Assessment of Cholinesterase inhibition activity of birds inhabiting pesticide exposed croplands and protected area in hot semi-arid region of Pakistan / Avaliação da atividade de inibição da colinesterase de pássaros que habitam áreas cultivadas e áreas protegidas expostas a pesticidas na região semiárida quente do Paquistão

Abstract Acetylcholinesterase (AChE) activity levels can be used as an indicator for AChE inhibition due to pesticide poisoning in bird species. We assessed the comparative brain cholinesterase (AChE) activity level of five bird species inhabiting pesticide exposed croplands and Protected Area i.e. Deva Vatala National Park (DVNP), Bhimber by using a spectrophotometric method. AChE activity levels ranged from 56.3 to 85.9 µmol/min/g of brain tissue of birds representing DVNP. However, AChE activity levels ranged from 27.6 to 79.9 µmol/min/g of brain tissue of birds representing croplands. AChE activity levels observed in Jungle babbler, Common babbler, and Red-vented bulbul showed significant differences (P < 0.05) at two sites. However, White wagtail and Black drongo demonstrated non-significant differences (P > 0.05). Maximum inhibition was recorded in Jungle babbler (53%) followed by Common babbler (35%), Red-vented bulbul (18%), White wagtail (15%), and Black drongo (7%). The brain cholinesterase inhibition levels under-protected ecosystems (DVNP, Bhimber) and agricultural landscape suggest insecticidal contamination and its impact on avifauna diversity. The study also emphasizes on the importance of pesticide-free zones to protect the biodiversity of birds.

Resumo Os níveis de atividade da acetilcolinesterase (AChE) podem ser usados ​​como um indicador para a inibição da AChE devido ao envenenamento por pesticidas em espécies de aves. Avaliamos o nível de atividade comparativa da colinesterase cerebral (AChE) de cinco espécies de aves que habitam áreas cultivadas expostas a pesticidas e Área Protegida, ou seja, Deva Vatala National Park (DVNP), Bhimber, usando um método espectrofotométrico. Os níveis de atividade da AChE variaram de 56,3 a 85,9 µmol / min / g de tecido cerebral de aves representando DVNP. No entanto, os níveis de atividade da AChE variaram de 27,6 a 79,9 µmol / min / g de tecido cerebral de aves representando áreas de cultivo. Os níveis de atividade de AChE observados no tagarela da selva, tagarela comum e bulbul vermelho exalado mostraram diferenças significativas (P < 0,05) em dois locais. No entanto, alvéola branca e drongo preto demonstraram diferenças não significativas (P > 0,05). A inibição máxima foi registrada no tagarela da selva (53%), seguido pelo tagarela comum (35%), bulbul vermelho (18%), alvéola branca (15%) e drongo preto (7%). Os níveis de inibição da colinesterase cerebral nos ecossistemas subprotegidos (DVNP, Bhimber) e na paisagem agrícola sugerem contaminação por inseticida e seu impacto na diversidade da avifauna. O estudo também enfatiza a importância das zonas livres de pesticidas para proteger a biodiversidade das aves.

The acetylcholinesterase as indicative of intoxication for pesticide in farmers of conventional and organic cultivation / A acetilcolinesterase como indicativo de intoxicação por pesticidas em agricultores de cultivo convencional e orgânico

In this sense the objective of assessing the levels of pesticide poisoning in rural farmers of San Sebastian and take AL, using acetylcholinesterase enzymes Erythrocyte and plasma as biological indicator of intoxication. This is a prospective, transversal and descriptive variables analyzed were: year whose, sex, age group, education, location, condition, route of exposure. The data were acquired by collecting blood samples and socio demographic information of farmers. Was put as the determining factor the type of conventional and organic farming, and periods of drought and rainy. 56 volunteers were analyzed. The analyses were performed in the automatic biochemical Analyzer Cobas Integra 400 plus®. According to the results of the analyses, it was the largest number of individuals with reduced values of cholinesterase, specifically the Group of conventional farming, the period of greatest change index was in the rainy season, where the activity of AChE, expressive values presented in the city of São Sebastião, with 80% result of intoxicated, in the city of the foot take, 21.73% over the same period. On analysis of the AChP, São Sebastião has obtained the highest number of contaminated with 18.75% and 30% respectively, in the District Take Foot stood between 10 and 21.73% of reduced levels of cholinesterase. This sets the organic system of cultivation, as the best alternative for prevention of future diseases, in addition to bringing quality of life for rural workers, as well as for consumers.(AU)

Nesse sentido objetivou-se avaliar os níveis de intoxicação por agrotóxicos em agricultores rurais de São Sebastião e Pé Leve - AL, utilizando as enzimas acetilcolinesterase Eritrocitária e Plasmática, como indicador biológico de intoxicação. Trata - se de um estudo prospectivo, transversal e descritivo cujas variáveis analisadas foram: ano, sexo, faixa etária, escolaridade, local, circunstância, via de exposição. Os dados foram adquiridos através da coleta das amostras de sangue e das informações sócio demográficas dos agricultores. Foi posto como fator determinante o tipo de cultivo convencional e orgânico, e os períodos de estiagem e chuvoso. Foram analisados 56 voluntários. As análises foram realizadas no analisador automático de bioquímica Cobas Integra® 400 plus. De acordo com os resultados das análises, percebeu-se maior número de indivíduos com valores diminuídos da colinesterase, especificamente no grupo de cultivo convencional, o período de maior índice de alteração foi na época chuvosa, onde a atividade da AChE, apresentou valores expressivos na cidade de São Sebastião, com resultado de 80% de intoxicados, na cidade do Pé Leve, obteve-se 21,73% no mesmo período. Na análise da AChP, São Sebastião obteve maior número de contaminados com 18,75% e 30% respectivamente, já no Distrito Pé Leve ficou entre 10 e 21,73% de níveis diminuídos da colinesterase. Isso define o sistema orgânico de cultivo, como a melhor alternativa para prevenção de futuras patologias, além de trazer qualidade de vida para os trabalhadores rurais, como também para os consumidores.(AU)

Kinetic and toxicological effects of synthesized palladium(II) complex on snake venom (Bungarus sindanus) acetylcholinesterase

