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Id: biblio-1117073
Autor: Matheus, Tibisay; Aular, Yalitza; Bolaños, Alba; Fernández, Yolima; Barrios, Emilia; Hung, Mai-Lyng.
Título: Actividad de butirilcolinesterasa y micronúcleos en trabajadores agrícolas expuestos a mezclas de plaguicidas / Butyrylcholinesterase activity and micronuclei in agricultural workers exposed to pesticide mixtures
Fonte: Salud trab. (Maracay);25(1):23-36, jun. 2017. tab, ilus.
Idioma: es.
Resumo: Los plaguicidas son xenobióticos de gran utilidad para el control de las plagas y su uso es una realidad para obtener mayor rendimiento en los cultivos. Sin embargo, tienen el riesgo de producir toxicidad, por lo que es necesario el monitoreo biológico de los trabajadores expuestos a estas sustancias. El objetivo de este estudio fue evaluar la actividad de la butirilcolinesterasa (BCh) y la presencia de micronúcleos (MN) en trabajadores expuestos a mezclas de plaguicidas en el municipio Urdaneta, estado Lara. Participaron 82 individuos de sexo masculino, 41 expuestos (GE) y 41 no expuestos (GNE), la determinación de la butirilcolinesterasa se realizó en muestras de sangre, y la de micronúcleos en muestras epiteliales de la mucosa bucal. Los resultados fueron presentados empleando estadísticos descriptivos, frecuencias absolutas y porcentajes, utilizando el paquete libre PAST v.2.04. Los valores de actividad de BCh en el GE (3528,75+/- 1162,45U/L) mostraron diferencias estadísticamente significativas (P<0,001) en relación al GNE (5764,41+/-1641,43U/L). La frecuencia de MN presentó mayor mediana en el GE respecto al GNE (3,09 vs 0,73) con una diferencia significativa (P<0,001). Al asociar el tiempo de exposición con la actividad de BCh y la frecuencia de MN, se presentó una correlación negativa con la actividad de BCh y una correlación positiva con los MN, estadísticamente significativas P<0,001 y P<0,05. Los hallazgos obtenidos reflejan que los plaguicidas fueron utilizados en forma de mezclas siendo los más usados: organofosforados, carbamatos y piretroides produciendo modificaciones en los valores de actividad de BCh y la frecuencia de MN en individuos expuestos a plaguicidas(AU)

Pesticides are xenobiotics, useful in controlling pests and their use ileads to greater crop yields. However, they carry a risk of toxicity so biological monitoring of exposed workers is necessary. The aim of this study was to evaluate the cholinesterase activity and the presence of micronuclei in workers exposed to pesticide mixtures in the town of Urdaneta, Lara. Eighty-two workers participated, 41 exposed (EG) and 41 nonexposed (NEG), all of whome were male. Blood samples were obtained for the determination of butyrylcholinesterase (BCh); buccal mucosal epithelial samples were obtained for micronuclei (MN) sampline. The results were presented as descriptive statistics, absolute frequencies and percentages, using the PAST v.2.04 a free online software package. The BCh activity values in the EG (3528.75+/-1162.45U/L) showed statistically significant differences (P<0.001) in relation to the UEG (5764.41 +/- 1641.43U/L). Median MN frequency was highest in the EG compared to UEG (3.09vs 0.73), a significant difference (P<0.001). By associating exposure time with BCh activity and MN frequency, a negative correlation was found with BCh activity and a positive correlation with MN, both statistically significant (P<0.001 and P<0.05, respectively). The results suggested pesticide mixtures were the most often used: organophosphates, carbamates and pyrethroids produced changes in the activity values of BCh and the frequency of MN in individuals exposed to pesticides(AU)
Descritores: Praguicidas/toxicidade
Condições de Trabalho
Butirilcolinesterase
Carbamatos
Colinesterases
Doenças dos Trabalhadores Agrícolas/prevenção & controle
Monitoramento Biológico
Limites: Humanos
Masculino
Responsável: VE1.1 - Biblioteca Humberto Garcia Arocha


