, which enables CDs to be released. In addition, the CDs has good biocompatibility and stability, indicating that it has excellent potential in bioimaging. This discovery will expand the application of CDs in the fields of biosensing and imaging.


Assuntos
Carbono , Pontos Quânticos , Corantes Fluorescentes , Ferro , Nitrogênio , Compostos de Sulfidrila , Enxofre
4.
Sci Total Environ ; 805: 150262, 2022 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-34536861

RESUMO

Plants are either recognized to produce nitrous oxide (N2O) or considered as a medium to transport soil-produced N2O. To date, it is not clear whether in their habitat plants conduit N2O produced in soil or are a natural source. We aimed to understand role of plants in N2O emissions in field conditions. Therefore, rubber plants (Ficus elastica) were planted in the field; then plant and soil chambers were deployed simultaneously to collect gas samples, and 15N site preference (SP) of N2O was evaluated. The mean SP values of plant and soil emitted N2O were -20.85 ± 2.8‰ and -8.85 ± 1.08‰, respectively, and were significantly different (p < 0.0001); while bulk 15N of plant and soil emitted N2O were -10.83 ± 3.33‰ and -22.56 ± 3.37‰, respectively and were similar (p = 0.06). In the current study, soil always acted as a source of N2O, while plants were both source and sink. Plant and soil N2O fluxes had significant positive exponential relationship with both soil and air temperature. Soil water-filled pore space (WFPS) had significant negative linear relationship with only soil N2O fluxes. Plant N2O fluxes had significant positive linear relationship with plant respiration rates and negative linear relationship with plant surface areas. Based on the relationship between plant respiration rates and N2O fluxes, we suggest that mitochondria are the possible sites of N2O formation in plant cells while the relationship between plant surface areas and N2O fluxes suggests that roots are the parts of its formation in natural and field conditions. Our results suggest that plants are a natural source of N2O even at field conditions and challenge a view that plants are a medium to transport soil-produced N2O into the atmosphere.


Assuntos
Óxido Nitroso , Solo , Atmosfera , Óxido Nitroso/análise , Plantas , Água
5.
J Ethnopharmacol ; 283: 114701, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34606948

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Xuanfei Baidu Decoction (XFBD), one of the "three medicines and three prescriptions" for the clinically effective treatment of COVID-19 in China, plays an important role in the treatment of mild and/or common patients with dampness-toxin obstructing lung syndrome. AIM OF THE STUDY: The present work aims to elucidate the protective effects and the possible mechanism of XFBD against the acute inflammation and pulmonary fibrosis. METHODS: We use TGF-ß1 induced fibroblast activation model and LPS/IL-4 induced macrophage inflammation model as in vitro cell models. The mice model of lung fibrosis was induced by BLM via endotracheal drip, and then XFBD (4.6 g/kg, 9.2 g/kg) were administered orally respectively. The efficacy and molecular mechanisms in the presence or absence of XFBD were investigated. RESULTS: The results proved that XFBD can effectively inhibit fibroblast collagen deposition, down-regulate the level of α-SMA and inhibit the migration of fibroblasts. IL-4 induced macrophage polarization was also inhibited and the secretions of the inflammatory factors including IL6, iNOS were down-regulated. In vivo experiments, the results proved that XFBD improved the weight loss and survival rate of the mice. The XFBD high-dose administration group had a significant effect in inhibiting collagen deposition and the expression of α-SMA in the lungs of mice. XFBD can reduce bleomycin-induced pulmonary fibrosis by inhibiting IL-6/STAT3 activation and related macrophage infiltration. CONCLUSIONS: Xuanfei Baidu Decoction protects against macrophages induced inflammation and pulmonary fibrosis via inhibiting IL-6/STAT3 signaling pathway.


