RESUMO
Fungicides are often used prophylactically, to control fungal diseases. Although fungicides have been designed to control pests/fungi, they frequently share molecular targets with non-target species, including humans. Tebuconazole, a fungicide belonging to the class of triazoles, is widely employed, has moderate to high persistence in soil, and can be found in different environmental levels. This fungicide is metabolized to the main hydroxy-derived metabolite, Tebuconazole-tert-butyl-hydroxy (or hydroxytebuconazole). This study aims to unveil the action mechanism of Tebuconazole and the role played by its metabolite, Tebuconazole-tert-butyl-hydroxy (5-(4-Chlorophenyl)-2,2-dimethyl-3-(1H-1,2,4-triazol-1-ylmethyl)-1,3-pentanediol), within the expected spectrum of toxicity. In silico and in vitro analyses (MTT assay, cell cycle evaluation, annexin/PI assay, ROS accumulation assay, and mitochondrial membrane potential determination) were performed in HepG2 cells for 24 h and 48 h. Although in silico analysis suggested that both Tebuconazole and Tebuconazole-tert-butyl-hydroxy are potentially hepatotoxic, only Tebuconazole affected the tested cell line. Reduced MTT metabolism, and decreased mitochondrial membrane potential were the main findings. In conclusion, the action mechanism of Tebuconazole may be related to mitochondrial dysfunction. However, the findings of this study pointed out that Tebuconazole-tert-butyl-hydroxy does not play an important role in Tebuconazol toxicity. The study has generated new data that will help to understand how fungicides behave in the environment.
Assuntos
Fungicidas Industriais , Potencial da Membrana Mitocondrial , Triazóis , Triazóis/toxicidade , Humanos , Fungicidas Industriais/toxicidade , Células Hep G2 , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacosRESUMO
Tebuconazole (TEB), a widely used pesticide in agriculture to combat fungal infections, is commonly detected in global food, potable water, groundwater, and human urine samples. Despite its known in vivo toxicity, its impact on heart function remains unclear. In a 28-day study on male Wistar rats (approximately 100 g), administering 10 mg/kg/day TEB or a vehicle (control) revealed no effect on body weight gain or heart weight, but an increase in the infarct area in TEB-treated animals. Notably, TEB induced time-dependent changes in in vivo electrocardiograms, particularly prolonging the QT interval after 28 days of administration. Isolated left ventricular cardiomyocytes exposed to TEB exhibited lengthened action potentials and reduced transient outward potassium current. TEB also increased reactive oxygen species (ROS) production in these cardiomyocytes, a phenomenon reversed by N-acetylcysteine (NAC). Furthermore, TEB-treated animals, when subjected to an in vivo dobutamine (Dob) and caffeine (Caf) challenge, displayed heightened susceptibility to severe arrhythmias, a phenotype prevented by NAC. In conclusion, TEB at the no observed adverse effect level (NOAEL) dose adversely affects heart electrical function, increases arrhythmic susceptibility, partially through ROS overproduction, and this phenotype is reversible by scavenging ROS with NAC.
Assuntos
Arritmias Cardíacas , Dobutamina , Triazóis , Humanos , Ratos , Animais , Masculino , Espécies Reativas de Oxigênio , Ratos Wistar , Arritmias Cardíacas/induzido quimicamente , Acetilcisteína , Miócitos CardíacosRESUMO
The present work explores the genotoxicity of the fungicides iprodione (IP) and tebuconazole (TB) using the Allium cepa assay as an in vivo biological model. Both short-term and long-term exposures were studied, revealing concentration- and time-dependent cytological and genotoxic effects. IP exhibited genotoxicity over a wider concentration range (5-50 µg/ml) and required 30 h of exposure, while TB showed genotoxicity at higher concentrations (10 and 30 µg/ml) within a 4-h exposure period. The study highlights the importance of assessing potential risks associated with fungicide exposure, including handling, disposal practices, and concerns regarding food residue. Moreover, the research underscores the genotoxic effects of IP and TB on plant cells and provides valuable insights into their concentration and time-response patterns.