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Id: biblio-887597
Autor: Santos, Willian dos; Tureck, Luciane Viater; Saliba, Louise Farah; Schenknecht, Caroline Schovanz; Scaraboto, Débora; Souza, Ricardo Lehtonen R; Furtado-Alle, Lupe.
Título: Effects of energetic restriction diet on butyrylcholinesterase in obese women from southern Brazil - A longitudinal study
Fonte: Arch. endocrinol. metab. (Online);61(5):484-489, Sept.-Oct. 2017. tab.
Idioma: en.
Resumo: Objective Butyrylcholinesterase (BChE) activity has been associated with obesity, lipid concentrations, and CHE2 locus phenotypes. This, the aim of this study was to evaluate the effects of an energetic restriction diet intervention on anthropometrical and biochemical variables and on absolute and relative BChE activity in CHE2 C5+ and CHE2 C5- individuals. Subjects and methods One hundred eleven premenopausal obese women from Southern Brazil participated in an energetic restriction diet intervention (deficit of 2500 kJ/day) for 8 weeks. Their anthropometric and biochemical parameters were evaluated before and after the intervention. Plasma BChE activity was measured, and BChE bands in plasma and CHE2 locus phenotypes were detected by electrophoresis. Results The dietetic intervention decreased anthropometric and biochemical parameters as well as absolute BChE activity and relative activity of the G4 band. The CHE2 C5+ phenotype presented a different effect when compared with the CHE2 C5- phenotype. The CHE2 C5+ phenotype showed an effect in absolute BChE activity and in the relative activity of the G4 form, maintaining higher BChE activity regardless of the metabolic changes. Conclusion In our study, 8 weeks was not sufficient time to lower the body mass index to normal, but it was enough to significantly reduce the absolute BChE activity, which became similar to the levels in nonobese individuals. CHE2 C5+ individuals were resistant to the decrease in BChE activity compared to CHE2 C5- individuals. This shows that the diet did not affect the CHE2 and G4 fraction complex and that the products of the CHE2 locus in association with BChE have a role in energy metabolism, maintaining high levels of enzymatic activity even after dietary intervention.
Descritores: Butirilcolinesterase/metabolismo
Restrição Calórica
Obesidade/dietoterapia
Obesidade/enzimologia
-Fenótipo
Brasil
Análise de Regressão
Estudos Longitudinais
Metabolismo Energético
Limites: Humanos
Feminino
Adulto
Pessoa de Meia-Idade
Responsável: BR1.1 - BIREME


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Id: lil-609578
Autor: Oré, Raquel; Suárez, Silvia; Rojas, Luis; Valdivieso, Rubén; Oriondo, Rosa; Tapia, Fernando; Trabuco, Juan.
Título: Efecto del extracto acuoso de maca sobre la función cognitiva en ratas recién destetadas / Effect of aqueous extract of maca on cognitive function in weaning infant rats
Fonte: An. Fac. Med. (Perú);72(1):13-16, ene.-mar. 2011. tab, graf.
Idioma: es.
Resumo: Introducción: La maca, Lepidium meyenii walp, es una planta que crece en las alturas de los andes peruanos; es usada como alimento, por su valor nutricional y sus propiedades etnomedicinales, unidos a la fertilidad y vitalidad. En la actualidad, se ha incrementado el interés público en los polifenoles, que tendrían efecto inhibitorio sobre la actividad acetilcolinesterasa y butirilcolinesterasas, y de esta manera se mejoraría las funciones cognitivas, aunque los mecanismos aún no han sido dilucidados. Por esta razón, se ha propuesto que la maca es un adaptógeno, que aumenta la energía, resistencia y reduce el estrés. Objetivos: Demostrar y evaluar el efecto energizante de la maca amarilla sobre la memoria y el aprendizaje por medio de pruebas bioquímicas, en un modelo animal de ratas destetadas. Diseño: Estudio experimental. Institución: Centro de Investigación de Bioquímica y Nutrición. Facultad de Medicina, Universidad Nacional Mayor de San Marcos. Lima, Perú. Material biológico: Ratas recién destetadas y extracto acuoso de maca amarillo. Intervenciones: A ratas recién destetadas se les administró extracto acuoso de maca amarillo (0,4 mg, 0,8 mg y 1,2 mg/g de peso), durante 15 días, y luego se les sometió a la prueba de aprendizaje espacial acuática de Morris. También, se tomó muestras de cerebro para determinaciones bioquímicas. Principales medidas de resultados: Mejoría del aprendizaje y la memoria. Resultados: Se encontró inhibición de la butirilcolinesterasa, cuando se administró dosis crecientes de maca, excepto el grupo que recibió 0,8 mg/g. Los niveles de lipoperoxidación en el cerebro (daño oxidativo) disminuyeron al incrementar la dosis de maca; así mismo, los tiempos (s) en hallar la plataforma en la prueba de Morris disminuyeron al incrementar la dosis de maca amarilla. La concentración de glutatión en el cerebro se incrementó con la administración de maca, pero sin ser significativo. Conclusiones: La administración de extracto acuoso de maca mejora el aprendizaje y la memoria en animales de experimentación, así como las defensas antioxidantes en cerebro.

