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1.
Rev Bras Parasitol Vet ; 29(2): e019819, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32609242

RESUMO

We investigated the in vitro acaricide activity of the methanolic extract (ME) and alkaloid-rich fraction (AF) of Prosopis juliflora on Rhipicephalus microplus and correlated this effect with acetylcholinesterase (AChE) inhibition. The acaricide activity was evaluated using adult and larval immersion tests. Also, we studied the possible interaction mechanism of the major alkaloids present in this fraction via molecular docking at the active site of R. microplus AChE1 (RmAChE1). Higher reproductive inhibitory activity of the AF was recorded, with effective concentration (EC50) four times lower than that of the ME (31.6 versus 121 mg/mL). The AF caused mortality of tick larvae, with lethal concentration 50% (LC50) of 13.8 mg/mL. Both ME and AF were seen to have anticholinesterase activity on AChE of R. microplus larvae, while AF was more active with half-maximal inhibitory concentration (IC50) of 0.041 mg/mL. The LC-MS/MS analyses on the AF led to identification of three alkaloids: prosopine (1), juliprosinine (2) and juliprosopine (3). The molecular docking studies revealed that these alkaloids had interactions at the active site of the RmAChE1, mainly relating to hydrogen bonds and cation-pi interactions. We concluded that the alkaloids of P. juliflora showed acaricide activity on R. microplus and acted through an anticholinesterase mechanism.


Assuntos
Alcaloides , Colinesterases , Extratos Vegetais , Prosopis , Rhipicephalus , Acaricidas/farmacologia , Alcaloides/farmacologia , Animais , Colinesterases/metabolismo , Cromatografia Líquida , Ativação Enzimática/efeitos dos fármacos , Larva , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Prosopis/química , Rhipicephalus/efeitos dos fármacos , Rhipicephalus/enzimologia , Espectrometria de Massas em Tandem
2.
Arch Environ Contam Toxicol ; 79(2): 233-245, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32613299

RESUMO

Natural resource managers are concerned about the impacts of aerial ultra-low volume spray (ULV) of insecticides for mosquito control (i.e., mosquito adulticides) and seek science-driven management recommendations that reduce risk but allow vector control for nearby human populations. Managers at the National Key Deer Refuge (Florida Keys, FL) are concerned for ULV effects upon conservation efforts for imperiled butterflies (Florida leafwing [Anaea troglodyta floridalis] and Bartram's hairstreak [Strymon acis bartrami] butterflies). No-spray zones were designated for protection of those butterflies, but their effectiveness for mitigation is unclear. To address this uncertainty, cholinesterase activity (ChE) and mortality were monitored for caged butterflies gulf fritillary [Agraulis vanilla] and great southern white [Ascia monuste]) deployed on the Refuge during three aerial ULV applications of the insecticide naled. Residue samplers also were deployed to estimate butterfly exposure. Spray efficacy against mosquitoes was assessed by deploying caged mosquitoes at the same locations as the butterflies. Average naled residue levels on filter paper samplers in the target area (1882-2898 µg/m2) was significantly greater than in the no-spray zone (9-1562 µg/m2). Differences between the no-spray zone and target area for butterfly mortality and ChE were inconsistent. Average mortality was significantly lower, and average ChE was significantly higher in the no-spray zone for larvae of one species but not for larvae of the other species. Mosquito mortality did not differ significantly between the two areas. Data from the present study reflect the inconsistent effectiveness of no-spray zones on the Refuge using standard methods employed at the time by the vector control agency in the Florida Keys and possibly by other vector control agencies in similar coastal environments. Furthermore, these findings helped to guide the design and to improve the conservation value of future no-spray zone delineations while allowing for treatment in areas where mosquito control is necessary for vector-borne disease reduction.