Assuntos
Aminoimidazol Carboxamida/análogos & derivados , Fungicidas Industriais , Hidantoínas , Cebolas , Triazóis , Meristema , Fungicidas Industriais/toxicidade , Dano ao DNA , Raízes de Plantas , Aberrações CromossômicasRESUMO
Tebuconazole (TBZ) and azoxystrobin (AZX) are fungicides frequently used in rice cultivation. Despite protecting crops against fungal diseases, these compounds can contaminate the natural environments close to the crops, exerting negative effects on non-target organisms, the present study aimed to characterize the contamination by fungicides of a river that flows in an area dominated by rice cultivation in the north of the state of Santa Catarina, SC, Brazil. Concentrations of TBZ and AZX found in the field were used to evaluate their negative effects on development, biochemical biomarkers and histopatology of the liver of a native tadpole species, the hammerfrog (Boana faber). Tadpoles were exposed for 16 days to the lowest (1.20 µg/L) and highest (2.60 µg/L) concentration of TBZ, lowest (0.70 µg/L) and highest (1.60 µg/L) concentration of AZX, and the mix of both fungicides at lowest and highest concentration of each found in field analyses. Exposure to the lower TBZ concentration and both concentrations of the Mix accelerated the development of tadpoles. AZX caused an increase in the activities of glutathione S-transferase (GST), carboxylesterase (CbE) and glucose-6-phosphate dehydrogenase (G6PDH) in the liver, an increase in the levels of protein carbonyls (PC) in the liver and an increase in the activity of acetylcholinesterase (AChE) in muscle of tadpoles. TBZ, on the other hand, generated an increase in GST, G6PDH, PC and histopathological severity scores in liver and in muscle AChE activity. The effects were more intense in the groups exposed to the Mix of contaminants. No treatment altered brain AChE. The data showed that the fungicides from in rice cultivation found in natural aquatic environments around the crops pose risks to the health of the animals, compromising their metabolism and development.
Assuntos
Fungicidas Industriais , Oryza , Poluentes Químicos da Água , Animais , Fungicidas Industriais/toxicidade , Acetilcolinesterase , Produtos Agrícolas , Glutationa Transferase , Poluentes Químicos da Água/toxicidade , LarvaRESUMO
Agrochemicals cause diverse effects on aquatic communities, and amphibian species are particularly threatened due the high susceptibility to contamination. Present study evaluates the toxicity of a widely used fungicide tebuconazole (Trigal®) by the assessment of mortality and developmental alterations at acute, subchronic, and chronic exposure during the embryo-larval development of the South American toad Rhinella arenarum. Also, the sensitivity of the different embryonic stages was evaluated with 24-h pulse exposure treatments. The results demonstrated that larvae were more sensitive than embryos at acute exposure (LC50-24 and 96 h = 74.62, 31.92 mg/L and 24.27, 16.81 mg/L for embryos and larvae, respectively). Nevertheless, embryos toxicity increased significantly achieving a sensitivity very similar to larvae at chronic exposure (LC50-168 and 504 h = 13.31, 4.35 mg/L and 14.47, 6.83 mg/L for embryos and larvae, respectively). Embryos exhibited several sublethal effects from 5 mg/L at 96 h onwards, such as delayed development, reduce body size, edemas, tail/axial flexures, weakness, and absence of movements. The teratogenic index at 96 h was 10.13, indicating the severe teratogenic potential of the fungicide. 24-h pulse exposure treatments showed an increased sensitivity in intermediate stages as S.11, S.18, S20, and S.23 (NOEC-96 h = 100, 200, 75, and 20 mg/L, respectively), while stage S.25 was the most sensitive to the fungicide (NOEC-96 h = 5 mg/L). About metamorphic process, tebuconazole caused an acceleration of metamorphosis at the lowest concentration (0.001 mg/L), but also an increase in mortality and in addition, significant differences in the weight in all treatments. The results obtained throughout this work indicate that tebuconazole cause several adverse effects in Rhinella arenarum embryo-larval development.
Assuntos
Fungicidas Industriais , Triazóis , Poluentes Químicos da Água , Animais , Fungicidas Industriais/toxicidade , Bufo bufo , Embrião não Mamífero , Bufonidae , Bufo arenarum , Larva , América do Sul , Poluentes Químicos da Água/toxicidadeRESUMO
The fungicide Tebuconazole is a widely used pesticide in agriculture and may cause cardiotoxicity. In our present investigation the effect of Tebuconazole on the sodium current (INa) of human cardiac sodium channels (NaV1.5) was studied using a heterologous expression system and whole-cell patch-clamp techniques. Tebuconazole reduced the amplitude of the peak INa in a concentration- and voltage-dependent manner. At the holding potential of -120 mV the IC50 was estimated at 204.1 ± 34.3 µM, while at -80 mV the IC50 was 0.3 ± 0.1 µM. The effect of the fungicide is more pronounced at more depolarized potentials, indicating a state-dependent interaction. Tebuconazole caused a negative shift in the half-maximal inactivation voltage and delayed recovery from fast inactivation of INa. Also, it enhanced closed-state inactivation, exhibited use-dependent block in a voltage-dependent manner. Furthermore, Tebuconazole reduced the increase in late sodium current induced by the pyrethroid insecticide ß-Cyfluthrin. These results suggest that Tebuconazole can interact with NaV1.5 channels and modulate INa. The observed effects may lead to decreased cardiac excitability through reduced INa availability, which could be a new mechanism of cardiotoxicity to be attributed to the fungicide.
