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1.
Bioorg Med Chem ; 45: 116329, 2021 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-34329818

RESUMO

Agrimonia pilosa (AP), Galla rhois (RG), and their mixture (APRG64) strongly inhibited SARS-CoV-2 by interfering with multiple steps of the viral life cycle including viral entry and replication. Furthermore, among 12 components identified in APRG64, three displayed strong antiviral activity, ursolic acid (1), quercetin (7), and 1,2,3,4,6-penta-O-galloyl-ß-d-glucose (12). Molecular docking analysis showed these components to bind potently to the spike receptor-binding-domain (RBD) of the SARS-CoV-2 and its variant B.1.1.7. Taken together, these findings indicate APRG64 as a potent drug candidate to treat SARS-CoV-2 and its variants.


Assuntos
Agrimonia/química , Antivirais/química , Produtos Biológicos/química , Tratamento Farmacológico da COVID-19 , Extratos Vegetais/química , SARS-CoV-2/efeitos dos fármacos , Sequência de Aminoácidos , Antivirais/farmacologia , Produtos Biológicos/farmacologia , Descoberta de Drogas , Humanos , Taninos Hidrolisáveis/química , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Ligação Proteica , Quercetina/química , Glicoproteína da Espícula de Coronavírus/química , Triterpenos/química , Internalização do Vírus/efeitos dos fármacos , Ácido Ursólico
2.
Int J Emerg Med ; 9(1): 22, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27456667

RESUMO

BACKGROUND: Acupuncture is a form of traditional Chinese medicine being increasingly used as complementary therapy in many countries. It is relatively safe and rarely associated with deep infections. CASE PRESENTATION: In this case report, we describe a middle-aged Chinese patient who presented acutely to our emergency department with cauda equina syndrome secondary to acupuncture-related epidural abscesses, which were treated with surgical decompression and intravenous antibiotics. We also present a review of case reports of this rare condition in available literature. CONCLUSION: Emergency physicians should be aware that spinal abscesses may occur after acupuncture, with a broad spectrum of clinical presentations. If a history of recent acupuncture over the symptomatic area is elicited, a high index of suspicion should be maintained and appropriate imaging performed to establish the diagnosis. Treatment is directed by a number of factors, such as severity and duration of neurological deficit and progression of symptoms.

3.
Brain Imaging Behav ; 9(4): 821-7, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25511521

RESUMO

Subtle cognitive and behavioral changes are common in early Parkinson's disease. The cause of these symptoms is probably multifactorial but may in part be related to extra-striatal dopamine levels. 6-[(18) F]-Fluoro-L-dopa (FDOPA) positron emission tomography has been widely used to quantify dopamine metabolism in the brain; the most frequently measured kinetic parameter is the tissue uptake rate constant, Ki. However, estimates of dopamine turnover, which also account for the small rate of FDOPA loss from areas of specific trapping, may be more sensitive than Ki for early disease-related changes in dopamine biosynthesis. The purpose of the present study was to compare effective distribution volume ratio (eDVR), a metric for dopamine turnover, to cognitive and behavioral measures in Parkinson's patients. We chose to focus the investigation on anterior cingulate cortex, which shows highest FDOPA uptake within frontal regions and has known roles in executive function. Fifteen non-demented early-stage PD patients were pretreated with carbidopa and tolcapone, a central catechol-O-methyl transferase (COMT) inhibitor, and then underwent extended imaging with FDOPA PET. Anterior cingulate eDVR was compared with composite scores for language, memory, and executive function measured by neuropsychological testing, and behavior change measured using two informant-based questionnaires, the Cambridge Behavioral Inventory and the Behavior Rating Inventory of Executive Function-Adult Version. Lower mean eDVR (thus higher dopamine turnover) in anterior cingulate cortex was related to lower (more impaired) behavior scores. We conclude that subtle changes in anterior cingulate dopamine metabolism may contribute to dysexecutive behaviors in Parkinson's disease.


Assuntos
Dopamina/metabolismo , Giro do Cíngulo/diagnóstico por imagem , Giro do Cíngulo/metabolismo , Doença de Parkinson/metabolismo , Doença de Parkinson/psicologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Antiparkinsonianos/farmacologia , Benzofenonas/farmacologia , Carbidopa/farmacologia , Catecol O-Metiltransferase/metabolismo , Inibidores de Catecol O-Metiltransferase/farmacologia , Dopamina/análogos & derivados , Feminino , Giro do Cíngulo/efeitos dos fármacos , Humanos , Masculino , Pessoa de Meia-Idade , Testes Neuropsicológicos , Nitrofenóis/farmacologia , Doença de Parkinson/diagnóstico por imagem , Tomografia por Emissão de Pósitrons , Compostos Radiofarmacêuticos , Tolcapona
4.
Synapse ; 68(8): 325-31, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-24710997