Assuntos
Borboletas/fisiologia , Inibidores da Colinesterase/toxicidade , Controle de Mosquitos/métodos , Naled/toxicidade , Animais , Borboletas/efeitos dos fármacos , Colinesterases/metabolismo , Cervos , Florida , Humanos , Inseticidas , Larva/efeitos dos fármacos , Medição de Risco
4.
Life Sci ; 250: 117585, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32243928

RESUMO

AIMS: Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) have been associated with risk factors for metabolic syndrome (MetS). Our objective was to evaluate the effect of nicotinamide (NAM) on the activities, expression and protein content of cholinesterases in a MetS model. MAIN METHODS: MetS was induced in male rats administrating 40% fructose to the drinking water for 16 weeks. Additionally, from 5th week onward, the carbohydrate solution was replaced by NAM, at several concentrations for 5 h each morning for the next 12 weeks. In the 15th week, the glucose tolerance test was conducted, and blood pressure was measured. After the treatment period had concluded, the biochemical profile; oxidant stress; proinflammatory markers; and the activity, quantity and expression of cholinesterases were evaluated, and molecular docking analysis was performed. KEY FINDINGS: The MetS group showed anthropometric, hemodynamic and biochemical alterations and increased cholinesterase activity, inflammation and stress markers. In the liver, cholinesterase activity and mRNA, free fatty acid, tumor necrosis factor-alpha (TNF-α), and thiobarbituric acid-reactive substance (TBARS) levels were increased, while reduced glutathione (GSH) levels were decreased. NAM partially or totally decreased risk factors for MetS, markers of stress and inflammation, and the activity (serum and liver) and expression (liver) of cholinesterases. Molecular docking analysis showed that NAM has a greater affinity for cholinesterases than acetylcholine (ACh), suggesting NAM as an inhibitor of cholinesterases. SIGNIFICANCE: Supplementation with 40% fructose induced MetS, which increased the activity and expression of cholinesterases, oxidative stress and the inflammation. NAM attenuated these MetS-induced alterations and changes in cholinesterases.


Assuntos
Inflamação/metabolismo , Síndrome Metabólica/tratamento farmacológico , Niacinamida/uso terapêutico , Estresse Oxidativo , Receptores Colinérgicos/metabolismo , Acetilcolinesterase/metabolismo , Animais , Antropometria , Anti-Inflamatórios/uso terapêutico , Arildialquilfosfatase/metabolismo , Butirilcolinesterase/metabolismo , Colinesterases/metabolismo , Frutose , Regulação da Expressão Gênica , Teste de Tolerância a Glucose , Hemodinâmica , Humanos , Peroxidação de Lipídeos , Fígado/enzimologia , Masculino , Síndrome Metabólica/induzido quimicamente , Simulação de Acoplamento Molecular , Ratos , Ratos Sprague-Dawley
5.
Klin Lab Diagn ; 65(4): 212-215, 2020.
Artigo em Russo | MEDLINE | ID: mdl-32227725

RESUMO

Cholinesterase activity in mixed saliva of patients with somatic pathology was investigated. The results showed differences in enzyme activity depending on the disease. The highest salivary cholinesterase activity was detected in patients with bronchopulmonary pathology, and the lowest - in cardiovascular diseases. A reliable relationship between the changes in the activity of cholinesterase in saliva and the rate of salivation, and with patients taking atypical antipsychotics and M, H-anticholinergic drugs, was revealed.


Assuntos
Colinesterases/fisiologia , Pneumopatias/patologia , Saliva/enzimologia , Salivação , Antipsicóticos/administração & dosagem , Doenças Cardiovasculares , Antagonistas Colinérgicos/administração & dosagem , Humanos
6.
Zhonghua Wei Zhong Bing Ji Jiu Yi Xue ; 32(1): 44-49, 2020 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-32148230

