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1.
Rev. Inst. Adolfo Lutz ; 80(Único): e37277, dez. 2021. ilus, tab
Article in Portuguese | ColecionaSUS, LILACS, ColecionaSUS, SES-SP, CONASS, SESSP-ACVSES, SESSP-IALPROD, SES-SP, SESSP-IALACERVO | ID: biblio-1361863

ABSTRACT

A inibição da enzima colinesterase plasmática (BChE) pode ser utilizada como biomarcador para os efeitos da intoxicação por organofosforados e carbamatos. Nas aves, esta inibição ocorre de forma mais acentuada que nos mamíferos, porém poucos são os trabalhos publicados nestas espécies. O objetivo do estudo fo a dosagem da BChE em gansos-egípcios (Alopochen aegyptiacus) e nos anseriformes domésticos: gansos-domésticos (Anser anser domesticus) e marrecos (Anas platyrhynchos domesticus), para o estabelecimento de valores de referência normais. O trabalho possui ineditismo com relação à determinação desta enzima nos gansos-egípcios e domésticos. Os gansos e marrecos são mantidos em confinamento com fornecimento de alimentos e água ad libitum e em espaço adequado à sua manutenção no Instituto Adolfo Lutz (IAL), com a finalidade de fornecimento de sangue para a alimentação de triatomídeos do insetário de criação no Núcleo de Parasitoses Sistêmicas. Nos Alopochen aegyptiacus a média e o desvio padrão da BChE foram de 1.868 + 263,6 U/L, nos Anser anser domesticus 2.311 + 673,2 U/L e nos Anas platyrhynchos domesticus 4.290 + 86,11 U/L. (AU)


The inhibition of the plasma cholinesterase enzyme (BChE) can be used as a biomarker for the effects of intoxication by organophosphates and carbamates. In birds, this inhibition is more pronounced than in mammals, however there are few specific studies were conducted in this field. The aim of this study was to measure BChE in Egyptian geese (Alopochen aegyptiacus) and domestic anseriforms: domestic geese (Anser anser domesticus) and mallards (Anas platyrhynchos domesticus), not exposed to pesticides, for the establishment of normal values. The work is unprecedented regarding the determination of this enzyme in egyptian geese and domestic geese. Geese and mallards are kept in confinement with ad liditum food and water supply and in adequate space for their maintenance at the Adolfo Lutz Institute (IAL), for the purpose of supplying blood for the feeding of triatomines from the insectary of the Nucleus of Systemic Parasitoses. In Alopochen aegyptiacus the mean and standard deviation of BChE were 1,868 + 263,6 U/L, in Anser anser domesticus 2,311 + 673,2 U/L and in Anas platyrhynchos domesticus 4,290 + 86.11 U/L. (AU)


Subject(s)
Animals , Cholinesterases/blood , Anseriformes/blood , Geese/blood , Reference Values , Carbamates/adverse effects , Biomarkers/blood , Insecticides, Organophosphate/adverse effects
2.
Pesqui. vet. bras ; 40(1): 72-76, Jan. 2020. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1091652

ABSTRACT

The objective of this study was to evaluate the enzymatic activity of plasma cholinesterase in Chelonia mydas marine turtles belonging to two populations, according to their capture sites, under the absence and probable influence of anthropic effects. A total of 74 animals were used and later divided into two groups, based on the capture site. Blood samples were collected from all captured animals, which were then released into the sea at the site of capture. A descriptive statistical analysis of the plasma cholinesterase activity values and an analysis comparing these values based on the capture site were performed. Samples of heparinized plasma from animals captured at the two different sites were analyzed. Plasma cholinesterase activity ranged from 121 to 248U/L, with a mean and standard deviation of 186.1±30.68U/L. When comparing plasma cholinesterase activity values in individuals based on the capture site, a significant difference was observed. Establishing reference values for different sea turtle populations is necessary to interpret future sampling results and to allow sea turtles to be used as sentinels of ecosystem health. Future studies are needed to evaluate other populations and the activity of plasma cholinesterase in juvenile marine turtles, in relation to environmental contamination.(AU)


O objetivo desse estudo foi avaliar a atividade enzimática da colinesterase plasmática em tartarugas marinhas da espécie Chelonia mydas em duas populações de acordo com o local de captura, sob ausência e provável influência de efeito antrópico. Foi utilizado um total de 74 animais e posteriormente divididos em dois grupos de acordo com o local de captura. Foram coletadas amostras de sangue de todos os animais capturados e em seguida liberados ao mar no mesmo local. Foi realizada uma análise estatística descritiva dos valores da atividade plasmática de colinesterase do total de animais e análise comparando os valores de acordo com o local de captura. Foram analisadas amostras de plasma heparinizado de animais capturados em dois locais distintos. Os valores da atividade plasmática de colinesterase variaram de 121 a 248U/L, com média e desvio padrão de 186.1±30.7U/L. Quando comparados os valores de atividade plasmática da colinesterase nos indivíduos de acordo com o local de captura, foi observada diferença significativa. O estabelecimento de valores de referência para diferentes populações de tartarugas marinhas são necessários para interpretar os futuros resultados amostrais e permitir que as tartarugas marinhas sejam usadas como sentinelas da saúde do ecossistema. Estudos futuros são necessários para avaliar outras populações e a atividade da colinesterase plasmática de tartarugas marinhas juvenis em relação à contaminação ambiental.(AU)