Background: Maca, Lepidium meyenii walp, is a plant that grows in Peruvian AndesÆ highlands. It is used as food because of its nutritional value and its ethnical and medical properties related to fertility and vitality. Currently public interest has increased on food and dietetic supplements that contain active principles like polyphenol compounds with inhibitory effect on acetylcholinesterase and butyrylcholinesterase activities, thus improving cognitive functions through mechanisms yet unknown; for this reason maca has been proposed as an adaptogen that increases energy and resistance and diminishes stress. Objectives: To determine the energetic effect of yellow maca on memory and learning by biochemical tests, in an animal model of weaning rats. Design: Experimental study. Setting: Biochemistry and Nutrition Research Center, Faculty of Medicine, Universidad Nacional Mayor de San Marcos, Lima, Peru. Biologic material: Weaning rats and aqueous yellow maca extract. Interventions: Weaning rats received yellow maca liquid extract (0.4 mg, 0.8 mg, and 1.2 mg/g de peso) during 15 days followed then by Morris spatial aquatic test. Brain samples were taken for biochemistry tests. Main outcome measures: Improvement of both learning and memory. Results: Butyrylcholinesterase inhibition was found with increasing dosis of maca except the group receiving 0.8 mg/g. Brain lipoperoxidation level (oxidative damage) decreased with increasing maca dosis; also time (s) in finding Morris platform test decreased with increasing yellow maca dosis. Brain total glutation concentration increased not significatively with maca supply. Conclusions: Maca liquid extract supplement improved learning and memory in experimental animals as well as brain antioxidant defenses.
Descritores: Aprendizagem
Butirilcolinesterase
Glutationa
Lepidium
Memória
Peroxidação de Lipídeos
-Epidemiologia Experimental
Limites: Animais
Ratos
Responsável: PE13.1 - Oficina de Biblioteca, Hemeroteca y Centro de Documentación


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Id: lil-356999
Autor: Vásquez, Llermén; Osorio Terrones, Jorge; Sandoval Vegas, Miguel.
Título: Variación de la actividad de la enzima butirilcolinesterasa en usuarias de anticonceptivos hormonales / Enzyme butilcholinesterase activity variation in hormonal contraception users
Fonte: An. Fac. Med. (Perú);61(4):271-277, oct. 2000. tab, graf.
Idioma: es.
Resumo: OBJETIVO: Evaluar la actividad de la enzima butirilcolinesterasa en mujeres usuarias de dos anticonceptivos hormonales, norgestrel etinilestradiol y acetato de medroxiprogesterona, utilizando como marcador hepático indirecto la fosfatasa alcalina. MATERIAL Y MÉTODOS: Mujeres que asistían al programa de Planificación Familiar del C. S. "7 de Octubre" - El Agustino, continuadoras en los métodos de anticoncepción hormonal (mayor de seis meses). Se extrajo sangre en ayunas y realizó la medición sérica de la actividad enzimática. RESULTADOS: Las usuarias de ambos tipos de anticonceptivos tuvieron aumento significativo de la actividad butirilcolinesterasa respecto al grupo control, observándose en las usuarias de medroxiprogesterona 30 por ciento más con cifras elevadas. El 12 por ciento de usuarias de norgestrel etinilestradiol y el 18 por ciento de medroxiprogesterona tuvo valores fuera del promedio ñ2 DE. La actividad de fosfatasa alcalina tuvo aumento significativo de 8 por ciento sólo en usuarias de medroxiprogesterona. CONCLUSIONES: El uso del anticonceptivo acetato de medroxiprogesterona originó mayor variación de la actividad butirilcolinesterasa y por más tiempo que el del norgestrel etinilestradiol.
Descritores: Butirilcolinesterase
Anticoncepcionais Orais Hormonais
Medroxiprogesterona
Norgestrel
Anticoncepção
Limites: Humanos
Feminino
Responsável: PE13.1 - Oficina de Biblioteca, Hemeroteca y Centro de Documentación


