Efeitos dos agrotóxicos na saúde do agricultor familiar dos municípios de Capitólio e Pimenta - Minas Gerais: avaliação de biomarcadores colinesterase eritrocitárias e plasmática / Effects of pesticides on the health of family farmers in the cities of Capitólio and Pimenta - Minas Gerais: evaluation of erythrocyte and plasma cholinesterase biomarkers

O Brasil é o maior consumidor global de agrotóxico tendo como consequência intoxicações de um grande número de trabalhadores, com altos gastos com a saúde e prejuízos ambientais. Objetivo geral: avaliar os efeitos do uso de agrotóxicos sobre a saúde de trabalhadores atuantes na agricultura familiar. Método: estudo transversal, analítico e comparativo entre o Grupo (1) composto por 80 trabalhadores rurais atuantes na agricultura familiar, expostos diretamente a agrotóxicos e o Grupo (2) composto por 60 usuários dos Programas de Saúde da Família (PSF) dos municípios de Capitólio e Pimenta - Minas Gerais - não diretamente expostos a agrotóxicos sendo o grupo controle por meio da análise de biomarcadores colinesterase eritrocitária e plasmática. Resultados: dos 140 participantes deste estudo, a maioria (51,2%) não referiu problemas de saúde e tratamento medicamentoso, 6,3% deles, expostos a agrotóxicos, referiram intoxicações e 42,5% relataram terem algum sinal e/ou sintoma de intoxicação com predominância (33,8%) para a dor de cabeça. O biomarcador colinesterase eritrocitária apresentou normalidade em 63,8% dos trabalhadores rurais e 36,2% com alteração na butirilcolinesterase. Conclusão: a butirilcolinesterase encontrada em 1/3 dos participantes expostos a agrotóxicos correlacionam-se à presença dos sintomas dor de cabeça e irritabilidade/nervosismo. Existe, portanto, a necessidade da educação e capacitação dos agricultores no uso de agrotóxicos para limitar níveis de exposição e efeitos nocivos à saúde para prevenir, diagnosticar e tratar possíveis disfunções causadas por esses produtos químicos

Brazil is the largest global consumer of pesticides, resulting in the intoxication of a large number of workers, with high expenditures on health and environmental damage. General objective: to evaluate the effects of the use of pesticides on the health of rural workers working in family farming in terms of intoxication through the evaluation of the erythrocyte and plasma cholinesterase biomarkers. Method: cross-sectional, analytical and comparative study between Group (1) of rural workers working in family farming, directly exposed to pesticides and Group (2) of users of Family Health Programs (PSF), in the municipalities of Capitólio and Pimenta - Minas Gerais State (Brazil) - not directly exposed to pesticides, being a control group through the analysis of biomarkers. Results: in this study of 140 participants, the most of them did not report health problems and drug treatment, 6.3% of participants, exposed to pesticides, reported poisoning and 42.5% reported having any signs and/or symptoms of intoxication with predominance for headache. The erythrocyte cholinesterase biomarker showed normality in 63.8% rural workers and 36.2% with alteration in butyrylcholinesterase. Conclusion: butyrylcholinesterase alteration was proven in 36.2% of participants exposed to pesticides and these results correlate with the presence of headache and irritability/nervousness symptoms. There is, therefore, a need for education and training of farmers to limit levels of exposure and harmful health effects to prevent, diagnose and treat possible dysfunctions caused by these chemicals applied to agriculture