RESUMO

OBJECTIVE: To investigate the relationship between serum cholinesterase (SChE) level and the prognosis of patients with septic shock (SS). METHODS: A total of 594 patients with SS admitted to the First Affiliated Hospital of Zhengzhou University from June 2013 to June 2017 were enrolled. General data such as gender, age, acute physiology and chronic health evaluation II (APACHE II) score were recorded as well as routine blood test, procalcitonin (PCT), hepatic function, renal function, coagulation function and blood gas analysis parameters within 48 hours of SS diagnosis. The patients were followed by telephone from September to October in 2019, and the outcome was recorded. The primary outcome was all-cause death 28 days after discharge. The secondary outcomes were all-cause death in intensive care unit (ICU) and 2 years after discharge, and the length of ICU stay. The patients were divided into two groups according to prognosis of 28 days: the survival group and the death group. The clinical data of the two groups were compared. Multivariate Cox regression analysis was used to screen prognostic risk factors of 28 days in patients with SS. The receiver operating characteristic (ROC) curve was used to explore predictive value of liver function parameter SChE for 28-day prognosis of patients with SS. The patients were divided into two groups according to the levels of SChE: the low SChE group (SChE ≤ 4 000 U/L) and the normal SChE group (SChE > 4 000 U/L). Kaplan-Meier survival curves were used to compare the cumulative survival rates without endpoint event of patients with different SChE levels. RESULTS: A total of 385 patients with SS were enrolled according to the inclusion and exclusion criteria, and a total of 356 patients were followed up successfully, with a follow-up rate of 92.5% (356/385). There were 142 survival patients and 214 death patients at 28 days, with a 28-day mortality rate of 60.1% (214/356). There were 116 survival patients and 240 death patients at 2 years, with a 2-year mortality rate of 67.4% (240/356). Compared with the 28-day survival group, the patients in the death group were older and had higher APACHE II score, partial hepatic and renal function parameters, higher level of blood lactate (Lac) and lower levels of white blood cell count (WBC), platelet count (PLT) and SChE with statistically significant differences. Multivariate Cox regression analysis showed that the age [relative risk (RR) = 1.444, 95% confidence interval (95%CI) was 1.090-1.914, P = 0.010], APACHE II score (RR = 2.249, 95%CI was 1.688-2.997, P = 0.000), SChE (RR = 1.469, 95%CI was 1.057-2.043, P = 0.022), and Lac (RR = 2.190, 95%CI was 1.636-2.931, P = 0.000) were independent risk factors for 28-day mortality of patients with SS. The ROC curve analysis showed that SChE had a weak prognostic value for 28-day prognosis of patients with SS [the area under ROC curve (AUC) was 0.574]. However, the combined predictive value of SChE, APACHE II score and Lac was greater than APACHE II score or Lac alone for prediction (AUC: 0.807 vs. 0.785, 0.697), with a sensitivity of 79.9% and a specificity of 68.5%. Compared with the normal SChE group (n = 88), the 28-day mortality of patients in the low SChE group (n = 268) was significantly increased [63.1% (169/268) vs. 51.1% (45/88), P < 0.05], but ICU mortality [59.7% (160/268) vs. 48.9% (43/88)], 2-year mortality [69.8% (187/268) vs. 60.2% (53/88)] or the length of ICU stay [days: 4 (2, 7) vs. 5 (2, 9)] between the two groups showed no statistical significance (all P > 0.05). Kaplan-Meier survival curve analysis showed that the cumulative survival rate without endpoint event of patients in the low SChE group was significantly lower than that in the normal SChE group (Log-Rank test: χ2 = 5.852, P = 0.016). CONCLUSIONS: Increased risk of 28-day mortality in patients with SS whose SChE is below normal. The level of SChE is an independent risk factor for 28-day death in SS patients, and it is one of the indicators to evaluate the short-term prognosis of patients with SS.


