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Braz. j. biol ; 83: e248842, 2023. tab, graf
Article in English | MEDLINE, LILACS, VETINDEX | ID: biblio-1339343


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.

Animals , Pesticides/toxicity , Pakistan , Acetylcholinesterase , Birds , Cholinesterase Inhibitors/toxicity , Ecosystem , Crops, Agricultural
Braz. j. biol ; 81(3): 632-641, July-Sept. 2021. tab
Article in English | LILACS | ID: biblio-1153394


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.

Humans , Pesticides , Occupational Exposure/analysis , Acetylcholinesterase , Quality of Life , Prospective Studies , Farmers
J. venom. anim. toxins incl. trop. dis ; 27: e20210009, 2021. tab, graf, ilus, mapas
Article in English | LILACS, VETINDEX | ID: biblio-1279406


Spider venom is a rich cocktail of neuroactive compounds designed to prey capture and defense against predators that act on neuronal membrane proteins, in particular, acetylcholinesterases (AChE) that regulate synaptic transmission through acetylcholine (ACh) hydrolysis - an excitatory neurotransmitter - and beta-secretases (BACE) that primarily cleave amyloid precursor proteins (APP), which are, in turn, relevant in the structural integrity of neurons. The present study provides preliminary evidence on the therapeutic potential of Phlogiellus bundokalbo venom against neurodegenerative diseases. Methods Spider venom was extracted by electrostimulation and fractionated by reverse-phase high-performance liquid chromatography (RP-HPLC) and characterized by matrix-assisted laser desorption ionization-time flight mass spectrometry (MALDI-TOF-MS). Neuroactivity of the whole venom was observed by a neurobehavioral response from Terebrio molitor larvae in vivo and fractions were screened for their inhibitory activities against AChE and BACE in vitro. Results The whole venom from P. bundokalbo demonstrated neuroactivity by inducing excitatory movements from T. molitor for 15 min. Sixteen fractions collected produced diverse mass fragments from MALDI-TOF-MS ranging from 900-4500 Da. Eleven of sixteen fractions demonstrated AChE inhibitory activities with 14.34% (± 2.60e-4) to 62.05% (± 6.40e-5) compared with donepezil which has 86.34% (± 3.90e-5) inhibition (p > 0.05), while none of the fractions were observed to exhibit BACE inhibition. Furthermore, three potent fractions against AChE, F1, F3, and F16 displayed competitive and uncompetitive inhibitions compared to donepezil as the positive control. Conclusion The venom of P. bundokalbo contains compounds that demonstrate neuroactivity and anti-AChE activities in vitro, which could comprise possible therapeutic leads for the development of cholinergic compounds against neurological diseases.(AU)

Animals , Acetylcholinesterase , Spider Venoms/toxicity , Neurotransmitter Agents , Neurodegenerative Diseases , In Vitro Techniques
J. venom. anim. toxins incl. trop. dis ; 27: e20200047, 2021. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1287090


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)

Animals , Bungarus , Elapid Venoms/toxicity , Synthetic Biology , Palladium , Acetylcholinesterase
Chinese Journal of Biotechnology ; (12): 4047-4055, 2021.
Article in Chinese | WPRIM | ID: wpr-921485


The biocompatibility of nanomaterials has attracted much attention. Graphene oxide (GO) is a nanomaterial widely used in biomedicine, but its toxicity can not be ignored. In this study, the effect of GO on the blood system (the hemolysis rate, the fragility of erythrocyte, and acetylcholinesterase activity) was systematically investigated. The results showed that the hemolysis rate of erythrocytes was lower than 8% when the GO concentration was below 100 μg/mL (P5 μm (LGO) increased the activity of acetylcholinesterase by 42.67% (P<0.05). Then molecular dynamics simulation was used to study how GO interacted with acetylcholinesterase and increased its activity. The results showed that GO was attached to the cell membrane, thus may provide an electronegative environment that helps the hydrolysate to detach from the active sites more quickly so as to enhance the activity of acetylcholinesterase.