The venom of the krait (Bungarus sindanus), an Elapidae snake, is highly toxic to humans and contains a great amount of acetylcholinesterase (AChE). The enzyme AChE provokes the hydrolysis of substrate acetylcholine (ACh) in the nervous system and terminates nerve impulse. Different inhibitors inactivate AChE and lead to ACh accumulation and disrupted neurotransmission. Methods: The present study was designed to evaluate the effect of palladium(II) complex as antivenom against krait venom AChE using kinetics methods. Results: Statistical analysis showed that krait venom AChE inhibition decreases with the increase of Pd(II) complex (0.025-0.05 µM) and exerted 61% inhibition against the AChE at a fixed concentration (0.5 mM) of ACh. Kinetic analysis using the Lineweaver Burk plot showed that Pd(II) caused a competitive inhibition. The compound Pd(II) complex binds at the active site of the enzyme. It was observed that K m (Michaelis-Menten constant of AChE-ACh into AChE and product) increased from 0.108 to 0.310 mM (45.74 to 318.35%) and V max remained constant with an increase of Pd(II) complex concentrations. In AChE K Iapp was found to increase from 0.0912 to 0.025 µM (29.82-72.58%) and did not affect the V maxapp with an increase of ACh from (0.05-1 mM). K i (inhibitory constant) was estimated to be 0.029µM for snake venom; while the K m was estimated to be 0.4 mM. The calculated IC50 for Pd(II) complex was found to be 0.043 µM at constant ACh concentration (0.5 mM). Conclusions: The results show that the Pd(II) complex can be deliberated as an inhibitor of AChE.(AU)

Kinetic and toxicological effects of synthesized palladium(II) complex on snake venom (Bungarus sindanus) acetylcholinesterase

The venom of the krait (Bungarus sindanus), an Elapidae snake, is highly toxic to humans and contains a great amount of acetylcholinesterase (AChE). The enzyme AChE provokes the hydrolysis of substrate acetylcholine (ACh) in the nervous system and terminates nerve impulse. Different inhibitors inactivate AChE and lead to ACh accumulation and disrupted neurotransmission. Methods: The present study was designed to evaluate the effect of palladium(II) complex as antivenom against krait venom AChE using kinetics methods. Results: Statistical analysis showed that krait venom AChE inhibition decreases with the increase of Pd(II) complex (0.025-0.05 µM) and exerted 61% inhibition against the AChE at a fixed concentration (0.5 mM) of ACh. Kinetic analysis using the Lineweaver Burk plot showed that Pd(II) caused a competitive inhibition. The compound Pd(II) complex binds at the active site of the enzyme. It was observed that K m (Michaelis-Menten constant of AChE-ACh into AChE and product) increased from 0.108 to 0.310 mM (45.74 to 318.35%) and V max remained constant with an increase of Pd(II) complex concentrations. In AChE K Iapp was found to increase from 0.0912 to 0.025 µM (29.82-72.58%) and did not affect the V maxapp with an increase of ACh from (0.05-1 mM). K i (inhibitory constant) was estimated to be 0.029µM for snake venom; while the K m was estimated to be 0.4 mM. The calculated IC50 for Pd(II) complex was found to be 0.043 µM at constant ACh concentration (0.5 mM). Conclusions: The results show that the Pd(II) complex can be deliberated as an inhibitor of AChE.(AU)

Determination of acute median lethal concentration and sublethal effects on AChE activity of Gymnotus carapo (Teleostei: Gymnotidae) exposed to trichlorfon / Determinação da concentração letal média e efeitos subletais da atividade AchE de Gymnotus carapo (Teleostei: Gymnotidae) exposto ao triclorfon

Trichlorfon (TRF) is a pesticide widely used in aquaculture to control fish ectoparasites. This pesticide is an inhibitor of acetylcholinesterase, an essential enzyme for termination of nerve impulses. High rates of TRF use generate risks to the environment and human health. In the environment, pesticides can affect the local fauna and generate an ecological breakdown. There are several studies performed with fish production; however, gaps are created for native fish with other commercial values. The tuvira (Gymnotus carapo) is a fish native to Brazilian fauna and has great commercial importance in sport fishing. The present study aimed to determine the lethal concentration of trichlorfon (Masoten) in Gymnotus carapo and its sublethal effects on the enzyme AChE. In this study, the acute toxicity (the concentrations to kill 50% of the fish LC50) of TRF in tuviras (Gymnotus carapo) and acetylcholinesterase inhibition in liver and muscle tissue of tuviras submitted to sublethal concentrations were evaluated. For the acute assay, concentrations of 0.0, 5.0, 7.5, 15, 22.5, 30, 37.5 and 45 mg L-1 were used for a period of 96 h. After the acute exposure period, a LC50 of 6.38 mg L-1 was determined. In the sublethal assay, concentrations of 0.0, 0.238, 0.438 and 0.638 mg L-1 were used, based on 10% of the LC50, over a period of 14 days. Two collections were performed: one at seven days and the other at the end (day 14). Inhibition of acetylcholinesterase in the liver was only shown (p < 0.05) for the treatment with 0.638 mg L-1 after 14 days of exposure. At seven days, muscle activity showed a significant difference only for the treatments 0.438 and 0.638 mg L-1, compared with the treatment 0.238 mg L-1 and control. At 14 days of exposure, only the treatment 0.638 mg L-1 showed significant differences in relation to the other groups, thus showing that enzyme recovery had occurred. The value found in the acute test allowed the conclusion that TRF presents moderately toxic characteristics to Gymnotus carapo. The toxicity parameter values calculated in the present study assisted in estimation of maximum allowable limits in bodies of water when combined with test data from other non-target organisms.(AU)

O triclorfon (TRC) é um pesticida muito utilizado na aquicultura para o controle de ectoparasitos de peixes. Este pesticida é um inibidor da acetilcolinesterase, uma enzima essencial para a finalização de impulsos nervosos. As altas concentrações utilizadas de TRC geram riscos ao meio ambiente e à saúde humana. No ambiente, os pesticidas podem afetar a fauna local e gerar um colapso ecológico. Existem vários estudos com peixes de produção, no entanto, há lacunas para peixes nativos com outros valores comerciais. A tuvira (Gymnotus carapo) é um peixe nativo da fauna brasileira e possui grande importância comercial na pesca esportiva. O presente trabalho, delineado para determinar a concentração letal de triclorfon (Masoten) em Gymnotus carapo e seus efeitos subletais na enzima AChE, avaliou a toxicidade aguda (concentrações para matar 50% dos peixes CL50) do TRC em tuviras (Gymnotus carapo) e a inibição da acetilcolinesterase no fígado e tecido muscular de tuviras. Para o ensaio agudo, foram utilizadas concentrações de 0,0, 5,0, 7,5, 15, 22,5, 30, 37,5 e 45 mg L-1por um período de 96 horas. Após o período de exposição aguda, foi determinado uma CL50 de 6,38 mg L-1. No ensaio subletal, foram utilizadas concentrações de 0,0, 0,238, 0,438 e 0,638 mg L-1, com base em 10% do CL50, durante um período de catorze dias. Foram realizadas duas colheitas: uma aos sete dias e a outra ao final (décimo quarto dia). A inibição da acetilcolinesterase no fígado foi demonstrada apenas (p <0,05) para o tratamento com 0,638 mg L-1 após catorze dias de exposição. Aos sete dias, a atividade muscular mostrou diferença significativa apenas para os tratamentos 0,438 e 0,638 mg L-1, em comparação com o tratamento 0,238 mg L-1 e controle. Aos catorze dias de exposição, apenas o tratamento 0,638 mg L-1 apresentou diferenças significativas em relação aos demais grupos, demonstrando a recuperação enzimática. O valor encontrado no teste agudo permitiu concluir que o TRC apresenta características moderadamente tóxicas para Gymnotus carapo. Os valores dos parâmetros de toxicidade calculados no presente estudo permitiram o estabelecimento da estimativa dos limites máximos permitidos em corpos d'água quando combinados com dados de testes de outros organismos não-alvo.(AU)