Efeitos dos agrotóxicos na saúde do agricultor familiar dos municípios de Capitólio e Pimenta - Minas Gerais: avaliação de biomarcadores colinesterase eritrocitárias e plasmática / Effects of pesticides on the health of family farmers in the cities of Capitólio and Pimenta - Minas Gerais: evaluation of erythrocyte and plasma cholinesterase biomarkers

portuguêsO Brasil é o maior consumidor global de agrotóxico tendo como consequência intoxicações de um grande número de trabalhadores, com altos gastos com a saúde e prejuízos ambientais. Objetivo geral: avaliar os efeitos do uso de agrotóxicos sobre a saúde de trabalhadores atuantes na agricultura familiar. Método: estudo transversal, analítico e comparativo entre o Grupo (1) composto por 80 trabalhadores rurais atuantes na agricultura familiar, expostos diretamente a agrotóxicos e o Grupo (2) composto por 60 usuários dos Programas de Saúde da Família (PSF) dos municípios de Capitólio e Pimenta - Minas Gerais - não diretamente expostos a agrotóxicos sendo o grupo controle por meio da análise de biomarcadores colinesterase eritrocitária e plasmática. Resultados: dos 140 participantes deste estudo, a maioria (51,2%) não referiu problemas de saúde e tratamento medicamentoso, 6,3% deles, expostos a agrotóxicos, referiram intoxicações e 42,5% relataram terem algum sinal e/ou sintoma de intoxicação com predominância (33,8%) para a dor de cabeça. O biomarcador colinesterase eritrocitária apresentou normalidade em 63,8% dos trabalhadores rurais e 36,2% com alteração na butirilcolinesterase. Conclusão: a butirilcolinesterase encontrada em 1/3 dos participantes expostos a agrotóxicos correlacionam-se à presença dos sintomas dor de cabeça e irritabilidade/nervosismo. Existe, portanto, a necessidade da educação e capacitação dos agricultores no uso de agrotóxicos para limitar níveis de exposição e efeitos nocivos à saúde para prevenir, diagnosticar e tratar possíveis disfunções causadas por esses produtos químicos

Brazil is the largest global consumer of pesticides, resulting in the intoxication of a large number of workers, with high expenditures on health and environmental damage. General objective: to evaluate the effects of the use of pesticides on the health of rural workers working in family farming in terms of intoxication through the evaluation of the erythrocyte and plasma cholinesterase biomarkers. Method: cross-sectional, analytical and comparative study between Group (1) of rural workers working in family farming, directly exposed to pesticides and Group (2) of users of Family Health Programs (PSF), in the municipalities of Capitólio and Pimenta - Minas Gerais State (Brazil) - not directly exposed to pesticides, being a control group through the analysis of biomarkers. Results: in this study of 140 participants, the most of them did not report health problems and drug treatment, 6.3% of participants, exposed to pesticides, reported poisoning and 42.5% reported having any signs and/or symptoms of intoxication with predominance for headache. The erythrocyte cholinesterase biomarker showed normality in 63.8% rural workers and 36.2% with alteration in butyrylcholinesterase. Conclusion: butyrylcholinesterase alteration was proven in 36.2% of participants exposed to pesticides and these results correlate with the presence of headache and irritability/nervousness symptoms. There is, therefore, a need for education and training of farmers to limit levels of exposure and harmful health effects to prevent, diagnose and treat possible dysfunctions caused by these chemicals applied to agriculture

Correlation study between Erythrocyte Acetylcholinesterase activity, Serum Malondialdehyde and Insulin sensitivity in Agricultural workers and non-agricultural workers in Nat-Kan Village, Magway Township / Journal of the ASEAN Federation of Endocrine Societies

Objective@#This study determined the correlation between erythrocyte acetylcholinesterase (AChE) activity, serum malondialdehyde (MDA) and insulin sensitivity in agricultural workers and non-agricultural workers.@*Methodology@#The cross-sectional comparative study was undertaken in 45 agricultural and 45 non-agricultural workers from Nat-Kan Village, Magway Township. Erythrocyte acetylcholinesterase activity and serum malondialdehyde were measured by spectrophotometric method. Insulin sensitivity was calculated by homeostasis model assessment (HOMA-IR).@*Results@#Mean erythrocyte AChE activity was significantly lower in agricultural (3553.99 IU/L) compared with non-agricultural workers (4432.68 IU/L) (p<0.001). A significant high level of mean serum MDA was observed in agricultural workers (0.74 versus 0.28 μmol/L, p<0.001). Median HOMA-IR value was significantly higher in agricultural (2.74) than that of non-agricultural workers (2.28) (p<0.05). The risk of insulin resistance was 2.8 times greater in agricultural workers than non-agricultural workers (OR 2.8, 95% CI, 1.18 to 6.72). Erythrocyte AChE activity had weak negative correlation with serum MDA level (r=-0.357, p<0.001) and HOMA-IR (ρ= -0.305, p<0.05). There was a significant but weak positive correlation between serum MDA level and HOMA-IR (ρ=0.355, p<0.001).@*Conclusion@#Organophosphate pesticide exposure lowered erythrocyte AChE activity and increased oxidative stress. Oxidative stress is partly attributed to the development of insulin resistance