Acetylcholinesterase , Erythrocytes , Graphite , Nanostructures
Article in Chinese | WPRIM | ID: wpr-888142


The chemical constituents from the roots of Aconitum kongboense were studied. Twenty-five diterpenoid alkaloids were isolated from the 95% methanol extract of the roots of A. kongboense by silica gel, reverse-phase silica gel and basic alumina column chromatography. They included a new aconitine-type diterpenoid alkaloid, named as kongboensenine(1), and twenty-four known ones(2-25), i.e., acotarine F(2), acotarine G(3), 14-acetyltalatisamine(4), talatisamine(5), indaconitine(6), yunaconitine(7), chasmanine(8), 6-epi-foresticine(9), homochasmanine(10), 8-deacetyl-yunaconitine(11), chasmaconitine(12), ajaconine(13), franchetine(14), ezochasmanine(15), crassicautine(16), 14-O-deacylcrassicausine(17), genicunine A(18), falconeridine(19), sachaconitine(20), liljestrandisine(21), 8-methyl-14-acetyltalatisamine(22), kongboendine(23), 14-benzoylchasmanine(24) and pseudaconine(25). Their structures were elucidated by common spectroscopic methods including high-resolution electrospray ionization mass spectrometry(HR-ESI-MS) and nuclear magnetic resonance(NMR) techniques. Compounds 2-4, 10, 13, 15-19 and 21-22 were isolated from this plant for the first time. Experimental results showed that all compounds did not have a significant inhibitory activity against acetylcholinesterase(AChE).

Acetylcholinesterase , Aconitum/metabolism , Alkaloids , Diterpenes , Magnetic Resonance Spectroscopy , Molecular Structure , Plant Roots/metabolism
Braz. J. Pharm. Sci. (Online) ; 57: e19154, 2021. tab, graf
Article in English | LILACS | ID: biblio-1350235


Hippeastrum puniceum is a species that belongs to the Amaryllidaceae family. A particular characteristic of this family is the consistent and very specific presence of isoquinoline alkaloids, which have demonstrated a wide range of biological activities such as antioxidant, antiviral, antifungal, antiparasitic, and acetylcholinesterase inhibitory activity, among others. In the present work, fifteen alkaloids were identified from the bulbs of Hippeastrum puniceum (Lam.) Kuntz using a GC-MS approach. The alkaloids 9-O-demethyllycoramine, 9-demethyl-2α-hydroxyhomolycorine, lycorine and tazettine were isolated through chromatographic techniques. The typical Amaryllidaceae alkaloids lycorine and tazettine, along with the crude and ethyl acetate extract from bulbs of the species were evaluated for their inhibitory potential on α-amylase, α-glucosidase, tyrosinase and acetylcholinesterase activity. Although no significant inhibition activity was observed against α-amylase, α-glucosidase and tyrosinase from the tested samples, the crude and ethyl acetate extracts showed remarkable acetylcholinesterase inhibitory activity. The biological activity results that correlated to the alkaloid chemical profile by GC-MS are discussed herein. Therefore, this study contributed to the knowledge of the chemical and biological properties of Hippeastrum puniceum (Lam.) and can subsidize future studies of this species

Amaryllidaceae Alkaloids/analysis , Amaryllidaceae/classification , Acetylcholinesterase/adverse effects , Cholinesterase Inhibitors/pharmacology , Acetates/agonists , Antioxidants/pharmacology
Braz. J. Pharm. Sci. (Online) ; 57: e18310, 2021. tab, graf
Article in English | LILACS | ID: biblio-1350230


This study aimed to evaluate the anticholinesterase activities of extracts and fractions of Ocotea daphnifolia in vitro and characterize its constituents. The effects of hexane, ethyl acetate, and ethanolic extracts on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activity were determined with a spectrophotometry assay. All extracts inhibited cholinesterase activity, and the ethanolic extract (2 mg/mL) exhibited the highest inhibition of both enzymes (99.7% for BuChE and 82.4% for AChE). The ethanolic extract was fractionated by column chromatography resulting in 14 fractions that were also screened for their anticholinesterase effects. Fraction 9 (2 mg/mL) showed the highest activity, inhibiting AChE and BuChE by 71.8% and 90.2%, respectively. This fraction was analyzed by high-performance liquid chromatography high-resolution mass spectrometry which allowed the characterization of seven glycosylated flavonoids (containing kaempferol and quercetin nucleus) and one alkaloid (reticuline). In order to better understand the enzyme-inhibitor interaction of the reticuline toward cholinesterase, molecular modeling studies were performed. Reticuline targeted the catalytic activity site of the enzymes. Ocotea daphnifolia exhibits a dual cholinesterase inhibitory activity and displays the same pattern of intermolecular interactions as described in the literature. The alkaloid reticuline can be considered as an important bioactive constituent of this plant.