Subject(s)
Animals , Turtles/blood , Cholinesterases/analysis , Biomarkers , Environmental Biomarkers
3.
São Paulo; s.n; 2020. 195 p.
Thesis in Portuguese | LILACS | ID: biblio-1050627

ABSTRACT

Introdução: O uso excessivo e descuidado de pesticidas tem se tornado um problema global de saúde pública, especialmente nos países de baixa e média renda. O Brasil é o maior consumidor mundial de pesticidas desde 2018, mas poucos estudos epidemiológicos exploram os seus efeitos à saúde. Objetivos: Avaliar os efeitos da exposição aos pesticidas à saúde de agricultores familiares em São José de Ubá (SJU), Estado do Rio de Janeiro, e analisar os efeitos respiratórios em crianças por exposição aos pesticidas, a partir de revisão da literatura. Métodos: Na safra de 2014, 82 agricultores familiares convenientemente selecionados foram entrevistados sobre a exposição aos pesticidas e submetidos à avaliação clínica com anamnese, avaliação respiratória (questionário e espirometria) e rastreamento de saúde mental (SRQ-20). Analisou-se as enzimas colinesterase (AChE e BChE) como biomarcadores de efeito. A avaliação respiratória foi repetida na entressafra de 2015 para comparação entre os períodos de maior e menor uso de pesticidas. Os participantes foram comparados com valores de referência e entre os grupos ocupacionais (aplicadores ou ajudantes) e os efeitos respiratórios foram analisados por regressão múltipla. Para ampliar o olhar aos riscos da exposição ambiental, realizou-se uma revisão sistemática sobre os efeitos dos pesticidas à saúde respiratória de crianças. Resultados: Os agricultores familiares avaliados em SJU estavam ocupacionalmente e ambientalmente expostos aos pesticidas desde tenra idade, trabalhavam sem apoio técnico e uso de equipamentos de proteção individual (EPI) completo, estavam expostos a complexas misturas de pesticidas frequentemente e apresentaram diversos sintomas de intoxicação aguda, mentais, respiratórios e alterações na espirometria. No geral, observou-se uma maior prevalência de efeitos respiratórios na safra do que na entressafra e associações significativas entre alterações espirométricas e os indicadores de exposição tanto na safra quanto na entressafra. Enquanto os aplicadores eram principalmente homens e apresentaram mais alterações de BChE, os ajudantes eram majoritariamente mulheres, tiveram ainda menos treinamento, usavam menos EPI e relataram maior prevalência de sintomas de intoxicação, saúde mental e o dobro apresentou um possível transtorno mental comum (depressão e ansiedade). A revisão da literatura sobre efeitos da exposição aos pesticidas agrícolas à saúde infantil apresentou vasta evidência sobre efeitos respiratórios e alérgicos. Conclusões: É fundamental melhorar o apoio técnico e treinamento ocupacional dos agricultores familiares brasileiros e promover práticas laborais e alternativas de cultivo mais sustentáveis. São necessários mais estudos sobre os efeitos dos pesticidas à saúde dos agricultores familiares e à saúde respiratória de crianças no Brasil e em outros países de menor renda, que usam métodos mais convencionais de cultivo e possuem maior população infantil no campo. Recomenda-se o fortalecimento de políticas públicas e a implementação de ações integrais e transversais a todos os níveis de atenção à saúde e áreas de governo, além da promoção de estratégias mais abrangentes de mitigação de riscos e intervenções comportamentais para reduzir o uso de pesticidas, a exposição e os riscos à saúde.


Introduction: Excessive and careless use of pesticides has become a global public health problem, especially in low- and middle-income countries. Brazil is the world's largest consumer of pesticides since 2018, but few epidemiological studies explore its health effects. Objectives: To evaluate the health effects of pesticide exposure on family farmers in São José de Ubá (SJU), State of Rio de Janeiro, and to analyze the respiratory effects of pesticide exposure among children, based on a literature review. Methods: In the crop season of 2014, 82 family farmers conveniently selected were interviewed about pesticide exposure and subjected to clinical evaluation with anamnesis, respiratory assessment (questionnaire and spirometry), and mental health screening (SRQ-20). Cholinesterase enzymes (AChE and BChE) were analyzed as effect biomarkers. The respiratory assessment was repeated in the off-season period (2015) to compare periods of higher and lower pesticide use. Participants were compared with reference values and between occupational groups (applicators or helpers), and respiratory effects were analyzed by multiple regression. A systematic review of the pesticide effects of children's respiratory health was conducted to broaden the understanding of the pesticide risks of environmental exposure. Results: Family farmers evaluated in SJU were occupationally and environmentally exposed to pesticides from an early age, worked without technical support and use of full personal protection equipment (PPE), were frequently exposed to complex mixtures of pesticides and presented several symptoms of acute intoxication, mental, respiratory, and changes in spirometry. Overall, there was a higher prevalence of respiratory effects in the crop season than in the off-season and significant associations between spirometric changes and exposure indicators in both the crop season and off-season. While the applicators were mostly men and had more BChE depletion, the helpers were mostly women, had even less occupational training, used less PPE, and reported a higher prevalence of pesticide poisoning symptoms, mental health, and twice as much as a probable common mental disorder (depression and anxiety). The literature review on the effects of agricultural pesticide exposure on children's health has provided ample evidence on respiratory and allergic effects. Conclusions: It is essential to improve the technical support and occupational training of Brazilian family farmers and to promote more sustainable labor practices and farming alternatives. Further studies are needed on the effects of pesticides on family farmer's health and children's respiratory health in Brazil and other lower-income countries that use more conventional cultivation methods and have a larger child population in the countryside. Strengthening public policies and implementing comprehensive and crosscutting actions at all levels of health care and areas of government is recommended, along with the promotion of broader risk mitigation strategies and behavioral interventions to reduce pesticide use, exposure, and health risks.


