Effects of malathion and cadmium on acetylcholinesterase activity and metallothionein levels in the fish Seriola dumerilli

The potential use of acetylcholinesterase (AChE) and metallothionein (MT) responses as biomarker of organophosphorous (OPs) and trace metal were assessed in fish Seriola dumerilli exposed to 0, 4, 6 mg/kg of malathion for 2, 7 and 13 days, and to 0, 50, 100, 250 mu g/kg of Cd for 2 days. Brain AChE was significantly inhibited after 2 and 7 days of malathion exposure, in a dose-response manner, but no inhibition was observed after 13 days of exposure. When exposed to Cd for 2 days, S. dumerelli presented an increase in AChE activity at a concentration of 50 mu g/kg, but a strong and dose-dependent AChE inhibition at 100 and 250 mu g/kg. Cd treatment also caused a rapid increase in MTs concentration in liver, even at the lower concentration. Our experiments indicate that the measurement of hepatic MT concentration and brain AChE activity in S. dumerilli would be useful biomarkers of OP and Cd exposure and/or effects.

Clinical, cytogenetic and toxicological studies in rural workers exposed to pesticides in Botucatu, São Paulo, Brazil

Pesticidas podem causar mutações gênicas e aberrações cromossômicas em indivíduos expostos. Investigamos 24 trabalhadores expostos a pesticidas, nos quais foram executados exames clínicos e testes citogenéticos e toxicológicos. Dez indivíduos não expostos foram usados como controles. Dosagem toxicológica de cobre, zinco e manganês (metais encontrados em alguns pesticidas), dosagem de enzimas hepáticas (GOT, GPT, AP) e atividade de acetilcolinesterase foram executadas em 16 trabalhadores e oito controles. Nos trabalhadores expostos, os sintomas clínicos mais pertinentes foram digestão pobre, com sensação de plenitude após alimentação, olhos irritados, enxaqueca e fasciculações. O grupo exposto mostrou dosagem de manganês e atividade de acetilcolinesterase significativamente mais baixas, e nível significativamente mais alto de fosfatase alcalina. Estudos citogenéticos mostraram freqüências de aberrações cromossômicas significativamente mais altas no grupo exposto quando comparado ao grupo de controle. Embora usassem vestuário protetor contra névoa de pesticidas, o qual incluía calças de borracha, botas, luvas, máscara e chapéu, os resultados clínicos revelaram que os trabalhadores foram contaminados. Concluímos que estudos citogenéticos, toxicológicos, juntamente com exames clínicos, são importantes no controle da saúde do trabalhador, mesmo em condições de proteção.

Screening for antifungal, DNA-damaging and anticholinesterasic activities of Brazilian plants from the Atlantic Rainforest: Ilha do Cardoso State Park

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Quantification of methomyl levels in cabbage, tomato, and soya milk using a renewable amperometric biosensor

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Estudo químico dos alcalóides piridínicos encontrados em Senna multijuga

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Contaminação por herbicidas em corpos hídricos da microbacia do Córrego Rico (SP) e aspectos toxicológicos de atrazine a juvenis de Piaractus mesopotamicus

Pós-graduação em Agronomia (Produção Vegetal) - FCAV

Espectrometria de massas aplicada aos estudos de biossíntese de alcalóides de Senna spectabilis

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

A candidate short-term toxicity test using Ampelisca brevicornis to assess sublethal responses to pharmaceuticals bound to marine sediments

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Diterpenos tetranorlabdanos e isocumarinas produzidos por Botryosphaeria parva, um fungo endofítico em Eugenia jambolana Lam. (Myrtaceae)