In Vitro Techniques/instrumentation , Cholinesterase Inhibitors/analysis , Lauraceae/classification , Ocotea/adverse effects , Molecular Docking Simulation/instrumentation , Plants, Medicinal/anatomy & histology , Acetylcholinesterase/adverse effects , Spectrophotometry/instrumentation , Flavonoids , Butyrylcholinesterase/adverse effects , Alkaloids
Article in English | AIM, AIM | ID: biblio-1342398


Afr. J. Biomed. Res. Vol. 24 (May, 2021); 257- 263 Research Article Protective Effect of Alkaloid-rich Extract of Brimstone Tree (Morinda lucida) on Neurotoxicity in the Fruit-fly (Drosophila melanogaster) Model Nwanna E.E. Functional Food, Nutraceutical and Phytomedicine unit Department of Biochemistry, Federal University of Technology Akure PMB 704, Nigeria ABSTRACT Brimstone plant is one of the medicinal plants found in Nigeria used in fore-lore medicine with little scientific information on its alkaloid constituents. This study was aimed at investigating the effect of alkaloid-rich compounds from the plant in manganese- induced (MgCl2) neurotoxicity in the fruit fly. In addition, alkaloid compounds will be characterized using gas chromatograph coupled with flame ionization detector (GC-FID). Alkaloid-rich extract was prepared by solvent extraction method, fruit flies were pre-treated with the extract (0.5 ­ 1.0mg/ml) in a fortified diet before induction with MgCl2. The survival rate and negative geotaxis were observed. Thereafter, the activity of acetylcholinesterase (AChE) enzyme, antioxidantive potentials in in -vivo reactive oxygen species (ROS) thiobarbituric acid reactive species (TBARS), total thiol content, nitric oxide (NO*), hydroxyl oxide (OH*) scavenging ability, ferric reducing antioxidant property (FRAP) and 2, 2'-azino-bis (3-ethylbenzthiazoline-6- sulphonic acid) (ABTs*) radical scavenging ability were carried out on the flies' homogenate. Results obtained revealed that the alkaloid-rich extract regulated the neuro-protective activity of AchE, reduced the reactive oxygen species level in the induced flies with an increased in antioxidantive potential, higher survival rate and increases in the life span of the flies with 50% reduction in the mortality rate. The GC-MS showed a total of (1.55/100mg) of different plant-derived alkaloids such as dicentrine, atropine, aporphine. These alkaloids-rich compounds were found to have anti-oxidative, anti-nociceptive, anti-inflammatory and anti- cholinergic activities. In conclusion, this study suggests that alkaloids from brimstone plant could be the reason for the observed biological activities for the prevention of neuronal related complications.

Humans , Sulfur , Neurotoxicity Syndromes , Acetylcholinesterase , Drosophila Proteins , Alkaloids
Acta amaz ; 50(4): 355-362, out. - dez. 2020.
Article in English | LILACS | ID: biblio-1146381


A deltametrina é um inseticida piretróide amplamente utilizado no controle de pragas na agricultura brasileira. O uso intensivo e desordenado desse pesticida na Amazônia pode carreá-lo aos ecossistemas aquáticos de várias maneiras, mas principalmente por escoamento e lixiviação. O presente estudo foi concebido para determinar a toxicidade aguda (LC50) de um pesticida à base de deltametrina (PBD) e caracterizar seus efeitos sobre dois biomarcadores bioquímicos, a glutationa-S-transferase (GST) e a acetilcolinesterase (AChE), em tecidos do peixe elétrico Microsternarchus cf. bilineatus. Os peixes foram expostos a concentrações de 1, 2, 3, 4 e 5 µg L-1 de PBD por até 96 horas. Para cada tratamento, foi analisada a atividade absoluta das enzimas GST (músculo e fígado) e AChE (músculo e tecido nervoso). A CL50-96 h para Microsternarchus cf. bilineatus foi de 2,15 µg L-1, a menor concentração registrada para um peixe amazônico até o momento. Nenhuma das concentrações testadas deste inseticida afetou a atividade da AChE para o período de exposição testado. Um aumento significativo da atividade de GST no músculo foi detectado somente para as concentrações de 2 e 3 µg L-1. (AU)

Acetylcholinesterase , Biomarkers , Glutathione S-Transferase pi , Insecticides
Electron. j. biotechnol ; 48: 53-61, nov. 2020. ilus, graf
Article in English | LILACS | ID: biblio-1254710