Histopathological and cholinesterase changes in the gills of Clarias gariepinus as a result of cadmium exposure

Aim: The cholinesterase (ChE) based inhibition and histopathological studies from fish were investigated and represented in this study to develop as one of the great potential biomarkers for heavy metals monitoring. Methodology: In this study, the histopathological study of gills were observed a under microscope. The capability of ChE extracted from the gills of Clarias gariepinus was assessed for declining Cd. ChE was purified through affinity chromatography and continued with the optimisation and inhibition study (IC50) of cholinesterase. Results: Histopathological study of gills was carried out and several changes such as aneurysm, necrosis and lamella fusion were noted. Purification fold obtained from purified enzyme was 1.15 with 30% a yield specific activity 20.726. The optimum temperature for purified AChE was 35°C along with acetylthiocholine iodide (ATC) as a preferable substrate that had the highest Vmax value of 0.5452 U mg-1 and the lowest Km value of 0.0311 mM. The optimum pH was observed to be 10 of Tris-HCl as a medium. Meanwhile, the IC50 of cadmium was 6.808 mg l-1 with R2 value of 0.9532. Interpretation: The result of the study can be used as a tool for further developing a biomarker for the detection of heavy metals in aquatic ecosystems. In addition, the baseline data provided can also be used for designing a kit, which would give rapid and accurate result.

Status and preliminary mechanism of resistance to insecticides in a field strain of housefly (Musca domestica, L)

ABSTRACT Resistance profiles of houseflies (Gol-RR) collected from a field in Golmud city, Qinghai province, China, were determined for seven insecticides using topical bioassays. Resistance ratios of >1219.51, 153.17, >35.43, 6.12, 3.24, 1.73, and 0.86-fold were obtained for propoxur, cypermethrin, imidacloprid, indoxacarb, chlorpyrifos, fipronil, and chlorfenapyr, respectively, relative to a laboratory susceptible strain (SS). Synergism experiments showed that piperonyl butoxide (PBO), triphenylphosphate (TPP), and diethyl maleate (DEM) increased propoxur toxicity by >105.71, >7.88, and >5.15-fold in the Gol-RR strain, compared with 5.25, 2.00, and 1.39-fold in the SS strain, indicating the involvement of P450 monooxygenases, esterases, and glutathione-S-transferase in conferring resistance. Although cypermethrin resistance was significantly suppressed with PBO, TPP, and DEM in the Gol-RR strain, the synergistic potential of these agents to cypermethrin was similar in the SS strain, demonstrating that metabolism-mediated detoxification was not important for conferring resistance to cypermethrin in the Gol-RR strain. However, the three agents did not act synergistically with imidacloprid, indicating that other mechanisms may be responsible for the development of resistance to this insecticide. Acetylcholinesterase (AChE) activity was 13.70-fold higher in the Gol-RR than in the SS strain, suggesting the properties of the AChE enzyme were altered in the Gol-RR strain. Thus, rotation of chlorfenapyr insecticide with other agents acting through a different mode with minimal/no resistance could be an effective resistance management strategy for housefly.