Determination of acute median lethal concentration and sublethal effects on AChE activity of Gymnotus carapo (Teleostei: Gymnotidae) exposed to trichlorfon / Determinação da concentração letal média e efeitos subletais da atividade AchE de Gymnotus carapo (Teleostei: Gymnotidae) exposto ao triclorfon

Trichlorfon (TRF) is a pesticide widely used in aquaculture to control fish ectoparasites. This pesticide is an inhibitor of acetylcholinesterase, an essential enzyme for termination of nerve impulses. High rates of TRF use generate risks to the environment and human health. In the environment, pesticides can affect the local fauna and generate an ecological breakdown. There are several studies performed with fish production; however, gaps are created for native fish with other commercial values. The tuvira (Gymnotus carapo) is a fish native to Brazilian fauna and has great commercial importance in sport fishing. The present study aimed to determine the lethal concentration of trichlorfon (Masoten) in Gymnotus carapo and its sublethal effects on the enzyme AChE. In this study, the acute toxicity (the concentrations to kill 50% of the fish LC50) of TRF in tuviras (Gymnotus carapo) and acetylcholinesterase inhibition in liver and muscle tissue of tuviras submitted to sublethal concentrations were evaluated. For the acute assay, concentrations of 0.0, 5.0, 7.5, 15, 22.5, 30, 37.5 and 45 mg L-1 were used for a period of 96 h. After the acute exposure period, a LC50 of 6.38 mg L-1 was determined. In the sublethal assay, concentrations of 0.0, 0.238, 0.438 and 0.638 mg L-1 were used, based on 10% of the LC50, over a period of 14 days. Two collections were performed: one at seven days and the other at the end (day 14). Inhibition of acetylcholinesterase in the liver was only shown (p < 0.05) for the treatment with 0.638 mg L-1 after 14 days of exposure. At seven days, muscle activity showed a significant difference only for the treatments 0.438 and 0.638 mg L-1, compared with the treatment 0.238 mg L-1 and control. At 14 days of exposure, only the treatment 0.638 mg L-1 showed significant differences in relation to the other groups, thus showing that enzyme recovery had occurred. The value found in the acute test allowed the conclusion that TRF presents moderately toxic characteristics to Gymnotus carapo. The toxicity parameter values calculated in the present study assisted in estimation of maximum allowable limits in bodies of water when combined with test data from other non-target organisms.(AU)

O triclorfon (TRC) é um pesticida muito utilizado na aquicultura para o controle de ectoparasitos de peixes. Este pesticida é um inibidor da acetilcolinesterase, uma enzima essencial para a finalização de impulsos nervosos. As altas concentrações utilizadas de TRC geram riscos ao meio ambiente e à saúde humana. No ambiente, os pesticidas podem afetar a fauna local e gerar um colapso ecológico. Existem vários estudos com peixes de produção, no entanto, há lacunas para peixes nativos com outros valores comerciais. A tuvira (Gymnotus carapo) é um peixe nativo da fauna brasileira e possui grande importância comercial na pesca esportiva. O presente trabalho, delineado para determinar a concentração letal de triclorfon (Masoten) em Gymnotus carapo e seus efeitos subletais na enzima AChE, avaliou a toxicidade aguda (concentrações para matar 50% dos peixes CL50) do TRC em tuviras (Gymnotus carapo) e a inibição da acetilcolinesterase no fígado e tecido muscular de tuviras. Para o ensaio agudo, foram utilizadas concentrações de 0,0, 5,0, 7,5, 15, 22,5, 30, 37,5 e 45 mg L-1por um período de 96 horas. Após o período de exposição aguda, foi determinado uma CL50 de 6,38 mg L-1. No ensaio subletal, foram utilizadas concentrações de 0,0, 0,238, 0,438 e 0,638 mg L-1, com base em 10% do CL50, durante um período de catorze dias. Foram realizadas duas colheitas: uma aos sete dias e a outra ao final (décimo quarto dia). A inibição da acetilcolinesterase no fígado foi demonstrada apenas (p <0,05) para o tratamento com 0,638 mg L-1 após catorze dias de exposição. Aos sete dias, a atividade muscular mostrou diferença significativa apenas para os tratamentos 0,438 e 0,638 mg L-1, em comparação com o tratamento 0,238 mg L-1 e controle. Aos catorze dias de exposição, apenas o tratamento 0,638 mg L-1 apresentou diferenças significativas em relação aos demais grupos, demonstrando a recuperação enzimática. O valor encontrado no teste agudo permitiu concluir que o TRC apresenta características moderadamente tóxicas para Gymnotus carapo. Os valores dos parâmetros de toxicidade calculados no presente estudo permitiram o estabelecimento da estimativa dos limites máximos permitidos em corpos d'água quando combinados com dados de testes de outros organismos não-alvo.(AU)

The acetylcholinesterase as indicative of intoxication for pesticide in farmers of conventional and organic cultivation

Abstract In this sense the objective of assessing the levels of pesticide poisoning in rural farmers of San Sebastian and take AL, using acetylcholinesterase enzymes Erythrocyte and plasma as biological indicator of intoxication. This is a prospective, transversal and descriptive variables analyzed were: year whose, sex, age group, education, location, condition, route of exposure. The data were acquired by collecting blood samples and socio demographic information of farmers. Was put as the determining factor the type of conventional and organic farming, and periods of drought and rainy. 56 volunteers were analyzed. The analyses were performed in the automatic biochemical Analyzer Cobas Integra 400 plus®. According to the results of the analyses, it was the largest number of individuals with reduced values of cholinesterase, specifically the Group of conventional farming, the period of greatest change index was in the rainy season, where the activity of AChE, expressive values presented in the city of São Sebastião, with 80% result of intoxicated, in the city of the foot take, 21.73% over the same period. On analysis of the AChP, São Sebastião has obtained the highest number of contaminated with 18.75% and 30% respectively, in the District Take Foot stood between 10 and 21.73% of reduced levels of cholinesterase. This sets the organic system of cultivation, as the best alternative for prevention of future diseases, in addition to bringing quality of life for rural workers, as well as for consumers.

