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1.
BMC Med ; 21(1): 362, 2023 09 19.
Artículo en Inglés | MEDLINE | ID: mdl-37726759

RESUMEN

BACKGROUND: Overtreatment poses a challenge to healthcare systems due to harmful consequences of avoidable side-effects and costs. This study presents the first account for examining the feasibility of placebo use for reducing overtreatment in primary care, including whether public attitudes support the use of different placebo types in place of inappropriate prescriptions of antibiotics, antidepressants, or analgesics. METHODS: We used a multi-study, mixed-methods design, including patient and public (PPI) consultations, focus groups (Study 1) and two pre-registered online experiments (Studies 2 and 3). RESULTS: Study 1 (N = 16) explored everyday conceptions and practicalities of potential placebo use in the context of respiratory infections. Findings highlighted the importance of trusting doctor-patient relationships and safety-netting. Study 2 employed a randomised experiment with a representative UK sample (N = 980), investigating attitudes towards 5 different treatment options for respiratory infections: (1) blinded + pure placebo, (2) open-label + pure placebo, (3) open-label + impure placebo, (4) antibiotic treatment, and (5) no treatment. Study 2 also examined how attitudes varied based on wording and individual differences. Findings indicated general support (ηp2 = .149, large effect size) for replacing inappropriate antibiotics with open-label + impure placebos, although personal placebo acceptability was lower. Also, older people, individuals suffering from chronic illness or those showing higher levels of health anxiety appeared less amenable to placebo use. Study 3 (N = 1177) compared attitudes towards treatment options across three clinical scenarios: respiratory infection, depression and pain. Findings suggested significant differences in the acceptability of placebo options based on the clinical context. In the infection scenario, options for open-label + pure placebos, open-label + impure placebos and no treatment were rated significantly more acceptable (ηp2 = .116, medium effect size) compared to the depression and pain scenarios. Again, general support for placebos was higher than placebo acceptability for personal use. CONCLUSIONS: Findings from PPI and three studies indicate general support for combatting overprescribing in primary care through clinical placebo use. This is an indicator for wider UK public support for a novel, behavioural strategy to target a long-standing healthcare challenge. General acceptability appears to be highest for the use of open-label + impure placebos in the context of antibiotic overprescribing.


Asunto(s)
Antibacterianos , Ansiedad , Humanos , Anciano , Sobretratamiento , Dolor , Atención Primaria de Salud
2.
Bioorg Chem ; 110: 104786, 2021 05.
Artículo en Inglés | MEDLINE | ID: mdl-33740676

RESUMEN

Studies displaying the combination of mefloquine (MFL) with anti-tuberculosis (TB) substances are limited in the literature. In this work, the effect of MFL-association with two first-line anti-TB drugs and six fluoroquinolones was evaluated against Mycobacterium tuberculosis drug resistant strains. MFL showed synergistic interaction with isoniazid, pyrazinamide, and several fluoroquinolones, reaching fractional inhibitory concentration indexes (FICIs) ranging from 0.03 to 0.5. In order to better understand the observed results, two approaches have been explored: (i) spectroscopic responses attributed to the effect of MFL on physicochemical properties related to a liposomal membrane model composed by soybean asolectin; (ii) molecular dynamics (MD) simulation data regarding MFL interaction with a membrane model based on PIM2, a lipid constituent of the mycobacterial cell wall. FTIR and NMR data showed that MFL affects expressively the region between the phosphate and the first methylene groups of soybean asolectin membranes, disordering these regions. MD simulations results detected high MFL density in the glycolipid interface and showed that the drug increases the membrane lateral diffusion, enhancing its permeability. The obtained results suggest that synergistic activities related to MFL are attributed to its effect of lipid disorder and membrane permeability enhancement.


