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1.
BMC Psychiatry ; 24(1): 244, 2024 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-38566055

RESUMO

BACKGROUND: Patients with schizophrenia (SZ) or bipolar disorder (BD) may have increased risk of complications from prescribed opioids, including opioid-induced respiratory depression. We compared prescription opioid pain medication dispensing for patients with SZ or BD versus controls over 5 years to assess dispensing trends. METHODS: This retrospective, observational study analysed US claims data from the IBM® MarketScan® Commercial and Multi-State Medicaid databases for individuals aged 18-64 years with prevalent SZ or BD for years 2015-2019 compared with age- and sex-matched controls. Baseline characteristics, comorbidities, and medication use were assessed. Proportions of individuals dispensed prescription opioids chronically (ie, ≥70 days over a 90-day period or ≥ 6 prescriptions annually) or nonchronically (≥1 prescription, chronic definition not met) were assessed. RESULTS: In 2019, the Commercial and Medicaid databases contained records for 4773 and 30,179 patients with SZ and 52,780 and 63,455 patients with BD, respectively. Patients with SZ or BD had a higher prevalence of comorbidities, including pain, versus controls in each analysis year. From 2015 to 2019, among commercially insured patients with SZ, chronic opioid-dispensing proportions decreased from 6.1% (controls: 2.7%) to 2.3% (controls: 1.2%) and, for patients with BD, from 11.4% (controls: 2.7%) to 6.4% (controls: 1.6%). Chronic opioid dispensing declined in Medicaid-covered patients with SZ from 15.0% (controls: 14.7%) to 6.7% (controls: 6.0%) and, for patients with BD, from 27.4% (controls: 12.0%) to 12.4% (controls: 4.7%). Among commercially insured patients with SZ, nonchronic opioid dispensing decreased from 15.5% (controls: 16.4%) to 10.7% (controls: 11.0%) and, for patients with BD, from 26.1% (controls: 17.5%) to 20.0% (controls: 12.2%). In Medicaid-covered patients with SZ, nonchronic opioid dispensing declined from 22.5% (controls: 24.4%) to 15.1% (controls: 12.7%) and, for patients with BD, from 32.3% (controls: 25.9%) to 24.6% (controls: 13.6%). CONCLUSIONS: The proportions of individuals dispensed chronic or nonchronic opioid medications each year were similar between commercially and Medicaid-insured patients with SZ versus controls and were higher for patients with BD versus controls. From 2015 to 2019, the proportions of individuals who were dispensed prescription opioids chronically or nonchronically decreased for patients with SZ or BD and controls.


Assuntos
Transtorno Bipolar , Esquizofrenia , Humanos , Analgésicos Opioides/uso terapêutico , Transtorno Bipolar/tratamento farmacológico , Dor , Padrões de Prática Médica , Prescrições , Estudos Retrospectivos , Esquizofrenia/tratamento farmacológico , Estados Unidos , Masculino , Feminino , Adolescente , Adulto Jovem , Adulto , Pessoa de Meia-Idade
2.
J Appl Toxicol ; 44(3): 344-354, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37718569

RESUMO

Narcissin is a natural flavonoid from some edible and traditional medicinal plants. It has been proven to have multiple biological functions and exhibits potential therapeutic effects on hypertension, cancer, and Alzheimer's disease. However, the toxicity of narcissin is largely unknown. Here, we revealed that narcissin treatment led to reduced hatchability, increased malformation rate, shorter body length, and slowed blood flow in zebrafish. Furthermore, bradycardia, pericardial edema, increased SV-BA distance, diminished stroke volume, ejection fraction, and ventricular short-axis shortening rate were also found. A large accumulation of ROS, increased apoptotic cells, and histopathological changes were detected in the heart region. Moreover, the gene expression profiles and molecular docking analysis indicated that Nrf2/HO-1 and calcium signaling pathways were involved in narcissin-induced toxicity. In conclusion, here we provide the first evidence that demonstrates narcissin-induced developmental toxicity and cardiotoxicity in zebrafish via Nrf2/HO-1 and calcium signaling pathways for the first time.