Assuntos
COVID-19/tratamento farmacológico , Medicamentos de Ervas Chinesas , Inflamação/tratamento farmacológico , Macrófagos/efeitos dos fármacos , SARS-CoV-2 , Transdução de Sinais/efeitos dos fármacos , Animais , Sobrevivência Celular/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Fibroblastos/efeitos dos fármacos , Regulação da Expressão Gênica/efeitos dos fármacos , Redes Reguladoras de Genes , Humanos , Interleucina-6/antagonistas & inibidores , Interleucina-6/genética , Interleucina-6/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Células NIH 3T3 , Fitoterapia , Fibrose Pulmonar/patologia , Fibrose Pulmonar/prevenção & controle , Células RAW 264.7 , Fator de Transcrição STAT3/antagonistas & inibidores , Fator de Transcrição STAT3/genética , Fator de Transcrição STAT3/metabolismo
6.
Sci Total Environ ; 802: 149695, 2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-34438127

RESUMO

Particle number size distribution (PNSD) is of importance for understanding the mechanisms of particle growth, haze formation and climate impacts. However, the measurements of PNSD aloft in megacities are very limited. Here we report the first simultaneous winter measurements of size-resolved particle number concentrations along with collocated gaseous species and aerosol composition at ground level and 260 m in Beijing. Our study showed that the vertical differences of particle number concentrations between ground level and aloft varied significantly as a function of particle size throughout the study. Further analysis illustrated the impacts of boundary dynamics and meteorological conditions on the vertical differences of PNSD. In particular, the temperature and relative humidity inversions were one of the most important factors by decoupling the boundary layer into different sources and processes. Positive matrix factorization analysis identified six sources of PNSD at both ground level and city aloft. The local source emissions dominantly contributed to Aitken-mode particles, and showed the largest vertical gradients in the city. Comparatively, the regional particles were highly correlated between ground level and city aloft, and the vertical differences were relatively stable throughout the day. Our results point towards a complex vertical evolution of PNSD due to the changes in boundary layer dynamics, meteorological conditions, sources, and processes in megacities.


Assuntos
Poluentes Atmosféricos , Aerossóis/análise , Poluentes Atmosféricos/análise , Pequim , China , Monitoramento Ambiental , Tamanho da Partícula , Material Particulado/análise , Estações do Ano
7.
Sci Total Environ ; 803: 150010, 2022 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-34487897

RESUMO

This study investigates the impact of aerosol liquid water content (ALWC) and related factors, i.e., relative humidity (RH), aerosol mass concentration (PM2.5), and aerosol hygroscopicity, on aerosol optical properties, based on field measurements made in the Pearl River Delta (PRD) region of China at the surface (1 November 2019 to 21 January 2020) and in the upper boundary layer (the 532-m Guangzhou tower from 1 February to 21 March 2020). In general, temporal variations in the ambient aerosol backscattering coefficient (ßp) and ALWC followed each other. However, the surface ßp and 532-m ßp had generally opposite diurnal variation patterns, caused by dramatic differences in PM2.5 and ambient RH between the surface and the upper boundary layer. The ambient 532-m RH was systematically higher than the surface RH, with the latter having a much pronounced diurnal cycle than the former. The surface PM2.5 concentration was systematically higher than the PM2.5 concentration at 532 m, and their diurnal cycle patterns were overall opposite. These dramatic differences reveal that the atmospheric variables, i.e., ambient RH and the PM2.5 concentration in the upper boundary layer, cannot be directly represented by the same variables at the surface. Vertical variability should be considered. Clear differences in the sensitivities of aerosol light scattering to ambient RH, PM2.5, and aerosol hygroscopicity between the two levels were found and examined. Aerosol chemical composition played a minor role in causing the differences between the two levels. In particular, ßp was more sensitive to PM2.5 at the surface level but more to the ambient RH in the upper boundary layer. The larger contribution of aerosol loading to the variability in ßp at the surface implies that local emission controls can decrease ßp and further improve atmospheric visibility effectively at the surface during winter in the PRD region.