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Id: biblio-1102238
Autor: Rahmani-Nezhad, Samira; Dianat, Shima; Mahdizadeh, Valiollah; Fooladi, Zahra; Hariri, Roshanak; Najafi, Zahra; Firuzi, Omidreza; Vahedi-Mazdabadi, Yasaman; Farjadmand, Fatemeh; Akbarzadeh, Tahmineh; Saeedi, Mina; Ardekan, Mohammadreza Shams.
Título: Investigation of polysaccharide extracts from Iranian and French strains of Agaricus subrufescens against enzymes involved in Alzheimer's disease / Investigación de extractos de polisacáridos de cepas iraníes y francesas de Agaricus subrufescens contra enzimas relevantes para la enfermedad de Alzheimer
Fonte: Bol. latinoam. Caribe plantas med. aromát;18(6):544-554, nov. 2019. tab, ilus.
Idioma: en.
Projeto: Tehran University of Medical Sciences.
Resumo: In this work, the inhibitory activity of a wide range of polysaccharide extracts from two Iranian and French strains of Agaricus subrufescens were evaluated toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, two extracts S9 and S'7 obtained from Iranian and French strains under different extraction conditions showed selective AChE inhibitory activity with IC50 values of 154.63 and 145.43 µg/mL, respectively. It should be noted that all extracts from both strains demonstrated no BChE inhibitory activity. S9 and S'7 were also tested for their effect on amyloid beta (Aß) aggregation, antioxidant activity, and neuroprotectivity. Their activity against Aß aggregation was comparable to that of donepezil as the reference drug but they induced moderate antioxidant activity by DPPH radical scavenging activity and negligible neuroprotectivity against Aß-induced damage.

En este trabajo, se evaluó la actividad inhibitoria de acetilcolinesterasa (AChE) y butirilcolinesterasa (BChE) para varios extractos de polisacáridos de dos cepas iraníes y francesas de Agaricus subrufescens. Los extractos más potentes mostraron valores de IC50 de 154,63 y 145 µg/ml para las cepas iraní (S9) y francesa (S'7), respectivamente, las cuales se obtuvieron de diferentes condiciones de extracción; sin embargo, todos los extractos no mostraron actividad inhibitoria de BChE. Además, S9 y S'7 se probaron para determinar su efecto sobre la agregación de beta-amiloide (Aß), así como su actividad antioxidante y neuroprotectora. Su actividad inhibitoria de la agregación de Aß fue comparable con donepezil, fármaco de referencia, pero indujeron una actividad antioxidante moderada, medida mediante la captación de radicales DPPH, y una neuroprotectora insignificante contra el daño inducido por Aß.
Descritores: Agaricus/química
Doença de Alzheimer/tratamento farmacológico
Amiloide/efeitos dos fármacos
Antioxidantes/farmacologia
-Picratos
Compostos de Bifenilo
Butirilcolinesterase
Inibidores da Colinesterase/farmacologia
Fármacos Neuroprotetores
Doença de Alzheimer/enzimologia
Polissacarídeos Fúngicos/farmacologia
Responsável: CL1.1 - Biblioteca Central