Assuntos
Flavonóis , Fator 2 Relacionado a NF-E2 , Peixe-Zebra , Animais , Peixe-Zebra/metabolismo , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Cardiotoxicidade , Sinalização do Cálcio , Simulação de Acoplamento Molecular , Embrião não Mamífero , Estresse Oxidativo
3.
Pak J Med Sci ; 39(3): 752-756, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37250537

RESUMO

Objectives: To investigate the difference of application of core needle biopsy histology and fine needle aspiration cytology in cervical lymphadenopathy. Methods: A retrospective analysis was made on 80 patients with cervical lymphadenopathy admitted to Baoding No.1 Central Hospital from to October 2018 to February 2020, and they were randomly divided into two groups: core needle group and fine needle group. Patients in the core needle group were given core needle biopsy histology, while those in the fine needle group were given fine needle aspiration cytology, and the puncture results and surgical complications were compared between the two groups. Results: The accuracy rates of the core needle group and the fine needle group in the diagnosis of malignant cervical lymph nodes were 95.83% and 72.22% respectively, with a statistically significant difference (χ²=4.683, p=0.030). The sensitivity, specificity, positive predictive value and negative predictive value of the core needle group were 100.00%, 93.75%, 95.83% and 100.00% respectively, while those of the fine needle group were 86.67%, 90.00%, 86.67% and 90.00% respectively, with no statistically significant differences between the two groups (p>0.05). The complication rate in the core needle group was 22.50%, which was higher than the 5.00% in the fine needle group (χ²=5.165, p=0.023). Conclusions: No significant difference was observed between core needle biopsy histology and fine needle aspiration cytology in diagnosing cervical lymphadenopathy, but the former has a high complication rate.

4.
Pak J Med Sci ; 38(6): 1477-1482, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35991229

RESUMO

Objectives: To compare the diagnostic efficacy of fine needle aspiration (FNA) and core needle biopsy (CNB) for metastatic lymph nodes guided by contrast-enhanced ultrasound (CEUS), and to provide reference for clinical selection of puncture methods. Methods: A total of 168 patients who were admitted to Baoding No.1 Central Hospital from June 2020 to January 2021 and required puncture of the diseased lymph nodes were included. Seventy six patients were guided by conventional ultrasound, of which 37 received FNA and 39 received CNB. 92 patients were guided by CEUS, of which 41 received FNA and 51 received CNB. The diagnostic accuracy of FNA and CNB guided by conventional ultrasound and CEUS was compared, and the sensitivity, specificity, positive predictive value, and negative predictive value of FNA and CNB in the diagnosis of metastatic lymph nodes guided by CEUS were further compared. Results: The diagnostic accuracy of FNA and CNB guided by CEUS were higher than that guided by conventional ultrasound, with a statistically significant difference (P<0.05). The sensitivity, specificity, positive predictive value, and negative predictive value of FNA and CNB in the diagnosis of metastatic lymph nodes were 95.0%, 95.2%, 95.0%, 95.2%, 100%, 100%, 100%, 100%, respectively, with statistically significant differences (P>0.05). Conclusion: CEUS can guide puncture and improve diagnosis accuracy. No statistical difference can be seen in the diagnostic efficacy of CNB and FNA for metastatic lymph nodes, CNB can provide more diagnostic information, while FNA can replace CNB for metastatic lymph nodes adjacent to blood vessels and difficult to operate.

5.
J Synchrotron Radiat ; 28(Pt 1): 207-213, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-33399570

RESUMO

Hard X-ray nanodiffraction provides a unique nondestructive technique to quantify local strain and structural inhomogeneities at nanometer length scales. However, sample mosaicity and phase separation can result in a complex diffraction pattern that can make it challenging to quantify nanoscale structural distortions. In this work, a k-means clustering algorithm was utilized to identify local maxima of intensity by partitioning diffraction data in a three-dimensional feature space of detector coordinates and intensity. This technique has been applied to X-ray nanodiffraction measurements of a patterned ferroelectric PbZr0.2Ti0.8O3 sample. The analysis reveals the presence of two phases in the sample with different lattice parameters. A highly heterogeneous distribution of lattice parameters with a variation of 0.02 Šwas also observed within one ferroelectric domain. This approach provides a nanoscale survey of subtle structural distortions as well as phase separation in ferroelectric domains in a patterned sample.

