Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 13.011
Filtrar
1.
Parasitol Res ; 121(1): 453-460, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34993633

RESUMO

Pebrine disease is caused by microporidia (Nosema bombycis) and is destructive to sericulture production. A carbendazim-based drug FangWeiLing (FWL) has a significant control effect on the disease, which is a successful example of drug treatment of microsporidia. In this study, the therapeutic effect and critical action time of FWL were investigated by silkworm rearing biological test. Besides, the hemolymph samples from silkworms in the control group, model group, and FWL group were analyzed by metabonomics based on gas chromatography-mass spectrometry (GC/MS). The results showed that FWL had a significant therapeutic effect on pebrine disease, and the critical action time was 24 ~ 48 h post inoculation. Forty-seven different metabolites related to pebrine disease were screened out, and correlated with starch and sucrose metabolism; aminoacyl-tRNA biosynthesis; arginine biosynthesis; glycine, serine, and threonine metabolism; and phenylalanine, tyrosine, and tryptophan biosynthesis. After pretreatment with FWL, the metabolites were all effectively regulated, indicating productive intervention. Principal component analysis (PCA) also showed that the overall metabolic profile of the FWL group tended toward the control group. Compared with the control group, 16 different metabolites were obtained from the hemolymph of B.mori in FWL group, mainly involving aminoacyl-tRNA biosynthesis and taurine and hypotaurine metabolism. It indicated that FWL had some effect on silkworm metabolism, which might be related to the decrease in cocoon quality. In conclusion, combined with the life cycle of N. bombycis, the mechanism of carbendazim in the treatment of pebrine disease can be fully revealed. Carbendazim can effectively reduce the destruction of amino acid metabolism and carbohydrate metabolism by N. Bombycis infection by inhibiting the proliferation of the meronts in silkworms, thus maintaining the normal physiological state of B. mori and achieve therapeutic effects. GC/MS-based metabonomics is a valuable and promising strategy to understand the disease mechanism and drug treatment of pebrine disease.


Assuntos
Bombyx , Microsporidiose , Nosema , Animais , Benzimidazóis , Carbamatos , Cromatografia Gasosa-Espectrometria de Massas , Metabolômica
2.
Arch Microbiol ; 204(1): 117, 2022 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-34985559

RESUMO

The present study was designed to screen the Mesorhizobium strains (50) for tolerance with four recommended pesticides in chickpea. In-vitro, robust pesticide tolerant strains were developed in pesticides amended media over several generations. Further, verification of the multifunctional traits of pesticide tolerant mesorhizobia under pesticide stress was conducted in-vitro. Among different pesticides, significantly high tolerance in Mesorhizobium strains was observed with recommended doses of pendimethalin (37%) and ready-mix (36%) followed by chlorpyrifos (31%) and carbendazim (30%), on an overall basis. Based on multifunctional traits, Mesorhizobium strains viz. MR2, MR17 and recommended MR33 were the most promising. Ecological performance of the potential Mesorhizobium strains alone and in dual-inoculation with recommended PGP rhizobacterium strain RB-1 (Pseudomonas argenttinensis JX239745.1) was subsequently analyzed in field following standard pesticide application in PBG-7 and GPF-2 chickpea varieties for two consecutive rabi seasons (2015 and 2016). Dual-inoculant treatments; recommended RB-1 + MR33 (4.1%) and RB-1 + MR2 (3.8%) significantly increased the grain yield over Mesorhizobium alone treatments viz MR33 and MR2, respectively. Grain yield in PBG7 variety was significantly affected (7.3%) by the microbial inoculant treatments over GPF2 variety. Therefore, the potential pesticide tolerant strains MR2 and MR33 can be further explored as compatible dual-inoculants with recommended RB-1 for chickpea under environmentally stressed conditions (pesticide application) at multiple locations. Our approach using robust multifunctional pesticide tolerant Mesorhizobium for bio-augmentation of chickpea might be helpful in the formulation of effective bio-inoculants consortia in establishing successful chickpea-Mesorhizobium symbiosis.


Assuntos
Clorpirifos , Cicer , Mesorhizobium , Praguicidas , Compostos de Anilina , Benzimidazóis , Carbamatos , Simbiose
3.
Food Chem ; 368: 130742, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34416485

RESUMO

Carbendazim (CBZ) is a fungicide employed in grape crop disease controls, and its maximum residue limit in food is regulated by specialized agencies. This study aimed to determine the CBZ content in the grape juices in a semi-quantitative classification model based on portable Ultraviolet-Visible spectroscopy and partial least squares with discriminant analysis. The sensitivity and specificity of the obtained model ranged from 83 to 100%, with the external validation set. These results are therefore promising for industrial application, and the model presents robustness for the evaluation of grape juices produced from a different grape variety. The VIP scores allowed identifying important variables involved in class modeling. This study suggests a methodology that is fast and demands minimal sample preparation (only dilution), besides being less expensive compared to the traditional methods, free of reagent/solvent, contributing to quality control in the juice industry.