Assuntos
Colinesterases/sangue , Choque Séptico/diagnóstico , APACHE , Humanos , Unidades de Terapia Intensiva , Prognóstico , Curva ROC , Estudos Retrospectivos , Choque Séptico/enzimologia , Choque Séptico/mortalidade
7.
Toxicol Appl Pharmacol ; 394: 114954, 2020 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-32171570

RESUMO

Learning and memory deficits are obvious symptoms that develop over time in patients with poorly controlled diabetes. Hyperactivity of the renin-angiotensin system (RAS) is directly associated with ß-cell dysfunction and diabetic complications, including cognitive impairment. Here, we investigated the protective and molecular effects of two RAS modifiers, aliskiren; renin inhibitor and captopril; angiotensin converting enzyme inhibitor, on cognitive deficits in the rat hippocampus. Injection of low dose streptozotocin for 4 days resulted in type 1 diabetes. Then, poorly controlled diabetes was mimicked with ineffective daily doses of insulin for 4 weeks. The hyperglycaemia and pancreatic atrophy caused memory disturbance that were identifiable in behavioural tests, hippocampal neurodegeneration, and the following significant changes in the hippocampus, increases in the inflammatory marker interleukin 1ß, cholinesterase, the oxidative stress marker malondialdehyde and protein expression of phosphorylated extracellular-signal-regulated kinase and glycogen synthase kinase-3 beta versus decrease in the antioxidant reduced glutathione and protein expression of phosphorylated glycogen synthase kinase-3 beta. Blocking RAS with either drugs along with insulin amended all previously mentioned parameters. Aliskiren stabilized the blood glucose level and restored normal pancreatic integrity and hippocampal malondialdehyde level. Aliskiren showed superior protection against the hippocampal degeneration displayed in the earlier behavioural modification in the passive avoidance test, and the aliskiren group outperformed the control group in the novel object recognition test. We therefore conclude that aliskiren and captopril reversed the diabetic state and cognitive deficits in rats with poorly controlled STZ-induced diabetes through reducing oxidative stress and inflammation and modulating protein expression.


Assuntos
Amidas/uso terapêutico , Captopril/uso terapêutico , Disfunção Cognitiva/tratamento farmacológico , Disfunção Cognitiva/psicologia , Diabetes Mellitus Experimental/psicologia , Fumaratos/uso terapêutico , Quinase 3 da Glicogênio Sintase/antagonistas & inibidores , Hipocampo/efeitos dos fármacos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Animais , Aprendizagem da Esquiva/efeitos dos fármacos , Encéfalo/patologia , Colinesterases/metabolismo , Disfunção Cognitiva/etiologia , Diabetes Mellitus Experimental/patologia , Hipocampo/enzimologia , Hipocampo/patologia , Interleucina-1beta/biossíntese , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Pâncreas/patologia , Ratos , Ratos Sprague-Dawley , Reconhecimento Psicológico/efeitos dos fármacos
8.
Ecotoxicology ; 29(3): 314-326, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32107698

RESUMO

Anthropogenic activities promote changes in community structure and decrease the species abundance of amphibians. The aim of this study was to assess potential alterations in the antioxidant system and cholinesterase activity, histopathological and oxidative damage in Lithobates catesbeianus tadpoles exposed to water from the Cascavel River, in Southern Brazil. Water samples (140 L each) were collected from the headwater, urban and rural areas of the river. Tadpoles were acclimated for seven days. After acclimatization tadpoles were reared in water from the river, except for the control aquarium. After seven days, a portion of the liver was removed and prepared for cholinesterase (ChE), superoxide dismutase (SOD), catalase (CAT) and lipid peroxidation (LPO) analysis; another part of the tissue was prepared for histological examination. An elevation of CAT activity was observed for water from both urban and rural environments. A decrease in LPO reaction was detected, mainly among the tadpoles exposed to water from the rural area. These alternations can cause delay the metamorphosis and lead to metabolic dysfunction, interfering in survival capacity and diminishing, not only individual fitness, but that of the whole population.