Los niveles de acetilcolinesterasa en pacientes con inestabilidad hemodinámica descartan sepsis como causa de choque / The levels of acetylcholinesterase in patients with hemodynamic instability discard sepsis as a cause of shock / Níveis de acetilcolinesterase em pacientes com instabilidade hemodinâmica descartam sepse como causa de choque

Resumen: Introducción: La detección temprana de sepsis es fundamental para disminuir la mortalidad de este padecimiento. Hasta el momento, ninguna escala clínica ni biomarcador ha sido útil en su diagnóstico y detección precoz. Los niveles de actividad de la acetilcolinesterasa se han propuesto como un biomarcador muy prometedor para la detección de sepsis y choque séptico. Objetivo: Estudiar la utilidad de los niveles de acetilcolinesterasa en el diagnóstico de sepsis. Material y métodos: Estudio observacional y prospectivo, en pacientes de la Unidad de Cuidados Intensivos del Hospital San Ángel Inn Universidad con diagnóstico de inestabilidad hemodinámica, clasificados con presencia o no de sepsis, tomándose niveles de acetilcolinesterasa al ingreso. Resultados: Se evaluaron 44 pacientes, 27% con sepsis. Los valores de acetilcolinesterasa tuvieron validez diagnóstica para predecir sepsis (AUC: 0.852 IC 95%: 0.726-0.977, p < 0.001), con un punto de corte de 3,956 U/L, sensibilidad = 81%, especificidad = 75%. El valor de neutrófilos con corte < 74% también tuvo valor predictor de sepsis (AUC: 0,710 IC 95%: 0,512-0,907, p = 0.034) sensibilidad = 75%, especificidad = 75%. Conclusiones: En pacientes con inestabilidad hemodinámica con niveles de acetilcolinesterasa mayores de 4,000 U/L se descarta sepsis como causa de choque.

Abstract: Introduction: Early detection of sepsis is essential to reduce mortality from this condition. So far, no clinical scale or biomarker has been useful in its diagnosis and early detection. Levels of acetylcholinesterase activity have been proposed as a very promising biomarker for the detection of sepsis and septic shock. Objective: To study the usefulness of acetylcholinesterase levels in the diagnosis of sepsis. Material and methods: Observational and prospective study in patients of the Intensive Care Unit of the Hospital San Ángel Inn Universidad with diagnosis of hemodynamic instability, classified with or without sepsis, taking acetylcholinesterase levels at admission. Results: 44 patients were evaluated, 27% with sepsis. The acetylcholinesterase values ​​presented a normal distribution and had diagnostic validity to predict sepsis (AUC: 0.852 95% CI: 0.726-0.977, p < 0.001), with a cut-off value of < 3,956 U/L, sensitivity = 81%, specificity = 75%. The value of neutrophils with a cut < 74% also had a predictive value of sepsis (AUC: 0.710 95% CI: 0.512-0.907, p = 0.034) sensitivity = 75%, specificity = 75%. Conclusions: In patients with hemodynamic instability with acetylcholinesterase levels greater than 4,000 U/L, sepsis is ruled out as the cause of shock.

Resumo: Introdução: A detecção precoce da sepse é fundamental para reduzir a mortalidade desta doença. Até agora nenhuma escala clínica ou biomarcador tem sido útil em seu diagnóstico e detecção precoce. Os níveis de atividade da acetilcolinesterase têm sido propostos como um biomarcador muito promissor para a detecção de sepse e choque séptico. Objetivo: Estudar a utilidade dos níveis de acetilcolinesterase no diagnóstico da sepse. Material e métodos: Estudo observacional e prospectivo, realizado em pacientes da unidade de terapia intensiva do Hospital Universitário San Ángel Inn, com diagnóstico de instabilidade hemodinâmica, classificados com ou sem a presença de sepse, obtendo os níveis de acetilcolinesterase na admissão. Resultados: Foram avaliados 44 pacientes, 27% com sepse. Os valores de acetilcolinesterase apresentaram validade diagnóstica para predizer sepse (AUC: 0.852 IC 95%: 0.726-0.977, p < 0.001), com valor de corte 3956 U/L, sensibilidade = 81%, especificidade = 75%. O valor de neutrófilos com um corte < 74% também teve um valor preditivo de sepsis (AUC: 0.710 IC 95%: 0.512-0.907, p = 0.034) sensibilidade = 75%, especificidade = 75%. Conclusões: Em pacientes com instabilidade hemodinâmica com níveis de acetilcolinesterase superiores a 4,000 U/L a sepse é descartada como causa de choque.