Resumo Nesse sentido objetivou-se avaliar os níveis de intoxicação por agrotóxicos em agricultores rurais de São Sebastião e Pé Leve - AL, utilizando as enzimas acetilcolinesterase Eritrocitária e Plasmática, como indicador biológico de intoxicação. Trata - se de um estudo prospectivo, transversal e descritivo cujas variáveis analisadas foram: ano, sexo, faixa etária, escolaridade, local, circunstância, via de exposição. Os dados foram adquiridos através da coleta das amostras de sangue e das informações sócio demográficas dos agricultores. Foi posto como fator determinante o tipo de cultivo convencional e orgânico, e os períodos de estiagem e chuvoso. Foram analisados 56 voluntários. As análises foram realizadas no analisador automático de bioquímica Cobas Integra® 400 plus. De acordo com os resultados das análises, percebeu-se maior número de indivíduos com valores diminuídos da colinesterase, especificamente no grupo de cultivo convencional, o período de maior índice de alteração foi na época chuvosa, onde a atividade da AChE, apresentou valores expressivos na cidade de São Sebastião, com resultado de 80% de intoxicados, na cidade do Pé Leve, obteve-se 21,73% no mesmo período. Na análise da AChP, São Sebastião obteve maior número de contaminados com 18,75% e 30% respectivamente, já no Distrito Pé Leve ficou entre 10 e 21,73% de níveis diminuídos da colinesterase. Isso define o sistema orgânico de cultivo, como a melhor alternativa para prevenção de futuras patologias, além de trazer qualidade de vida para os trabalhadores rurais, como também para os consumidores.

Biological screening of extracts from leaf and stem bark of Croton floribundus Spreng. (Euphorbiaceae) / Triagem biológica de extratos das folhas e caules de Croton floribundus Spreng. (Euphorbiaceae)

This work describes the preliminary evaluation of cytotoxic, antimicrobial, molluscicidal, antioxidant and anticholinesterase activities from leaf (LECF) and stem bark alcoholic extracts (BECF) of the species Croton floribundus Spreng. (Euphorbiaceae), popularly known as capixingui or tapixingui. BECF presented significant toxicity (LC50 = 89.6 μg/ml) in the Artemia salina Leach, 1819 (Crustacea: Branchiopoda) bioassay, whereas LECF did not show activity (LC50 > 1000 μg/ml). From DPPH method, the values of IC50 for the LECF and BECF were 61.2 μg/ml and 62.2 μg/ml, respectively, showing that C. floribundus has an expressive antioxidant activity. Antimicrobial susceptibility was evaluated by microdilution technique and only BECF was active against Staphylococcus aureus (MIC = 39.6 μg/ml). The extracts did not present molluscicidal activity against snail Biomphalaria glabrata Say, 1818 (Gastropoda: Planorbidae). Both extracts revealed the presence of several components with an inhibiting capacity of acetylcholinesterase enzyme on the bioautographic assay. C. floribundus showed to be a promising species considering that it exhibited good biological activity in the most assays performed.(AU)

Este trabalho descreve a avaliação preliminar das atividades citotóxica, antimicrobiana, moluscicida, antioxidante e anticolinesterásica de extratos alcoólicos das folhas (LECF) e das cascas do caule (BECF) da espécie Croton floribundus Spreng. (Euphorbiaceae), popularmente conhecida como capixingui ou tapixingui. No bioensaio com Artemia salina Leach, 1819 (Crustacea: Branchiopoda), BECF apresentou toxicidade significante (LC50 = 89,6 µg/ml), enquanto que LECF não apresentou atividade (LC50 > 1000 µg/ml). A partir do método de DPPH, os valores de IC50 para o LECF e BECF foram 61,2 µg/ml e 62,2 µg/ml, respectivamente, evidenciando que C. floribundus tem uma atividade antioxidante expressiva. A susceptibilidade antimicrobiana foi avaliada pela técnica de microdiluição e apenas BECF foi ativo contra Staphylococcus aureus (MIC = 39,6 mg/ml). Os extratos não apresentaram atividade moluscicida contra o caramujo Biomphalaria glabrata Say, 1818 (Gastropoda: Planorbidae). Ambos os extratos revelaram a presença de componentes com capacidade inibidora da enzima acetilcolinesterase no ensaio bioautográfico. C. floribundus mostrou ser uma espécie promissora considerando que exibiu boa atividade biológica na maioria dos ensaios testados.(AU)

Antimicrobial activity and acetylcholinesterase inhibition by extracts from chromatin modulated fungi

Major health challenges as the increasing number of cases of infections by antibiotic multiresistant microorganisms and cases of Alzheimer's disease have led to searching new control drugs. The present study aims to verify a new way of obtaining bioactive extracts from filamentous fungi with potential antimicrobial and acetylcholinesterase inhibitory activities, using epigenetic modulation to promote the expression of genes commonly silenced. For such finality, five filamentous fungal species (Talaromyces funiculosus, Talaromyces islandicus, Talaromyces minioluteus, Talaromyces pinophilus, Penicillium janthinellum) were grown or not with DNA methyltransferases inhibitors (procainamide or hydralazine) and/or a histone deacetylase inhibitor (suberohydroxamic acid). Extracts from T. islandicus cultured or not with hydralazine inhibited Listeria monocytogenes growth in 57.66 ± 5.98% and 15.38 ± 1.99%, respectively. Increment in inhibition of acetylcholinesterase activity was observed for the extract from P. janthinellum grown with procainamide (100%), when compared to the control extract (39.62 ± 3.76%). Similarly, inhibition of acetylcholinesterase activity increased from 20.91 ± 3.90% (control) to 92.20 ± 3.72% when the tested extract was obtained from T. pinophilus under a combination of suberohydroxamic acid and procainamide. Concluding, increases in antimicrobial activity and acetylcholinesterase inhibition were observed when fungal extracts in the presence of DNA methyltransferases and/or histone deacetylase modulators were tested.(AU)

Potencial inibitório in vitro de chás comerciais e da quercetina sobre a atividade de acetilcolinesterase cerebral em cães / The inhibitory potential in vitro of commercial teas and quercetin on cerebral acetylcholinesterase activity in dogs

Com o aumento na expectativa de vida dos animais de companhia há um maior aparecimento de doenças neurodegenerativas, como a Disfunção Cognitiva Canina (DCC). A DCC apresenta diversas semelhanças à Doença de Alzheimer (DA) presente em seres humanos. Entre estas semelhanças é possível citar o nível reduzido de acetilcolina, o que justifica a busca por tratamentos que tenham como foco, a inibição da acetilcolinesterase (AChE), enzima responsável pela degradação deste neurotransmissor. Neste trabalho foi avaliado o potencial inibitório dos chás de maçã, de hortelã e de chá verde sobre a atividade de AChE presente em cérebro de cães. O chá verde foi o chá mais eficaz na inibição desta enzima, apresentando uma IC50 de aproximadamente 1.7 mg/mL. A quercetina, flavonol que segundo a literatura está presente no chá verde e ausente nos chás de maçã e hortelã, pode ser um dos constituintes responsáveis por esta inibição. Desta forma, também foi avaliado o potencial anticolinesterásico da quercetina em cérebro canino, obtendo-se uma IC50 de 0,41 mM. Uma vez que a quercetina já tem sido utilizada na medicina veterinária para outros fins, o potencial anticolinesterásico deste flavonol em cérebro canino mostra-se de grande relevância para os estudos da DCC.