Assuntos
Poluentes Atmosféricos , Material Particulado , Aerossóis/análise , Poluentes Atmosféricos/análise , China , Monitoramento Ambiental , Umidade , Material Particulado/análise , Molhabilidade
8.
Eur J Med Chem ; 229: 114044, 2022 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-34923430

RESUMO

In this study, we designed, synthesized, and evaluated a series of carbamate derivatives of N-salicyloyl tryptamine as multifunctional therapeutic agents for the treatment of Alzheimer's disease (AD). After screening the acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitory activities, target compound 1g stood out as a mixed type reversible dual inhibitor of AChE and BChE. In addition, molecular docking studies were conducted to explore the actions on AChE and BChE. The results showed that 1g could decrease the level of pro-inflammatory cytokines NO, iNOS, IL-6, TNF-α, and ROS, increase the level of anti-inflammatory cytokines IL-4, and inhibit the aggregation of Aß1-42. Moreover, the administration of 1g suppressed the activity of AChE in the brain. In a word, the compound 1g is effective for improving learning and memory behavior, blood-brain barrier permeation, pharmacokinetics, ChE inhibition, and anti-neuroinflammation. It may be considered as a promising multi-functional therapeutic agent for further investigation for the treatment of AD.

10.
Artigo em Inglês | MEDLINE | ID: mdl-34886197

RESUMO

The contrasting trends of surface particulate matter (PM2.5), ozone (O3), and nitrogen dioxide (NO2) and their relationships with meteorological parameters from 2015 to 2019 were investigated in the coastal city of Shanghai (SH) and the inland city of Hefei (HF), located in the Yangtze River Delta (YRD). In both cities, PM2.5 declined substantially, while O3 and NO2 showed peak values during 2017 when the most frequent extreme high-temperature events occurred. Wind speed was correlated most negatively with PM2.5 and NO2 concentrations, while surface temperature and relative humidity were most closely related to O3. All of the studied pollutants were reduced by rainfall scavenging, with the greatest reduction seen in PM2.5, followed by NO2 and O3. By contrast, air pollutants in the two cities were moderately strongly correlated, although PM2.5 concentrations were much lower and Ox (O3 + NO2) concentrations were higher in SH. Additionally, complex air pollution hours occurred more frequently in SH. Air pollutant concentrations changed more with wind direction in SH. A more effective washout effect was observed in HF, likely due to the more frequent strong convection and thunderstorms in inland areas. This research suggests pertinent air quality control measures should be designed accordingly for specific geographical locations.

11.
Wei Sheng Yan Jiu ; 50(6): 882-886, 2021 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-34949311

RESUMO

OBJECTIVE: To describe the feeding status of infant and young child aged 6-23 months in China. METHODS: Data was from the China Nutrition and Health Surveillance among 0-5 Years Old Children and Lactating Women in 2013.Stratified multistage cluster sampling method was used, and 9983 children aged 6-23 months were involved. We analyzed the infant and young child feeding practices with World Health Organization(WHO) 2021 updated indicators. Data analyses were conducted using the complex weight based on national census from National Bureau of Statistics in 2010.We used Rao-Scott Chi-square test for statistical difference. RESULTS: The proportions of children aged 6-23 months meeting minimum dietary diversity(MDD) was 34.5%(95% CI 28.8%-40.2%); it was over 50% in large cities, and only 20.4% in poor rural areas. The proportions of children aged 6-23 months meeting minimum meal frequency(MMF) was 69.2%(95% CI 64.7%-73.7%); it was about 80% in large cities, medium and small cities, and only 45.3% in poor rural areas. The proportions of children aged 6-23 months meeting minimum acceptable diet(MAD)was 23.7%(95% CI 19.2%-28.2%), it was 44.2% in large cities, and less than 10% in poor rural areas. No consistent differences were observed between boys and girls for all 3 dietary indicators(MDD, MMF and MAD), and there was significant difference in different areas and various months of age(P<0.05). CONCLUSION: The minimum dietary diversity and minimum acceptable diet among children aged 6-23 month were not optimal in China, especially in poor rural areas.