Red blood cell acetylcholinesterase activity among healthy dwellers of an agrarian region in Sri Lanka: a descriptive cross-sectional study

BACKGROUND@#Assessment of acetylcholinesterase-inhibitor insecticide (AChEII) toxicity depends on the measurement of red blood cell acetylcholinesterase (RBC-AChE) activity. Its interpretation requires baseline values which is lacking in scientific literature. We aim to find the measures of central tendency and variation for RBC-AChE activity among dwellers of Anuradhapura, where the use and abuse of AChEIIs were rampant for the last few decades.@*METHODS@#A descriptive cross-sectional study with a community-based sampling for 100 healthy non-farmers (male:female = 1:1) was done using pre-determined selection criteria. Duplicate measurements of RBC-AChE activity were performed according to the modified Ellman procedure. Pearson's correlation and regression analysis were sort for RBC-AChE activity against its possible determinants.@*RESULTS@#RBC-AChE activity had a mean of 449.8 (SD 74.2) mU/μM Hb with a statistical power of 0.847. It was similar to values of "healthy controls" from previous Sri Lankan toxicological studies but was low against international reference value [586.1 (SD 65.1) mU/μM Hb]. None of the possible determinants showed a significant strength of relationship with RBC-AChE activity.@*CONCLUSION@#The baseline RBC-AChE activity among people of Anuradhapura is low in comparison with international reference values. This arises a need to find a causative mechanism.

The Effects of Donepezil, an Acetylcholinesterase Inhibitor, on Impaired Learning and Memory in Rodents

A previous study in humans demonstrated the sustained inhibitory effects of donepezil on acetylcholinesterase (AChE) activity; however, the effective concentration of donepezil in humans and animals is unclear. This study aimed to characterize the effective concentration of donepezil on AChE inhibition and impaired learning and memory in rodents. A pharmacokinetic study of donepezil showed a mean peak plasma concentration of donepezil after oral treatment (3 and 10 mg/kg) of approximately 1.2 ± 0.4 h and 1.4 ± 0.5 h, respectively; absolute bioavailability was calculated as 3.6%. Further, AChE activity was inhibited by increasing plasma concentrations of donepezil, and a maximum inhibition of 31.5 ± 5.7% was observed after donepezil treatment in hairless rats. Plasma AChE activity was negatively correlated with plasma donepezil concentration. The pharmacological effects of donepezil are dependent upon its concentration and AChE activity; therefore, we assessed the effects of donepezil on learning and memory using a Y-maze in mice. Donepezil treatment (3 mg/kg) significantly prevented the progression of scopolamine-induced memory impairment in mice. As the concentration of donepezil in the brain increased, the recovery of spontaneous alternations also improved; maximal improvement was observed at 46.5 ± 3.5 ng/g in the brain. In conclusion, our findings suggest that the AChE inhibitory activity and pharmacological effects of donepezil can be predicted by the concentration of donepezil. Further, 46.5 ± 3.5 ng/g donepezil is an efficacious target concentration in the brain for treating learning and memory impairment in rodents.

Effects of penehyclidine hydrochloride injection combined with safflower injection on TLRs / NF-κB signaling pathway and T cell subsets in mononuclear cells of patients with organophosphorus pesticide poisoning / 中国生化药物杂志