Subject(s)
Pesticides , Signs and Symptoms, Respiratory , Spirometry , Mental Health , Cholinesterases , Occupational Health , Agrochemicals
4.
Article in English | WPRIM | ID: wpr-762273

ABSTRACT

BACKGROUND: The reversal of a neuromuscular blockade has typically been achieved with a cholinesterase inhibitor and the concomitant use of an anticholinergic agent, and this remains a popular method. Since the introduction of sugammadex in the market, its use has been increasing because of the rapid recovery from a neuromuscular blockade achieved by rocuronium. The occurrence of anaphylaxis or an anaphylactic reaction resulting from sugammadex is rare and has been reported sparsely. Thus, one may not recognize the possibility of sugammadex-induced hypersensitivity when sudden life-threatening hypotension occurs, especially without skin manifestations during the emergence of anesthesia. This may delay treatment and increase morbidity. CASE: We report a case of a sugammadex-related hypersensitivity reaction which manifested as pure cardiovascular collapse during the emergence of anesthesia. CONCLUSIONS: We emphasize that vigilance should be paid for at least five minutes following sugammadex administration in daily clinical practice.


Subject(s)
Anaphylaxis , Anesthesia , Cholinesterases , Hypersensitivity , Hypotension , Methods , Neuromuscular Blockade , Skin Manifestations
5.
Natural Product Sciences ; : 115-121, 2019.
Article in English | WPRIM | ID: wpr-760555

ABSTRACT

Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl(1→6)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-15β-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at 100 µM. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and π-π stacking interactions which could explain the compound potency to inhibit AChE and BChE.


Subject(s)
Acetylcholinesterase , Alzheimer Disease , Butyrylcholinesterase , Cholinesterases , Hydrogen , In Vitro Techniques , Neurodegenerative Diseases
6.
The Egyptian Journal of Hospital Medicine ; 76(7): 4662-4668, 2019. tab
Article in English | AIM, AIM | ID: biblio-1272787

ABSTRACT

Background: hepatitis C virus can cause both acute and chronic hepatitis. The acute process is self-limited, rarely causes hepatic failure and usually leads to chronic infection. Chronic HCV infection often follows a progressive course over many years and can ultimately result in cirrhosis, HCC and the need for liver transplantation. Objective: the aim of this study is to evaluate serum cholinesterase (CHE) level as a biomarker for detecting liver damage in patients with chronic hepatitis C. Patients and Methods: the current study was carried out on 50 subjects selected from the outpatient's clinic of Internal Medicine Department of Sayed Galal Hospital, Al-Azhar University and admitted to the internal department. The study was performed in the period between July-2014 to July -2019. Results: Sensitivity of cholinesterase is 100%, its specificity is 100% and its accuracy is 100%, in predicting liver injury in patients with chronic hepatitis C. Cholinesterase is positively correlated with Hb, platelets and albumin. Cholinesterase is negatively correlated with ALT, AST and ALP, total & direct bilirubin, PT, INR, urea, creatinine and AFP. There is significant increase of cholinesterase among compensated compared with decompensated cirrhotic patients. There is significant decrease of cholinesterase among compensated cirrhotic patients compared with controls. There is significant decrease of cholinesterase among decompensated cirrhotic patients compared with controls. Conclusion: cholinesterase is an excellent biomarker of cirrhosis with good sensitivity and specificity. Cholinesterase shows good correlation with albumin, PT, INR and Child-Puch score. Cholinesterase distinguishes decompensated cirrhosis from compensated cirrhosis well


Subject(s)
Cholinesterases , Hepacivirus , Liver , Serum
7.
Acta toxicol. argent ; 26(3): 104-112, Dec. 2018. ilus, tab
Article in Portuguese | LILACS | ID: biblio-1001122