Assuntos
Fenômenos Fisiológicos da Nutrição do Lactente , Lactação , Aleitamento Materno , Criança , Pré-Escolar , China , Dieta , Comportamento Alimentar , Feminino , Humanos , Lactente , Alimentos Infantis , Recém-Nascido , Masculino , Fatores Socioeconômicos , Organização Mundial da Saúde
12.
Wei Sheng Yan Jiu ; 50(6): 887-893, 2021 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-34949312

RESUMO

OBJECTIVE: To develop the physical activity questionnaire for Chinese children aged 6-17 years old, in order to evaluate the children's physical activity. METHODS: After systematic review, expert review and preliminary investigation, the "6-to 17-year-old Chinese children physical activity questionnaire(CCPAQ)" was established to measure the weekly physical activity. Based on the sample size estimation and inclusion and exclusion criteria, 120 children aged 6-17 were selected from one survey site in the south and north of China. SAS 9.4 software and Mplus 8.0 software were used for factor analyses to validate the modes and types of physical activity measured by CCPAQ. RESULTS: This study included 119 subjects in total. Exploratory factor analyses were used to assess the 33 modes and 7 types of physical activity time and extract four and one common factor, respectively. Confirmatory factor analysis fitted a second-order 4 factors model and first-order 7 factors model. The evaluation index of the two models were χ~2/df=1.41 and χ~2/df=1.61, respectively, showing that the models fitting were acceptable. CONCLUSION: CCPAQ established in this study can effectively measure the physical activity of Chinese children aged 6-17 years.


Assuntos
Exercício Físico , Adolescente , Criança , China , Análise Fatorial , Humanos , Reprodutibilidade dos Testes , Inquéritos e Questionários
13.
Wei Sheng Yan Jiu ; 50(6): 909-913, 2021 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-34949315

RESUMO

OBJECTIVE: To explore the status of malnutrition and dietary behavior characteristics of children aged 3-5 in Tonghua, Nanchang, Changsha, Kunming and Weinan, and to analyze the relationship between them. METHODS: Data was from National Nutrition and Health Systematic Survey for 0-18 Years Old Children in China. A total of 1741 children were randomly selected from five cities by multi-stage stratified cluster sampling, and their physical fitness was measured and investigated by questionnaire. Chi-square test and multivariate binomial Logistic regression analysis were used to assess the relationship between nutritional deficiency and diet and feeding behavior. RESULTS: Among the investigated children, the underweight rate, stunting rate and wasting rate were 0.52%, 1.09% and 1.03%, respectively. Dietary behavior restriction was the risk factor for stunting(OR=4.72, 95% CI 1.41-15.84), poor eating habits were the risk factor for wasting(OR=3.64, 95% CI 1.01-13.34). No statistical association was found between underweight and diet and feeding behavior. CONCLUSION: The incidence of malnutrition among children aged 3-5 years in five urban areas of China is low. There is a correlation between malnutrition and poor diet and feeding behavior. Measures should be taken to correct the poor eating habits of children and the feeding behavior of caregivers, so as to improve the nutritional status of children.


Assuntos
Desnutrição , Adolescente , Criança , Pré-Escolar , China/epidemiologia , Cidades , Dieta , Humanos , Lactente , Recém-Nascido , Desnutrição/epidemiologia , Estado Nutricional , Prevalência
14.
Int J Gen Med ; 14: 9537-9545, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34916835

RESUMO

Background: Stroke and myocardial infarction (MI) are associated with each other, as demonstrated in observational studies. However, it is unclear whether this relationship is causal, and the purpose of this study was to explore the bidirectional causality between stroke and MI. Methods: Causality between stroke and MI was assessed using two-sample Mendelian randomization (MR). All genetic instruments related to stroke (40,585 cases; 406,111 controls) and MI (43,676 cases; 128,199 controls) were derived from large published genome-wide association study. The MR analysis was calculated with inverse-variance weighting, MR-Egger, weighted mode, weighted median, and simple mode methods, and sensitivity analyses are used to detect the heterogeneity or pleiotropy. Results: Genetically predicted large-artery stroke (LAS) was causally related to higher odds of MI (odds ratio [OR] = 1.13, 95% confidence interval [CI]: 1.06-1.20, p = 1.0×10-4), and the causal effect of LAS on MI was significantly weakened (OR = 1.09, 95% CI: 1.02-1.17, p = 0.017) after excluding the multipotent single-nucleotide polymorphisms (SNPs). MI phenotypes were genetically correlated with all ischemic strokes (OR = 1.15, 95% CI: 1.03-1.28, p = 0.013) and LAS (OR = 1.39, 95% CI: 1.14-1.71, p = 0.001); but a causal effect of MI on all ischemic strokes (OR = 1.00, 95% CI: 0.95-1.28, p = 0.219) and LAS (OR = 1.26, 95% CI: 0.93-1.69, p = 0.130) was not observed after excluding the multipotent SNPs. Conclusion: This MR analysis provides evidence to support the causal effect of LAS subtype on MI, and some factors act as confiding factors whereas others may act as mediators.