6.
J Org Chem ; 86(9): 6698-6710, 2021 05 07.
Artigo em Inglês | MEDLINE | ID: mdl-33881860

RESUMO

A copper-catalyzed, ligand-free intramolecular C-N coupling of (E)-2-(2-bromophenyl)-3-arylacrylamides has been developed. This protocol provides an efficient and practical synthetic route for the biologically important (E)-3-arylideneindolin-2-ones from o-bromophenylacetic acids and aromatic or conjugated alkenyl aldehydes. Readily available starting materials, mild and noble metal-free conditions, high efficiency, and good tolerability for phenolic hydroxyl groups make this approach attractive and applicable.


Assuntos
Aldeídos , Cobre , Catálise , Ligantes
7.
J Enzyme Inhib Med Chem ; 30(6): 995-1001, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25792506

RESUMO

A series of tacrine-propargylamine derivatives were synthesised and evaluated as possible anti-Alzheimer's disease (AD) agents. Among these derivatives, compounds 3a and 3b exhibited superior activities and a favourable balance of AChE and BuChE activities (3a: IC50 values of 51.3 and 77.6 nM; 3b: IC50 values of 11.2 and 83.5 nM). Compounds 3a and 3b also exhibited increased hAChE inhibitory activity compared with tacrine by approximately 5- and 28-fold, respectively, and low neurotoxicity. Importantly, these compounds also had lower hepatotoxicity than tacrine. Based on these results, compounds 3a and 3b could be considered as potential lead compounds for the treatment of AD and other AChE related diseases, such as schizophrenia, glaucoma and myasthenia gravis.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/efeitos adversos , Inibidores da Colinesterase/farmacologia , Células Estreladas do Fígado/efeitos dos fármacos , Pargilina/análogos & derivados , Propilaminas/efeitos adversos , Propilaminas/farmacologia , Tacrina/análogos & derivados , Tacrina/farmacologia , Acetilcolinesterase/metabolismo , Doença de Alzheimer/enzimologia , Doença de Alzheimer/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Relação Dose-Resposta a Droga , Células Estreladas do Fígado/citologia , Humanos , Estrutura Molecular , Pargilina/efeitos adversos , Pargilina/química , Pargilina/farmacologia , Propilaminas/química , Relação Estrutura-Atividade , Tacrina/efeitos adversos , Tacrina/química
8.
World J Surg Oncol ; 13: 203, 2015 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-26084574

RESUMO

Periosteal osteosarcoma is a rare subtype of osteosarcoma. Wide surgical removal is the commonly used treatment-method algorithm. However, the limb-salvage procedure of periosteal osteosarcoma in the distal tibia is a technical challenge to orthopedic surgeons because of the scarcity of soft tissue and subcutaneous nature in the anteromedial aspect. We encountered a 16-year-old female patient with periosteal osteosarcoma in the distal half of the left tibia diagnosed preoperatively based upon the CT images and a needle biopsy. A unique identical surgical technique was applied in the case, including marginal resection of the periosteal osteosarcoma with part of the tibia retained at the same level of bone defect and reconstruction using the autologous fibula graft. A combination of cisplatin and doxorubicin was received as chemotherapy after the operation. Postoperative incisional biopsy was performed, and the hematoxylin-eosin-stained results confirmed the diagnosis of periosteal osteosarcoma. The patient was followed up for 11 years. Radiological and clinical evaluation was performed at each follow-up. The retained tibia incorporated well with the fibula autograft, and excellent limb functional recovery was achieved. The patient was free from neoplastic disease at the latest follow-up. In conclusion, young patients with periosteal osteosarcoma without intramedullary involvement can be treated by marginal resection of the lesion with part of the tibia retained at the level of bone defect and reconstructed using a long autologous fibula graft. Subsequent chemotherapy with administration of cisplatin and doxorubicin is recommended.