RESUMO
Tebuconazole (TEB) is a fungicide widely used in agriculture; however, its constant application has increased the emergence of resistant plant pathogenic fungal strains and reduced the effectiveness of fungi as biological control agents; for instance, the entomopathogenic and hyperparasitic fungus Akanthomyces lecanii, suitable for simultaneous biological control of insect pest and plant pathogenic fungi, is highly sensitive to fungicides. We carried out the induction of resistance to TEB in two wild type strains of A. lecanii by UV radiation and selective pressure in increasing fungicide gradients using a modified Microbial Evolution and Growth Arena (MEGA), to produce A. lecanii strains that can be used as biological control agent in the presence of tebuconazole. Nine UV-induced and three naturally adapted A. lecanii strains were resistant to TEB at the agriculturally recommended dose, and three irradiated strains were resistant to TEB concentration ten times higher; moreover, growth, sporulation rates, production of hydrolytic enzymes, and virulence against the hemipteran Coccus viridis, a major pest of coffee crops, were not affected in the TEB-resistant strains. These A. lecanii TEB-resistant strains would have a greater opportunity to develop and to establish themselves in fields where the fungicide is present and can be used in a combined biological-chemical strategy to improve insect and plant pathogenic fungal control in agriculture. Also, the selective pressure through modified MEGA plate methodology can be used for the adaptation of entomopathogenic filamentous fungi to withstand other chemical or abiotic stresses that limits its effectiveness for pest control.
Assuntos
Cordyceps , Fungicidas Industriais , Hemípteros , Animais , Raios Ultravioleta , Insetos , Fungicidas Industriais/farmacologiaRESUMO
Tebuconazole (TEB) is an important fungicide that belongs to the triazole family. It is widely used in agriculture and its use has experienced a tremendous increase in the last decade. The long-term exposure of humans to this pesticide is a real threat because it is stable in water and soil. The association between long-term exposure to TEB and damage of several biological systems, including hepatotoxicity and cardiotoxicity is evident, however, acute toxicological studies to reveal the toxicity of TEB are limited. This research paper addressed the acute exposure of TEB in murine hearts, cardiomyocytes, and human cardiomyocytes derived from an induced pluripotent stem cell (hiPSC-CMs), spelling out TEB's impact on electromechanical properties of the cardiac tissue. In ex vivo experiments, TEB dose dependently, caused significant electrocardiogram (ECG) remodeling with prolonged PR and QTc interval duration. The TEB was also able to change the action potential waveform in murine cardiomyocytes and hiPSC-CMs. These effects were associated with the ability of the compound to block the L-type calcium current (IC50 = 33.2 ± 7.4 µmol.l-1) and total outward potassium current (IC50 = 5.7 ± 1.5 µmol.l-1). TEB also increased the sodium/calcium exchanger current in its forward and reverse modes. Additionally, sarcomere shortening and calcium transient in isolated cardiomyocytes were enhanced when cells were exposed to TEB at 30 µmol.l-1. Combined, our results demonstrated that acute TEB exposure affects the cardiomyocyte's electro-contractile properties and triggers the appearance of ECG abnormalities.