BACKGROUND: Alzheimer's disease (AD) is a chronic, progressive neurodegenerative disease. Recent studies have reported the close association between cognitive function in AD and purinergic receptors in the central nervous system. In the current study, we investigated the effect of CD73 inhibitor α, ß-methylene ADP (APCP) on cognitive impairment of AD in mice, and to explore the potential underlying mechanisms. RESULTS: We found that acute administration of Aß1­42 (i.c.v.) resulted in a significant increase in adenosine release by using microdialysis study. Chronic administration of APCP (10, 30 mg/kg) for 20 d obviously mitigated the spatial working memory impairment of Aß1­42-treated mice in both Morris water maze (MWM) test and Y-maze test. In addition, the extracellular adenosine production in the hippocampus was inhibited by APCP in Aß-treated mice. Further analyses indicated expression of acetyltransferase (ChAT) in hippocampus of mice of was significantly reduced, while acetylcholinesterase (AChE) expression increased, which compared to model group. We observed that APCP did not significantly alter the NLRP3 inflammasome activity in hippocampus, indicating that anti-central inflammation seems not to be involved in APCP effect. CONCLUSIONS: In conclusion, we report for the first time that inhibition of CD73 by APCP was able to protect against memory loss induced by Aß1­42 in mice, which may be due to the decrease of CD73-driven adenosine production in hippocampus. Enhancement of central cholinergic function of the central nervous system may also be involved in the effects of APCP.

Animals , Male , Mice , Adenosine Diphosphate/analogs & derivatives , Neurodegenerative Diseases/prevention & control , Hippocampus , Nucleotidases/antagonists & inhibitors , Acetylcholinesterase , Adenosine Diphosphate/administration & dosage , Alzheimer Disease/prevention & control , Morris Water Maze Test , Mice, Inbred C57BL
Biosci. j. (Online) ; 36(2): 578-590, 01-03-2020. ilus, tab, graf
Article in English | LILACS | ID: biblio-1146424


Population growth has raised food production, and new sources are needed to increase quantity and quality of agricultural products. Carbamates and organophosphates are insecticide classes used worldwide as acetylcholinesterase (AChE) inhibitors. Plants have a natural resistance to insects, which can be employed in pest control as a new alternative to reduce the use of chemicals. An alternative may be the use of α-amylase inhibitors, which are digestive enzymes that impair pest species growth and development. Another would be acetylcholinesterase inhibitors since they damage the normal functioning of the central and peripheral nervous system, by releasing high concentrations of acetylcholine in cholinergic synapses. This substance accumulation increases stimulations that lead to behavioral changes, asphyxia, hyperactivity, and death. Botanical agrochemicals are believed to have advantages over synthetic ones, as they are rapidly degraded in the environment. In this scenario, plants have played an important role in pest control as sources of interest for the synthesis of new molecules for agricultural use. The present study evaluated acetylcholinesterase and α-amylase inhibition by microplate method, from leaf extracts of Mouriri elliptica Martius with different polarities.

O crescimento populacional tem aumentado a quantidade de produção alimentícia, sendo necessárias novas fontes para o aumento da quantidade e qualidade dos produtos agrícolas. Os carbamatos e organofosforados são classes de inseticidas utilizadas em todo o mundo, são inibidores da acetilcolinesterase (AChE). Os vegetais possuem uma resistência natural aos insetos, e esse método de resistência pode ser utilizado no controle das pragas como uma nova alternativa para redução do uso de inseticidas químicos, tais como os inibidores da α-amilase, enzima digestiva, a qual sua inibição prejudica o crescimento e desenvolvimento de espécies de pragas. E os inibidores da acetilcolinesterase que danificam o funcionamento normal do Sistema Nervoso Central e Periférico, através de elevadas concentrações da acetilcolina que ficam depositadas nas sinapses colinérgicas. Este acúmulo de ACh provoca uma grande estimulação que leva á alterações comportamentais, asfixia, hiperatividade e a morte. Estudos já realizados mostraram que os agrotóxicos botânicos têm vantagens sobre os sintéticos, sendo degradados rapidamente no meio ambiente. Neste cenário os vegetais têm desempenhado um importante papel no controle de pragas, através da síntese de novas moléculas para uso na agricultura. O presente trabalho avaliou a inibição das enzimas acetilcolinesterase e α-amilase através do método da microplaca a partir dos extratos das folhas de Mouriri elliptica Martius em diferentes polaridades.