Assuntos
Neoplasias Ósseas/cirurgia , Fíbula/transplante , Osteossarcoma/cirurgia , Periósteo/cirurgia , Procedimentos de Cirurgia Plástica/métodos , Tíbia/cirurgia , Adolescente , Feminino , Humanos , Transplante Autólogo
9.
Org Biomol Chem ; 12(31): 5936-44, 2014 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-24986600

RESUMO

Alzheimer's disease (AD) is currently one of the most difficult and challenging diseases to treat. Based on the 'multi-target-directed ligands' (MTDLs) strategy, we designed and synthesised a series of new compounds against AD by combining the pharmacophores of resveratrol and clioquinol. The results of biological activity tests showed that the hybrids exhibited excellent MTDL properties: a significant ability to inhibit self-induced ß-amyloid (Aß) aggregation and copper(II)-induced Aß aggregation, potential antioxidant behaviour (ORAC-FL value of 0.9­3.2 Trolox equivalents) and biometal chelation. Among these compounds, (E)-5-(4-hydroxystyryl)quinoline-8-ol (10c) showed the most potent ability to inhibit self-induced Aß aggregation (IC50 = 8.50 µM) and copper(II)-induced Aß aggregation and to disassemble the well-structured Aß fibrils generated by self- and copper(II)-induced Aß aggregation. Note that 10c could also control Cu(I/II)-triggered hydroxyl radical (OH˙) production by halting copper redox cycling via metal complexation, as confirmed by a Cu­ascorbate redox system assay. Importantly, 10c did not show acute toxicity in mice at doses of up to 2000 mg kg−1 and was able to cross the blood­brain barrier (BBB), according to a parallel artificial membrane permeation assay. These results indicate that compound 10c is a promising multifunctional compound for the development of novel drugs for AD.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Clioquinol/uso terapêutico , Bibliotecas de Moléculas Pequenas/uso terapêutico , Estilbenos/uso terapêutico , Absorção Fisiológica/efeitos dos fármacos , Doença de Alzheimer/patologia , Peptídeos beta-Amiloides/ultraestrutura , Animais , Antioxidantes/farmacologia , Barreira Hematoencefálica/efeitos dos fármacos , Barreira Hematoencefálica/patologia , Quelantes/química , Quelantes/uso terapêutico , Clioquinol/química , Cobre/toxicidade , Desenho de Fármacos , Radical Hidroxila/química , Camundongos , Oxirredução/efeitos dos fármacos , Permeabilidade/efeitos dos fármacos , Agregados Proteicos/efeitos dos fármacos , Resveratrol , Bibliotecas de Moléculas Pequenas/química , Espectrofotometria Ultravioleta , Estilbenos/química
10.
Bioorg Med Chem ; 22(4): 1355-61, 2014 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-24461494

RESUMO

A series of ebselen derivatives were designed, synthesised and evaluated as inhibitors of cholinesterases (ChEs) and glutathione peroxidase (GPx) mimics. Most of the compounds were found to be potent against AChEs and BuChE, compounds 5e and 5i, proved to be the most potent against AChE with IC50 values of 0.76 and 0.46 µM, respectively. Among these hybrids, most of the compounds were found to be good GPx mimics compare with ebselen. The selected compounds 5e and 5i were also used to determine the catalytic parameters and in vitro hydrogen peroxide scavenging activity. The results indicate that compounds 5e and 5i may be excellent multifunctional agents for the treatment of AD.