ABSTRACT

Anualmente milhões de agricultores são intoxicados no mundo, e destes, mais de 20 mil morrem em consequência da exposição a agrotóxicos. Intoxicações por organofosforados (OF) e carbamatos (CAR) representam as maiores ameaças à saúde dos trabalhadores rurais. Os OF e CAR atuam na inibição da enzima colinesterase, sendo assim a inibição desta mostra-se um excelente indicador da severidade da intoxicação. O objetivo deste estudo foi analisar o impacto do uso de OF e CAR em trabalhadores rurais na cidade de Mato Queimado/RS. Foi realizado um estudo transversal, prospectivo e experimental. Investigaramse 27 trabalhadores rurais expostos. Foram realizadas coletas sanguíneas e dados epidemiográficos nos meses de fevereiro e março de 2014. A atividade da colinesterase foi determinada através do método bioquímico cinético colorimétrico. A faixa etária média dos participantes foi 34,6 anos (± 8,5). A forma de contato mais prevalente foi a aplicação do produto (88,9%). O tempo médio de exposição foi de 10,7 anos. 70,4% relataram usar equipamentos de proteção individual (EPI), sendo mais frequente o uso de máscara (55,5%). A média dos valores de colinesterase para foi de 3244,45 U/I (± 345,8), níveis estes abaixo dos de referência. Através dos resultados obtidos nesta pesquisa torna-se imprescindível a utilização de meios de monitoramento biológico dos trabalhadores rurais na finalidade de prevenção e promoção da saúde.


Annually millions of rural workers are intoxicated in the world, and of these, more than 20,000 die as a result of exposure to pesticides. Intoxication by insecticides organophosphate (OF) and carbamates (CAR) represent the greatest threats to the health of rural workers. OF CAR and act on the inhibition of cholinesterase enzyme, thus inhibition of this proves to be an excellent indicator of the severity of the intoxication. The objective of this study was to analyze the impact of using OF CAR and in rural workers in the city of Mato Queimado/RS. A cross-sectional, prospective and experimental study was conducted. Twenty-three rural workers exposed were investigated. Sample collection and data demographic were conducted in February and March 2014. The cholinesterase activity was determined by biochemical kinetic colorimetric method. The average age of participants was 34.6 years (± 8.5). The most prevalent form of contact is via the application of the product (88.9%). The mean duration of exposure was 10.7 years. Still, 70.4% reported using personal protective equipment (PPE), more frequent use of mask (55.5%). The average values for cholinesterase was 3244.45 U/l (± 345.8) levels below those of the reference. The results obtained in this study are essential to use biological monitoring means of rural workers in purpose of prevention and health promotion.


Subject(s)
Humans , Male , Adult , Middle Aged , Rural Workers , Carbamates/poisoning , Carbamates/blood , Occupational Exposure/statistics & numerical data , Organophosphate Poisoning/blood , Brazil/epidemiology , Cholinesterase Inhibitors/blood , Cholinesterases/blood , Agrochemicals/poisoning
8.
Bol. méd. postgrado ; 34(1): 49-54, Ene-Jun. 2018. tab, graf
Article in Spanish | LILACS, LIVECS | ID: biblio-1121155

ABSTRACT

La succinilcolina es un fármaco neuromuscular despolarizante generalmente utilizado en el contexto de protocolo de intubación de secuencia rápida indicada en pacientes en los cuales es necesario asegurar la vía aérea en menos de sesenta segundos. Se realizó un estudio descriptivo transversal con el objetivo de determinar la duración del bloqueo neuromuscular con succinilcolina y los niveles de colinesterasa plasmática en pacientes sépticos intervenidos en el Hospital Central Universitario Dr. Antonio María Pineda. Se incluyeron 30 pacientes con sepsis con un promedio de edad de 49,6 ± 17,4 años y predominio del sexo masculino (70%); la principal indicación de cirugía abdominal fue obstrucción intestinal (36,6%) y peritonitis secundaria (23,3%). Los valores de colinesterasa plasmática se registraron disminuidos en 42,8% de los hombres y 33,3% de las mujeres encontrándose valores promedios de 5554,1 ± 1220,5 U/L y 4770,1 ± 1627,4 U/L, respectivamente. La duración del bloqueo neuromuscular fue mayor de 14 minutos en 66,6% de las mujeres; el promedio de duración fue de 14,4 ± 5,1 min (mujeres) y 9,4 ± 4,3 min en hombres. Hubo una pobre correlación entre los niveles de colinesterasa plasmática y la duración así como el tiempo de recuperación del bloqueo neuromuscular. En conclusión, el bloqueo neuromuscular prolongado debido a la baja actividad de la colinesterasa después de la administración de succinilcolina se presenta en menos de la mitad de los pacientes sépticos estudiados(AU)