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Id: biblio-892692
Autor: Manzano-Rincón, Yolima; Castillo-Cabellos, Jhuliana Mercedes; Gualdrón-Frías, Carlos Andrés; Vega-Useche, Leonel Santiago.
Título: Deficiencia de butirilcolinesterasa identificada después de la administración de succinilcolina. Reporte del caso / Butyrylcholinesterase deficiency identified after succinylcholine administration. Case report
Fonte: Iatreia;31(1):97-102, ene.-mar. 2018.
Idioma: es.
Resumo: RESUMEN La función principal de la enzima butirilcolinesterasa es hidrolizar ésteres exógenos como los que están presentes en el relajante neuromuscular succinilcolina, que se utiliza con frecuencia en procedimientos quirúrgicos de corta duración. Se considera que la herencia de butirilcolinesterasa atípica o deficiencia de butirilcolinesterasa es un rasgo autosómico recesivo que se presenta aproximadamente en una de cada 3200 a 5000 personas. Dicha deficiencia puede tener consecuencias graves en pacientes anestesiados con dicho relajante porque en ocasiones causa prolongación de la parálisis o apnea posoperatoria. Se presenta el caso de una paciente de 73 años admitida al servicio de cirugía para una tiroidectomía subtotal. Finalizada la intervención, no emergió espontáneamente del anestésico, presentó signos de relajación con mal esfuerzo inspiratorio y sin recuperar la respuesta neuromuscular; por ello se procedió a revertir con neostigmina, previa aplicación de atropina. La reversión falló por lo que fue trasladada a la unidad de cuidados intensivos. En los exámenes se halló reducido el nivel de colinesterasa sérica, lo que indicó una deficiencia de butirilcolinesterasa compatible con sus síntomas. Tal situación está descrita en la literatura médica.

SUMMARY The main function of the enzyme butyrylcholinesterase is to hydrolyze exogenous esters such as those present in the neuromuscular blocking agent succinylcholine, which is frequently used in short surgical procedures. Inheritance of atypical butyrylcholinesterase or butyrylcholinesterase deficiency is considered an autosomal recessive characteristic and occurs worldwide in approximately one out of 3200 to 5000 people. Such deficiency may have serious consequences for patients anesthetized with that relaxant because sometimes it causes an extension of paralysis or postoperative apnea. We report the case of a 73-year-old woman submitted to subtotal thyroidectomy. After surgery, she did not spontaneously emerge from anesthesia, had signs of relaxation with poor inspiratory effort, and no recovery of neuromuscular response. After application of atropine, reversal was attempted with neostigmine, but it failed, and she was transferred to the ICU. Laboratory results revealed a reduced level of serum cholinesterase indicating a deficiency in butyrylcholinesterase consistent with her symptoms. Such situation has been described in medical literature.
Descritores: Butirilcolinesterase
Enzimas
Limites: Humanos
Feminino
Idoso
Tipo de Publ: Relatos de Casos
Responsável: CO304.1 - Biblioteca Arturo Aparicio Jaramillo


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Texto completo SciELO Brasil
Andrade, C. M
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Id: lil-785713
Autor: Dalmolin, F; Lhamas, C. L; Pinto Filho, S. T. L; Feranti, J. P. S; Poerschke, A; Beck, R. C; Abdalla, F. H; Andrade, C. M; Brun, M. V.
Título: Biomarcadores inflamatórios e de estresse oxidativo em cadelas submetidas à ovário-histerectomia videoassistida ou convencional / Inflammation and oxidative stress indicators in bitches submitted to laparoscopic-assisted or conventional ovariohysterectomy
Fonte: Arq. bras. med. vet. zootec;68(3):687-694graf.
Idioma: pt.
Resumo: A videocirurgia é atualmente uma das principais ferramentas operatórias, com vantagens que incluem menor estresse, incisões e dor pós-operatória quando comparada aos procedimentos abertos. Objetivou-se comparar o processo inflamatório e o estresse oxidativo resultantes das técnicas de ovário-histerectomia (OVH) convencional e videoassistida, com dois portais em cadelas, por meio de hemograma, avaliação de acetilcolinesterase, butirilcolinesterase, catalase e malondialdeído séricos, imediatamente antes da operação e duas, seis, 12, 24, 48 e 72 horas após a cirurgia. Observou-se menor estresse cirúrgico nas pacientes operadas pela técnica videoassistida, e sugere-se que a técnica convencional possa implicar peroxidação lipídica, mesmo com o uso de anti-inflamatório.(AU)