Assuntos
Acetilcolinesterase/química , Antioxidantes/síntese química , Azóis/química , Azóis/síntese química , Materiais Biocompatíveis/síntese química , Inibidores da Colinesterase/síntese química , Compostos Organosselênicos/química , Compostos Organosselênicos/síntese química , Acetilcolinesterase/metabolismo , Doença de Alzheimer/tratamento farmacológico , Antioxidantes/metabolismo , Antioxidantes/uso terapêutico , Azóis/metabolismo , Azóis/uso terapêutico , Materiais Biocompatíveis/metabolismo , Materiais Biocompatíveis/uso terapêutico , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/metabolismo , Inibidores da Colinesterase/uso terapêutico , Glutationa Peroxidase/química , Glutationa Peroxidase/metabolismo , Humanos , Isoindóis , Compostos Organosselênicos/metabolismo , Compostos Organosselênicos/uso terapêutico , Ligação Proteica
11.
Eur J Med Chem ; 275: 116590, 2024 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-38908104

RESUMO

The C797S mutation of EGFR leads to Osimertinib resistance by blocking the covalent binding of Cys797. To develop new agents that can overcome EGFR mutation resistance, thirty seven new cyclopropane sulfonamide derivatives were synthesized and evaluated as EGFRL858R/T790M/C797S or EGFRDel19/T790M/C797S inhibitors by structure-based screening. Most of the synthesized compounds exhibit good to excellent anti proliferation activity against to BaF3-EGFR L858R/T790M/C797S and BaF3-C797S/Del19/T790M cancer cell lines. Representative compounds 8l showed inhibitory activity against the two cancer cell lines with the IC50 values of 0.0012 and 0.0013 µM, respectively. Another compound 8h, exhibited slightly lower activity (0.0042 and 0.0034 µM of the IC50 values) to both of the two tri-mutation cell lines, but excellent activities against H1975 and PC9 cells with IC50 values of 13 and 19 nM, respectively. Considering the acquired drug resistance of tumors is a gradual process, we chose 8h for further in vivo and mechanism study. 8h was demonstrated significantly inhibited tumor growth with 72.1 % of the TGI in the BaF3/EGFR-TM xenograft tumor model and 83.5 % in the H1975-DM xenograft tumor model. Compound 8h was confirmed to be safe with no significant side effects as showed by the results of in vitro assay of human normal cells and the sections of animals major organs. Mechanism studies showed that in addition to inhibiting EGFR mutations, 8h can also target the tumor microenvironment and induce tumor cell apoptosis. All these results indicate that 8h deserves further investigation as an EGFR inhibitor to overcome C797S-mediated resistance.


Assuntos
Antineoplásicos , Proliferação de Células , Ciclopropanos , Resistencia a Medicamentos Antineoplásicos , Receptores ErbB , Mutação , Inibidores de Proteínas Quinases , Sulfonamidas , Receptores ErbB/antagonistas & inibidores , Receptores ErbB/genética , Receptores ErbB/metabolismo , Humanos , Sulfonamidas/farmacologia , Sulfonamidas/química , Sulfonamidas/síntese química , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Animais , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Relação Estrutura-Atividade , Proliferação de Células/efeitos dos fármacos , Inibidores de Proteínas Quinases/farmacologia , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/síntese química , Ciclopropanos/farmacologia , Ciclopropanos/química , Ciclopropanos/síntese química , Camundongos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular , Descoberta de Drogas , Linhagem Celular Tumoral , Camundongos Nus
12.
Front Bioeng Biotechnol ; 11: 1249875, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37576984

RESUMO

The incidence and mortality of cancer are gradually increasing. The highly invasive and metastasis of tumor cells increase the difficulty of diagnosis and treatment, so people pay more and more attention to the diagnosis and treatment of cancer. Conventional treatment methods, including surgery, radiotherapy and chemotherapy, are difficult to eliminate tumor cells completely. And the emergence of nanotechnology has boosted the efficiency of tumor diagnosis and therapy. Herein, the research progress of nanotechnology used for tumor diagnosis and treatment is reviewed, and the emerging detection technology and the application of nanodrugs in clinic are summarized and prospected. The first part refers to the application of different nanomaterials for imaging in vivo and detection in vitro, which includes magnetic resonance imaging, fluorescence imaging, photoacoustic imaging and biomarker detection. The distinctive physical and chemical advantages of nanomaterials can improve the detection sensitivity and accuracy to achieve tumor detection in early stage. The second part is about the nanodrug used in clinic for tumor treatment. Nanomaterials have been widely used as drug carriers, including the albumin paclitaxel, liposome drugs, mRNA-LNP, protein nanocages, micelles, membrane nanocomplexes, microspheres et al., which could improve the drug accumulate in tumor tissue through enhanced permeability and retention effect to kill tumor cells with high efficiency. But there are still some challenges to revolutionize traditional tumor diagnosis and anti-drug resistance based on nanotechnology.