Assuntos
Antioxidantes/metabolismo , Colinesterases/metabolismo , Rana catesbeiana/fisiologia , Poluentes Químicos da Água/toxicidade , Animais , Brasil , Larva/fisiologia , Peroxidação de Lipídeos , Metamorfose Biológica/efeitos dos fármacos , Rios , Poluentes Químicos da Água/metabolismo
9.
Pesqui. vet. bras ; 40(1): 72-76, Jan. 2020. tab, graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1091652

RESUMO

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)


Assuntos
Animais , Tartarugas/sangue , Colinesterases/análise , Biomarcadores , Biomarcadores Ambientais
10.
Res Vet Sci ; 129: 90-95, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31954319

RESUMO

This study aims to evaluate the effect of the presence of food and the material used in a panel of biomarkers in saliva of horses. For the food effect study, clean saliva was incubated with a known amount of food consisting of oats, hay or grass. Significant changes were observed when saliva was incubated with oats for total protein (P = .050) and phosphorus (P = .008), with grass for total protein (P = .037), salivary alpha-amylase (sAA, P = .018), total esterase (TEA, P = .018), butyrilcholinesterase (BChE, P = .037), adenosine deaminase (ADA, P = .037), and total bilirubin (P = .018), and with hay for sAA (P = .018), phosphorus (P = .037), γ-glutamyl transferase (gGT, P = .004), and creatine kinase (CK, P = .016). For the material-based collection study, saliva using a sponge and a cotton role at the same time were collected and compared. Lower values were obtained in clean saliva collected with cotton role compared to sponge for sAA (P = .030), TEA (P = .034), BChE (P = .003), gGT (P = .002) and cortisol (P < .001) In conclusion, the presence of food and the material used for its collection, can influence the results obtained when analytes are measured in saliva of horses.


Assuntos
Ração Animal/análise , Contaminação de Alimentos , Cavalos , Saliva/química , Adenosina Desaminase/química , Adenosina Desaminase/metabolismo , Animais , Bilirrubina/química , Bilirrubina/metabolismo , Biomarcadores/química , Biomarcadores/metabolismo , Carboxilesterase/química , Carboxilesterase/metabolismo , Colinesterases/química , Colinesterases/metabolismo , Dieta/veterinária , Proteínas na Dieta/química , Proteínas na Dieta/metabolismo , Feminino , Humanos , Hidrocortisona , Masculino , Fósforo/química , Fósforo/metabolismo , alfa-Amilases/química , alfa-Amilases/metabolismo
11.
Sci Total Environ ; 711: 135228, 2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-31822418

RESUMO

Flower cultivation in greenhouses enhances productivity and ensures high-quality product supply throughout the year. However, under such protected environments, climate conditions are designed to favor flower growth and can intensify occupational exposure to pesticides. In this study, flower greenhouse workers were tested for cholinesterase inhibition, a valuable indicator of occupational exposure to organophosphate and carbamate pesticides. The quantified inhibition was also associated with working practices using these outcomes to explore ways in which provisions of regulatory Occupational Health Control Programs can be met considering the peculiarities of this working environment. Despite their preliminary nature, and considering that workers had not been previously tested, the obtained results suggested that the designed pre- and post-screening process, enabled biomonitoring of the exposed population. The pre-exposure sample was collected after 11 days from pesticide spraying and the post-exposure sample was collected no later than 10 days after pesticide spraying. AChE activity was significantly depressed in flower greenhouse workers, comparing pre- and post-exposure intervals. Nursery workers, often overlooked, presented greater inhibition of AChE activity. Such finding is consistent with effects believed to be associated with the described job and the way activities are conducted, once nursery workers are regularly exposed to low levels of pesticides owing to their continuous contact with sprayed crops. As predicted by Occupational Safety and Health Standards, establishing biomonitoring programs is achievable, despite the intensive use of pesticides. Quantification is important to target the exposed population but is not sufficient to assure good working conditions and avoid exposure. Administrative and working practices, such as job misclassification, non-compliance with national regulations for occupational health control, pesticide handling, lack of REI protocols, and unsuitable delivery of PPE, must be addressed. Anything less will contribute to worsening an already bleak picture in terms of occupational safety and health in flower and ornamental plant greenhouses.


Assuntos
Monitoramento Biológico , Exposição Ocupacional , Colinesterases , Flores , Humanos , Praguicidas
12.
São Paulo; s.n; 2020. 195 p.
Tese em Português | LILACS | ID: biblio-1050627

RESUMO

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.