Asunto(s)
Antituberculosos/farmacología , Mefloquina/farmacología , Simulación de Dinámica Molecular , Mycobacterium tuberculosis/efectos de los fármacos , Antituberculosos/síntesis química , Antituberculosos/química , Relación Dosis-Respuesta a Droga , Espectroscopía de Resonancia Magnética , Mefloquina/síntesis química , Mefloquina/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Isótopos de Fósforo , Espectroscopía Infrarroja por Transformada de Fourier , Relación Estructura-Actividad
3.
Appl Opt ; 57(16): 4524-4536, 2018 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-29877400

RESUMEN

A new model for turbulence-corrupted imagery is proposed based on the theory of optimal mass transport. By describing the relationship between photon density and the phase of the traveling wave, and combining it with a least action principle, the model suggests a new class of methods for approximately recovering the solution of the photon density flow created by a turbulent atmosphere. Both coherent and incoherent imagery are used to validate and compare the model to other methods typically used to describe this type of data. Given its superior performance in describing experimental data, the new model suggests new algorithms for a variety of atmospheric imaging and wave propagation applications.

4.
An Acad Bras Cienc ; 89(3 Suppl): 2359-2370, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-29044330

RESUMEN

During composting processes, the degradation of organic waste is accomplished and driven by a succession of microbial populations exhibiting a broad range of functional competencies. A total of 183 bacteria, isolated from a composting process, were evaluated for cellulase activity at different temperatures (37, 50, 60, and 70°C) and pH values. Out of the 22 isolates that showed activity, isolate 380 showed the highest cellulase activity. Its ability to produce cellulase was evaluated in culture medium supplemented with carboxymethyl cellulose, microcrystalline cellulose, wheat straw, and rice husk. The culture medium supplemented with carboxymethyl cellulose induced higher enzyme activity after 6 hours of incubation (0.12 UEA mL-1 min-1). For wheat straw and rice husk, the results were 0.08 UEA mL-1 min-1 for both, while for microcrystalline cellulose, 0.04 UEA mL-1 min-1 were observed. The highest carboxymethyl cellulase activity was observed at 60°C (0.14 UEA mL-1 min-1) for both crude and partially purified enzyme after 30 and 120 min of incubation, respectively. Alkalinization of the medium was observed during cultivation in all substrates. The cellulase had a molecular mass of 20 kDa determined by SDS-Page. Isolate 380 was identified as Bacillus licheniformis. This work provides a basis for further studies on composting optimization.


Asunto(s)
Bacillus licheniformis/enzimología , Carboximetilcelulosa de Sodio/farmacología , Celulasa/biosíntesis , Celulasa/aislamiento & purificación , Medios de Cultivo/farmacología , Bacillus licheniformis/efectos de los fármacos , Electroforesis en Gel de Poliacrilamida , Calor , Especificidad por Sustrato
5.
Cureus ; 16(3): e56312, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38629002

RESUMEN

Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used and prescribed medications because of their important role in reducing inflammation and pain, in addition to their non-addictive properties and safety profiles. However, some studies have documented an association between NSAIDs and delayed union or nonunion of joint arthrodesis procedures due to a potential inhibition of the bone's inflammatory healing response. As a result, some orthopedic surgeons hesitate to prescribe NSAIDs after an arthrodesis procedure. The purpose of this meta-analysis is to review all relevant literature regarding the effect of NSAIDs on union rates after arthrodesis and determine if NSAID therapy increases the risk of non-union in the setting of arthrodesis procedures. The study hypothesis was that NSAIDs would not have a significant effect on the risk of nonunion after arthrodesis. A thorough systematic review of Medline, Embase, the Cochrane Database of Systematic Reviews, and the Web of Science identified 3,050 articles to be screened. The variables of interest encompassed demographic factors, procedural details, type and administration of NSAIDs, the number of patients exposed to NSAIDs with and without successful union (case group), as well as the number of patients who did not receive NSAIDs with and without successful union (control group). All the data were analyzed using a maximum likelihood random-effects model. The number of non-union events versus routine healing from each study was used to calculate the odds ratio (OR) of successful healing after arthrodesis procedures with versus without NSAID therapy. Thirteen articles met the inclusion criteria for the meta-analysis. NSAID exposure showed an increased risk of nonunion, delayed union, or both following arthrodesis procedures; however, this did not meet statistical significance (OR, 1.48; confidence interval [CI], 0.96 to 2.30). A sub-analysis of pediatric and adult studies showed a significant increase in non-union risk in adults (OR, 1.717; CI, 1.012 to 2.914) when removing the pediatric cohort (p = 0.045). This meta-analysis provides evidence that NSAIDs can increase the risk of nonunion, delayed union, or both following arthrodesis procedures in adults. However, the study did not identify a risk of nonunion, delayed union, or both following arthrodesis procedures in the pediatric population.