Videosurgery is currently a very important surgical tool with several benefits over the open surgery, including less surgical stress, shorter incisions and less postoperative pain. The purpose of this study was to compare the inflammatory process and oxidative stress between conventional and two-port laparoscopic-assisted ovariohisterectomy (OVH) in bitches. Complete blood counting, serum acetylcholinesterase, butyrylcholinesterase, catalase and malondialdehyde were assessed on the baseline and at two, six, 12, 24, 48 and 72 hours after surgery. The patients submitted to the videoassisted technique presented lower inflammatory response. There are suggestions that the conventional technique promotes lipid peroxidation, even with the use of anti-inflammatories.(AU)
Descritores: Biomarcadores/análise
Ovariectomia/veterinária
Estresse Oxidativo
Cirurgia Vídeoassistida/veterinária
-Acetilcolinesterase
Butirilcolinesterase/análise
Peroxidação de Lipídeos
Limites: Animais
Cães
Responsável: BR1.1 - BIREME


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Id: lil-780276
Autor: Eger, Guilherme André; Ferreira, Vinícius Vialle; Batista, Camila Ribeiro; Lima, Daniela Delwing de; Wyse, Angela Terezinha de Souza; Cruz, Júlia Niehues da; Magro, Débora Delwing Dal; Cruz, José Geraldo Pereira da.
Título: Guanidinoacetate alters antioxidant defenses and butyrylcholinesterase activity in the blood of rats
Fonte: Clin. biomed. res;35(1):49-54, 2015. ilus.
Idioma: en.
Resumo: Deficiency of guanidinoacetate methyltransferase, the first described creatine biosynthesis defect, leads to depletion of creatine and phosphocreatine, and accumulation of guanidinoacetate (GAA) in brain and body fluids. The present study aimed to investigate the influence of GAA on the activities of antioxidant enzymes, as well as on thiobarbituric acid-reactive substances (TBARS) and butyrylcholinesterase (BuChE) activity in the blood of rats. We also evaluated the effect of trolox (6-hydr oxy-2,5,7,8-tetramethylchroman-2-carboxylic acid), GSH (glutathione) and L-NAME (NG-nitro-L-arginine methyl ester) on the alterations elicited by GAA. Methods: The rats were randomly divided into 8 groups: (1) control; (2) GAA (10, 30, 50, 100 mM/kg); (3) trolox (1 mM/kg) + control; (4) trolox (1 mM/kg) + GAA (100 mM/kg); (5) GSH (1 mM/kg) + control; (6) GSH (1 mM/kg) + GAA (100 mM/kg); (7) L-NAME (1 mM/kg) + control; (8) L-NAME + GAA (100 mM/kg). After the addition of compounds, erythrocytes and plasma were pre-incubated at 37°C for 1h and tested immediately. Results: GAA enhanced the activities of catalase (CAT) and glutathione peroxidase (GSH-Px) in the erythrocytes and BuChE activity. In addition, GAA enhanced TBARS levels in the plasma. Trolox, GSH and L-NAME addition prevented the majority of alterations in oxidative stress parameters and the increase of BuChE activity that were caused by GAA. Data suggest that GAA alters antioxidant defenses and induces lipid peroxidation in the blood, as well altering BuChE activity. However, in the presence of trolox, GSH and L-NAME some of these alterations in oxidative stress and BuChE activity were prevented. Conclusions: Our findings lend support to a potential therapeutic strategy for this condition, which may include the use of appropriate antioxidants for ameliorating the damage caused by GAA...
Descritores: Antioxidantes
Butirilcolinesterase
Guanidinoacetato N-Metiltransferase
Estresse Oxidativo
Limites: Animais
Ratos
Responsável: BR18.1 - Biblioteca FAMED/HCPA