Assuntos
Potenciais de Ação/efeitos dos fármacos , Arritmias Cardíacas/induzido quimicamente , Cardiotoxicidade/etiologia , Fungicidas Industriais/toxicidade , Células-Tronco Pluripotentes Induzidas/efeitos dos fármacos , Miócitos Cardíacos/efeitos dos fármacos , Triazóis/toxicidade , Animais , Modelos Animais de Doenças , Humanos , Camundongos , Camundongos Endogâmicos C57BLRESUMO
Tebuconazole (TEB) is a chiral triazole fungicide worldwide employed to control plant pathogens and preserve wood. People can be exposed to TEB either through diet and occupational contamination. This work investigates the in vitro inhibitory potential of rac-TEB, S-(+)-TEB, and R-(-)-TEB over the main cytochrome P450 enzymes (CYP450) using human liver microsomes to predict TEB in vivo inhibition potential. The IC50 values showed that in vitro inhibition was enantioselective for CYP2C9, CYP2C19, and CYP2D6, but not for CYP3A4/5. Despite enantioselectivity, rac-TEB and its single enantiomers were always classified in the same category. The inhibition mechanisms and constants were determined for rac-TEB and it has shown to be a mixed inhibitor of CYP3A4/5 (Ki = 1.3 ± 0.3 µM, αKi = 3.2 ± 0.5 µM; Ki = 0.6 ± 0.3 µM, αKi = 1.3 ± 0.3 µM) and CYP2C9 (Ki = 0.7 ± 0.1 µM, αKi = 2.7 ± 0.5 µM), and a competitive inhibitor of CYP2D6 (Ki = 11.9 ± 0.7 µM) and CYP2C19 (Ki = 0.23 ± 0.02 µM), respectively, suggesting that in some cases, rac-TEB has a higher or comparable inhibitory potential than well-known strong inhibitors of CYP450 enzymes, especially for CYP2C9 and CYP2C19. In vitro-in vivo extrapolations (IVIVE) were conducted based on the results and data available in the literature about TEB absorption and metabolism. R1 values were estimated based on the Food and Drug Administration guideline and suggested that in a chronic oral exposure scenario considering the acceptable daily intake dose proposed by the European Food and Safety Authority, the hypothesis of rac-TEB to inhibit the activities of CYP3A4/5, CYP2C9, and CYP2C19 in vivo and cause pesticide-drug interactions cannot be disregarded.
Assuntos
Inibidores das Enzimas do Citocromo P-450/farmacologia , Sistema Enzimático do Citocromo P-450/metabolismo , Praguicidas/farmacologia , Triazóis/química , Triazóis/farmacologia , Inibidores das Enzimas do Citocromo P-450/química , Humanos , Estrutura Molecular , Praguicidas/química , Relação Estrutura-AtividadeRESUMO
Despite the resistance problems in Monilinia fructicola, demethylation inhibitor fungicides (DMIs) are still effective for the disease management of brown rot in commercial stone fruit orchards in Brazil. This study aims to investigate the sensitivity of M. fructicola isolates and efficiency of DMIs to reduce brown rot. A set of 93 isolates collected from Brazilian commercial orchards were tested for their sensitivities to tebuconazole, propiconazole, prothioconazole, and myclobutanil. The isolates were analyzed separately according to the presence or absence of the G461S mutation in MfCYP51 gene, determined by allele-specific test. The mean EC50 values for G461S mutants and wild-type isolates were respectively 8.443 and 1.13 µg/ml for myclobutanil, 0.236 and 0.026 µg/ml for propiconazole, 0.115 and 0.002 µg/ml for prothioconazole, and 1.482 and 0.096 µg/ml for tebuconazole. The density distribution curves of DMI sensitivity for both genotypes showed that myclobutanil and prothioconazole curves were mostly shifted toward resistance and sensitivity, respectively. Incomplete cross-resistance was detected among propiconazole and tebuconazole in both wild-type (r = 0.45) and G461S (r = 0.38) populations. No cross-sensitivity was observed among wild-type isolates to prothioconazole and the others DMIs tested. Fungicide treatments on detached fruit inoculated with M. fructicola genotypes showed significant DMI efficacy differences when fruit were inoculated with wild-type and G461S isolates. Protective applications with prothioconazole were more effective for control of both G461S and wild-type isolates compared with tebuconazole. Curative applications with tebuconazole were most effective in reducing the incidence and lesion size of G461S isolates. Sporulation occurred only for G461S isolates treated with tebuconazole under curative and preventative treatments. The differences found among the performance of triazoles against M. fructicola isolates will form the basis for recommendations of rational DMI usage to control brown rot in Brazil.
Assuntos
Fungicidas Industriais , Brasil , Desmetilação , Farmacorresistência Fúngica , Frutas , Fungicidas Industriais/farmacologiaRESUMO
Polar Organic Chemical Integrative Samplers (POCIS) were deployed in two watersheds in Córdoba province and one watershed in Buenos Aires province in Argentina. The fungicides, tebuconazole, carbendazim and azoxystrobin, and the herbicides, atrazine, dicamba and 2,4-D were detected in POCIS deployed in each of the three watersheds. Estimated time weighted average concentrations of atrazine were greater than 2 µg/L at the outflow of Brava Lake in Buenos Aires province, and this concentration exceeds the Canadian water quality guideline for protection of aquatic life. The concentrations of all other pesticides were less than 400 ng/L. The distribution of pesticides detected in surface waters indicated that the sources were runoff from agricultural and urban lands and discharges from wastewater treatment plants.