6.
An Acad Bras Cienc ; 85(1): 365-70, 2013 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-23460428

RESUMEN

Saguinus niger popularly known as Sauim, is a Brazilian North primate. Sympathetic chain investigation would support traumatic and/or cancer diagnosis which are little described in wild animals. The aim of this study was to describe the morphology and distribution of sympathetic chain in order to supply knowledge for neurocomparative research. Three female young animals that came death by natural causes were investigated. Animals were fixed in formaldehyde 10% and dissected along the sympathetic chain in neck, thorax and abdomen. Cranial cervical ganglion was located at the level of carotid bifurcation, related to carotid internal artery. In neck basis the vagosympathetic trunk divides into the sympathetic trunk and the parasympathetic vagal nerve. Sympathetic trunk ran in dorsal position and originated the stellate ganglia, formed by the fusion of caudal cervical and first thoracic ganglia. Vagal trunk laid ventrally to heart and formed the cardiac plexus. In abdomen, on the right side, were found the celiac ganglion and cranial mesenteric ganglion; in the left side these ganglia were fusioned into the celiac-mesenteric ganglion displaced closely to the celiac artery. In both sides, the caudal mesenteric ganglion was located near to the caudal mesenteric artery.


Asunto(s)
Saguinus/anatomía & histología , Sistema Nervioso Simpático/anatomía & histología , Sistema Nervioso Simpático/cirugía , Animales , Femenino
7.
Cureus ; 15(5): e38475, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-37284370

RESUMEN

Acrometastasis accounts for 0.1% of all cases of metastatic cancer, with the most common primary tumor being lung cancer. Since acrometastasis is extremely rare and it generally has a nonspecific clinical presentation, it provides a diagnostic dilemma. We present a case of a 70-year-old female with a painful swollen right index finger which was found to be a metastatic lesion from adenocarcinoma of the lung. The patient expired within one month of diagnosis due to complications from her rapidly progressive metastatic cancer.

8.
Cureus ; 15(4): e37526, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37193437

RESUMEN

Chondroid syringoma is a relatively rare benign skin appendageal tumor with an incidence of <0.098%. Malignant chondroid syringoma (MCS) arises from cutaneous sweat glands and occurs on the extremities or trunk more commonly in women with only 51 reported cases. Due to the rarity of the disease and lack of published cases of MCS, the diagnostic criteria and treatment protocols are not clear. Based on available recommendations and histological criteria, MCS was diagnosed in a previously classified elbow lipoma following increased size and pain, and skin color changes in a 65-year-old woman.

9.
Am J Rhinol Allergy ; 37(4): 419-428, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-36847244

RESUMEN

BACKGROUND: Previous research has shown diminished nasal immune function following nasal saline irrigation (NSI), returning to baseline at 6 hours. The aim of this study was to examine the immune nasal proteome before and after 14 days of nasal irrigation. METHODS: Seventeen healthy volunteers received either isotonic (IsoSal) or low salt (LowNa) NSI. Nasal secretions were collected before and 30 min after NSI at baseline and again after 14 days. Specimens were analyzed using mass spectrometry to detect proteins of relevance to nasal immune function. RESULTS: One thousand eight hundred and sixty-five proteins were identified with significant changes in 71 proteins, of which 23 were identified as part of the innate immune system. Baseline analysis demonstrated an increase of 9 innate proteins after NSI, most after IsoSal. After 14 days, a greater increase in innate peptides was present, with most now in the LowNa group. When NSI solutions were compared, a significant increase in 4 innate proteins, including a 211% in lysozyme, was detected in the LowNa group. CONCLUSION: LowNa NSI demonstrates evidence of improving the innate immune secretions, especially lysozyme, in healthy volunteers.