Objective To investigate the effects of penehyclidine hydrochloride injection combined with safflower injection on TLRs/NF-κB signaling pathway and T cell subsets in mononuclear cells of patients with organophosphorus pesticide poisoning. Methods 80 cases of organophosphate poisoning patients from June 2014 to June 2016 in onglu first people's hospital were selected,randomly divided into control group and observation group, the control group was treated with penehyclidine hydrochloride,observation group were treated with Honghua injection based on the treatment of control group. The effects were compared between two groups of TLRs/NF-κB in peripheral blood mononuclear cells pathway and T cell subsets in peripheral blood, and compared two groups of patients with cholinesterase activity. Results On the third,fifth and 7th day of treatment,cholinesterase activity in both groups was higher than that before treatment,the activity of cholinesterase in the observation group was significantly higher than that in the control group (P<0.05).After treatment,compared with before treatment,the levels of TLR2,TLR4 and NF-κB in the two groups were significantly decreased,and TLR2,TLR4,NF-κB levels in the observation group were lower than those in the control group, the difference was statistically significant (P<0.05),Th17,Th17/Treg levels in the observation group were significantly lower,and lower than the control group,Treg content was significantly higher,and higher than the control group,the difference was statistically significant (P<0.05). Conclusion Penehyclidine hydrochloride injection combined with safflower injection can help to reduce Th17,Th17/Treg levels,increased Treg cell content,regulate the inflammatory response, and promote recovery of cholinesterase activity.

Active anti-acetylcholinesterase component of secondary metabolites produced by the endophytic fungi of Huperzia serrata

Background An endophytic fungus lives within a healthy plant during certain stages of, or throughout, its life cycle. Endophytic fungi do not always cause plant disease, and they include fungi that yield different effects, including mutual benefit, and neutral and pathogenic effects. Endophytic fungi promote plant growth, improve the host plant's resistance to biotic and abiotic stresses, and can produce the same or similar biologically active substances as the host. Thus, endophytic fungal products have important implications in drug development. Result Among the numerous endophytic fungi, we identified two strains, L10Q37 and LQ2F02, that have anti-acetylcholinesterase activity, but the active compound was not huperzine A. The aim of this study was to investigate the anti-acetylcholinesterase activity of secondary metabolites isolated from the endophytic fungi of Huperzia serrata. Microbial cultivation and fermentation were used to obtain secondary metabolites. Active components were then extracted from the secondary metabolites, and their activities were tracked. Two compounds that were isolated from endophytic fungi of H. serrata were identified and had acetylcholine inhibitory activities. In conclusion, endophytic fungal strains were found in H. serrata that had the same anti-acetylcholinesterase activity. Conclusion We isolated 4 compounds from the endophytic fungus L10Q37, among them S1 and S3 are new compounds. 6 compounds were isolated from LQ2F02, all 6 compounds are new compounds. After tested anti acetylcholinesterase activity, S5 has the best activity. Other compounds' anti acetylcholinesterase activity was not better compared with huperzine A.

Antioxidant and anti-acetylcholinesterase activities of extracts and secondary metabolites from Acacia cyanophylla

Objective: To investigate the antioxidant potential and anti-acetycholinesterase activity of compounds and extracts from Acacia cyanophylla (A. cyanophylla). Methods: Three polyphenolic compounds were isolated from ethyl acetate extract of A.cyanophylla flowers. They have been identified as isosalipurposide 1, quercetin 2 and naringenin 3. Their structures were elucidated by extensive spectroscopic methods including 1D and 2D NMR experiments as well as ES-MS. The prepared extracts and the isolated compounds 1-3 were tested for their antioxidant activity using 1’-1’-diphenylpicrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) scavenging assays and reducing power. They have been also investigated for inhibitory effect against acetylcholinesterase using the microplate assay.Results:(67.26 μg/mL). Isosalipurposide 1 showed a significant antiradical power against DPPH (81.9 μg/mL). All extracts showed a dose-dependent acetylcholinesterase inhibition. In terms of the IC50 value, the butanolic extract (16.03 μg/mL) was the most potent sample. Isosalipurposide 1 was found to be active against AChE with an IC50 value of 52.04 μg/mL. In the DPPH test, the EtOAc extract of flowers exhibited the highest antioxidant effect Conclusions: The results demonstrated the important antioxidant and anti-acetylcholinesterase activity of pure compounds and extracts from A. cyanophylla.