Assuntos
Monitoramento Ambiental/métodos , Água Doce/química , Fungicidas Industriais/análise , Praguicidas/análise , Poluentes Químicos da Água/análise , Agricultura , Argentina , Monitoramento Ambiental/instrumentação , Lagos/química , Metanol/química , Rios/química , Urbanização , Águas Residuárias/químicaRESUMO
Tebuconazole (TEB) is a chiral triazole fungicide that is globally marketed and used as a racemic mixture to control plant pathogens. Due to its use as a racemic mixture, TEB may exhibit enantioselective toxicokinetics toward nontarget organisms, including humans. Therefore, the in vitro enantioselective metabolism of TEB by cytochrome P450 enzymes (CYP450) was studied using human liver microsomes, and the in vivo toxicokinetic parameters were predicted. A new enantioselective, reversed-phase LC-MS/MS method was developed and validated to analyze the enantiomers of TEB and its main metabolite, 1-hydroxytebuconazole (TEBOH). In vitro metabolic parameters were obtained, and in vitro-in vivo extrapolations were performed. Michaelis-Menten and atypical biphasic kinetic profiles were observed with a total intrinsic clearance ranging from 53 to 19â¯mLâ¯min-1 mg-1. The in vitro-in vivo extrapolation results showed that TEB first passage effect by the liver seems to be negligible, with hepatic clearance and extraction ratios ranging from 0.53 to 5.0â¯mLâ¯min-1 kg-1 and 2.7-25%, respectively. Preferential metabolism of (+)-TEB to rac-TEB and (-)-TEB was observed, with preferential production of (+)-TEBOH. Furthermore, reaction phenotyping studies revealed that, despite the low hepatic clearance in the first pass metabolism of TEB, multiple human CYP450 isoforms were involved in TEB metabolism when TEBOH enantiomers were generated, mainly CYP3A4 and CYP2C9, which makes TEB accumulation in the human body more difficult due to multiple metabolic pathways.
Assuntos
Fungicidas Industriais/metabolismo , Microssomos Hepáticos/metabolismo , Triazóis/metabolismo , Cromatografia Líquida , Sistema Enzimático do Citocromo P-450/metabolismo , Fungicidas Industriais/química , Fungicidas Industriais/farmacocinética , Fungicidas Industriais/toxicidade , Humanos , Fígado/metabolismo , Estereoisomerismo , Espectrometria de Massas em Tandem , Toxicocinética , Triazóis/química , Triazóis/farmacocinética , Triazóis/toxicidadeRESUMO
Sand was studied as a solid support in ultrasound-assisted matrix solid-phase dispersion (UA-MSPD) for the extraction of different pesticide classes, including organophosphates, carbamates, triazoles and pyrethroids from fruits and vegetables, with determination by GC-MS and LC-MS/MS. The performance of sand was compared with that of different types of classic solid supports and alternative natural materials from renewable sources. The best results were obtained using 0.5â¯g sample, 1â¯g sand as a solid support, 20â¯mg activated charcoal and 5â¯mL ethyl acetate as elution solvent. Recoveries ranged from 55â¯toâ¯140% with an RSDâ¯≤â¯20%. LOQs varied from 0.005 to 0.5â¯mgâ¯kg-1 for all analytes. Thiamethoxam, captan, chlorpyrifos, dimethoate and pyrimethanil were found in strawberry samples at concentrations from 0.01 to 0.06â¯mgâ¯kg-1. Acephate and tebuconazole were found in a tomato sample at concentrations of 0.45 and 0.30â¯mgâ¯kg-1, respectively. The method developed was efficient, simple, cheap, robust, and environmentally friendly.
Assuntos
Cromatografia Gasosa-Espectrometria de Massas , Resíduos de Praguicidas/análise , Extração em Fase Sólida/métodos , Verduras/química , Cromatografia Líquida de Alta Pressão , Dimetoato/química , Frutas/química , Frutas/metabolismo , Limite de Detecção , Resíduos de Praguicidas/isolamento & purificação , Piretrinas/química , Sonicação , Espectrometria de Massas em Tandem , Triazóis/química , Verduras/metabolismoRESUMO
Brazil is the largest consumer of pesticides in the world. However, knowledge on how these pesticides affect wildlife is scarce. Among the vertebrates, amphibians are particularly important in research to assess the impact of pesticides because of the correlation between pesticide and the decline of these species. This study aimed to evaluate the acute and chronic toxicity of commercial formulations of pesticides, i.e., atrazine (herbicide), cypermethrin (insecticide), and tebuconazole (fungicide) in Physalaemus cuvieri tadpoles. Eggs were collected in nature and cultivated under controlled conditions in the laboratory. Toxicity tests were carried out under standard conditions to determine the lethal concentration (LC50) after 96 h of exposure and to determine the effect of sublethal concentrations after 7 days. In addition, we performed swimming activity tests on tadpoles exposed to sublethal concentrations. The lethal concentration (LC50) was 19.69 mg/L for atrazine, 0.24 mg/L for cypermethrin and 0.98 mg/L for tebuconazole. In the acute test, atrazine showed lower toxicity than cypermethrin and tebuconazole for P. cuvieri. Swimming activity was affected at sublethal doses of atrazine and cypermethrin, but was not after exposure to tebuconazole. Cypermethrin was the insecticide that most altered the swimming activity of the individuals tested. The risk evaluation analysis indicated risks for tadpoles exposed to three tested pesticides, specially cypermethrin.