Asunto(s)
Rinitis , Sinusitis , Humanos , Proteoma , Muramidasa , Proyectos Piloto , Solución Salina , Lavado Nasal (Proceso)/métodos , Inmunidad Innata , Irrigación Terapéutica/métodos
10.
An Acad Bras Cienc ; 84(4): 973-7, 2012 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-23207702

RESUMEN

The aim of this work is to study the morphological characteristics of the trachea of Saimiri sciureus through quantification and measurement of the cartilaginous rings, providing information to facilitate the election of more appropriate endotracheal tube, laryngeal mask or tracheostomy tube for anesthetic and emergency procedures, as it is a species of Neotropical primates most commonly used as biological models, and little is known about their morphology. Nine animals were investigated, being 4 adults and 5 young acquired from the Centro Nacional de Primatas (National Primate Center - CENP) - Ananindeua - PA, which died from natural causes and then fixed in aqueous buffered formalin 10%. Saimiri sciureus trachea comprises an average of 32.8 incomplete rings and an average length of 3.74 cm in young animals, while in adults it demonstrated an average of 30.25 rings and average length of 3.67 cm. The shape of the light and its proportion varied along the trachea. Endotracheal tube with a diameter the 2.0 - 2.5 mm, laryngeal mask number 1.0 or tracheostomy tube neonatal Shiley number 3.0, can be placed in animals weighing 600 g - 1.2 Kg. Given the great importance of the species studied, which is widely used as a biological model, the detailing on the morphology and morphometry of tracheal animal studies provides new approaches needed in respiratory emergency, as well as, facilitates the development of future anesthetic protocols.


Asunto(s)
Saimiri/anatomía & histología , Tráquea/anatomía & histología , Animales , Urgencias Médicas , Femenino , Intubación Intratraqueal , Máscaras Laríngeas , Masculino , Saimiri/cirugía , Tráquea/cirugía , Traqueostomía
11.
An Acad Bras Cienc ; 83(4): 1339-44, 2011 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-22146961

RESUMEN

Saimiri sciureus is a New World non-human primate (NHP) that inhabits Brazilian rain forests. Surgical interventions in wild NHPs can be considered common both for experimental studies procedures and corrective procedures for endangered species. Among various anesthetic procedures, the epidural anesthesia or blockades, depending on the surgical procedure, might be considered elective for wild monkeys, mostly based on its safeness, efficiency and non-time consuming characteristics. However its safeness would be limiting because of the spinal cord arrangement. Notwithstanding the available former studies on New World NHP anatomy, the description of the medullar cone of Saimiri sciureus is still scarce. Therefore, we believe that the better understanding the medullar cone of Saimiri sciureus would contribute to improve the applicability of epidural procedures in the species. Vertebrae architecture of Saimiri sciureus was composed by 9 lumbar, 3 sacral and 18 coccygeal vertebrae, and the medullar cone measured about 3.3 cm. We can conclude that the conus medullaris in Saimiri sciureus is situated more caudally in comparison to other species.


Asunto(s)
Saimiri/anatomía & histología , Médula Espinal/anatomía & histología , Anestesia Epidural , Animales , Femenino , Masculino
12.
Ann Nucl Med ; 35(2): 232-240, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33389651