15.
Int J Biol Macromol ; 2021 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-34742837

RESUMO

Curcumin has a wide range of pharmacological activities, but its poor water solubility, chemical instability, and low bioavailability extensively limit the further application in food and pharmaceutical systems. In this study, the potential of using soy protein (SP) to interact with, encapsulate and protect hydrophobic curcumin (Cur) by pH-shift method was evaluated. Results indicated that SP structure experienced a typical pathway from unfolding to refolding during the pH-shifting process (pH 7-12-7), which clearly expressed the encapsulation process of Cur by pH-shift method into SP. Then the physicochemical and morphological properties of soy protein-encapsulated curcumin nanoparticles (SP-Cur) were investigated. Fluorescence measurements and Isothermal Titration Calorimetry showed that the combination of Cur and SP was a spontaneous reaction with a decrease in Gibbs free energy, which was mainly driven by hydrophobic interaction. Fourier Transform Infra-Red and Ultraviolet Spectroscopy further showed that the Cur had successfully embedded into SP. SP-Cur had a spherical shape-like structure and relatively small size (d < 100 nm). The encapsulation efficiency of Cur showed a concentration-dependent manner, which could be as high as 97.43%. In addition, the SP-Cur exhibited enhanced thermal stability and photostability.

16.
Biomed Mater Eng ; 2021 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-34744059

RESUMO

BACKGROUND: The effectiveness and availability of conservative therapies for osteonecrosis of the femoral head (ONFH) are limited. Transplantation of bone marrow mesenchymal stem cells (BMSCs) combined with Bio-Oss, which is a good bone scaffold biomaterial for cell proliferation and differentiation, is a new potential therapy. Of note, the expression of miRNAs was significantly modified in cells cultured with Bio-Oss, and MiR-214 was correlated positively with osteonecrosis. Furthermore, miR-214 was upregulated in cells exposed to Bio-Oss. OBJECTIVE: To investigate whether targeting miR-214 further improves the transplantation effect. METHODS: We treated BMSCs with agomiR-214 (a miR-214 agonist), antagomiR-214 (a miR-214 inhibitor), or vehicle, followed by their transplantation into ONFH model rats. RESULTS: Histological and histomorphometric data showed that bone formation was significantly increased in the experimental groups (Bio-Oss and BMSCs treated with antagomiR-214) compared with other groups. CONCLUSIONS: miR-214 participates in the inhibition of osteoblastic bone formation, and the inhibition of miR-214 to bone formation during transplantation therapy with Bio-Oss combined with BMSCs for ONFH.

17.
Acta Pharm Sin B ; 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34745850

RESUMO

SARS-CoV-2 main protease (Mpro) is one of the most extensively exploited drug targets for COVID-19. Structurally disparate compounds have been reported as Mpro inhibitors, raising the question of their target specificity. To elucidate the target specificity and the cellular target engagement of the claimed Mpro inhibitors, we systematically characterize their mechanism of action using the cell-free FRET assay, the thermal shift-binding assay, the cell lysate Protease-Glo luciferase assay, and the cell-based FlipGFP assay. Collectively, our results have shown that majority of the Mpro inhibitors identified from drug repurposing including ebselen, carmofur, disulfiram, and shikonin are promiscuous cysteine inhibitors that are not specific to Mpro, while chloroquine, oxytetracycline, montelukast, candesartan, and dipyridamole do not inhibit Mpro in any of the assays tested. Overall, our study highlights the need of stringent hit validation at the early stage of drug discovery.