Canine Cognitive Dysfunction (CCD) is a neuodegenerative disease with very similar characteristics to humans Alzhemer’s disease. Currently, the increase of pets life expectancy leads to the more frequent appearance of neurodegenerative diseases in these species. Among the main hypotheses for the appearance of CCD has the reduction of acetylcholine levels in the synaptic cleft. This hypothesis justifies many researches that search CCD treatment based on acetylcholinesterase (AChE) inhibition, an acetylcholine degrading enzyme. In this work, inhibitory potential of some commecial teas (apple tea, peppermint tea and green tea) toward brain AChE activity of dogs was evaluated. Green tea is tea more effective to inhibit this enzyme, getting a IC 50 of approximately 1.7 mg / mL. Quercetin, flavonol which according to the literature is present in green tea and absent in apple and peppermint teas, may be one of the molecules that contribute to AChE inhibition. In this way, quercetn anticholinesterase potential in canine brain was also evaluated, obtaining an IC 50 of 0.41 mM. Since quercetin has already been used in veterinary medicine for other fins, the anticholinesterase potential of this flavonol toward canine brain is of great relevance for CCD studies.

Potencial inibitório in vitro de chás comerciais e da quercetina sobre a atividade de acetilcolinesterase cerebral em cães / The inhibitory potential in vitro of commercial teas and quercetin on cerebral acetylcholinesterase activity in dogs

Com o aumento na expectativa de vida dos animais de companhia há um maior aparecimento de doenças neurodegenerativas, como a Disfunção Cognitiva Canina (DCC). A DCC apresenta diversas semelhanças à Doença de Alzheimer (DA) presente em seres humanos. Entre estas semelhanças é possível citar o nível reduzido de acetilcolina, o que justifica a busca por tratamentos que tenham como foco, a inibição da acetilcolinesterase (AChE), enzima responsável pela degradação deste neurotransmissor. Neste trabalho foi avaliado o potencial inibitório dos chás de maçã, de hortelã e de chá verde sobre a atividade de AChE presente em cérebro de cães. O chá verde foi o chá mais eficaz na inibição desta enzima, apresentando uma IC50 de aproximadamente 1.7 mg/mL. A quercetina, flavonol que segundo a literatura está presente no chá verde e ausente nos chás de maçã e hortelã, pode ser um dos constituintes responsáveis por esta inibição. Desta forma, também foi avaliado o potencial anticolinesterásico da quercetina em cérebro canino, obtendo-se uma IC50 de 0,41 mM. Uma vez que a quercetina já tem sido utilizada na medicina veterinária para outros fins, o potencial anticolinesterásico deste flavonol em cérebro canino mostra-se de grande relevância para os estudos da DCC.(AU)

Canine Cognitive Dysfunction (CCD) is a neuodegenerative disease with very similar characteristics to humans Alzhemers disease. Currently, the increase of pets life expectancy leads to the more frequent appearance of neurodegenerative diseases in these species. Among the main hypotheses for the appearance of CCD has the reduction of acetylcholine levels in the synaptic cleft. This hypothesis justifies many researches that search CCD treatment based on acetylcholinesterase (AChE) inhibition, an acetylcholine degrading enzyme. In this work, inhibitory potential of some commecial teas (apple tea, peppermint tea and green tea) toward brain AChE activity of dogs was evaluated. Green tea is tea more effective to inhibit this enzyme, getting a IC 50 of approximately 1.7 mg / mL. Quercetin, flavonol which according to the literature is present in green tea and absent in apple and peppermint teas, may be one of the molecules that contribute to AChE inhibition. In this way, quercetn anticholinesterase potential in canine brain was also evaluated, obtaining an IC 50 of 0.41 mM. Since quercetin has already been used in veterinary medicine for other fins, the anticholinesterase potential of this flavonol toward canine brain is of great relevance for CCD studies.(AU)

The acetylcholinesterase as indicative of intoxication for pesticide in farmers of conventional and organic cultivation

Abstract In this sense the objective of assessing the levels of pesticide poisoning in rural farmers of San Sebastian and take AL, using acetylcholinesterase enzymes Erythrocyte and plasma as biological indicator of intoxication. This is a prospective, transversal and descriptive variables analyzed were: year whose, sex, age group, education, location, condition, route of exposure. The data were acquired by collecting blood samples and socio demographic information of farmers. Was put as the determining factor the type of conventional and organic farming, and periods of drought and rainy. 56 volunteers were analyzed. The analyses were performed in the automatic biochemical Analyzer Cobas Integra 400 plus®. According to the results of the analyses, it was the largest number of individuals with reduced values of cholinesterase, specifically the Group of conventional farming, the period of greatest change index was in the rainy season, where the activity of AChE, expressive values presented in the city of São Sebastião, with 80% result of intoxicated, in the city of the foot take, 21.73% over the same period. On analysis of the AChP, São Sebastião has obtained the highest number of contaminated with 18.75% and 30% respectively, in the District Take Foot stood between 10 and 21.73% of reduced levels of cholinesterase. This sets the organic system of cultivation, as the best alternative for prevention of future diseases, in addition to bringing quality of life for rural workers, as well as for consumers.

Resumo Nesse sentido objetivou-se avaliar os níveis de intoxicação por agrotóxicos em agricultores rurais de São Sebastião e Pé Leve - AL, utilizando as enzimas acetilcolinesterase Eritrocitária e Plasmática, como indicador biológico de intoxicação. Trata - se de um estudo prospectivo, transversal e descritivo cujas variáveis analisadas foram: ano, sexo, faixa etária, escolaridade, local, circunstância, via de exposição. Os dados foram adquiridos através da coleta das amostras de sangue e das informações sócio demográficas dos agricultores. Foi posto como fator determinante o tipo de cultivo convencional e orgânico, e os períodos de estiagem e chuvoso. Foram analisados 56 voluntários. As análises foram realizadas no analisador automático de bioquímica Cobas Integra® 400 plus. De acordo com os resultados das análises, percebeu-se maior número de indivíduos com valores diminuídos da colinesterase, especificamente no grupo de cultivo convencional, o período de maior índice de alteração foi na época chuvosa, onde a atividade da AChE, apresentou valores expressivos na cidade de São Sebastião, com resultado de 80% de intoxicados, na cidade do Pé Leve, obteve-se 21,73% no mesmo período. Na análise da AChP, São Sebastião obteve maior número de contaminados com 18,75% e 30% respectivamente, já no Distrito Pé Leve ficou entre 10 e 21,73% de níveis diminuídos da colinesterase. Isso define o sistema orgânico de cultivo, como a melhor alternativa para prevenção de futuras patologias, além de trazer qualidade de vida para os trabalhadores rurais, como também para os consumidores.