RESUMEN

INTRODUCTION: Radiosynovectomy (RS) with 90Y-hydroxyapatite (90Y-HyA) aims to control knee hemarthrosis in hemophiliac patients to prevent secondary arthropathy. However, knee RS using 153Sm-hydroxyapatite (153Sm-HyA) is considered less suitable due to the lower average soft tissue range and energy of 153Sm for large joints, such as the knees. PURPOSE: The objective of this investigation was to assess the efficacy and safety of knee RS with 153Sm-HyA, compared to 90Y-HyA. METHODS: Forty patients were prospectively assigned to undergo knee RS with 153Sm-HyA (n = 19) or with 90Y-HyA (n = 21). The frequency of hemarthrosis episodes before and after treatment were compared. RESULTS: After six months of knee RS, 153Sm-HyA and 90Y-HyA promoted a similar reduction of hemarthrosis episodes (50% and 66.7%, respectively). However, after 12 months of knee RS, the reduction of hemarthrosis episodes was significantly (p = 0.037) higher using 153Sm-HyA (87.5%) compared to 90Y-HyA (50.0%). This discrepancy was more pronounced (p = 0.002) for 153Sm-HyA compared to 90Y-HyA in adults/adolescents. CONCLUSION: Knee radiosynovectomy with 153Sm-HyA is safe, reduces hemarthrosis episodes after 12 months of treatments, especially in adults/adolescents and even with grades III/IV arthropathy, similar to 90Y-HyA. 90Y-HyA seems to promote better hemarthrosis control in small children.


Asunto(s)
Durapatita/química , Hemartrosis/radioterapia , Articulación de la Rodilla/efectos de la radiación , Radioisótopos/química , Samario/química , Radioisótopos de Itrio/química , Adolescente , Adulto , Anciano , Niño , Preescolar , Humanos , Masculino , Persona de Mediana Edad , Estudios Prospectivos , Radioisótopos/efectos adversos , Radioisótopos/uso terapéutico , Medición de Riesgo , Samario/efectos adversos , Samario/uso terapéutico , Factores de Tiempo , Resultado del Tratamiento , Radioisótopos de Itrio/efectos adversos , Radioisótopos de Itrio/uso terapéutico
13.
Med Care ; 47(1): 15-22, 2009 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-19106726

RESUMEN

OBJECTIVES: In seeking to identify modifiable, system-level factors affecting emergency department (ED) use, we used a statewide Medicaid database to study community variation in ED use and ascertain community characteristics associated with higher use. METHODS: This historical cohort study used administrative data from July 1, 2003 to December 31, 2004. Residence ZIP codes were used to assign all 555,219 Medicaid enrollees to 130 primary care service areas (PCSAs). PCSA characteristics studied included rural/urban status, presence of hospital(s), driving time to hospital, and several measures of primary care capacity. Statistical analyses used a 2-stage model. In the first stage (enrollee level), ED utilization rates adjusted for enrollee demographics and medical conditions were calculated for each PCSA. In the second stage (community level), a mixed effects linear model was used to determine the association between PCSA characteristics and ED use. RESULTS: ED utilization rates varied more than 20-fold among the PCSAs. Compared with PCSAs with primary care capacity less than need, PCSAs with capacity 1 to 2 times the need had 0.12 (95% CI: -0.044, -0.20) fewer ED visits/person/yr. Compared with PCSAs with the nearest hospital accessible within 10 minutes, PCSAs with the nearest hospital >30 minutes' drive had 0.26 (95% CI: -0.38, -0.13) fewer ED visits/person/yr. CONCLUSIONS: Within this Medicaid population, ED utilization was determined not only by patient characteristics but by community characteristics. Better understanding of system-level factors affecting ED use can enable communities to improve their health care delivery systems-augmenting access to care and reducing reliance on EDs.


Asunto(s)
Áreas de Influencia de Salud/estadística & datos numéricos , Servicio de Urgencia en Hospital/estadística & datos numéricos , Medicaid/estadística & datos numéricos , Aceptación de la Atención de Salud/estadística & datos numéricos , Atención Primaria de Salud/estadística & datos numéricos , Características de la Residencia/clasificación , Adolescente , Adulto , Niño , Preescolar , Enfermedad Crónica/etnología , Bases de Datos Factuales , Grupos Diagnósticos Relacionados , Femenino , Encuestas de Atención de la Salud , Accesibilidad a los Servicios de Salud/estadística & datos numéricos , Mal Uso de los Servicios de Salud/estadística & datos numéricos , Humanos , Lactante , Recién Nacido , Masculino , Persona de Mediana Edad , Análisis Multivariante , Aceptación de la Atención de Salud/etnología , Características de la Residencia/estadística & datos numéricos , Población Rural , Transportes , Estados Unidos , Población Urbana , Revisión de Utilización de Recursos , Adulto Joven
14.
Curr Top Med Chem ; 19(9): 683-689, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30836914

