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1.
Psychol Res Behav Manag ; 16: 2045-2057, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37305220

RESUMO

Background: Workplace violence (WPV) had always been the focus of attention in all walks of lives, especially in the health fields. Previous studies had shown it adversely affected mental health for healthcare workers. In addition, both sleep quality and physical activity were supported to have impact on mental health. However, the mechanism of sleep quality and physical activity influence the association between WPV and mental health had not been explored, so the purpose of this paper was to explore this mechanistic link among workplace violence, sleep quality, physical activity, and mental health in Chinese health technicians. Methods: Cross-sectional study was conducted in 3 cities of China, totally 3426 valid questionnaires were collected. WPV, physical activity, and social-demographic variables were evaluated. The Pittsburgh Sleep Quality Index and the Kessler Psychological Distress Scale were used to measure sleep quality and mental health. Descriptive analysis, univariate analysis, Pearson correlation, and moderated mediation analysis were used to estimate prevalence of WPV, association between WPV and mental health, and the role of sleep quality and physical activity on association between WPV and mental health. Results: The prevalence of WPV was 52.2% among Chinese health technicians. After controlling social-demographic and work-related variables, sleep quality partially mediated the effect of WPV on mental health (indirect effect=0.829). Physical activity moderated the relationship between WPV and sleep quality (ß=0.235, p=0.013), but not find the moderating role between WPV and mental health (ß=0.140, p=0.474), and between sleep quality and mental health (ß=0.018, p=0.550). Conclusion: The rate of WPV among health technicians remained at an alarming level. Sleep quality and physical activity could mitigate the adverse effect of WPV on mental health. In the future, we could improve sleep quality and encourage health technicians to engage physical activity to decrease the negative effect of WPV on mental health.

2.
Bioorg Chem ; 129: 106193, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36242982

RESUMO

Anti-virulence strategy represents an emerging alternative strategy in the war against increasing prevalence of methicillin-resistant Staphylococcus aureus (MRSA) due to its milder selection pressure on bacterial resistance. Sortase A (SrtA), as an important virulence factor, is a membrane-localized cysteine transpeptidase which anchors cell surface proteins to the cell wall. Natural products in medicinal plants are the source of targeting bacterial virulence factors. Here, we found polyphenolic glycosides (1-15), including thirteen new derivatives isolated from the stems of Caesalpinia cucullata, exhibited weak to moderate SrtA inhibitory activity without affecting the growth of MRSA, and compound 7 (53.7 % inhibition at 100 µM) was superior to the positive control curcumin. Meanwhile, compounds 2, 4 and 8 could effectively reduce the dose of ceftiofur in combination in vitro with fractional inhibitory concentration index (FICI) ranging from 0.188 to 0.375, which meant polyphenolic glycosides have got antibacterial activity with different ways. Here, we reported all new compounds structures determined by spectroscopy methods and their antibacterial activities, together, the relationship between structures with the inhibitory efficiency. The results indicated that polyphenolic glycosides could be used as promising therapeutic agents to prevent resistance development for S. aureus infections.


Assuntos
Antibacterianos , Caesalpinia , Glicosídeos , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Caesalpinia/química , Glicosídeos/química , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana
3.
Expert Rev Respir Med ; 16(1): 79-89, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-34541972

RESUMO

BACKGROUND: To assess the efficacy and safety of corticosteroids in COVID-19 patients compared with standard care or placebo. METHODS: Electronic databases were searched to identify relevant studies. The mortality, adverse events, and other data from studies were pooled for statistical analysis. RESULTS: Ten randomized clinical trials were eligible for inclusion. Corticosteroid treatment in COVID-19 patients did not significantly reduce the risk of death (RR: 0.93; CI: 0.82, 1.05) and the need for mechanical ventilation (RR: 0.82; CI: 0.62, 1.08). No mortality reduction was also observed in the subgroup of patients requiring mechanical ventilation (RR: 0.90; CI: 0.79-1.03). The use of corticosteroids increased mortality in the subgroup of patients not requiring oxygen support (RR: 1.24; CI: 1.00-1.55). The survival benefit was observed in a low dosage of corticosteroids (RR: 0.90; CI: 0.84-0.97) and dexamethasone (RR: 0.90; 95% CI: 0.79-1.04). There was no difference in the rates of adverse events (RR: 1.13; CI: 0.58, 2.20) and secondary infections (RR: 0.87; CI: 0.66, 1.15). CONCLUSION: Corticosteroid treatment did not convincingly improve survival in severe COVID-19 patients. Low-dose dexamethasone could be considered as a drug for the treatment of COVID-19 patients. More high-quality trials are needed to further verify this conclusion.Expert Opinion: The effect of corticosteroids on patient survival highly depended on the selection of the right dosage and type and in a specific subgroup of patients. This meta-analysis, which included more RCTs, evaluated the safety and efficacy in severe COVID-19 patients and analyzed the effects of different types of corticosteroid treatments. Corticosteroid treatment did not convincingly improve survival in severe COVID-19 patients. But the low dose dexamethasone appear to have a role in the management of severe COVID-19 patients.