Assuntos
Atrazina/toxicidade , Larva/efeitos dos fármacos , Piretrinas/toxicidade , Triazóis/toxicidade , Poluentes Químicos da Água/toxicidade , Animais , Anuros/crescimento & desenvolvimento , Anuros/fisiologia , Fungicidas Industriais/toxicidade , Herbicidas/toxicidade , Inseticidas/toxicidade , Testes de Toxicidade Aguda , Testes de Toxicidade CrônicaRESUMO
Cryptococcus gattii and Cryptococcus neoformans are environmental fungi that cause cryptococcosis, which is usually treated with amphotericin B and fluconazole. However, therapeutic failure is increasing because of the emergence of resistant strains. Because these species are constantly isolated from vegetal materials and the usage of agrochemicals is growing, we postulate that pesticides could be responsible for the altered susceptibility of these fungi to clinical drugs. Therefore, we evaluated the influence of the pesticide tebuconazole on the susceptibility to clinical drugs, morphophysiology, and virulence of C. gattii and C. neoformans strains. The results showed that tebuconazole exposure caused in vitro cross-resistance (CR) between the agrochemical and clinical azoles (fluconazole, itraconazole, and ravuconazole) but not with amphotericin B. In some strains, CR was observed even after the exposure ceased. Further, tebuconazole exposure changed the morphology, including formation of pseudohyphae in C. neoformans H99, and the surface charge of the cells. Although the virulence of both species previously exposed to tebuconazole was decreased in mice, the tebuconazole-exposed colonies recovered from the lungs were more resistant to azole drugs than the nonexposed cells. This in vivo CR was confirmed when fluconazole was not able to reduce the fungal burden in the lungs of mice. The tolerance to azoles could be due to increased expression of the ERG11 gene in both species and of efflux pump genes (AFR1 and MDR1) in C. neoformans Our study data support the idea that agrochemical usage can significantly affect human pathogens present in the environment by affecting their resistance to clinical drugs.
Assuntos
Cryptococcus gattii/efeitos dos fármacos , Cryptococcus neoformans/efeitos dos fármacos , Farmacorresistência Fúngica Múltipla/efeitos dos fármacos , Fungicidas Industriais/farmacologia , Triazóis/farmacologia , Animais , Antifúngicos/farmacologia , Criptococose/tratamento farmacológico , Criptococose/microbiologia , Cryptococcus gattii/patogenicidade , Cryptococcus gattii/fisiologia , Cryptococcus neoformans/patogenicidade , Cryptococcus neoformans/fisiologia , Fluconazol/farmacologia , Masculino , Camundongos Endogâmicos C57BL , Testes de Sensibilidade Microbiana , Virulência/efeitos dos fármacosRESUMO
In this study, we evaluated the effects of tebuconazole on morphology and exploratory larvae behavior and adult locomotion. Furthermore, we analyzed the effects of this fungicide on AChE activity and gene expression in zebrafish larvae and in the adult zebrafish brain. Tebuconazole (4 mg/L) increased the ocular distance in larvae and reduced the distance travelled, absolute turn angle, line crossing and time outside area in exposed larvae. Moreover, adult zebrafish that were exposed to this fungicide (4 and 6 mg/L) showed a decrease in distance travelled and mean speed when compared to the control group. However, tebuconazole did not alter the number of line crossings or time spent in the upper zone. Tebuconazole inhibited AChE activity at concentrations of 4 mg/L for larvae and 4 and 6 mg/L in the adult zebrafish brain. However, this fungicide did not alter AChE gene expression in the adult zebrafish brain but increased AChE mRNA transcript levels in larvae. These findings demonstrated that tebuconazole could modulate the cholinergic system by altering AChE activity and that this change may be associated with the reduced locomotion of these animals.