Succinylcholine is a depolarizing neuromuscular drug generally used in the context of rapid sequence intubation indicated in patients in whom it is necessary to secure the airway in less than sixty seconds. A descriptive cross-sectional study was conducted in order to determine the duration of neuromuscular blockade with succinylcholine and plasma cholinesterase levels in septic patients admitted at Hospital Central Universitario Dr. Antonio Maria Pineda. A sample of 30 patients with sepsis were studied, with a mean age of 49.6 ± 17.4 years, predominantly male (70%). The main indication for abdominal surgery was intestinal obstruction (36.6%) and secondary peritonitis (23.3%). Diminished values of plasma cholinesterase were recorded in 42.8% of men and 33.3% of women; mean plasma levels were 5554.1 ± 1220.5 U/L and 4770.1 ± 1627.4 U/L, respectively. Duration of neuromuscular blockade was longer in women (66.6%) with an average duration of 14.4 ± 5.1 min and 9.4 ± 4.3 min for men. A poor correlation between cholinesterase plasmatic levels and duration as well as time of recovery of neuromuscular blockage was found. Prolonged neuromuscular blockade is due to low cholinesterase activity after administration of succinylcholine and occurs in less than half of septic patients studied(AU)


Subject(s)
Humans , Male , Female , Succinylcholine/pharmacology , Rapid Sequence Induction and Intubation , Anesthesia, Endotracheal , Cholinesterases , Sepsis , Patient Care
9.
Article in English | WPRIM | ID: wpr-717096

ABSTRACT

OBJECTIVE: In severe organophosphate (OP) poisoning, administration of atropine via continuous intravenous infusion is typically considered. To date, there have been no studies on predicting successful atropine discontinuation through plasma cholinesterase (PChE) and serum lactate levels, which are monitored during critical care in severe acute OP poisoning. Therefore, we retrospectively evaluated the usefulness of serum lactate and PChE as predictors of successful discontinuation of atropine infusion. METHODS: This retrospective observational study was performed on consecutive adult patients treated for severe acute OP poisoning between March 2011 and December 2016. We sequentially evaluated serum lactate and PChE levels on emergency department arrival and before a discontinuation trial of atropine infusion. Discontinuation of atropine intravenous infusion was attempted in patients after clearance of respiratory secretions and cessation of bronchoconstriction. Discontinuation of atropine infusion attempts were divided into successful and failed trials. RESULTS: A total of 95 trials were conducted in 62 patients. Serum lactate levels before trials were significantly different between patients with successful and failed trials. The area under the curve for prediction of successful atropine discontinuation using serum lactate levels before trial discontinuation were 0.742 (95% confidence interval, 0.638 to 0.846). PChE level was not significantly different between two groups. CONCLUSION: Serum lactate levels before the discontinuation trial of atropine infusion served to predict successful discontinuation in severe acute OP poisoning.


Subject(s)
Adult , Atropine , Bronchoconstriction , Cholinesterases , Critical Care , Emergency Service, Hospital , Humans , Infusions, Intravenous , Lactic Acid , Observational Study , Organophosphate Poisoning , Plasma , Poisoning , Prognosis , Retrospective Studies
10.
Yonsei Medical Journal ; : 982-988, 2018.
Article in English | WPRIM | ID: wpr-717930

ABSTRACT

PURPOSE: Organophosphates, commonly used in agricultural pesticides, pose high risks and incidences of poisoning. In the present study, we investigated the relative risk and clinical severity, including laboratory results, of non-oral route poisoning (NORP) patients, compared to oral route poisoning (ORP) patients. MATERIALS AND METHODS: A single institutional toxicology database registry was utilized to gain information on clinical laboratory results on organophosphate poisoning patients who visited the emergency department (ED) between January 2000 and October 2016. Clinical outcomes, such as mortality and complication rates, were compared using 1:2 propensity score matching in the total cohort. RESULTS: Among a total of 273 patients in our study, 34 experienced NORP. After 1:2 propensity score matching, rates of respiratory complications and mortality were higher in the ORP group than in the NORP group. However, there was no difference in hospitalization time and time spent in the intensive care unit between the two groups. Compared with ORP patients after matching, the relative risk of mortality in NORP patients was 0.34, and the risk of respiratory distress was 0.47. The mean level of pseudocholinesterase was significantly higher in the NORP group than in the ORP group, while recovery rates were similar between the two groups. CONCLUSION: Although the majority of NORP patients were admitted to the ED with unintentional poisoning and the relative risk of NORP was lower than that for ORP, we concluded that NORP is as critical as ORP. Considerable medical observation and intensive therapeutic approaches are also needed for NORP patients.


Subject(s)
Cholinesterases , Cohort Studies , Emergency Service, Hospital , Hospitalization , Humans , Incidence , Intensive Care Units , Mortality , Organophosphate Poisoning , Organophosphates , Pesticides , Poisoning , Propensity Score , Butyrylcholinesterase , Toxicology
11.
Natural Product Sciences ; : 259-265, 2018.
Article in English | WPRIM | ID: wpr-741632

ABSTRACT

The three flavone glycosides, 4′-O-methylisoscutellarein 7-O-(6‴-O-acetyl)-β-D-allopyranosyl(1→2)-β-D-glucopyranoside (1), isoscutellarein 7-O-(6‴-O-acetyl)-β-D-allopyranosyl(1→2)-β-D-glucopyranoside (3), and isoscutellarein 7-O-β-D-allopyranosyl(1→2)-β-D-glucopyranoside (4) in addition to a flavonol glycoside, kaempferol 3-O-β-D-glucopyranoside (astragalin, 2), were isolated from Stachys japonica (Lamiaceae). In cholinesterase inhibition assay, compound 1 significantly inhibited aceylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities (IC₅₀s, 39.94 µg/ml for AChE and 86.98 µg/ml for BChE). The content of isolated compounds were evaluated in this plant extract by HPLC analysis. Our experimental results suggest that the flavonoid glycosides of S. japonica could prevent the memory impairment of Alzheimer's disease.