Pós-graduação em Química - IQ

Selective activity of butyrylcholinesterase in serum by a chemiluminescent assay

In a previous study, we showed that purified commercial esterase activity can be detected in a chemiluminescent assay based on the hydrolysis of 2-methyl-1-propenylbenzoate (MPB) to 2-methyl-1-propenol, which is subsequently oxidized by the horseradish peroxidase (HRP)-H2O2 system. The purpose of this study was to verify the applicability of this assay to human serum. The existence of an esterase activity capable of hydrolysing MPB is indicated by the fact that the MPB-scruin-HRP-H2O2 System consumes oxygen and emits light. Both signals were abolished by prior serum heat inactivation and were preserved when serum was stored at less than or equal to4 degreesC. Addition of aliesterase inhibitors, such as fluoride ion and trichlorfon or the cholinesterase inhibitor eserine, totally prevents light emission. The butyrylcholinesterase-specific substrate benzoylcholine causes a delay in both O-2 uptake and light emission, while the specific acetylcholinesterase substrate, acetyl-beta -methylcholine, had practically no effect. Purified butyrylcholinesterase, but not acetylcholinesterase, triggered light emission. The finding that butyryleholinesterase is responsible for the hydrolysis of MPB in serum should serve as the basis for the development of a specific chemiluminescent assay for this enzyme. Copyright (C) 2001 John Wiley & Sons, Ltd.

Pyridine Alkaloids from Senna multijuga As Acetylcholinesterase Inhibitors

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Acetylcholinesterase Inhibitory Pyridine Alkaloids of the Leaves of Senna multijuga

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors

As part of our study on bioactive agents from Brazilian rainforest plants, two new glucoalkaloids, 3,4-dehydro-strictosidine (1) and 3,4-dehydro-strictosidinic acid (2), were isolated from Chimarrhis turbinata, along with seven known glucoalkaloids, cordifoline (3), strictosidinic acid (4), strictosidine (5), 5alpha-carboxystrictosidine (6), turbinatine (7), desoxycordifoline (8), and harman-3-carboxylic acid (9). The structures of the new alkaloids were established on the basis of comprehensive spectral analysis, mainly 1D and 2D NMR experiments, as well as high-resolution HRESIMS. Alkaloid 3 showed strong free-radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) as well as pronounced antioxidant activity evidenced by redox properties measured by ElCD-HPLC. Additionally, alkaloids 1-9 were submitted to TLC screening for acetylcholinesterase inhibitors. Both 7 and 8 were shown to be moderate acetylcholinesterase inhibitors at a concentration of 0.1 and 1.0 muM, respectively. In an in vitro rat brain assay, 7 showed moderate activity (IC50 1.86 muM), compared to the standard compound, galanthamine (IC50 0.92 muM).

New anti-Alzheimer drugs from biodiversity: the role of the natural acetylcholinesterase inhibitors

Alzheimer's disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays, drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by regulation of the synthesis and release of acetylcholine in the brain. There are only four commercial medicines approved for treatment of AD, and natural products have played an important alternative role in the research for new acetylcholinesterase inhibitors, as exemplified through the discovery of galantamine. This profile conducts us to give in this paper an overview relating the several classes of natural products with anti-cholinesterasic activity as potential templates to the design of new selective and powerful anti-Alzheimer drugs.

In vitro and in vivo inhibition of acetylcholinesterase and carboxylesterase by metals in zebrafish (Danio rerio)

Metals are natural components in ecosystems; however, if these elements are in excess, they can have adverse effects on living organisms. This study analyzes the interference of copper, lead, iron and cadmium in acetylcholinesterase (AChE) and carboxylesterase (CbE) activities in zebrafish. AChE was significantly inhibited in vitro by copper, iron, lead and cadmium at higher concentrations (10 and 20 mmol/L), whereas CbE was inhibited only at a concentration of 20 mmol/L. In vivo, only lead and cadmium were able to cause AChE inhibition at higher concentrations, while iron didn't cause any changes, and copper promoted an increase in AChE activity at a concentration of 0.06 mg/L. CbE activity did not change at any of the times (two and seven days) and concentrations tested, except in the case of copper exposure, which resulted in a decrease in CbE activity. Indeed, iodoacetamide treatment didn't changed AChE neither CbE activities, results which indicate that the metal inhibiting effect is probably not due to its biding to thiol groups close the active site of the enzyme. This outcome reveals that metals are important esterase inhibitors in zebrafish, and should be considered in environmental monitoring studies that use esterase inhibition as exposure biomarkers of organophosphate and carbamate pesticides. © 2012 Elsevier Ltd. All rights reserved.