Assuntos
Fungicidas Industriais/toxicidade , Triazóis/toxicidade , Poluentes Químicos da Água/toxicidade , Peixe-Zebra/fisiologia , Animais , Comportamento Animal/efeitos dos fármacos , Encéfalo/efeitos dos fármacos , Comportamento Exploratório , Fungicidas Industriais/metabolismo , Larva/efeitos dos fármacos , Locomoção/efeitos dos fármacos , Poluentes Químicos da Água/metabolismo , Peixe-Zebra/metabolismoRESUMO
An analytical method for the simultaneous determination of propiconazole isomers and tebuconazole residues in blueberries was developed using solid-phase microextraction (SPME) coupled to gas chromatography. Confirmation was performed by gas chromatography-mass spectrometry in selected-ion monitoring mode. The SPME fibre coating selected was CWX-DVB, and the pH was adjusted to 7 with NaOH. The method is selective with adequate precision and high accuracy and sensitivity. Recoveries ranged between 97.4% and 98.9% for all compounds; and detection and quantification limits were respectively 0.21 and 0.49 µg kg-1 for propiconazole I; 0.16 and 0.22 µg kg-1 for propiconazole II; and 0.16 and 0.48 µg kg-1 for tebuconazole. The degradation of these fungicides in blueberries followed first-order rate kinetics. The half-life times for flowering and fruit set applications were respectively 4.0 and 10.3 days for propiconazole I, 4.0 and 11.4 days for propiconazole II, and 3.5 and 12.4 days for tebuconazole.
Assuntos
Mirtilos Azuis (Planta)/química , Frutas/química , Resíduos de Praguicidas/análise , Microextração em Fase Sólida/métodos , Microextração em Fase Sólida/normas , Triazóis/análise , Argentina , Cromatografia Gasosa , CinéticaRESUMO
Tebuconazole (TBZ) nanoemulsions (NEs) were formulated using a low energy method. TBZ composition directly affected the drop size and surface tension of the NE. Water fraction and the organic-to-surfactant-ratio (RO/S) were evaluated in the range of 1-90 and 1-10 wt %, respectively. The study was carried out with an organic phase (OP) consisting of an acetone/glycerol mixture containing TBZ at a concentration of 5.4 wt % and Tween 80 (TW80) as a nonionic and Agnique BL1754 (AG54) as a mixture of nonionic and anionic surfactants. The process involved a large dilution of a bicontinuous microemulsion (ME) into an aqueous phase (AP). Pseudo-ternary phase diagrams of the OP//TW80//AP and OP//AG54//AP systems at T = 25 °C were determined to map ME regions; these were in the range of 0.49-0.90, 0.01-0.23, and 0.07-0.49 of OP, AP, and surfactant, respectively. Optical microscope images helped confirm ME formation and system viscosity was measured in the range of 25-147 cP. NEs with drop sizes about 9 nm and 250 nm were achieved with TW80 and AG54, respectively. An innovative low-energy method was used to develop nanopesticide TBZ formulations based on nanoemulsion (NE) technology. The surface tension of the studied systems can be lowered 50% more than that of pure water. This study's proposed low-energy NE formulations may prove useful in sustainable agriculture.
RESUMO
The popcorn culture is extremely susceptible to foliar diseases that relate to plants, reduce photosynthetic area, considerably reducing production. Although there are fungicides registered for the control of these diseases, there are still questions to which fungicides and times which apply the product to greater efficiency in control. The objective of this study was to evaluate the performance of three fungicide (pyraclostrobin + epoxyconazol 0.75 L c.p. ha-1 , trifloxystrobin + protioconazol to 1.00 L c.p. ha-1 and carbendazim + tebuconazole + cresoxim methyl 0,5 L c.p. ha-1 and the check without fungicide) in the Exserohilum turcicum control. Fungicides were applied at four growth stages of popcorn: V8, VT, R2 and V8 plus R2, totaling 16 treatments with six replications. The assay was performed in the agricultural season 2012/2013 on the campus of the Faculdade Integrado de Campo Mourão-PR. We used the design on track with split plots. In this assay were evaluated: the area under the disease progress curve (AUDPC), and plant height, ear, number of rows of grain and grain number in row, yield per plant and expandability. There was a trend for lower AUDPC treatments with fungicides pyraclostrobin + epoxyconazol for all application times compared to the other treatments evaluated. However, the lowest AUDPC were observed with the application of fungicides pyraclostrobin + epoxyconazol and carbendazim + tebuconazole + cresoximmethyl applied at V8 plus R2.