Subject(s)
Alzheimer Disease , Butyrylcholinesterase , Cholinesterases , Chromatography, High Pressure Liquid , Glycosides , Lamiaceae , Memory , Plants , Stachys
12.
Article in English | WPRIM | ID: wpr-741612

ABSTRACT

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor (12.65 ± 1.57 µg/ml) while garcinexanthone G (6) was the most active BChE inhibitor (18.86 ± 2.41 µg/ml). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.


Subject(s)
Butyrylcholinesterase , Catalytic Domain , Cholinesterase Inhibitors , Cholinesterases , Computer Simulation , Drug Design , Garcinia , Hydrogen Bonding , In Vitro Techniques , Quercetin , Xanthones
13.
Salud trab. (Maracay) ; 25(1): 23-36, jun. 2017. tab, ilus
Article in Spanish | LILACS, LIVECS | ID: biblio-1117073

ABSTRACT

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)


Subject(s)
Humans , Male , Pesticides/toxicity , Working Conditions , Butyrylcholinesterase , Carbamates , Cholinesterases , Agricultural Workers' Diseases/prevention & control , Biological Monitoring
14.
Article in English | WPRIM | ID: wpr-61398

ABSTRACT

Pneumatosis cystoides intestinalis and portomesenteric venous gas are uncommon radiological findings, but are found commonly in cases of bowel ischemia, or as a result of various non-ischemic conditions. A 72-year-old man visited an emergency center with altered mental status 2 hours after ingestion of an unknown pesticide. On physical examination, he showed the characteristic hydrocarbon or garlic-like odor, miotic pupils with no response to light, rhinorrhea, shallow respiration, bronchorrhea, and sweating over his face, chest and abdomen. Laboratory results revealed decreased serum cholinesterase, as well as elevated amylase and lipase level. We made the clinical diagnosis of organophosphate poisoning in this patient based on the clinical features, duration of symptoms and signs, and level of serum cholinesterase. Activated charcoal, fluid, and antidotes were administered after gastric lavage. A computerized tomography scan of the abdomen with intravenous contrast showed acute pancreatitis, poor enhancement of the small bowel, pneumatosis cystoides intestinalis, portomesenteric venous gas and ascites. Emergent laparotomy could not be performed because of his poor physical condition and refusal of treatment by his family. The possible mechanisms were believed to be direct intestinal mucosal damage by pancreatic enzymes and secondary mucosal disruption due to bowel ischemia caused by shock and the use of inotropics. Physicians should be warned about the possibility of pneumatosis cystoides intestinalis and portomesenteric venous gas as a complication of pancreatitis following anticholinesterase poisoning.


Subject(s)
Abdomen , Aged , Amylases , Antidotes , Ascites , Charcoal , Cholinesterases , Diagnosis , Eating , Emergencies , Gastric Lavage , Humans , Ischemia , Laparotomy , Lipase , Odorants , Organophosphate Poisoning , Pancreatitis , Physical Examination , Pneumatosis Cystoides Intestinalis , Poisoning , Pupil , Respiration , Shock , Sweat , Sweating , Thorax , Treatment Refusal
15.
Article in English | WPRIM | ID: wpr-166104

ABSTRACT

Neuromuscular blockade plays an important role in the safe management of patient airways, surgical field improvement, and respiratory care. Rapid-sequence induction of anesthesia is indispensable to emergency surgery and obstetric anesthesia, and its purpose is to obtain a stable airway, adequate depth of anesthesia, and appropriate respiration within a short period of time without causing irritation or damage to the patient. There has been a continued search for new neuromuscular blocking drugs (NMBDs) with a rapid onset of action. Factors that affect the onset time include the potency of the NMBDs, the rate of NMBDs reaching the effect site, the onset time by dose control, metabolism and elimination of NMBDs, buffered diffusion to the effect site, nicotinic acetylcholine receptor subunit affinity, drugs that affect acetylcholine (ACh) production and release at the neuromuscular junction, drugs that inhibit plasma cholinesterase, presynaptic receptors responsible for ACh release at the neuromuscular junction, anesthetics or drugs that affect muscle contractility, site and methods for monitoring neuromuscular function, individual variability, and coexisting disease. NMBDs with rapid onset without major adverse events are expected in the next few years, and the development of lower potency NMBDs will continue. Anesthesiologists should be aware of the use of NMBDs in the management of anesthesia. The choice of NMBD and determination of the appropriate dosage to modulate neuromuscular blockade characteristics such as onset time and duration of neuromuscular blockade should be considered along with factors that affect the effects of the NMBDs. In this review, we discuss the factors that affect the onset time of NMBDs.