Acetylcholinesterase , Pest Control , Cholinesterase Inhibitors , alpha-Amylases , Pesticides , Food Production , Chromatography , Agrochemicals , Crops, Agricultural , Grassland
Arq. bras. med. vet. zootec. (Online) ; 72(1): 169-176, Jan.-Feb. 2020. graf
Article in Portuguese | LILACS, VETINDEX | ID: biblio-1088908


O fipronil é um inseticida de toxicidade seletiva amplamente empregado na agricultura e na medicina veterinária. Porém, há relatos de efeitos neurotóxicos dessa substância, que geram prejuízos para vertebrados. Avaliou-se a atividade locomotora, a coordenação motora e a atividade da enzima acetilcolinesterase cerebral em ratos expostos ao fipronil. Ratos Wistar machos adultos (n=15) receberam fipronil em dose de 30mg/kg, por via oral, durante 15 dias; o grupo controle (n=15) foi tratado com solução fisiológica, por via oral, no mesmo período. No 16° dia de experimentação, os animais foram submetidos aos testes de arena de campo aberto e hole board. No 17° dia, foram anestesiados e eutanasiados, procedendo-se à coleta de órgãos, e posteriormente foi feita a avaliação da AChE cerebral. A exposição ao fipronil não provocou alterações significativas sobre a coordenação motora e a atividade locomotora, porém gerou inibição significativa da atividade da acetilcolinesterase cerebral. Esses achados sugerem que o fipronil pode provocar efeitos neurotóxicos em curto prazo, os quais podem ser exacerbados caso a exposição seja prolongada.(AU)

Fipronil is a selective-toxicity insecticide widely used in agriculture and veterinary medicine. However, there are reports of neurotoxic effects of this substance, causing damages to vertebrates. We evaluated the locomotor activity, motor coordination and the activity of brain acetylcholinesterase in rats exposed to fipronil. Adult male Wistar rats (n= 15) received fipronil at a dose of 30mg/kg orally for 15 days; the Control group (n= 15) was treated with oral solution in the same period. On the 16th day of experimentation, the animals were submitted to the open field arena test and hole-board test. On the 17th day, they were anesthetized and euthanized, and organs were collected, and subsequently brain AChE was evaluated. Exposure to fipronil yielded no significant changes on motor coordination and locomotor activity but caused significant inhibition of brain acetylcholinesterase activity. These findings suggest that fipronil may cause short-term neurotoxic effects, which may be exacerbated if exposure is prolonged.(AU)

Animals , Rats , Pesticides/toxicity , Acetylcholinesterase/analysis , Pesticide Exposure , Neurotoxicity Syndromes/veterinary , Mental Status and Dementia Tests , Rats, Wistar
Rev. Pesqui. (Univ. Fed. Estado Rio J., Online) ; 11(5): 1319-1325, out.-dez. 2019. tab, ilus, graf
Article in English, Portuguese | LILACS, BDENF | ID: biblio-1022203


Objective: The study's goal has been to analyze if environmental or occupational exposure to pesticides can produce changes in pregnant women living in a countryside municipality. Methods: The participants of this study were twenty-three pregnant women, who both answered a questionnaire and donated biological material in order to perform Micronucleus (MN) Tests in lymphocytes, oral epithelial cells, and also for measuring the enzyme activity of erythrocyte acetylcholinesterase. Results: Considering the total analyzed samples, the following was found: an average of 8 ± 2.92 MN/1000 oral epithelial cells from urban participants; an average of 6.82 ± 3.43 MN/1000 oral epithelial cells from rural participants; and 100% of the microscope slides contained cells with two MN, which shows high intensity lesions to the DNA. There was found a high frequency of spontaneous abortions (34.8%), greater than in Brazil. Conclusion: The exposure of pregnant women living in a countryside municipality to pesticides may increase the rate of spontaneous abortions, as well as the chances of mutagenic effects

Objetivo: Analisar se a exposição ambiental ou ocupacional aos agrotóxicos causa alterações em gestantes residentes em um município rural. Métodos: Compuseram a amostra 23 gestantes, que responderam a um questionário e doaram amostras biológicas para a realização dos testes de micronúcleos (MN) em linfócitos, em células do epitélio oral, e para a dosagem da atividade da enzima acetilcolinesterase eritrocitária. Resultados: Obteve-se uma média de 8 ± 2,92 MN/1000 células do epitélio oral analisadas em amostras de participantes da zona urbana, 6,82 ± 3,43 MN/1000 de participantes da zona rural, e 100% das lâminas continham células com dois MN, o que demonstra lesões ao DNA de maior intensidade. Encontrou-se uma frequência elevada de casos de abortos espontâneos (34,8%), superior à encontrada no Brasil. Conclusão: A exposição de gestantes residentes em um município rural aos agrotóxicos eleva a taxa de abortos espontâneos, bem como as chances de ocorrência de efeitos mutagênicos