Antioxidant and anti-acetylcholinesterase activities of extracts and secondary metabolites from Acacia cyanophylla

<p><b>OBJECTIVE</b>To investigate the antioxidant potential and anti-acetycholinesterase activity of compounds and extracts from Acacia cyanophylla (A. cyanophylla).</p><p><b>METHODS</b>Three polyphenolic compounds were isolated from ethyl acetate extract of A. cyanophylla flowers. They have been identified as isosalipurposide 1, quercetin 2 and naringenin 3. Their structures were elucidated by extensive spectroscopic methods including 1D and 2D NMR experiments as well as ES-MS. The prepared extracts and the isolated compounds 1-3 were tested for their antioxidant activity using 1'-1'-diphenylpicrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) scavenging assays and reducing power. They have been also investigated for inhibitory effect against acetylcholinesterase using the microplate assay.</p><p><b>RESULTS</b>In the DPPH test, the EtOAc extract of flowers exhibited the highest antioxidant effect (67.26 µg/mL). Isosalipurposide 1 showed a significant antiradical power against DPPH (81.9 µg/mL). All extracts showed a dose-dependent acetylcholinesterase inhibition. In terms of the IC50 value, the butanolic extract (16.03 µg/mL) was the most potent sample. Isosalipurposide 1 was found to be active against AChE with an IC50 value of 52.04 µg/mL.</p><p><b>CONCLUSIONS</b>The results demonstrated the important antioxidant and anti-acetylcholinesterase activity of pure compounds and extracts from A. cyanophylla.</p>

Biologically active compounds from cyanobacteria extracts: in vivo and in vitro aspects

An investigation was directed towards the antiacetylcholinesterase activity of the acid aqueous and methanolic extracts of five cyanobacterial taxa, which encompasses an enzymatic inhibition essay and the evaluation of the physiological responses of mice to cyanobacterial extracts along with toxicological observations. The strains Calothrix sp. CCIBt 3320, Tolypothrix sp. CCIBt 3321, Phormidium cf. amoenum CCIBt 3412, Phormidium sp. CCIBt 3265, and Geitlerinema splendidum CCIBt 3223 were from the São Paulo Botanical Institute Cyanobacterial Culture Collection and all of them showed inhibitory effect on acetylcholinesterase activity (in vitro) and caused systemic effects similar to those described for anticholinesterase drugs (in vivo). With the exception of G. splendidum and Tolypothrix sp. strains, all extracts produced reversible antiacetylcolinesterase effects in mice. Complementary histopathological studies were carried out on tissues from animals administered with Phormidium sp. and P. cf. amoenum.

Composição química volátil e não-volátil de Eupatorium ballotifolium Kunth, Asteraceae

Este trabalho descreve a composição química dos óleos essenciais e o isolamento de onze substâncias de Eupatorium ballotifolium Kunth, Asteraceae. Os óleos essenciais foram obtidos por hidrodestilação, analisados por CG-EM e avaliados quanto às suas atividades frente à enzima acetilcolinesterase. O rendimento dos óleos foi de 0,11 por cento para as folhas e 0,03 por cento para os talos. Os principais constituintes dos óleos foram os sesquiterpenos β-cariofileno (24,9 e 22,2 por cento), espatulenol (17,7 e 12,4 por cento) e epóxi-allo-aromadendreno (23,0 e 23,6 por cento). Do extrato hexânico da parte aérea foi isolada a mistura de β-sitosterol e estigmasterol, incluindo suas formas glicosiladas, e os triterpenos acetato de taraxasterila e taraxasterol, enquanto, do extrato etanólico foram isolados os flavonóides nepetina and 3-O-glicosil-quercetina. Do extrato hexânico das raízes foram isolados os triterpenos epi-friedelanol e damara-20,24-dien-3β-ol e do extrato etanólico a cumarina 11-hidroxi-11,12-di-hidroobliquina. As estruturas de todos os compostos foram determinadas usando técnicas espectroscópica tais como IV, EM e RMN ¹H e 13C.