18.
J Clin Nurs ; 2021 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-34738289

RESUMO

AIMS: The study aimed to examine the impact of prenatal depression and diabetes management self-efficacy on postpartum stress and postpartum depression in women with gestational diabetes mellitus. BACKGROUND: Poor perinatal mental health is linked to various adverse pregnancy outcomes in women with gestational diabetes mellitus. DESIGNS: A predictive study design and the guidelines for the STROBE checklist were used for the study. METHODS: A total of 119 pregnant women with a positive 75 g-glucose challenge test were recruited at a medical centre. The Taiwanese depression questionnaire (TDQ), the diabetes management self-efficacy scale (DMSES) and the Hung postpartum stress scale (Hung PSS) were used for data collection at the 24th week of pregnancy and the first week after childbirth. RESULTS: Diabetes management self-efficacy was correlated with postpartum stress in women with gestational diabetes mellitus. Moreover, prenatal depression was a predictor of postpartum stress and postpartum depression, respectively, in women with gestational diabetes mellitus. CONCLUSIONS: Healthcare providers should assess those women's diabetes management self-efficacy and mood status during prenatal visits and offer the needed intervention to reduce the levels of postpartum stress and postpartum depression of those women after childbirth. RELEVANCE TO CLINICAL PRACTICE: A holistic care approach integrated diabetic care and mental health for women with gestational diabetes mellitus in a timely manner is warranted to promote perinatal mental health in women with gestational diabetes mellitus.

19.
Artigo em Inglês | MEDLINE | ID: mdl-34799045

RESUMO

The exploitation of efficient electrocatalyst is significantly important for degradation of refractory organic pollutants. Herein, a novel Ti/CoTiO3/Ce-PbO2 composite electrocatalyst (abbreviated as CTO/CP) is successfully constructed via facile consecutive immersion pyrolysis and electro-deposition method and then systematically characterized by scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), Fourier Transform infrared spectroscopy (FT-IR), energy dispersive spectroscopy (EDS) and near infrared chemical imaging (NIR-CI). Importantly, the electrochemical measurements demonstrate that the CTO/CP possesses numerous prominent properties such as lower charge transfer resistance, larger electroactive area, higher oxygen evolution potential than those of the pristine Ti/CoTiO3 (CTO) and Ti/Ce-PbO2 (CP). Thereby, the CTO/CP exhibits an enhanced electrocatalytic degradation performance with the degradation efficiency as high as 90.0% and COD removal rate of 88.3% at 180 min for the optimal CTO/CP (denoted as 10 layers of CTO and 1 h electrodeposition of CP), in which the ·OH is the major reactive species. Additionally, the optimal CTO/CP also shows a higher ICE/ACE together with lower EEC and desirable stability, universal applicability for many different dyes and reusability. Overall, this work offers a promising approach for enhancing the electrocatalytic properties of CTO via introducing CP.

20.
Food Funct ; 2021 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-34842883

RESUMO

Curcumin (Cur) is a bioactive phytochemical which is claimed to have several health-promoting benefits, whose applications are challenging due to its poor water-solubility, chemical instability, and low bioavailability. In this research, Cur was encapsulated in the cod protein (CP) using a pH-driven method to enhance its solubility and stability. The physicochemical and structural properties of cod protein-curcumin nanoparticles (CP-Cur) formed were characterized. Fluorescence spectroscopy (FL), ultraviolet spectroscopy (UV), circular dichroism (CD), and dynamic light scattering (DLS) results collectively suggest that the protein originally with a molten-globule state refolded into a more ordered structure after neutralization, during which Cur was incorporated. Fluorescence quenching and isothermal titration calorimetry (ITC) further showed that the CP/Cur binding was mainly driven by hydrophobic interactions, resulting in static fluorescence quenching and energy release. Up to 99.50% of Cur was loaded in the CP delivery system. Furthermore, the thermal stability and photostability of Cur were greatly improved due to the protection of the protein. The present study proved that cod protein could be a great potential edible carrier for encapsulating curcumin.

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