Objetivo: Analizar si la exposición ambiental o ocupacional a los agrotóxicos causa cambios en gestantes residentes en un municipio rural. Métodos: Compusieron la muestra 23 gestantes, que respondieron a un cuestionario y donaron muestras biológicas para la realización de las pruebas de micronúcleos (MN) en linfocitos, en células del epitelio oral, y para la dosificación de la actividad de la enzima acetilcolinesterasa eritrocitaria. Resultados: Se obtuvieron una media de 8 ± 2,92 MN / 1000 células del epitelio oral analizadas en muestras de participantes de la zona urbana, 6,82 ± 3,43 MN / 1000 de participantes de la zona rural, y el 100% de las láminas contenían células con dos MN, lo que demuestra lesiones al ADN de mayor intensidad. Se encontró una frecuencia elevada de casos de abortos espontáneos (34,8%), superior a la encontrada en Brasil. Conclusión: La exposición de gestantes residentes en un municipio rural a los agrotóxicos eleva la tasa de abortos espontáneos, así como las posibilidades de ocurrencia de efectos mutagênicos

Humans , Female , Pregnancy , Adolescent , Adult , Agrochemicals/toxicity , Abortion , Mutagenicity Tests/methods , Acetylcholinesterase/pharmacology , Rural Health/statistics & numerical data , Occupational Exposure/adverse effects
Bol. latinoam. Caribe plantas med. aromát ; 18(5): 527-532, sept. 2019. ilus, tab
Article in English | LILACS | ID: biblio-1008292


Chemical constituents and biological activities of the aerial parts of Piper erecticaule C.DC. have been studied for the first time. Fractionation and purification of the extracts afforded aristolactam AII (1), aristolactam BII (2), piperolactam A (3), piperolactam C (4), piperolactam D (5), together with terpenoids of ß-sitosterol, ß-sitostenone, taraxerol, and lupeol. The structures of these compounds were obtained by analysis of their spectroscopic data, as well as the comparison with that of reported data. Acetylcholinesterase inhibitory activity revealed that compounds 1 and 3 showed strong AChE inhibitory effects with the percentage inhibition of 75.8% and 74.8%, respectively.

Se estudiaron por primera vez los constituyentes químicos y actividad biológica de las partes aéreas de Piper erecticaule C.DC. El fraccionamiento y la purificación de los extractos proporcionaron aristolactama AII (1), aristolactama BII (2), piperolactama A (3), piperolactama C (4), piperolactama D (5), junto con terpenoides de ß-sitosterol, ß-sitostenona, taraxerol, y el lupeol. Las estructuras de estos compuestos se obtuvieron mediante el análisis de sus datos espectroscópicos, así como mediante la comparación con datos ya informados. La actividad inhibidora de la acetilcolinesterasa reveló que los compuestos 1 y 3 mostraron un potente efecto inhibidor de la AChE con un porcentaje de inhibición del 75.8% y 74.8%, respectivamente.

Aporphines/pharmacology , Acetylcholinesterase/drug effects , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology , Piper/chemistry , Alkaloids/pharmacology , Aporphines/chemistry , Terpenes/isolation & purification , Cholinesterase Inhibitors/chemistry , Indole Alkaloids/chemistry , Alkaloids/chemistry , Lactams/chemistry
Med. leg. Costa Rica ; 36(1): 110-117, ene.-mar. 2019.
Article in Spanish | LILACS | ID: biblio-1002564