Assuntos
Praguicidas , Sinais e Sintomas Respiratórios , Espirometria , Saúde Mental , Colinesterases , Saúde do Trabalhador , Agroquímicos
13.
Phytochemistry ; 169: 112162, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31627115

RESUMO

Twelve undescribed triterpenoid pentacyclic glycosides, medicagenic acid (3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 3-O-ß-D-glucuronopyranosyl-28-O-{[α-L-rhamnopyranosyl-(1 → 2)]-[ß-D-apiofuranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 3-O-ß-D-glucuronopyranosyl-28-O-{[α-L-rhamnopyranosyl-(1 → 2)]-3,4-O-diacetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[2-O-acetyl-α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[3-O-acetyl-α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[4-O-acetyl-α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[ß-D-glucopyranosyl-(1 → 2)]-[ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid), zanhic acid (3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}2ß,3ß,16α-trihydroxyolean-12-ene-23,28-dioic acid, 3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-ß-D-fucopyranosyl-(1→)}-2ß,3ß,16α-trihydroxyolean-12-ene-23,28-dioic acid), 29-hydroxy-medicagenic acid (3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß,29ß-trihydroxyolean-12-ene-23,28-dioic acid) and herniaric acid (28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-18-ene-23,28-dioic acid) were isolated from the whole plant extract of Herniaria glabra L. (Caryophyllaceae), wild growing in the Ukraine. In addition, five known triterpenoid saponins; i.e. herniariasaponins 1, 4, 5, 6, and 7 were also isolated. Their structures were elucidated by HRESIMS, 1D and 2D NMR spectroscopy, as well as by comparison with the literature data. Twelve herniariasaponins, the purified crude extract, and the saponin fraction were evaluated in vitro for their xanthine oxidase, collagenase, elastase, and tyrosinase inhibitory activity. Moreover, herniariasaponins 4, 5, and 7 were screened for their cholinesterase inhibitory potential. As a result, no or low inhibition towards the mentioned enzymes was observed.


Assuntos
Caryophyllaceae/química , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Animais , Colinesterases/metabolismo , Colagenases/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Conformação Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Elastase Pancreática/antagonistas & inibidores , Elastase Pancreática/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Saponinas/química , Saponinas/isolamento & purificação , Estereoisomerismo , Ucrânia , Xantina Oxidase/antagonistas & inibidores , Xantina Oxidase/metabolismo
14.
Pestic Biochem Physiol ; 162: 23-28, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31836050

RESUMO

Glyphosate (GLP) is one of the most common herbicides worldwide. The serum cholinesterase (ChE) may be affected when exposed to glyphosate. Reduction of serum ChE by herbicides is probably related to cytochrome P450 (CYP450) family polymorphisms. We suspect that the abnormal ChE caused by GLP could be correlated with the CYP family members. To determine whether CYP1B1 (rs1056827 and rs1056836) and CYP1A1 (rs1048943) gene polymorphisms and individual susceptibility to GLP-induced ChE abnormalities were interrelated in the Chinese Han population, we performed this genetic association study on a total of 230 workers previously exposed to GLP, including 115 cases with reduced serum ChE and 115 controls with normal serum ChE. Two even groups of cases and controls were enrolled. The CYP1A1 and CYP1B1 polymorphisms in both groups were genotyped using TaqMan. Subjects with the CYP1A1 rs619586 genotypes showed an increased risk of GLP-induced reduction of serum ChE, which was more evident in the following subgroups: female, > 35 years old, history of GLP exposure time <10 years and >10 years, nonsmoker and nondrinker. The results show that CYP1A1 rs619586 was significantly associated with the GLP-induced reduction in serum ChE and could be a biomarker of susceptibility for Chinese GLP exposed workers. Because of a large number of people exposed to glyphosate, this study has a significance in protecting their health.