Assuntos
COVID-19 , Corticosteroides/efeitos adversos , Humanos , Ensaios Clínicos Controlados Aleatórios como Assunto , Respiração Artificial , SARS-CoV-2
4.
Bioorg Chem ; 111: 104886, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33836342

RESUMO

Our present and previous phytochemical investigations on Leptopus lolonum have resulted in the isolation of almost 30 phenylpropanoid-conjugated pentacyclic triterpenoids (PCPTs). During the continuous study on PCPTs, this kind of triterpenoid ester is considered as a natural product with low toxicity because of it's widely distribution in natural plants and edible fruits including kiwi fruit, durian, jujube, pawpaw, apple and pear. In the present work, we report the isolation, structural elucidation and cytotoxic evaluation of four new PCPTs (1-4) which obtained from L. lolonum. In addition, the possible biosynthesis pathway for 28-norlupane triterpenoid and potent effect of phenylpropanoid moiety for increasing the cytotxic effect of triterpenoids were also discussed. Among these compounds, compound 1 exhibited the highest cytotoxic effect on HepG2 cells with IC50 value of 11.87 µM. Further flow cytometry and western blot analysis demonstrated that 1 caused G1 cell cycle arrest by up-regulated the expression of phosphorylated p53 protein in HepG2 cells and induced cell apoptosis via MAPK and Akt pathways. These results emphasized the potential of PCPTs as lead compounds for developing anti-cancer drugs.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Malpighiales/química , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais/química , Propanóis/química , Propanóis/isolamento & purificação , Propanóis/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
5.
Bioorg Chem ; 107: 104628, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33461038

RESUMO

Most of Euphorbiaceae plants are considered as folk medicinal plants because of their various pharmacological effects. However, there are eight Leptopus genus plants which belong to Euphorbiaceae have never be investigated. Thus, four Leptopus genus plants were collected to study their chemical constituents and pharmacological activities. In the present work, the cytotoxicities of the extracts of four Leptopus genus plants were evaluated before phytochemical experiments. And nine new phenylpropanoid-conjugated pentacyclic triterpenoids, along with twenty-two known compounds were isolated from the whole plants of Leptopus lolonum. The structures of these new compounds were unequivocally elucidated by HRESIMS and 1D/2D NMR data. All triterpenoids were screened for their cytotoxicities against four cancer cell lines including HepG2, MCF-7, A549 and HeLa. Among these isolates, the triterpenoid with a phenylpropanoid unit showed increasing cytotoxicity on cancer cells, which suggested the importance of the phenylpropanoid moiety.


Assuntos
Antineoplásicos Fitogênicos/química , Malpighiales/química , Propanóis/química , Triterpenos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Malpighiales/metabolismo , Conformação Molecular , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Plantas Medicinais/química , Plantas Medicinais/metabolismo , Relação Estrutura-Atividade , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
6.
ACS Macro Lett ; 10(1): 9-13, 2021 01 19.
Artigo em Inglês | MEDLINE | ID: mdl-35548979

RESUMO

We report a simple and effective method to synthesize composite bowl-shaped colloidal particles composed of a magnetic bottom and polymer wall. The bowl-shape is determined by the stirring and the resulting centrifugal force acting on the components during the synthesis. By systematically varying the stirring speed, we have found the lower and upper bounds for the bowl formation. Moreover, the size and thickness of the bowl can be tuned by changing the amount of the TPM monomer during synthesis. Functional groups can be easily introduced in the solidifying step through the polymerization of TPM by adding initiators and functional monomers. For example, by copolymerization of glycomonomer with TPM, bowl-shaped particles with biological activity can be obtained. In addition, such composite particles can be further modified to produce micromotors with well-controlled motions.


Assuntos
Magnetismo , Polímeros , Polimerização
7.
Bioorg Chem ; 96: 103573, 2020 03.
Artigo em Inglês | MEDLINE | ID: mdl-31962203

RESUMO

In this paper, chemical investigation on the chloroform soluble fraction of seed kernels of Caesalpinia bonduc resulted in the isolation of five new cassane diterpenoids: norcaesalpinin O (1), norcaesalpinin P (2), caesalpinin MQ (3), caesall O/P (4/5) and seven known compounds (6-12). Compounds structures were elucidated by 1H NMR, 13C NMR, 2D NMR, HR-MS and ECD (electronic circular dichroism) spectral analysis. The characters for new compounds with the presence of an aromatized C ring or demethyl group at C-17 position in the structures were found. By means of bioactive screenings, the inhibitory effect on type-4 phosphodiesterase (PDE4, the target protein of asthma disease) and nuclear factor-kappa B (NF-κB) expression were valued. Compound 1 was found to exhibit moderate inhibitory activity on PDE4 and much better binding affinity than other structures by docking studies for interaction analyzing. Compounds 6, 10 and 11 displayed considerable inhibitory strength against NF-κB expression with inhibitory ratio 48.6%, 42.9% and 37.1% at 10 µM, respectively. The isolation of cassane-type diterpenoids with anti-inflammation activity from C. bonduc implied that this plant might be a good source for anti-inflammation agents finding.