Resumen La intoxicación por organofosforados es de gran importancia en el campo de la medicina, debido a su uso frecuente en la actividad agrícola, las intoxicaciones producidas por estos agentes pueden ser ocupacionales, accidentales, y con mayor frecuencia por ingesta voluntaria. Una de las mayores repercusiones de los organofosforados es la inhibición del acetil colinesterasa, enzima encargada de hidrolizar el acetil colina. Las manifestaciones clínicas de la intoxicación aguda se deben a la estimulación de receptores muscarínicos y nicotínicos, entre ellas broncorrea, salivación, lagrimeo, broncoespasmo, defecación, emesis, miosis, entre otros. El diagnóstico se realiza mediante la historia clínica y examen físico, de manera adicional con la detección de los niveles en sangre eritrocitaria de acetil colinesterasa o de los metabolitos de los organofosforados. El manejo incluye la descontaminación del agente, la revisión del estado respiratorio y el acceso al soporte ventilatorio, posteriormente se procede con el tratamiento farmacológico que incluye el uso de la atropina, pralidoxima y diazepam. El presente artículo constituye una revisión bibliográfica sobre la intoxicación por organofosforados, sus manifestaciones clínicas, diagnóstico y tratamiento.

Abstract Organophosphorus poisoning is of great importance in the field of medicine due to its frequent use in agriculture, the poisoning by exposure to these agents can be occupational, accidental, and frequently due to voluntary intake. Organophosphorus' intake most notable effects are produced by the inhibition of the acetyl cholinesterase, responsible for hydrolyzing acetyl choline. Clinical manifestations of acute intoxication typically include bronchorrhea, salivation, lacrimation, bronchospasm, defecation, emesis, miosis, among others and they occur due to the stimulation of muscarinic and nicotinic receptors. Diagnosis is made through the interrogation and physical examination, in addition to the detection of acetyl cholinesterase levels or the organophosphates' metabolites in blood testing. Management includes decontamination of the agent, review of respiratory status and access to ventilatory support, followed by pharmacological treatment that includes the use of atropine, pralidoxime and diazepam. The present article constitutes a bibliographic review about the organopho sphorus intoxication, its clinical manifestations, diagnosis and treatment.

Humans , Organophosphorus Compounds , Pesticides , Acetylcholinesterase , Agricultural Zones , Organophosphate Poisoning/diagnosis
Natural Product Sciences ; : 115-121, 2019.
Article in English | WPRIM | ID: wpr-760555


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

Acetylcholinesterase , Alzheimer Disease , Butyrylcholinesterase , Cholinesterases , Hydrogen , In Vitro Techniques , Neurodegenerative Diseases
Article in English | WPRIM | ID: wpr-758898


Acetylcholinesterase (AChE) activity level can be used as a diagnostic marker for anticholinesterase pesticide poisoning. In this study, we aimed to establish a baseline level of normal brain AChE activity in wild birds. AChE activity was measured in the brains of 87dead wild birds (26 species). The level of AChE activity ranged from 6.40 to 15.9 µmol/min/g of brain tissue in normal wild birds. However, the brain tissue AChE activity level in wild birds exposed to organophosphate (OP) pesticide was 48.0%–96.3% of that in the normal birds. These results may serve as reference values to facilitate routine diagnosis and monitoring of OP-poisoned wild birds.

Acetylcholinesterase , Birds , Brain , Diagnosis , Organophosphates , Poisoning , Reference Values
Article in Chinese | WPRIM | ID: wpr-773731


A total of 27 endophytic fungal strains were isolated from Huperzia serrata,which were richly distributed in the stems and leaves while less distributed in roots. The 27 strains were identified by Internal Transcribed Spacer( ITS) r DNA molecular method and one of the strains belongs to Basidiomycota phylum,and other 26 stains belong to 26 species,9 general,6 families,5 orders,3 classes of Ascomycota Phylum. The dominant strains were Colletotrichum genus,belonging to Glomerellaceae family,Glomerellales order,Sordariomycetes class,Ascomycota Phylum,with the percentage of 48. 15%. The inhibitory activities of the crude extracts of 27 endophytic fungal strains against acetylcholinesterase( ACh E) and nitric oxide( NO) production were evaluated by Ellman's method and Griess method,respectively. Crude extracts of four fungi exhibited inhibitory activities against ACh E with an IC50 value of 42. 5-62. 4 mg·L~(-1),and some fungi's crude extracts were found to inhibit nitric oxide( NO) production in lipopolysaccharide( LPS)-activated RAW264. 7 macrophage cells with an IC50 value of 2. 2-51. 3 mg·L~(-1),which indicated that these fungi had potential anti-inflammatory activities.The chemical composition of the Et OAc extract of endophytic fungus HS21 was also analyzed by LCMS-IT-TOF. Seventeen compounds including six polyketides,four diphenyl ether derivatives and seven meroterpenoids were putatively identified.