Megaesófago secundario a la miastenia gravis / Megaesophagus secondary to myasthenia gravis / gravis

Astenia esofágica o megaesófago se define por una dilatación patológica del esófago y caracterizado por una insuficiencia progresiva de las olas peristálticas. Esta enfermedad se puede clasificar en: idiopática, congénita o adquirida secundaria. La causa más común del megaesófago secundario es Miastenia gravis. Esta enfermedad se caracteriza por ser una neuropatía que desencadena un trastorno neuromuscular que causa debilidad del músculo esquelético, el esófago, la faringe y la laringe. La debilidad muscular se correlaciona con la mejoría tras el descanso y empeora con el ejercicio. El megaesófago secundario adquirido a la miastenia gravis se caracteriza por la interrupción del reflejo nervioso, controlador de la deglutición que afecta el funcionamiento de los músculos del esófago, lo que lleva a la dilatación pasiva del órgano. Razas como Pastor Alemán, Golden Retriever y Setter Irlandés tienen una mayor predisposición a la enfermedad.(AU)

Esophageal asthenia or megaesophagus is defined as a pathological dilation and progressive failure of peristaltic waves. This disease can be classified in: idiopathic, congenity or acquired secondary. The most common cause of acquired secondary megaesophagus is myasthenia gravis. This disease is defined as a neuropathy that develops a neuromuscular disorder, resulting in muscle weakness, of the esophagus, of the larynx and of the pharynx. The muscle weakness is related to improvement after rest and worsening with exercise. The megaesophagus secondary to myasthenia gravis is defined to nervous reflex breakdown, swallowing controller or lesions that affect the esophageal muscle function, resulting in an organ passive dilation. Breeds like German Shepherd, Golden Retriever and Irish Setter have a greater predisposition to disease.(AU)

Astenia esofágica ou megaesôfago é definido por uma dilatação patológica do esôfago e caracterizado por uma falha progressiva das ondas peristálticas. Essa doença pode ser classificada em: idiopática, congênita ou secundária adquirida. A causa mais comum de megaesôfago secundário adquirido é a miastenia gravis. Tal doença é caracterizada por ser uma neuropatia que desencadeia uma desordem neuromuscular, provocando fraqueza de musculatura esquelética, esôfago, faringe e laringe. A fraqueza muscular está correlacionada com melhora após o descanso e piora com o exercício. O megaesôfago adquirido secundário a miastenia gravis é caracterizado pelo rompimento do reflexo nervoso, controlador da deglutição ou que afeta o funcionamento da musculatura esofágica, levando a dilatação passiva do órgão. Raças como Pastor Alemão, Golden Retriever e Setter Irlandês possuem maior predisposição à doença.(AU)

Megaesófago secundario a la miastenia gravis / Megaesophagus secondary to myasthenia gravis / gravis

Astenia esofágica o megaesófago se define por una dilatación patológica del esófago y caracterizado por una insuficiencia progresiva de las olas peristálticas. Esta enfermedad se puede clasificar en: idiopática, congénita o adquirida secundaria. La causa más común del megaesófago secundario es Miastenia gravis. Esta enfermedad se caracteriza por ser una neuropatía que desencadena un trastorno neuromuscular que causa debilidad del músculo esquelético, el esófago, la faringe y la laringe. La debilidad muscular se correlaciona con la mejoría tras el descanso y empeora con el ejercicio. El megaesófago secundario adquirido a la miastenia gravis se caracteriza por la interrupción del reflejo nervioso, controlador de la deglutición que afecta el funcionamiento de los músculos del esófago, lo que lleva a la dilatación pasiva del órgano. Razas como Pastor Alemán, Golden Retriever y Setter Irlandés tienen una mayor predisposición a la enfermedad.

Esophageal asthenia or megaesophagus is defined as a pathological dilation and progressive failure of peristaltic waves. This disease can be classified in: idiopathic, congenity or acquired secondary. The most common cause of acquired secondary megaesophagus is myasthenia gravis. This disease is defined as a neuropathy that develops a neuromuscular disorder, resulting in muscle weakness, of the esophagus, of the larynx and of the pharynx. The muscle weakness is related to improvement after rest and worsening with exercise. The megaesophagus secondary to myasthenia gravis is defined to nervous reflex breakdown, swallowing controller or lesions that affect the esophageal muscle function, resulting in an organ passive dilation. Breeds like German Shepherd, Golden Retriever and Irish Setter have a greater predisposition to disease.

Astenia esofágica ou megaesôfago é definido por uma dilatação patológica do esôfago e caracterizado por uma falha progressiva das ondas peristálticas. Essa doença pode ser classificada em: idiopática, congênita ou secundária adquirida. A causa mais comum de megaesôfago secundário adquirido é a miastenia gravis. Tal doença é caracterizada por ser uma neuropatia que desencadeia uma desordem neuromuscular, provocando fraqueza de musculatura esquelética, esôfago, faringe e laringe. A fraqueza muscular está correlacionada com melhora após o descanso e piora com o exercício. O megaesôfago adquirido secundário a miastenia gravis é caracterizado pelo rompimento do reflexo nervoso, controlador da deglutição ou que afeta o funcionamento da musculatura esofágica, levando a dilatação passiva do órgão. Raças como Pastor Alemão, Golden Retriever e Setter Irlandês possuem maior predisposição à doença.

Reduced expression of exocytotic proteins caused by anti-cholinesterase pesticides in Brachionus calyciflorus (Rotifera: Monogononta) / Redução da expressão de proteínas de exocitose causados por pesticidas anti-colinesterase em Brachionus calyciflorus (Rotifera: Monogononta)

The organophosphate and carbamate pesticides methyl-parathion and carbaryl have a common action mechanism: they inhibit acetylcholinesterase enzyme by blocking the transmission of nerve impulses. However, they can alter the expression of exocytotic membrane proteins (SNARE), by modifying release of neurotransmitters and other substances. This study evaluated the adverse effects of the pesticides methyl-parathion and carbaryl on expression of SNARE proteins: Syntaxin-1, Syntaxin-4 and SNAP-23 in freshwater rotifer Brachionus calyciflorus. Protein expression of these three proteins was analyzed before and after exposure to these two pesticides by Western Blot. The expression of Syntaxin-1, Syntaxin-4 and SNAP-23 proteins in B. calyciflorussignificantly decreases with increasing concentration of either pesticides. This suggests that organophosphates and carbamates have adverse effects on expression of membrane proteins of exocytosis by altering the recognition, docking and fusion of presynaptic and vesicular membranes involved in exocytosis of neurotransmitters. Our results demonstrate that the neurotoxic effect of anticholinesterase pesticides influences the interaction of syntaxins and SNAP-25 and the proper assembly of the SNARE complex.(AU)