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Id: lil-778412
Autor: Rubab, Kaniz; Abbasi, Muhammad Athar; Aziz-ur-Rehman; Siddiqui, Sabahat Zahra; Ashraf, Muhammad; Shaukat, Ayesha; Ahmad, Irshad; Lodhi, Muhammad Arif; Khan, Farman Ali; Shahid, Muhammad; Akhtar, Muhammad Nadeem.
Título: Convergent synthesis of new N -substituted 2-{[5-(1H -indol-3-ylmethyl)-1, 3, 4-oxadiazol-2-yl]sulfanyl}acetamides as suitable therapeutic agents
Fonte: Braz. j. pharm. sci;51(4):931-947, Oct.-Dec. 2015. tab, graf.
Idioma: en.
Resumo: abstract A series of N-substituted 2-{[5-(1H-indol-3-ylmethyl)-1,3,4-oxadiazol-2-yl]sulfanyl}acetamides (8a-w) was synthesized in three steps. The first step involved the sequential conversion of 2-(1H-indol-3-yl)acetic acid (1) to ester (2) followed by hydrazide (3) formation and finally cyclization in the presence of CS2 and alcoholic KOH yielded 5-(1H-indole-3-yl-methyl)-1,3,4-oxadiazole-2-thiol (4). In the second step, aryl/aralkyl amines (5a-w) were reacted with 2-bromoacetyl bromide (6) in basic medium to yield 2-bromo-N-substituted acetamides (7a-w). In the third step, these electrophiles (7a-w) were reacted with 4 to afford the target compounds (8a-w). Structural elucidation of all the synthesized derivatives was done by 1H-NMR, IR and EI-MS spectral techniques. Moreover, they were screened for antibacterial and hemolytic activity. Enzyme inhibition activity was well supported by molecular docking results, for example, compound 8q exhibited better inhibitory potential against α-glucosidase, while 8g and 8b exhibited comparatively better inhibition against butyrylcholinesterase and lipoxygenase, respectively. Similarly, compounds 8b and 8c showed very good antibacterial activity against Salmonella typhi, which was very close to that of ciprofloxacin, a standard antibiotic used in this study. 8c and 8l also showed very good antibacterial activity against Staphylococcus aureus as well. Almost all compounds showed very slight hemolytic activity, where 8p exhibited the least. Therefore, the molecules synthesized may have utility as suitable therapeutic agents.

resumo Uma série de acetamidas 2-{[5-(1H-indol-3-ilmetil)-1,3,4-oxadiazol-2-il]sulfanila} N-substituídas (8a-w) foi sintetizada em três fases. A primeira etapa envolveu a conversão sequencial de ácido 2-(1H-indol-3-il)acético (1) a éster (2), seguido por hidrazida (3) e, finalmente, a e ciclização na presença de CS2 e KOH alcoólico produziu 5-(1H-indol-3-il- metil)-1,3,4-oxadiazole-2-tiol (4). Na segunda etapa, aminas arílicas/aralquílicas(5a-w) reagiram com brometo de 2-bromoacetila (6​​), em meio básico, para se obter acetamidas 2-bromo-N-substituídas (7a-w). Na terceira etapa, estes eletrófilos (7a- w) reagiram com 4, para se obter os compostos alvo (8a-w). A elucidação estrutural de todos os derivados sintetizados foi realizada por 1H-NMR, IR e técnicas de espectrometria de EI-MS. Além disso, eles foram submetidos a triagem de atividade antibacteriana e hemolítica. Análise da inibição enzimática foi bem apoiada pelos resultados de docking molecular. Por exemplo, o composto 8q exibiu melhor potencial inibitório contra α-glicosidase, e os compostos 8g e 8b exibiram, comparativamente, melhor inibição contra butirilcolinesterase (BChE) elipoxigenase (LOX), respectivamente. Do mesmo modo os compostos 8b e 8c mostraram excelente potencial antibacteriano contra SalmonellaTyphi, semelhante ao do ciprofloxacino, antibiótico padrão usado neste estudo. Os compostos 8c e 8l também mostraram excelente potencial antibacteriano contra Staphylococcus aureus . Quase todos os compostos mostraram pequena atividade hemolítica, sendo que o composto 8p apresentou menor atividade. Assim, as moléculas sintetizadas podem ter a sua utilidade como agentes terapêuticos adequados.
Descritores: Acetamidas/análise
Ácido Hidroxi-Indolacético/análise
-Butirilcolinesterase/análise
Ensaio de Atividade Hemolítica de Complemento/classificação
Glicosídeo Hidrolases/farmacocinética
Lipoxigenases/farmacocinética
Responsável: BR1.1 - BIREME