Subject(s)
Acetylcholine , Anesthesia , Anesthesia, Obstetrical , Anesthetics , Cholinesterases , Diffusion , Drug Interactions , Emergencies , Humans , Metabolism , Neuromuscular Blockade , Neuromuscular Blocking Agents , Neuromuscular Junction , Neuromuscular Monitoring , Pharmacokinetics , Plasma , Receptors, Nicotinic , Receptors, Presynaptic , Respiration
16.
Braz. J. Pharm. Sci. (Online) ; 53(1): e15237, 2017. tab, graf
Article in English | LILACS | ID: biblio-839448

ABSTRACT

Abstract In the study presented here, a new series of 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives was targeted. The synthesis was initiated by the treatment of different secondary amines (1a-h) with 4-bromomethylbenzenesulfonyl chloride (2) to obtain various 1-{[4-(bromomethyl)phenyl]sulfonyl}amines (3a-h). 2-Furyl(1-piperazinyl)methanone (2-furoyl-1-piperazine; 4) was then dissolved in acetonitrile, with the addition of K2CO3, and the mixture was refluxed for activation. This activated molecule was further treated with equi-molar amounts of 3a-h to form targeted 2-furyl(4-{4-[(substituted)sulfonyl]benzyl}-1-piperazinyl)methanone derivatives (5a-h) in the same reaction set up. The structure confirmation of all the synthesized compounds was carried out by EI-MS, IR and 1H-NMR spectral analysis. The compounds showed good enzyme inhibitory activity. Compound 5h showed excellent inhibitory effect against acetyl- and butyrylcholinesterase with respective IC50 values of 2.91±0.001 and 4.35±0.004 µM, compared to eserine, a reference standard with IC50 values of 0.04±0.0001 and 0.85±0.001 µM, respectively, against these enzymes. All synthesized molecules were active against almost all Gram-positive and Gram-negative bacterial strains tested. The cytotoxicity of the molecules was also checked to determine their utility as possible therapeutic agents.


Subject(s)
Computer Simulation/statistics & numerical data , Anti-Infective Agents/analysis , Piperazines/analysis , Complement Hemolytic Activity Assay , Cholinesterases/pharmacology
17.
Rev. Soc. Bras. Med. Trop ; 49(6): 693-697, Dec. 2016. tab, graf
Article in English | LILACS | ID: biblio-829668

ABSTRACT

Abstract: INTRODUCTION: Dengue fever is a viral disease transmitted by the Aedes aegypti Linn. (1792) (Diptera: Culicidae) mosquito, which is endemic in several regions of Brazil. Alternative methods for the control of the vector include botanical insecticides, which offer advantages such as lower environmental contamination levels and less likelihood of resistant populations. Thus, in this study, the ability of botanical insecticide formulations to inhibit the activity of the liver enzymes serum cholinesterase and malate dehydrogenase was evaluated. METHODS: Inhibition profiles were assessed using in vitro assays for cholinesterase and malate dehydrogenase activity and quantitated by ultraviolet-visible spectroscopy at 410nm to 340nm. RESULTS Insecticide products formulated from cashew nutshell liquid [A] and ricinoleic acid [B] showed cholinesterase activity levels of 6.26IU/mL and 6.61IU/mL, respectively, while the control level for cholinesterase was 5-12IU/mL. The products did not affect the level of 0.44IU/mL established for malate dehydrogenase, as the levels produced by [A] and [B] were 0.43IU/mL and 0.45IU/mL, respectively. CONCLUSIONS Our findings show that in vitro testing of the formulated products at concentrations lethal to A. aegypti did not affect the activity of cholinesterase and malate dehydrogenase, indicating the safety of these products.


Subject(s)
Humans , Animals , Ricinoleic Acids/pharmacology , Cholinesterase Inhibitors/pharmacology , Cholinesterases/drug effects , Anacardium/chemistry , Insecticides/pharmacology , Liver/enzymology , Malate Dehydrogenase/antagonists & inhibitors , Spectrophotometry, Ultraviolet , In Vitro Techniques , Ricinoleic Acids/isolation & purification , Aedes , Insect Vectors/drug effects , Insecticides/isolation & purification
18.
Mycobiology ; : 291-301, 2016.
Article in English | WPRIM | ID: wpr-729711

ABSTRACT

Culinary mushroom Pleurotus pulmonarius has been popular in Asian countries. In this study, the anti-oxidant, cholinesterase, and inflammation inhibitory activities of methanol extract (ME) of fruiting bodies of P. pulmonarius were evaluted. The 1,1-diphenyl-2-picryl-hydrazy free radical scavenging activity of ME at 2.0 mg/mL was comparable to that of butylated hydroxytoluene, the standard reference. The ME exhibited significantly higher hydroxyl radical scavenging activity than butylated hydroxytoluene. ME showed slightly lower but moderate inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase than galantamine, a standard AChE inhibitor. It also exhibited protective effect against cytotoxicity to PC-12 cells induced by glutamate (10~100 µg/mL), inhibitory effect on nitric oxide (NO) production and inducible nitric oxide synthase protein expression in lipopolysaccharide-stimulated RAW 264.7 macrophages, and carrageenan-induced paw edema in a rat model. High-performance liquid chromatography analysis revealed the ME of P. pulmonarius contained at least 10 phenolic compounds and some of them were identified by the comparison with known standard phenolics. Taken together, our results demonstrate that fruiting bodies of P. pulmonarius possess antioxidant, anti-cholinesterase, and inflammation inhibitory activities.