A cultura do milho pipoca é extremamente suscetível a doenças foliares, que ao incidirem nas plantas,diminuem a área fotossintética, reduzindo consideravelmente a produção. Apesar de existirem fungicidasregistrados para o controle destas doenças no milho (Zea mays), ainda há dúvidas de quais fungicidas e emquais épocas aplicar o produto para uma maior eficiência no controle. Objetivou-se neste trabalho avaliar odesempenho de três fungicidas (piraclostrobina + epoxiconazol a 0,75 L p.c. ha-1, trifloxistrobina +protioconazol a 1,00 L p.c. ha-1e carbendazim + tebuconazol + cresoxim-metílico a 0,5 L p.c. ha-1, além deuma testemunha) no controle da helmintosporiose. Os fungicidas foram aplicados em quatro estádiosfenológicos da cultura do milho pipoca: V8, VT, R2 e em V8 e R2, totalizando 16 tratamentos, com seisrepetições. O ensaio foi realizado no ano agrícola 2012/2013 no Campus da Faculdade Integrado de CampoMourão-PR. Utilizou-se o delineamento em faixa com parcelas subdivididas. Neste ensaio foram avaliadas:a área abaixo da curva de progresso da doença (AACPD), altura de plantas e de inserção de espiga, númerode fileiras de grãos e número de grãos na fileira, produção por planta e capacidade de expansão. Verificouseuma tendência de menor AACPD com os tratamentos fungicidas piraclostrobina + epoxiconazol paratodas as épocas de aplicação comparadas aos demais tratamentos avaliados. Porém, as menores AACPDforam observadas com a aplicação dos fungicidas piraclostrobina + epoxiconazol e carbendazim +tebuconazol + cresoxim-metílico aplicados em V8 e R2.
Assuntos
Folhas de Planta/fisiologia , Fungicidas Industriais/administração & dosagem , Zea mays/fisiologia , Controle de Pragas/métodosRESUMO
The popcorn culture is extremely susceptible to foliar diseases that relate to plants, reduce photosynthetic area, considerably reducing production. Although there are fungicides registered for the control of these diseases, there are still questions to which fungicides and times which apply the product to greater efficiency in control. The objective of this study was to evaluate the performance of three fungicide (pyraclostrobin + epoxyconazol 0.75 L c.p. ha-1 , trifloxystrobin + protioconazol to 1.00 L c.p. ha-1 and carbendazim + tebuconazole + cresoxim methyl 0,5 L c.p. ha-1 and the check without fungicide) in the Exserohilum turcicum control. Fungicides were applied at four growth stages of popcorn: V8, VT, R2 and V8 plus R2, totaling 16 treatments with six replications. The assay was performed in the agricultural season 2012/2013 on the campus of the Faculdade Integrado de Campo Mourão-PR. We used the design on track with split plots. In this assay were evaluated: the area under the disease progress curve (AUDPC), and plant height, ear, number of rows of grain and grain number in row, yield per plant and expandability. There was a trend for lower AUDPC treatments with fungicides pyraclostrobin + epoxyconazol for all application times compared to the other treatments evaluated. However, the lowest AUDPC were observed with the application of fungicides pyraclostrobin + epoxyconazol and carbendazim + tebuconazole + cresoximmethyl applied at V8 plus R2.(AU)
A cultura do milho pipoca é extremamente suscetível a doenças foliares, que ao incidirem nas plantas,diminuem a área fotossintética, reduzindo consideravelmente a produção. Apesar de existirem fungicidasregistrados para o controle destas doenças no milho (Zea mays), ainda há dúvidas de quais fungicidas e emquais épocas aplicar o produto para uma maior eficiência no controle. Objetivou-se neste trabalho avaliar odesempenho de três fungicidas (piraclostrobina + epoxiconazol a 0,75 L p.c. ha-1, trifloxistrobina +protioconazol a 1,00 L p.c. ha-1e carbendazim + tebuconazol + cresoxim-metílico a 0,5 L p.c. ha-1, além deuma testemunha) no controle da helmintosporiose. Os fungicidas foram aplicados em quatro estádiosfenológicos da cultura do milho pipoca: V8, VT, R2 e em V8 e R2, totalizando 16 tratamentos, com seisrepetições. O ensaio foi realizado no ano agrícola 2012/2013 no Campus da Faculdade Integrado de CampoMourão-PR. Utilizou-se o delineamento em faixa com parcelas subdivididas. Neste ensaio foram avaliadas:a área abaixo da curva de progresso da doença (AACPD), altura de plantas e de inserção de espiga, númerode fileiras de grãos e número de grãos na fileira, produção por planta e capacidade de expansão. Verificouseuma tendência de menor AACPD com os tratamentos fungicidas piraclostrobina + epoxiconazol paratodas as épocas de aplicação comparadas aos demais tratamentos avaliados. Porém, as menores AACPDforam observadas com a aplicação dos fungicidas piraclostrobina + epoxiconazol e carbendazim +tebuconazol + cresoxim-metílico aplicados em V8 e R2.(AU)