Os pesticidas organofosforados e carbamatos metil- paration e carbaril tem um mecanismo de ação comum: eles inibem a enzima acetilcolinesterase, bloqueando a transmissão dos impulsos nervosos. No entanto, eles podem alterar a expressão de proteínas de membrana de exocitose (SNARE), através da modificação da libertação de neurotransmissores e outras substâncias. Este estudo avaliou os efeitos adversos dos pesticidas metil- paration e carbaril sobre a expressão de proteínas SNARE: Sintaxina -1, Sintaxina-4 e SNAP-23 em rotíferos de água doce Brachionus calyciflorus. A expressão destas três proteínas foi analisada antes e depois da exposição a estes dois pesticidas por Western Blot. A expressão das proteínas Sintaxina-1, Sintaxina-4 e SNAP-23 em B. calyciflorus diminui significativamente com o aumento da concentração de ambos os pesticidas. Isto sugere que os organofosfatos e carbamatos têm efeitos adversos sobre a expressão de proteínas de membrana de exocitose, alterando o reconhecimento, de encaixe e fusão de membranas pré-sinápticas e vesiculares envolvidas na exocitose de neurotransmissores. Nossos resultados demonstram que o efeito neurotóxico de pesticidas anticolinesterásicos influencia a interação de sintaxinas e SNAP-25 e a montagem correta do complexo SNARE.(AU)

Enzymatic and biochemical characterization of Bungarus sindanus snake venom acetylcholinesterase

This study analyses venom from the elapid krait snake Bungarus sindanus, which contains a high level of acetylcholinesterase (AChE) activity. The enzyme showed optimum activity at alkaline pH (8.5) and 45ºC. Krait venom AChE was inhibited by substrate. Inhibition was significantly reduced by using a high ionic strength buffer; low ionic strength buffer (10 mM PO4 pH 7.5) inhibited the enzyme by 1. 5mM AcSCh, while high ionic strength buffer (62 mM PO4 pH 7.5) inhibited it by 1 mM AcSCh. Venom acetylcholinesterase was also found to be thermally stable at 45ºC; it only lost 5% of its activity after incubation at 45ºC for 40 minutes. The Michaelis-Menten constant (Km) for acetylthiocholine iodide hydrolysis was found to be 0.068 mM. Krait venom acetylcholinesterase was also inhibited by ZnCl2, CdCl2, and HgCl2 in a concentrationdependent manner. Due to the elevated levels of AChE with high catalytic activity and because it is more stable than any other sources, Bungarus sindanus venom is highly valuable for biochemical studies of this enzyme.(AU)

Leishmanicidal and cholinesterase inhibiting activities of phenolic compounds of Dimorphandra gardneriana and Platymiscium floribundum, native plants from Caatinga biome / Atividade inibitória Leishmanicida e Colinesterásica de Compostos Fenólicos de Dimorphandra gardneriana e Platymiscium fliribunbum, plantas nativas do bioma Caatinga

In recent years, the Brazilian Health Ministry and the World Health Organization have supported research into new technologies that may contribute to the surveillance, new treatments, and control of visceral leishmaniasis within the country. In light of this, the aim of this study was to isolate compounds from plants of the Caatinga biome, and to investigate their toxicity against promastigote and amastigote forms of Leishmania infantum chagasi, the main responsible parasite for South American visceral leishmaniasis, and evaluate their ability to inhibit acetylcholinesterase enzyme (AChE). A screen assay using luciferase-expressing promastigote form and an in situ ELISA assay were used to measure the viability of promastigote and amastigote forms, respectively, after exposure to these substances. The MTT colorimetric assay was performed to determine the toxicity of these compounds in murine monocytic RAW 264.7 cell line. All compounds were tested in vitro for their anti-cholinesterase properties. A coumarin, scoparone, was isolated from Platymiscium floribundum stems, and the flavonoids rutin and quercetin were isolated from Dimorphandra gardneriana beans. These compounds were purified using silica gel column chromatography, eluted with organic solvents in mixtures of increasing polarity, and identified by spectral analysis. In the leishmanicidal assays, the compounds showed dose-dependent efficacy against the extracellular promastigote forms, with an EC50 for scoporone of 21.4µg/mL, quercetin and rutin 26 and 30.3µg/mL, respectively. The flavonoids presented comparable results to the positive control drug, amphotericin B, against the amastigote forms with EC50 for quercetin and rutin of 10.6 and 43.3µg/mL, respectively. All compounds inhibited AChE with inhibition zones varying from 0.8 to 0.6, indicating a possible mechanism of action for leishmacicidal activity.(AU)

Nos últimos anos, o Ministério da Saúde do Brasil e a Organização Mundial da Saúde tem apoiado a investigação de novas tecnologias que possam contribuir para a vigilância, novos tratamentos e controle da leishmaniose visceral no país. Assim, o objetivo deste trabalho foi isolar compostos de plantas do bioma Caatinga, e investigar a toxicidade destes compostos contra as formas promastigotas e amastigotas de Leishmania infantum chagasi, principal parasita responsável pela leishmaniose visceral na América do Sul, e avaliar a sua capacidade para inibir a enzima acetil-colinesterase (AChE). Após a exposição aos compostos em estudo, foram realizados testes utilizando a forma promastigota que expressa luciferase e ELISA in situ para medir a viabilidade das formas promastigotas e amastigota, respectivamente. O ensaio colorimétrico MTT foi realizado para determinar a toxicidade destas substâncias utilizando células monocíticas murina RAW 264.7. Todos os compostos foram testados in vitro para as sua propriedade anti-colinesterásica. Um cumarina, escoparona, foi isolada a partir de hastes de Platymiscium floribundum, e os flavonóides, rutina e quercetina, foram isolados a partir de grãos de Dimorphandra gardneriana. Estes compostos foram purificados, utilizando cromatografia em coluna gel eluída com solventes orgânicos em misturas de polaridade crescente, e identificados por análise espectral. Nos ensaios leishmanicidas, os compostos fenólicos mostraram eficácia contra as formas extracelulares promastigotas, com EC50 para escoporona de 21.4µg/mL e para quercetina e rutina 26 e 30.3µg/mL, respectivamente. Os flavonóides apresentaram resultados comparáveis à droga controle, a anfotericina B, contra as formas amastigotas com EC50 para quercetina e rutina de 10.6 e 43.3µg/mL, respectivamente. Os compostos inibiram a enzima AChE com halos de inibição variando de 0,8 a 0,6cm, indicando um possível mecanismo de ação para a atividade leishmanicida.(AU)

Acetylcholinesterase inhibition by somes promising Brazilian medicinal plants / Plantas medicinais brasileiras promissoras para inibição da acetilcolinesterase

A microplate assay and a thin-layer chromatography (TLC) "in situ" assay based on the Ellman assay was used to screen for acetylcholinesterase inhibitors from ethyl acetate and methanol extracts of Brazilian medicinal plants of families that, according to the literature, have traditional uses that might be connected with acetylcholinesterase inhibition. Eighteen species belonging to Convolvulaceae, Crassulaceae, Euphorbiaceae, Leguminosae, Malvaceae, Moraceae, Nyctaginaceae and Rutaceae families were tested. The most active plants were Ipomoea asarifolia (IC50 = 0.12 mg/mL), Jatropha curcas (IC50 = 0.25 mg/mL), Jatropha gossypiifolia (IC50 = 0.05 mg/mL), Kalanchoe brasiliensis (IC50 = 0.16 mg/mL) and Senna alata (IC50 = 0.08 mg/mL). The most promising extracts were the Jatropha gossypiifolia and Senna alata species assuming there were compounds with a similar activity to galanthamine, which should contain about 1 percent of an active compound, or if present at lower levels even more active compounds than galanthamine (IC50 = 0.37 x 10-3 mg/mL) should be present.(AU)