RESUMO

6-[(18)F]-Fluoro-L-dopa (FDOPA) has been widely used as a biomarker for catecholamine synthesis, storage, and metabolism--its intense uptake in the striatum, and fainter uptake in other brain regions, is correlated with the symptoms and pathophysiology of Parkinson's disease (PD). 6-[(18)F]fluoro-m-tyrosine (FMT), which also targets L-amino acid decarboxylase, has potential advantages over FDOPA as a radiotracer because it does not form catechol-O-methyltransferase (COMT) metabolites. The purpose of the present study was to compare the regional distribution of these radiotracers in the brains of PD patients. Fifteen Parkinson's patients were studied with FMT and FDOPA positron emission tomography (PET) as well as high-resolution structural magnetic resonance imaging (MRI). MRI's were automatically parcellated into neuroanatomical regions of interest (ROIs) in Freesurfer (http://surfer.nmr.mgh.harvard.edu); region-specific uptake rate constants (Kocc) were generated from coregistered PET using a Patlak graphical approach. The essential findings were as follows: (1) regional Kocc were highly correlated between the radiotracers and in agreement with a previous FDOPA studies that used different ROI selection techniques; (2) FMT Kocc were higher in extrastriatal regions of relatively large uptake such as amygdala, pallidum, brainstem, hippocampus, entorhinal cortex, and thalamus, whereas cortical Kocc were similar between radiotracers; (3) while subcortical uptake of both radiotracers was related to disease duration and severity, cortical uptake was not. These results suggest that FMT may have advantages for examining pathologic changes within allocortical loop structures, which may contribute to cognitive and emotional symptoms of PD.


Assuntos
Encéfalo/metabolismo , Di-Hidroxifenilalanina/análogos & derivados , Radioisótopos de Flúor , Levodopa , Doença de Parkinson/metabolismo , Compostos Radiofarmacêuticos , Tirosina/análogos & derivados , Encéfalo/diagnóstico por imagem , Encéfalo/patologia , Progressão da Doença , Feminino , Humanos , Processamento de Imagem Assistida por Computador , Imageamento por Ressonância Magnética , Masculino , Pessoa de Meia-Idade , Doença de Parkinson/diagnóstico por imagem , Doença de Parkinson/patologia , Tomografia por Emissão de Pósitrons , Fatores de Tempo
5.
Am J Emerg Med ; 27(1): 8-15, 2009 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-19041528

RESUMO

INTRODUCTION: Intraosseous (IO) access is an alternative to conventional intravenous access. The proximal tibia and proximal humerus have been proposed as suitable sites for IO access. METHODS: A nonrandomized, prospective, observational study comparing flow rates and insertion success with tibial and humeral IO access in adults using the EZ-IO-powered drill device was conducted. The tibia was the first site of insertion, and a second IO was inserted in the humerus if clinically indicated for the same patient. RESULTS: Twenty-four patients were recruited, with 24 tibial and 11 humeral insertions. All EZ-IO insertions were successful at the first attempt except for 1 tibial insertion that was successful on the second attempt. All insertions were achieved within 20 seconds. Mean ease of IO insertion score (1=easiest to 10=most difficult) was 1.1 for both sites. We found tibial flow rates to be significantly faster using a pressure bag (165 mL/min) compared with those achieved without a pressure bag (73 mL/min), with a difference of 92 mL/min (95% confidence interval [CI]: 52, 132). Similarly, humeral flow rates were significantly faster using a pressure bag (153 mL/min) compared with humeral those achieved without pressure bag (84 mL/min), with a difference of 69 mL/min (95% CI: 39, 99). Comparing matched pairs (same patient), there was no significant difference in flow rates between tibial and humeral sites, with or without pressure bag infusion. CONCLUSIONS: Both sites had high-insertion success rates. Flow rates were significantly faster with a pressure bag infusion than without. However, we did not find any significant difference in tibial or humeral flow rates.


Assuntos
Úmero , Infusões Intraósseas/instrumentação , Ressuscitação/instrumentação , Tíbia , Adolescente , Adulto , Desenho de Equipamento , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Adulto Jovem
6.
Int J Emerg Med ; 2(3): 155-60, 2009 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-20157465

RESUMO

BACKGROUND: Intraosseous (IO) access is an alternative to conventional intravenous access. AIMS: We evaluate the use of the EZ-IO as an alternative vascular access for patients in the emergency department. METHODS: A non-randomized, prospective, observational study was performed in adults using the EZ-IO powered drill device. RESULTS: Twenty-four patients were recruited. There were 35 intraosseous insertions, including 24 tibial and 11 humeral insertions. All EZ-IO insertions were achieved within 20 s and were successful at the first attempt except for one. Of the intraosseous insertions, 88.6% were reported to be easier than intravenous cannulation. We found flow rates to be significantly faster using a pressure bag. The seniority of operators did not affect the success of insertion. Complications included a glove being caught in the drill device and extravasation of fluid although they were easily preventable. CONCLUSION: The use of the EZ-IO provides a fast, easy and reliable alternative mode of venous access, especially in the resuscitation of patients with no venous vascular access in the emergency department. Flow rates may be improved by the use of pressure bags.

7.
Ann Emerg Med ; 50(6): 744-5; discussion 745, 2007 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-18023763
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