Assuntos
Caesalpinia/química , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , NF-kappa B/antagonistas & inibidores , Inibidores de Fosfodiesterase/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Diterpenos/química , Simulação de Acoplamento Molecular , Estrutura Molecular , NF-kappa B/metabolismo , Análise Espectral/métodos
8.
Fitoterapia ; 134: 226-249, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30825578

RESUMO

Natural products, especially diterpenoids, are enriched with numerous compounds with a broad spectrum of therapeutic indications, suggesting that functional moieties serve as a core pharmacophore. Cassane diterpenoids (CAs), as the main and characteristic constituents of medical plants in the Caesalpinia genus, have been widely studied due to their bioactivities, and >450 compounds have been reported since the 1960s, including 283 compounds that have been reported in the past decade. There are five main types of structures for these compounds: tricyclic cassane diterpenoids with a fused furan ring (I) or butanolide lactone (II), tricyclic cassane diterpenoids (III), norcassane diterpenoids (IV), and other types (V). CAs derivatives have a wide range of biological properties, including anti-inflammatory, antimalarial, antitumour, antiviral, antimicrobial, antinociceptive, and antioxidant effects. This review highlights the role of the biosynthetic pathway, including those with abnormal skeletons, as well as advances in structure, pharmacological activities and primarily mechanisms of CAs obtained from the Caesalpinia genus. The findings herein provide new insights into the development of this kind of natural diterpenoids.


Assuntos
Caesalpinia/química , Diterpenos/química , Vias Biossintéticas , Diterpenos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia
9.
J Chem Inf Model ; 59(5): 2309-2323, 2019 05 28.
Artigo em Inglês | MEDLINE | ID: mdl-30801189

RESUMO

Cassane diterpenoids (CAs), recognized as main constituents of many medical plants of the genus Caesalpinia, exhibit diverse bioactivities, including anti-inflammatory and immunomodulatory activity, and also showed a therapeutic effect on rheumatoid arthritis (RA) according to previous work, including ours. In this study, 102 CA compounds were selected to explore the possible molecular mechanism of this class of natural products on anti-inflammatory and immunomodulatory activity using RA as a disease model through a series of in silico methods: chemical-similarity-based target prediction, molecular docking, and molecular dynamics (MD) simulation. As a consequence, four signaling pathways (TCR signaling pathway, TLR signaling pathway, VEGF signaling pathway, and osteoclast differentiation pathway) by which CAs exert their effect on inflammation and immunomodulation were identified. Furthermore, the binding modes of CAs complexing with several crucial targets, which were picked out by credible docking results and took part in these signaling pathways, were explored by MD simulations. This is the first time that the molecular mechanism of the anti-RA activity of natural CAs has been investigated with in silico methods, and these findings might explain the activity of CAs on anti-inflammation and immunomodulation, which could supply a valuable reference for drug design research on CAs.


Assuntos
Anti-Inflamatórios/farmacologia , Simulação por Computador , Diterpenos/farmacologia , Fatores Imunológicos/farmacologia , Anti-Inflamatórios/metabolismo , Caesalpinia/química , Diterpenos/metabolismo , Fatores Imunológicos/metabolismo , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Conformação Proteica , Transdução de Sinais/efeitos dos fármacos , Termodinâmica
10.
Polymers (Basel) ; 10(4)2018 Apr 21.
Artigo em Inglês | MEDLINE | ID: mdl-30966493

RESUMO

Shape is an essential property of polymeric particles. Herein, we propose a simple method to synthesize polymeric particles with a well-controlled concave shape. Our method takes advantage of the powerful seeded emulsion polymerization strategy with the well-known principle of "like dissolves like" in solvent chemistry. We first prepared polystyrene (PS) particles with a single dimple by seeded emulsion polymerization. Then the dimpled PS particles were dispersed in a dimethylformamide (DMF) and water mixture. Consequently, the non-crosslinked polymer chains inside the particle were dissolved by DMF, a good solvent for PS, and the PS chains migrated out of the particle, causing buckling of the dimple and enlargement of the concave. By systematic change of the fraction of DMF in the solvent mixture, we changed the amount of the dissolved PS chains, and achieved polymeric particles with precisely tuned degree of concaveness. These concave particles were found to readily self-assemble, driven by polymer-induced depletion interaction. The concave PS particles reported here provide potential building blocks for self-assembled polymeric materials, and new model systems for condensed matter research.

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