Acetylcholinesterase , Animals , Anti-Inflammatory Agents , Pharmacology , Ascomycota , Chemistry , Classification , Cholinesterase Inhibitors , Metabolism , Endophytes , Classification , Huperzia , Microbiology , Mice
Braz. j. biol ; 78(2): 217-223, May-Aug. 2018. graf
Article in English | LILACS | ID: biblio-888868


Abstract Sciatic nerve transection (SNT), a model for studying neuropathic pain, mimics the clinical symptoms of "phantom limb", a pain condition that arises in humans after amputation or transverse spinal lesions. In some vertebrate tissues, this condition decreases acetylcholinesterase (AChE) activity, the enzyme responsible for fast hydrolysis of released acetylcholine in cholinergic synapses. In spinal cord of frog Rana pipiens, this enzyme's activity was not significantly changed in the first days following ventral root transection, another model for studying neuropathic pain. An answerable question is whether SNT decreases AChE activity in spinal cord of frog Lithobates catesbeianus, a species that has been used as a model for studying SNT-induced neuropathic pain. Since each animal model has been created with a specific methodology, and the findings tend to vary widely with slight changes in the method used to induce pain, our study assessed AChE activity 3 and 10 days after complete SNT in lumbosacral spinal cord of adult male bullfrog Lithobates catesbeianus. Because there are time scale differences of motor endplate maturation in rat skeletal muscles, our study also measured the AChE activity in bullfrog tibial posticus (a postural muscle) and gastrocnemius (a typical skeletal muscle that is frequently used to study the motor system) muscles. AChE activity did not show significant changes 3 and 10 days following SNT in spinal cord. Also, no significant change occurred in AChE activity in tibial posticus and gastrocnemius muscles at day 3. However, a significant decrease was found at day 10, with reductions of 18% and 20% in tibial posticus and gastrocnemius, respectively. At present we cannot explain this change in AChE activity. While temporally different, the direction of the change was similar to that described for rats. This similarity indicates that bullfrog is a valid model for investigating AChE activity following SNT.

Resumo A transecção do nervo isquiático (SNT), um modelo para estudar dor neuropática, simula os sintomas clínicos do "membro fantasma", uma condição dolorosa que ocorre nos humanos após amputação ou secção completa da medula espinal. Essa condição muda a atividade da acetilcolinesterase (AChE), a enzima responsável pela rápida hidrólise da acetilcolina liberada nas sinapses colinérgicas, em alguns tecidos de vertebrados. Em medula espinal de rã Rana pipiens, a atividade da AChE não foi significativamente alterada nos primeiros dias após a secção da raiz ventral, outro modelo para o estudo da dor neuropática. Uma questão ainda não respondida é se a SNT diminui a atividade da AChE na medula espinal de rã Lithobates catesbeianus, uma espécie que vem sendo usada como modelo em estudos da dor neuropática induzida por SNT. Como cada modelo animal é criado a partir de metodologia específica, e seus resultados tendem a variar com pequenas mudanças na metodologia de indução da dor, o presente estudo avaliou a atividade da AChE em medula espinal lombossacral de rã-touro Lithobates catesbeianus, adultos, machos, 3 e 10 dias após a completa SNT. Como há diferenças temporais na maturação de placas motoras em músculos esqueléticos de ratos, nosso estudo ainda demonstrou, na rã-touro, os efeitos da SNT sobre a atividade da AChE nos músculos esqueléticos tibial posticus, um músculo postural, e gastrocnêmio, um músculo frequentemente usado em estudos do sistema motor. A atividade da AChE não mudou significativamente na medula espinal aos 3 e 10 dias após a SNT. Nos músculos, a atividade não alterou significativamente aos 3 dias após a lesão, mas reduziu de forma significativa aos 10 dias após a SNT. Aos 10 dias, a diminuição foi 18% no músculo tibial posticus e 20% no gastrocnêmio. No momento, nós não temos explicação para essa mudança na atividade da AChE. Embora temporalmente diferente, o sentido da mudança é similar ao que é descrito em ratos. Esta similaridade torna a rã-touro um modelo válido para se estudar questões ainda não respondidas da SNT sobre a AChE.

Animals , Acetylcholinesterase/metabolism , Sciatic Nerve/enzymology , Sciatic Nerve/physiopathology , Sciatic Nerve/injuries , Spinal Cord/physiology , Muscle, Skeletal/innervation , Rana catesbeiana