This work describes the chemical composition of the essential oils and the isolation of eleven substances from Eupatorium ballotifolium Kunth, Asteraceae. The essential oils were obtained by hydrodistillation, analyzed by GC/MS and evaluated towards the acetylcholinesterase enzyme. The oils yield was of 0.11 percent for the leaves and 0.03 percent for the stems. The main constituents of the oils were the sesquiterpenes β-caryophyllene (24.9 and 22.2 percent), spathulenol (17.7 and 12.4 percent) and epoxy-allo-aromadendrene (23.0 and 23.6 percent). From the hexane extract of the aerial part were isolated a mixture of sitosterol and stigmasterol, its glucosides, and the triterpenes taraxasteryl acetate and taraxasterol, while from the ethanol extract were obtained the flavonoids nepetin and 3-O-glucoside-quercetin. The triterpenes epi-friedelanol and dammara-20,24-dien-3β-ol were obtained from the hexane extract of roots, while the coumarin 11-hydroxy-11,12-di-hydroobliquine was obtained from the ethanol extract. The structures of all compounds were determinate based on spectroscopic methods such as IR, MS and ¹H and 13C NMR.

Serum cholinesterase and erythrocyte acetylcholinesterase activity in patients with neuroblastoma.

Serum cholinesterase (ChE), red cell acetylcholinesterase (AChE), were determined in 18 neuroblastoma patients ages ranged from 8 months to 4 years. Sixteen patients (89%) were anemic and 15 patients (83%) showed bone marrow invasion and/or liver involvement. Both mean values of serum ChE and red cell AChE activities were significantly lower than those of 80 normal subjects. There was no relationship between red cell AChE and Hb, Ht or white blood cell count. The cause and mechanism of reduced serum ChE and red cell AChE activities in patients with neuroblastoma were possibly due to the invasion of the liver and bone marrow by the tumor cells. Although neuroblastoma cells can synthesize AChE which is inversely regulated by the rate of cell division, determination of serum ChE and red cell AChE could not serve to distinguish neuroblastoma from the other types of human tumour cells.

Acetylcholinesterase activity in the amniotic fluid of normal Thai pregnant women.

Acetylcholinesterase (AChE) activity was determined for 112 amniotic fluid samples obtained by amniocentesis from normal Thai pregnant women at gestational ages of 34 to 40 weeks. The method for estimation was based on inhibition the of non-specific cholinesterase (ChE) with ethoprorpazine and the expression of residual AChE activity as a percentage of total cholinesterase activity. The mean values of AChE and total ChE activities were found to be 3.65ฑ1.97 U/1 (range 1.10-7.72 U/1) and 7.61ฑ 2.55 U/1 (range 3.31-14.34 U/1) respectively. These values were in the same order of magnitude as results reported earlier in normal pregnant women. There were no relationships between gestational ages and amniotic fluid AChE, ChE or total ChE activities. As the concentration of AChE in the amniotic fluid is the index of the secreted AChE from neurons, it therefore increases considerably in fetus with open neural tube defect (NTD). The results for this pregnant women study is a base-line data for normal Thai pregnant women which will be useful in detecting the NTD in the fetus.

Acetylcholinesterase activity in cord serum and human milk.

Acetycholinesterase (AChE) and pseudocholinesterase (ChE) were determined on 44 cord serum and 72 human milk samples. The mean values of AChE were found to be 87 U/1 (rang 66-176 U/1 (range 1.1-6.6 U/1) in the cord serum and human milk respectively. There were no significant difference between the mean values of AChE in the milk samples collected on day 3 to day 12 after delivery. There was a tendency for increased AChE in the milk in the multi-gravidas more than in the first gravida. As the function of AChE in the milk is not exactly known at the neonatal gut because such systems required for the degradation of various amino acids are still not fully developed in the newborn. As AChE could not be detected in the neonatal serum aged 5 days, this indicatied that the enzyme in the milk. Cord serum contained a significantly lower ChE level than that of adult serum. As this low level rose in the first day and reached a double value within 3 weeks after delivery, this could not be due to the intake of the relatively low ChE in the human milk.