Os ensaios de microplaca e cromatografia em camada delgada com base no ensaio de Ellman foram usados para triagem de inibidores da acetilcolinesterase dos extratos acetato de etila e metanol de plantas medicinais brasileiras de famílias que, segundo a literatura, tem usos tradicionais que podem estar relacionadas com a inibição da acetilcolinesterase, enzima associada ao mal de Alzheimer. Dezoito plantas das famílias: Convolvulaceae, Crassulaceae, Euphorbiaceae, Leguminosae, Malvaceae, Moraceae, Nyctaginaceae e Rutaceae foram testadas. As espécies mais ativas foram Ipomoea asarifolia (CI₅₀ = 0,12 mg/mL), Jatropha curcas (CI₅₀ = 0,25 mg/mL), Jatropha gossypiifolia (CI₅₀ = 0,05 mg/mL), Kalanchoe brasiliensis (CI₅₀ = 0,16 mg/mL) e Senna alata (CI₅₀ = 0,08 mg/mL). Os extratos mais promissores foram os das espécies Jatropha gossypiifolia e Senna alata, assumindo a presença de compostos com atividade semelhante à galantamina que deve conter cerca de 1 por cento de um composto ativo, ou se presentes em menores níveis ainda mais compostos ativos que a galantamina (CI₅₀ = 0,37 x10^–3 mg/mL) devem estar presentes.(AU)

Intoxicação por organofosforados em bezerros no Uruguai / Organophosphate poisoning in Calves in Uruguay

Background: Organophosphate compounds are used worldwide in animal agriculture as pesticides, inseticides and herbicides. The inappropriate use of these anticholinesterasic agents may cause poisoning, apart of great economic losses. Organophosphate poisoning may affect all animal species. Organophosphate overdose induce increase in tissue acetylcholine content and, therefore, enhanced parasympathetic and post-ganglionic sympathetic nerve activities. The toxic effects are shown as muscarinic, nicotinic and central nervous system signs. The muscarinic signs are characterized by increased peristaltism, salivation, lacrimation, nasal discharge, bronchial constrition, miosis and sudoresis, among others. The nicotinic signs are mainly locomotor signs and include muscular tremors, weakness, and flaccid paralysis. The effects on the central nervous system include inquietation, ataxia, convulsions, depression and coma. Minimal differences may be seen in the diseases caused by different compounds; nevertheless, the route of administration may facilitate the exacerbation of some signs instead of others. Case: This paper report an outbreak of organophosphate poisoning in calves. The disease occurred in a dairy farm located in Florida, Uruguay and affected female Holstein 15-day-old calves. The main owner complaints were apathy, standing difficulty and sialorrhea. Seven out of twenty calves presented neurological signs such as incoordination and sternal recumbency. The clinical examination revealed prostration, lacrimation, tongue protusion, muscular weakness and miosis. At anamnesis, the previous application, in the day before, of a pour-on inseticide was noticed. The composition of the commercial product was ethion (15%), which is an insecticide organophosphate widely used as an antiparasitic drug. Affected animals were treated with intravenous atropine sulfate 1% (0.50 mg/kg) and sodium chloride 0.9%. Atropine sulfate is a potent parasympatholytic agent that inhibits the effects of acetylcholine at the postganglionic parasympathetic neuroeffector junctions. Ten minutes after the treatment, most calves showed an improvement in health status. Only one calf needed two extra doses at 1-hour intervals to recuperate. The presumptive diagnosis was based on the clinical findings and supported by depressed blood cholinesterase level. Discussion: The rapid therapeutic response of affected animals to specific treatment also supports the hypothesis. The outcome of this outbreak relies in the aggressive approach of the team and adequate treatment choice. In spite of other differential diagnosis possibilities such as poisoning by carbamate and pyrethroid, the clinical findings, laboratory result and therapeutic response allowed us to attribute this outbreak to the misuse of organophosphate. The key to an excellent outcome, when dealing with organophosphate poisoning, is immediate treatment.

Intoxicação por organofosforados em bezerros no Uruguai / Organophosphate poisoning in Calves in Uruguay

Background: Organophosphate compounds are used worldwide in animal agriculture as pesticides, inseticides and herbicides. The inappropriate use of these anticholinesterasic agents may cause poisoning, apart of great economic losses. Organophosphate poisoning may affect all animal species. Organophosphate overdose induce increase in tissue acetylcholine content and, therefore, enhanced parasympathetic and post-ganglionic sympathetic nerve activities. The toxic effects are shown as muscarinic, nicotinic and central nervous system signs. The muscarinic signs are characterized by increased peristaltism, salivation, lacrimation, nasal discharge, bronchial constrition, miosis and sudoresis, among others. The nicotinic signs are mainly locomotor signs and include muscular tremors, weakness, and flaccid paralysis. The effects on the central nervous system include inquietation, ataxia, convulsions, depression and coma. Minimal differences may be seen in the diseases caused by different compounds; nevertheless, the route of administration may facilitate the exacerbation of some signs instead of others. Case: This paper report an outbreak of organophosphate poisoning in calves. The disease occurred in a dairy farm located in Florida, Uruguay and affected female Holstein 15-day-old calves. The main owner complaints were apathy, standing difficulty and sialorrhea. Seven out of twenty calves presented neurological signs such as incoordination and sternal recumbency. The clinical examination revealed prostration, lacrimation, tongue protusion, muscular weakness and miosis. At anamnesis, the previous application, in the day before, of a pour-on inseticide was noticed. The composition of the commercial product was ethion (15%), which is an insecticide organophosphate widely used as an antiparasitic drug. Affected animals were treated with intravenous atropine sulfate 1% (0.50 mg/kg) and sodium chloride 0.9%. Atropine sulfate is a potent parasympatholytic agent that inhibits the effects of acetylcholine at the postganglionic parasympathetic neuroeffector junctions. Ten minutes after the treatment, most calves showed an improvement in health status. Only one calf needed two extra doses at 1-hour intervals to recuperate. The presumptive diagnosis was based on the clinical findings and supported by depressed blood cholinesterase level. Discussion: The rapid therapeutic response of affected animals to specific treatment also supports the hypothesis. The outcome of this outbreak relies in the aggressive approach of the team and adequate treatment choice. In spite of other differential diagnosis possibilities such as poisoning by carbamate and pyrethroid, the clinical findings, laboratory result and therapeutic response allowed us to attribute this outbreak to the misuse of organophosphate. The key to an excellent outcome, when dealing with organophosphate poisoning, is immediate treatment.(AU)