RESUMEN

Background and Introduction: Mefloquine, a drug used to prevent and treat malaria is described possessing activity against the Mycobacterium tuberculosis (Mtb) as well as against multidrugresistant tuberculosis (MDR) and other types of bacteria. Despite their importance, few compounds based on the Mefloquine nucleus have been synthesized and evaluated against TB. MATERIALS AND METHODS: For the synthesis of all the compounds based on the Mefloquine nucleus we used a synthetic route which utilized the key derivative 4-methoxy-2,8-bis(trifluoromethyl)quinoline 2 as starting material. The compounds 3 (a-c), 4 (a-b) were synthesized after one step by reaction of 2 with appropriate amines substituted. The chloro derivatives 5 and 6 were obtained from compounds 4b and 4a by treatment with SOCl2 in CH2Cl2 at reflux in 75 and 80% yield, respectively. The analogue 6 was converted to 7 after treatment with ethanolamine under heating at 90oC in 64% yield and to the azido derivative 8 in 56% after reaction with sodium azide in MeOH at reflux for 2 h. The analogue 9 was obtained after reaction of 5 with ethanolamine at 90oC for 1 h in 90% yield. All the new compounds were identified by detailed spectral data, including 1H NMR, 13C NMR and high resolution mass spectra. All the compound were evaluated for their in vitro antibacterial activity against sensitive Mycobacterium tuberculosis ATCC 27294, using the microplate Alamar Blue assay (MABA). The more active compounds 3c, 7, and 9 were also evaluated against resistant strain SR 2571/0215 (resistant to Rifampicin and Isoniazid) by above method. All compounds were tested against three cancer cell lines: SF-295 (glioblastoma), HCT-116 (colon) and PC-3 (prostate) using the MTT assay. RESULTS: All the planned ten compounds were synthetically obtained in good global yield, displaying activity against sensitive Mycobacterium tuberculosis in vitro, with exception of one, with MIC values between 37.2 and 154.8 µM. The compounds 3c (37.2 µM), 7 (68.1 µM) and 9 (65.6 µM) showed the highest activity in this series with MIC values similar when compare to the standard Mefloquine (30 - 60 µM), being 3c the most potent. The more active compounds 3c, 7, and 9 were also evaluated against resistant strain, displaying MIC of 37.2, 136.2 and 65.6 µM, respectively. All compounds were tested against three cancer cell lines and showed low cytotoxicity. CONCLUSION: All synthesized compounds, with the exception of 5, exhibited activity against the Mtb. Compound 3c was the most potent against resistant and sensitive Mtb in this series, with MIC value of 37.2 µM. All compounds showed low cytotoxicity. These findings could be considered a good model to develop possible lead compounds in the fight against TB based on Mefloquine nucleus.


Asunto(s)
Antituberculosos/farmacología , Farmacorresistencia Bacteriana/efectos de los fármacos , Mefloquina/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Antituberculosos/síntesis química , Antituberculosos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Humanos , Mefloquina/síntesis química , Mefloquina/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular
15.
Eur J Med Chem ; 127: 334-340, 2017 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-28068604

RESUMEN

Zika virus (ZIKV), an arthropod-born Flavivirus, has been associated with a wide range of neurological diseases in adults, foetuses and neonates. Since no vaccine is available, repurposing of antiviral drugs currently in medical use is necessary. Mefloquine has confirmed anti-ZIKV activity. We used medicinal chemistry-driven approaches to synthesize and evaluate the ability of a series of new 2,8-bis(trifluoromethyl)quinoline derivatives to inhibit ZIKV replication in vitro, in order to improve the potency of mefloquine. We found that quinoline derivatives 3a and 4 were the most potent compounds within this series, both with mean EC50 values of 0.8 µM, which represents a potency 5 times that of mefloquine. These results indicate that new 2,8-bis(trifluoromethyl)quinoline chemical structures may be promising for the development of novel anti-ZIKV drugs.