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Id: lil-762714
Autor: Sánchez, Luz Helena; Medina, Olga Marcela; Gómez, Guillermo; González, Clara Isabel; Flórez-Vargas, Óscar.
Título: Laboratory genetic-based reference values for cholinesterase activity in a Colombian population: A step forward in personalized diagnostics / Valores de referencia basados en el contexto genético de la actividad enzimática de la colinesterasa en una población colombiana: un paso hacia el diagnóstico personalizado
Fonte: Biomédica (Bogotá);35(spe):20-29, ago. 2015. ilus, graf, tab.
Idioma: en.
Resumo: Introduction: The determination of cholinesterase (ChE) activity has been commonly applied in the biomonitoring of exposure to organophosphate and carbamate pesticides. However, ChE activity is influenced by genetic factors. Integrating genotype and phenotype information in clinical laboratory tests would increase the accuracy of the reference values in well-defined populations. Objective: To establish genetic-based reference values for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity in a Colombian population. Materials and methods: A total of 397 healthy adults from Bucaramanga were included in the study. AChE and BChE activities were measured in blood samples by potentiometry and spectrophotometry, respectively. Genotyping for ACHE rs17880573 and BCHE rs1803274 was performed using the TaqMan allelic discrimination assay. The statistical analyses to obtain the reference values were performed with the MedCalc® software. Results: Allele frequencies were 10.58% for rs17880573 A and 8.82% for rs1803274 A. People with genotypes rs1803274 AA and AG showed a reduction of 20.69% and 10.92% respectively in mean BChE activity compared to people with genotype GG. No significant differences were identified in AChE activity between rs17880573 alleles or genotypes. In the overall sample, the corresponding reference values were as follows: for AChE activity, 0.62-0.98 D pH/h and for BChE activity, 4796.3-10321.1 U/L for people carrying the allele rs1803274A and 5768.2-11180.4 U/L for people carrying the genotype rs1803274 GG. Conclusion: We strongly recommend using these genetic-based reference values for ChE enzymes in our well-defined population in daily clinical practice.

Introducción. La determinación de la actividad enzimática de la colinesterasa se utiliza comúnmente en la vigilancia biológica de la exposición a pesticidas organofosforados y carbamatos. Sin embargo, los factores genéticos afectan la actividad de la colinesterasa, por lo que la integración de la información sobre genotipos y fenotipos en las pruebas de laboratorio clínico, incrementaría la precisión de los valores de referencia. Objetivo. Establecer los valores de referencia basados en el contexto genético para la actividad enzimática de la acetilcolinesterasa (AChE) y la butirilcolinesterasa (BChE), en una población colombiana. Materiales y métodos. Se incluyeron 397 adultos sanos. La actividad de la acetilcolinesterasa y la de la butirilcolinesterasa, se determinaron en muestras de sangre por potenciometría y espectrofotometría, respectivamente. Los genotipos de los ACHE rs17880573 y BCHE rs1803274 se obtuvieron mediante el ensayo TaqMan y los valores de referencia se estimaron con el programa MedCalc®. Resultados. La frecuencia alélica fue de 10,58 % para rs17880573 A y de 8,82 % para rs1803274 A. Las personas con los genotipos rs1803274 AA y AG, mostraron una reducción en el promedio de la actividad de la butirilcolinesterasa de 20,69 % y de 10,92 %, respectivamente, comparados con aquellas con el genotipo GG. No se encontraron diferencias significativas en la actividad de la acetilcolinesterasa con respecto a los alelos y genotipos del rs17880573. Los valores de referencia determinados para esta población fueron de 0,62-0,98 D pH/h para acetilcolinesterasa y de 4796,3-10321,1 U/L para butirilcolinesterasa, en las personas portadoras del alelo rs1803274 A, y de 5768,2-11180,4 U/L, en las portadoras del genotipo rs1803274 GG. Conclusión. Se recomienda el uso de estos valores de referencia basados en el contexto genético para las colinesterasas, en la práctica clínica diaria en esta población.
Descritores: Acetilcolinesterase/metabolismo
Butirilcolinesterase/metabolismo
Medicina de Precisão
-Acetilcolinesterase/genética
Butirilcolinesterase/genética
Colômbia
Valores de Referência
Limites: Adulto
Feminino
Humanos
Masculino
Pessoa de Meia-Idade
Adulto Jovem
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: CO332 - Facultad de Medicina



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