13.
Psychiatr Serv ; 74(6): 659-662, 2023 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-36415993

RESUMO

Certified peer specialists (CPSs) may be uniquely situated to help address inequities within the behavioral health system. However, CPSs and other mental health care providers often do not have opportunities to discuss their experiences with racism in the workplace. The Southeast Mental Health Technology Transfer Center and Georgia Mental Health Consumer Network offered the six-part Racism and Recovery event series as a space for such discussions (N=356 participants). Participant responses on the Government Performance and Results Act survey (N=239) and supplemental Qualtrics survey (N=213) identified potential actions at the individual and organizational levels for disrupting racism. The responses indicated that the series was a feasible and well-received model for engaging diverse participants.


Assuntos
Serviços de Saúde Mental , Racismo , Humanos , Racismo/psicologia , Saúde Mental , Inquéritos e Questionários , Audição
14.
Front Plant Sci ; 14: 1230517, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37680364

RESUMO

Introduction: Sugarcane stem node detection is one of the key functions of a small intelligent sugarcane harvesting robot, but the accuracy of sugarcane stem node detection is severely degraded in complex field environments when the sugarcane is in the shadow of confusing backgrounds and other objects. Methods: To address the problem of low accuracy of sugarcane arise node detection in complex environments, this paper proposes an improved sugarcane stem node detection model based on YOLOv7. First, the SimAM (A Simple Parameter-Free Attention Module for Convolutional Neural Networks) attention mechanism is added to solve the problem of feature loss due to the loss of image global context information in the convolution process, which improves the detection accuracy of the model in the case of image blurring; Second, the Deformable convolution Network is used to replace some of the traditional convolution layers in the original YOLOv7. Finally, a new bounding box regression loss function WIoU Loss is introduced to solve the problem of unbalanced sample quality, improve the model robustness and generalization ability, and accelerate the convergence speed of the network. Results: The experimental results show that the mAP of the improved algorithm model is 94.53% and the F1 value is 92.41, which are 3.43% and 2.21 respectively compared with the YOLOv7 model, and compared with the mAP of the SOTA method which is 94.1%, an improvement of 0.43% is achieved, which effectively improves the detection performance of the target detection model. Discussion: This study provides a theoretical basis and technical support for the development of a small intelligent sugarcane harvesting robot, and may also provide a reference for the detection of other types of crops in similar environments.

15.
Biomed Pharmacother ; 160: 114315, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36716661

RESUMO

Gastric ulcer (GU) is one of the most prevalent digestive system diseases in humans, and it has been linked to inflammation. Previous studies have demonstrated the anti-inflammatory potential of isoalantolactone (IAL), a sesquiterpene lactone isolated from Radix Inulae. However, the pharmacological effects of IAL on GU and its mechanism of action are still unclear. Hence, the present study is aimed to investigate the anti-inflammatory potential of IAL on GU. Firstly, we assessed the effect of IAL on ethanol-induced injury of human gastric epithelial cells and the levels of inflammatory cytokines in cell culture supernatants. Then, the anti-inflammatory effects of IAL were confirmed in vivo using zebrafish inflammation models. Furthermore, the mechanism of IAL against GU was preliminarily discussed through network pharmacology and molecular docking studies. Quantitative real-time PCR assays were also used to confirm the mechanism of IAL action. ALB, EGFR, SRC, HSP90AA1, and CASP3 were found for the first time as the key targets of the IAL anti-GU. PI3K-Akt signaling pathway and Th17 cell differentiation were identified to play a crucial role in the anti-GU effects of IAL. In conclusion, we found that IAL has anti-inflammatory effects both in vitro and in vivo, and showed potential protective effects against ethanol-induced GU.