Assuntos
Citocromo P-450 CYP1A1 , Polimorfismo Genético , Adulto , Estudos de Casos e Controles , Colinesterases , Feminino , Genótipo , Glicina/análogos & derivados , Humanos
15.
Artigo em Inglês | MEDLINE | ID: mdl-31874287

RESUMO

Pharmaceutical drugs are usually and continuously carried to the aquatic environment in different ways. Thus, they are pseudo-persistent in the environment, and they may exert deleterious effects on aquatic organisms. The objective of the present study was to investigate the acute and chronic effects of two widely used pharmaceutical drugs, paracetamol (analgesic and antipyretic) and propranolol (ß-blocker) on the activity of specific biomarkers (namely cholinesterase enzymes and lactate dehydrogenase) of the neotropical fish Phalloceros harpagos. The obtained results indicate an inhibition of the activity of the enzyme lactate dehydrogenase (LDH) after acute exposure to paracetamol, and an increase in cholinesterase activity in acutely propranolol-exposed fish. Chronic exposure to both drugs did not modify the enzymatic activities. Such short-term changes in enzymatic activities may be harmful to organisms, altering the preferential pathway of energy metabolism, and may induce behavioral changes that may compromise prey capture and predator escape, and in the longer term may induce population declines.


Assuntos
Acetaminofen/toxicidade , Colinesterases/metabolismo , Ciprinodontiformes/metabolismo , L-Lactato Desidrogenase/metabolismo , Propranolol/toxicidade , Poluentes Químicos da Água/toxicidade , Animais , Biomarcadores/metabolismo , Poluição Química da Água
16.
PLoS Pathog ; 15(12): e1008213, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31809524

RESUMO

Cholinesterase (ChE) function in schistosomes is essential for orchestration of parasite neurotransmission but has been poorly defined with respect to the molecules responsible. Interrogation of the S. mansoni genome has revealed the presence of three ChE domain-containing genes (Smche)s, which we have shown to encode two functional acetylcholinesterases (AChE)s (Smache1 -smp_154600 and Smache2 -smp_136690) and a butyrylcholinesterase (BChE) (Smbche1 -smp_125350). Antibodies to recombinant forms of each SmChE localized the proteins to the tegument of adults and schistosomula and developmental expression profiling differed among the three molecules, suggestive of functions extending beyond traditional cholinergic signaling. For the first time in schistosomes, we identified ChE enzymatic activity in fluke excretory/secretory (ES) products and, using proteomic approaches, attributed this activity to the presence of SmAChE1 and SmBChE1. Parasite survival in vitro and in vivo was significantly impaired by silencing of each smche, either individually or in combination, attesting to the essential roles of these molecules. Lastly, in the first characterization study of a BChE from helminths, evidence is provided that SmBChE1 may act as a bio-scavenger of AChE inhibitors as the addition of recombinant SmBChE1 to parasite cultures mitigated the effect of the anti-schistosome AChE inhibitor 2,2- dichlorovinyl dimethyl phosphate-dichlorvos (DDVP), whereas smbche1-silenced parasites displayed increased sensitivity to DDVP.


Assuntos
Colinesterases/metabolismo , Schistosoma mansoni/enzimologia , Animais , Camundongos , Transdução de Sinais/fisiologia
17.
BMJ Case Rep ; 12(10)2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31586958

RESUMO

Bilateral symmetrical weakness of acute onset is not very uncommon and the differential varies widely from life-threatening neurological illnesses to metabolic and electrolyte derangements. We report the case of a young female with severe muscle weakness, respiratory distress and hypokalemia who required immediate intubation on arrival to emergency department. During hospital course, even after normalisation of serum potassium and some improvement in limb weakness, patient failed multiple attempts of extubation because of type II respiratory failure. Subsequently, acetyl cholinesterase antibodies were checked which came out positive, and diagnosis of myasthenia gravis and hypokalemic periodic paralysis was made. She was successfully extubated after intravenous pulse steroids, pyridostigmine and plasmapheresis. Patient was finally discharged home on oral steroids, pyridostigmine and azathioprine. In a patient presenting with hypokalemic weakness, the suspicion of a second disorder should be very high if weakness fails to resolve following correction of hypokalemia.