Subject(s)
Acetylcholinesterase , Agaricales , Asian Continental Ancestry Group , Butylated Hydroxytoluene , Butyrylcholinesterase , Cholinesterases , Chromatography, Liquid , Edema , Fruit , Galantamine , Glutamic Acid , Humans , Hydroxyl Radical , Inflammation , Macrophages , Methanol , Models, Animal , Nitric Oxide , Nitric Oxide Synthase Type II , Phenol , Pleurotus
19.
Article in Chinese | WPRIM | ID: wpr-282983

ABSTRACT

<p><b>OBJECTIVE</b>To observe the effect of sodium bicarbonate combined with ulinastatin on cholinesterase activity for patients with acute phoxim pesticide poisoning.</p><p><b>METHODS</b>A total of 67 eligible patients with acute phoxim pesticide poisoning, Who were admitted to the emeryency department of hospital from March 2011 to February 2014, Acording to different treatments au patients were randomly divided into the conventional treatment group (n=34) and the sodium bicarbonate+ulinastatin group (n=35) . The conventional treatment group were given thorough gastric lavage with water, the sodium bicarbonate + ulinastatin group were given gastric lavage with 2% sodium bicarbonate solution. Both groups were given such treatments as catharsis, administration of oxygen, fluid infusion, diuresis, and antidotes such as atropine and pralidoxime methylchloride. On the basis of comprehensive treatment, people in the sodium bicarbonate+ulinastatin group were given 5% sodium bicarbonate injection and ulinastatin. The clinical effect of the two groups were compared.</p><p><b>RESULTS</b>The serum cholinesterase activity of the sodium bicarbonate+ulinastatin group was significantly higher than the conventional treatment group from the 5th day, and the difference was statistically significant (P<0.05) . The total atropine dosage, total pralidoxime methylchloride dosage and hospitalization days were better than the conventional treatment group, and the differences were statistically significant (P<0.05) . The difference in the time of atropinization between the two groups was not statistically significant (P>0.05) . The results of arterial blood pH, HCO3- of the sodium bicarbonate + ulinastatin group were higher than the conventional treatment group, and the difference of HCO3- at the 10th day was statistically significant (P<0.05) .</p><p><b>CONCLUSIONS</b>Sodium bicarbonate combined with ulinastatin can improve the therapeutic effect and reduce complications in the treatment of acute phoxim pesticide poisoning, and have beneficial effects on the recovery of cholinesterase activity.</p>


Subject(s)
Atropine , Therapeutic Uses , Cholinesterases , Metabolism , Glycoproteins , Therapeutic Uses , Humans , Organophosphate Poisoning , Drug Therapy , Organothiophosphorus Compounds , Poisoning , Pesticides , Poisoning , Pralidoxime Compounds , Therapeutic Uses , Sodium Bicarbonate , Therapeutic Uses
20.
Psychiatry Investigation ; : 341-348, 2016.
Article in English | WPRIM | ID: wpr-19524

ABSTRACT

OBJECTIVE: This study compares the efficacy of the cholinesterase inhibitor (ChEI) galantamine on cognition in patients with mild-to-moderate Alzheimer's dementia (AD) who were either naïve to ChEI drugs or who had failed a trial of the ChEI donepezil. METHODS: Outpatients with AD were sequentially referred for screening and enrollment. Current outpatients who had taken donepezil for at least 6 months without demonstrated efficacy on cognition were switched to galantamine (switched group). New outpatients with no ChEI prescription history were classified as the naïve group and were given galantamine. The primary outcome measures for the between-group comparison were response rate on cognition at 26 and 52 weeks (categorical) and change on the Korean version of the Alzheimer's Disease Assessment Scale-cognitive subscale (dimensional). Secondary cognitive outcomes were measured using the subset of frontal executive function and the Korean Mini-Mental State Examination. RESULTS: Seventy outpatients were enrolled and 66 were analyzed by Intent-to-treat (ITT). There were 42 cases in the naïve group and 24 in the switched group. Response rates did not differ at 26 weeks (71.4% naïve vs. 58.3% switched; p=0.277) or at 52 weeks (59.5% naïve vs. 41.6% switched; p=0.162). No significant differences were observed in the pattern of change over the 52 weeks on the primary and secondary cognitive scales. CONCLUSION: As the efficacy of galantamine on cognition was not inferior in the switched group compared to that in the naïve group, switching ChEI drugs is clinically feasible for non-responding patients with mild-to-moderate AD.


Subject(s)
Alzheimer Disease , Cholinesterases , Cognition , Dementia , Executive Function , Galantamine , Humans , Mass Screening , Outcome Assessment, Health Care , Outpatients , Prescriptions , Weights and Measures
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