Assuntos
Sesquiterpenos , Úlcera Gástrica , Animais , Humanos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Etanol/farmacologia , Simulação de Acoplamento Molecular , Peixe-Zebra/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/prevenção & controle , Transdução de Sinais , Sesquiterpenos/farmacologia , Sesquiterpenos/uso terapêutico , Anti-Inflamatórios/uso terapêutico
16.
Sci Rep ; 13(1): 16817, 2023 10 05.
Artigo em Inglês | MEDLINE | ID: mdl-37798399

RESUMO

Crop divider toes are an essential device of sugarcane harvester. Moving forward against the ground is a critical way to improve the harvesting rate of lodged sugarcane. Height detection is the basis for precise control of crop divider toes moving forward against the ground. Due to the current problem of operating difficulties in manually adjusting the height of crop divider, a height detection system based on a millimeter wave radar sensor was designed to detect the height of crop divider toes from the ground. This paper proposed a height detection method of crop divider toes for sugarcane harvester based on Kalman adaptive adjustment. The data measured by the sensor was pretreated to determine whether the height had changed. Reset the Kalman filter and adjust the parameters when changes occur to improve the filter response speed and ranging accuracy. To adapt to the scenario of quickly adjusting the height of crop divider during the traveling process of sugarcane harvester. A one-way ANOVA test and a two-way ANOVA test were conducted on a simulated test platform. The results of the one-way ANOVA test showed that both forward speed and vegetation cover thickness had a significant effect on height detection accuracy. The results of the two-way ANOVA test showed that the interaction of forward speed and vegetation cover thickness did not have a significant effect on ranging accuracy. It was verified through experiments that both the ranging accuracy and the response speed of height change were significantly improved after the processing of the method in this paper. The mean square error after processing was lower than 2.5 cm. The feasibility of the height detection system was verified by field trials. The results of this study will provide a reference for the design of automatic elevation of crop divider.


Assuntos
Saccharum , Grão Comestível , Radar , Dedos do Pé
17.
Bioorg Med Chem Lett ; 22(24): 7683-7, 2012 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-23127891

RESUMO

A series of novel resveratrol derivatives were designed, synthesised and evaluated as potential therapeutic agents for the treatment of Alzheimer's disease. Among these compounds, compound 7l, (E)-5-(4-(isopropylamino)styryl)benzene-1,3-diol, exhibited potent ß-amyloid aggregation inhibition activity, which was confirmed by a ThT fluorescence assay (71.65% at 20 µM) and transmission electron microscopy (TEM). Compound 7l also exhibited good antioxidant activity (4.12 Trolox equivalents in an oxygen radical absorbance capacity assay and a 37% reduction in reactive oxygen species in cells at 10 µM). The cytotoxicity analysis of compounds 7f, 7i, 7j and 7l indicated that these compounds have lower toxicities than resveratrol at 60 µM.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides/antagonistas & inibidores , Antioxidantes/farmacologia , Desenho de Fármacos , Fármacos Neuroprotetores/farmacologia , Fragmentos de Peptídeos/antagonistas & inibidores , Estilbenos/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Espécies Reativas de Oxigênio/metabolismo , Resveratrol , Estilbenos/síntese química , Estilbenos/química , Relação Estrutura-Atividade
18.
J Phys Chem B ; 126(28): 5320-5325, 2022 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-35730616

RESUMO

The structural relaxation processes in a Ge3As52S45 molecular chalcogenide glass sample were directly studied by X-ray photon correlation spectroscopy (XPCS). XPCS was conducted at the first sharp diffraction peak at q = 1.16 Å-1 at temperatures ranging from 123 K to above the glass transition at 328 K, and the results showed two different dynamical regimes. At a low temperature, the observed glass dynamics are slow and dominated by X-ray-photon-induced effects, which are temperature independent. At a higher temperature, we observed a dramatic decrease in the fluctuation timescales, indicating that the dynamics were mainly due to the intermolecular correlation of the As4S3 molecule in the glass. The timescales in this high-temperature range agree well with those determined from measurements of the Newtonian viscosity. Our XPCS studies suggest an extended length scale of the relaxation process in glassy Ge3As52S45 from the single molecule to the intermolecular range across the glass transition, providing a unique direct probe of the dynamics beyond the length scales of the individual molecule.