Assuntos
Paralisia Periódica Hipopotassêmica/diagnóstico , Miastenia Gravis/diagnóstico , Insuficiência Respiratória/diagnóstico , Adulto , Análise Química do Sangue , Colinesterases/sangue , Diagnóstico Diferencial , Evolução Fatal , Feminino , Humanos , Paralisia Periódica Hipopotassêmica/sangue , Paralisia Periódica Hipopotassêmica/complicações , Infusões Intravenosas , Debilidade Muscular/etiologia , Miastenia Gravis/sangue , Miastenia Gravis/complicações , Cloreto de Potássio/administração & dosagem , Cloreto de Potássio/uso terapêutico , Respiração Artificial , Insuficiência Respiratória/complicações
18.
Chem Biodivers ; 16(12): e1900434, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31587473

RESUMO

Terpenes are a widespread group of secondary metabolites that can be found in various family plants such as the Lamiaceae. In view of their numerous valuable biological activities, the industrial production of concrete terpenes and essential oils rich in the substances is intensively studied. Monoterpenes constitute a significant part of the whole group of the aforementioned secondary metabolites. This is due to their numerous biological activities and their ability to permeate the skin. Despite the fact that these substances have gain popularity, they are not comprehensively characterized. The presented review is based on studies of the biological activities of the most important monoterpenes and the essential oils rich in these compounds. The authors focused attention on antioxidant activity, inhibition towards acetyl- and butyrylcholinesterase, and α-amylase and α-glucosidase, antifungal, hepatoprotective, sedative properties, and their skin permeation enhancement.


Assuntos
Monoterpenos/química , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/patologia , Animais , Antioxidantes/química , Colinesterases/química , Colinesterases/metabolismo , Lamiaceae/química , Lamiaceae/metabolismo , Monoterpenos/farmacologia , Monoterpenos/uso terapêutico , Fator 2 Relacionado a NF-E2/química , Fator 2 Relacionado a NF-E2/metabolismo , Óleos Voláteis/química , Estresse Oxidativo/efeitos dos fármacos
19.
Arch Pharm (Weinheim) ; 352(11): e1900177, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31478569

RESUMO

No drug has been approved to prevent neuronal cell loss in patients suffering from Parkinson's disease (PD) or Alzheimer's disease (AD); despite increased comprehension of the underlying molecular causes, therapies target cognitive functional improvement and motor fluctuation control. Drug design strategies that adopt the "one protein, one target" philosophy fail to address the multifactorial aetiologies of neurodegenerative disorders such as AD and PD optimally. On the contrary, restoring neurotransmitter levels by combined combinatorial inhibition of cholinesterases, monoamine oxidases, and adenosine A2A A receptors, in conjunction with strategies to counter oxidative stress and beta-amyloid plaque accumulation, would constitute a therapeutically robust, multitarget approach. This extensive review delineates the therapeutic advantages of combining dual-acting molecules that inhibit monoamine oxidases and cholinesterases and/or adenosine A2A A receptors, and describes the structure-activity relationships of compound classes that include, but are not limited to, alkaloids, coumarins, chalcones, donepezil-propargylamine conjugates, homoisoflavonoids, resveratrol analogs, hydrazones, and pyrazolines. In the wake of recent advances in network biology, in silico approaches, and omics, this review emphasizes the need to consider conceptually informed research strategies for drug discovery, in the context of the mounting burden posed by chronic neurodegenerative diseases with complex aetiologies and pathophysiologies involving multiple signalling pathways and numerous drug targets.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/farmacologia , Colinesterases/metabolismo , Descoberta de Drogas , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/metabolismo , Doença de Parkinson/tratamento farmacológico , Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/antagonistas & inibidores , Peptídeos beta-Amiloides/metabolismo , Animais , Inibidores da Colinesterase/química , Humanos , Inibidores da Monoaminoxidase/química , Estresse Oxidativo/efeitos dos fármacos , Doença de Parkinson/metabolismo
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