Asunto(s)
Antivirales/química , Antivirales/farmacología , Mefloquina/farmacología , Quinolinas/química , Quinolinas/farmacología , Virus Zika/efectos de los fármacos , Animales , Antivirales/síntesis química , Antivirales/toxicidad , Chlorocebus aethiops , Diseño de Fármacos , Quinolinas/síntesis química , Quinolinas/toxicidad , Relación Estructura-Actividad , Células Vero , Replicación Viral/efectos de los fármacos , Virus Zika/fisiología
16.
J Mol Histol ; 36(1-2): 25-34, 2005 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-15703996

RESUMEN

Little is known about cerebral vasculature of capybara, which seems may serve as a natural model of studying changes in cerebral circulation due to internal carotid artery atrophy at animal sexual maturation. This is the first study of the light- and electron-immunocytochemical localisation of endothelin-1 (ET-1) and ETA and ETB endothelin receptors in the basilar artery of capybaras (6 to 12-month-old females and males) using an ExtrAvidin detection method. All animals examined showed similar patterns of immunoreactivity. Immunoreactivity for ET-1 was detected in the endothelium and adventitial fibroblasts, whilst immunoreactivity for ETA and ETB receptors was present in the endothelium, vascular smooth muscle, perivascular nerves and fibroblasts. In endothelial cells immunoreactivity to ET-1 was pronounced in the cytoplasm or on the granular endoplasmic reticulum. Similar patterns of immunolabelling were observed for ETA and ETB receptors, though cytoplasmic location of clusters of immunoprecipitate seems dominant. These results suggest that the endothelin system is present throughout the wall of the basilar artery of capybara.


Asunto(s)
Arteria Basilar/citología , Endotelina-1/análisis , Endotelio Vascular/química , Receptor de Endotelina A/análisis , Receptor de Endotelina B/análisis , Roedores/anatomía & histología , Animales , Endotelio Vascular/ultraestructura , Femenino , Masculino
17.
Sci Pharm ; 84(3): 467-483, 2015 Oct 18.
Artículo en Inglés | MEDLINE | ID: mdl-28117313

RESUMEN

Both sonochemical and classical methodologies have been employed to convert camphor, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one, C9H16C=O, into a number of derivatives including hydrazones, C9H16C=N-NHAr 3, imines, C9H16C=N-R 7, and the key intermediate nitroimine, C9H16C=N-NO2 6. Reactions of nitroamine 6 with nucleophiles by classical methods provided the desired compounds in a range of yields. In evaluations of activity against Mycobacterium tuberculosis, compound 7j exhibited the best activity (minimal inhibitory concentration (MIC) = 3.12 µg/mL), comparable to that of the antitubercular drug ethambutol. The other derivatives displayed modest antimycobacterial activities at 25-50 µg/mL. In in vitro tests against cancer cell lines, none of the synthesized camphor compounds exhibited cytotoxic activities.

18.
Am J Med ; 87(3B): 27S-33S, 1989 Sep 11.
Artículo en Inglés | MEDLINE | ID: mdl-2679067

RESUMEN

Plasma antithrombin III (ATIII) levels decrease early during gram-negative septicemia, and even a moderate decrease in this major inhibitor of the coagulation system is associated with serious disseminated intravascular coagulation (DIC). Herein the efficacy of high-dose (at least 250 units/kg) ATIII supplementation in animal models of Escherichia coli endotoxemia or bacteremia is reported. An endotoxemic rat model demonstrated that: (1) DIC occurs very early, before the appearance of deleterious cardiovascular abnormalities; (2) ATIII prophylaxis attenuates DIC, metabolic dysfunction, and organ damage; (3) ATIII prophylaxis increases permanent survival; (4) ATIII treatment one hour after endotoxin challenge attenuates DIC, metabolic dysfunction, and organ damage, although not as well as when given prophylactically, and survival is not increased. An endotoxemic sheep pulmonary dysfunction model demonstrated that: (1) ATIII prophylaxis prevents the typical decrease in arterial oxygen partial pressure; (2) ATIII prophylaxis combined with alpha-1-proteinase inhibitor significantly attenuates indices of pulmonary dysfunction. An E. coli bacteremic baboon model demonstrated that ATIII prophylaxis and treatment significantly attenuate indices of DIC and organ damage and prevent death in an otherwise completely lethal dose bacterial challenge. In conclusion, prophylactic treatment with high doses of ATIII may be efficacious in disease states of impending disseminated intravascular coagulation, such as primary or secondary gram-negative septicemia.