19.
Gen Hosp Psychiatry ; 70: 44-50, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33714795

RESUMO

OBJECTIVE: Suicide is a serious public health concern, but little is known about the relationship between access to mental health care and suicide deaths, and whether suicide rates differ by mental health provider Health Professional Shortage Areas (HPSAs). This study investigated the associations between mental health HPSAs and suicide rates. METHOD: We used generalized linear mixed models to test the associations between HPSAs and suicide rates from 2010 to 2018. For each county during a 3-year period, the total number of suicides was obtained from Centers for Disease Control and Prevention's Wide-ranging Online Data for Epidemiologic Research (WONDER). RESULTS: Mental health HPSAs had higher suicide rates (adjusted incidence rate ratio (IRR), 1.06 [95% CI, 1.03-1.09]). The interaction terms of mental health HPSAs and time (adjusted IRR, 1.01 [95% CI, 1.00-1.01]) showed that the association between mental health shortage areas and suicide rates has increased over time. CONCLUSIONS: Suicide rates are more common in mental health provider shortage areas, and this association has been growing over time. The study's findings suggest that many communities in the US are likely facing simultaneous challenges of limited access to mental health care, social and economic disadvantage, and high burden of suicide.


Assuntos
Saúde Mental , Suicídio , Adulto , Humanos , Estados Unidos/epidemiologia
20.
Front Sports Act Living ; 3: 757815, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34870194

RESUMO

Aims: One third of the U.S. adult population is estimated to have obesity-associated prediabetes. Hispanics have a 50% higher type 2 diabetes death rate compared to non-Hispanic whites, yet low participation in lifestyle change programs, making this subgroup an important target for prevention. Our objective was to determine the feasibility and the effects of an intervention implementing the Center for Disease Control and Prevention National Diabetes Prevention Program (NDPP) plus recreational soccer (RS) in Hispanic men. Methods: Overweight and obese Hispanic men, aged 30-57 years with prediabetes at screening were recruited (n = 41). Trained soccer coaches led 30-min facilitated discussion of the NDPP modules after each RS session, with two sessions per week for 12 weeks and once per week for the following 12 weeks. The 1-h RS sessions followed the Football Fitness curriculum. Assessments included body mass index, waist circumference, bioelectrical impedance analysis (InBody 270), blood pressure, glycated hemoglobin (HbA1c), and validated physical fitness tests. Multilevel mixed models assessed the outcomes as a function of time and cohort and incorporated an unstructured covariance structure to examine the changes from baseline to 24 weeks. All analyses were conducted as intent-to-treat using SAS v 9.4. Results: Hispanic males (n = 41; mean age 41.7 [0.1] years) were obese at baseline (mean BMI 32.7, standard error of mean [0.7], mean weight 93.9 [2.2] kg). Attendance rate was 65% overall at 12 weeks but differed between cohorts. Five mild injuries occurred over the trial. After 24 weeks of the NDPP+RS intervention, there were significant decreases in systolic and diastolic blood pressure (%change -4.7[SE 2.4]; 95% CI [-11.5, -1.7] and -6.1 [1.7] mmHg; [-9.6, -2.6], respectively), HbA1c (-0.2 [0.1]; [-0.3, -0.1]), Despite significant reductions in weight (-3.8 [0.7]; [-5.2, -2.5]), waist circumference (-6.6 [0.7] cm; [-8.0, -5.1]), body fat % (-1.9 [0.5]; [-2.8, -1.0]), lean body mass was preserved (-0.9 [0.3]; [-1.6, -0.2]). Conclusion: A 24-week soccer-based adaptation of the Diabetes Prevention Program is safe and feasible among middle-aged Latino men.

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