Asunto(s)
Antitrombina III/uso terapéutico , Coagulación Intravascular Diseminada/prevención & control , Infecciones por Escherichia coli/terapia , Sepsis/terapia , Animales , Endotoxinas , Escherichia coli , Masculino , Papio , Ratas , Ratas Endogámicas , Ovinos
19.
Surgery ; 90(5): 853-9, 1981 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-7029767

RESUMEN

Skeletal muscle glucose uptake during close, intra-arterial insulin infusion was studied before and during live Escherichia coli bacteremic shock in the dog. An in vivo, constant-flow perfused gracilis muscle preparation was used. Insulin infusion before shock resulted in a 395% increase in muscle glucose uptake, which was independent of changes in muscle lactate production or oxygen uptake. At 1, 2, and 3 hours of shock, insulin infusion had no effect on gracilis muscle glucose uptake. This loss of responsiveness to insulin occurred with no change in muscle oxygen uptake, muscle venous PO2, or muscle blood flow (held constant). On the other hand, during nonshock control experiments, muscle glucose uptake in response to insulin infusion was maintained during the 3-hour protocol. These data demonstrate that skeletal muscle insulin resistance develops early during bacteremic shock.


Asunto(s)
Infecciones por Escherichia coli/fisiopatología , Resistencia a la Insulina , Músculos/efectos de los fármacos , Choque Séptico/fisiopatología , Animales , Perros , Femenino , Glucosa/metabolismo , Lactatos/metabolismo , Ácido Láctico , Masculino , Músculos/metabolismo , Consumo de Oxígeno , Factores de Tiempo
20.
J Neurosurg ; 48(5): 724-9, 1978 May.
Artículo en Inglés | MEDLINE | ID: mdl-641552

RESUMEN

The effects of ethanol- and saline-base prostaglandin E1 (PGE1) on systemic arterial blood pressure ((ABP), cerebral blood flow (CBF), cerebral vascular resistance (CVR), and cerebrospinal fluid (CSF) pressure were determined in anesthetized dogs. Progressively greater carotid intra-arterial infusions of ethanol-base PGE1 moderately decreased systemic ABP and CVR while perfusion of the CSF system with PGE1 moderately increased ABP and CVR; CBF was unaffected by either route of administration and CSF pressure was constant except for a slight decrease at the lowest intraventricular perfusion rate. Similar infusions of PGE1 were administered in saline base solutions in another group of dogs. Carotid intra-arterial infusion decreased ABP and CBF moderately at the highest infusion rate and caused a transient increase in CSF pressure. Cerebrospinal fluid system perfusion increased ABP moderately but did not affect the other parameters. These data indicate that PGE1 does not have a significant effect on cerebral hemodynamics when infused via the CSF system, but may produce slight cerebral vasodilation when infused into the carotid arteries in an ethanol base. This vasodilation may be due to autoregulation.


Asunto(s)
Circulación Cerebrovascular/efectos de los fármacos , Prostaglandinas E/administración & dosificación , Animales , Presión Sanguínea/efectos de los fármacos , Arterias Carótidas , Líquido Cefalorraquídeo , Perros , Etanol , Femenino , Inyecciones Intraarteriales , Inyecciones Intraventriculares , Masculino , Perfusión , Prostaglandinas E/farmacología , Cloruro de Sodio , Soluciones , Resistencia Vascular/efectos de los fármacos
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