Assuntos
Vitis , Benzimidazóis , Carbamatos , Sucos de Frutas e Vegetais , Análise dos Mínimos Quadrados
4.
Gut ; 71(1): 176-184, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-33408122

RESUMO

OBJECTIVE: Data regarding the real-world effectiveness and safety of sofosbuvir/velpatasvir (SOF/VEL) with or without low-dose ribavirin (RBV) in patients with chronic hepatitis C virus (HCV) infection and severe renal impairment (RI) are limited. We evaluated the performance of SOF/VEL with or without low-dose RBV in HCV-infected patients with chronic kidney disease stage 4 or 5. DESIGN: 191 patients with compensated (n=181) and decompensated (n=10) liver diseases receiving SOF/VEL (400/100 mg/day) alone and SOF/VEL with low-dose RBV (200 mg/day) for 12 weeks were retrospectively recruited at 15 academic centres in Taiwan. The effectiveness was determined by sustained virological response at off-treatment week 12 (SVR12) in evaluable (EP) and per-protocol populations (PP). The safety profiles were assessed. RESULTS: The SVR12 rates by EP and PP analyses were 94.8% (95% CI 90.6% to 97.1%) and 100% (95% CI 97.9% to 100%). In patients with compensated liver disease, the SVR12 rates were 95.0% and 100% by EP and PP analyses. In patients with decompensated liver disease, the SVR12 rates were 90.0% and 100% by EP and PP analyses. Ten patients who failed to achieve SVR12 were attributed to non-virological failures. Among the 20 serious adverse events (AEs), none were judged related to SOF/VEL or RBV. The AEs occurring in ≥10% included fatigue (14.7%), headache (14.1%), nausea (12.6%), insomnia (12.0%) and pruritus (10.5%). None had ≥grade 3 total bilirubin or alanine aminotransferase elevations. CONCLUSION: SOF/VEL with or without low-dose RBV is effective and well-tolerated in HCV-infected patients with severe RI.


Assuntos
Antivirais/uso terapêutico , Carbamatos/uso terapêutico , Hepatite C Crônica/tratamento farmacológico , Compostos Heterocíclicos de 4 ou mais Anéis/uso terapêutico , Insuficiência Renal Crônica/complicações , Ribavirina/uso terapêutico , Sofosbuvir/uso terapêutico , Adulto , Idoso , Idoso de 80 Anos ou mais , Combinação de Medicamentos , Quimioterapia Combinada , Feminino , Hepatite C Crônica/complicações , Humanos , Masculino , Pessoa de Meia-Idade , Insuficiência Renal Crônica/classificação , Estudos Retrospectivos , Resposta Viral Sustentada , Adulto Jovem
5.
Food Chem ; 374: 131761, 2022 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-34896946

RESUMO

A rapid, selective, and sensitive method was developed for the detection of carbendazim and thiabendazole in edible vegetable oil. Two benzimidazole analytes were pre-concentrated by magnetic solid phase extraction (MSPE) using flowerlike Ni-NiO composite as sorbents and followed by LC-MS/MS analysis. The flowerlike Ni-NiO composite sorbent displayed a high affinity towards benzimidazole analytes due to the reversible coordination interaction between the Ni(Ⅱ) ion and the electron-donating imidazole group. In comparison to the previous methods, this procedure is less time-consuming and simpler during sample preparation. The parameters affecting the extraction efficiency were optimized in detail. The method was validated according to SANTE/12682/2019. The limits of detection were in the range of 0.001-0.003 mg•kg-1. The recoveries ranged from 89.3% to 110.7% with inter-day and inter-day precision less than 10.9%. The results indicate that flowerlike Ni-NiO composite might be a promising alternative for MSPE of benzimidazole compounds in foods.


Assuntos
Tiabendazol , Verduras , Benzimidazóis/análise , Carbamatos , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Fenômenos Magnéticos , Óleos Vegetais , Extração em Fase Sólida , Espectrometria de Massas em Tandem
6.
Pestic Biochem Physiol ; 180: 104984, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34955177

RESUMO

The predatory mite Neoseiulus californicus McGregor (Acari: Phytoseiidae) is an important natural enemy of phytophagous mites, and naturally established populations are often found in apple orchards. However, insecticide applications to control pests cause side effects to non-target organisms such as N. californicus. Pirimicarb, a widely used carbamate insecticide in apple orchards, is generally considered a selective aphidicide, however, toxicity to beneficial insects and predatory mites has been reported. Furthermore, the molecular basis for this selectivity, if present in N. californicus, is still largely unknown. In this study, 8 field-collected N. californicus populations were investigated and showed up to 27-fold resistance compared to a susceptible laboratory population. Selection in the laboratory for 5 consecutive generations resulted in a 69-fold pirimicarb resistance. Although there were no significant difference in terms of the acetlycholinesterase (AChE) activity between susceptible and field-collected populations, the selected population exhibited a significantly higher AChE activity. In addition, gene copy number variation of acetylcholinesterase (ace) gene among populations was detected and ranged from 1.6 to 2.1-fold relative to the susceptible population. All field-collected populations, but not the selected population, had a significantly higher ace copy number compared to the susceptible population (t-test, p < 0.05). Molecular analysis of the target-site (AChE) revealed, for the first time, a phenylalanine to tryptophan substition at position 331 in AChE (Torpedo californica numbering), both in field-collected and the selected population, but not in the susceptible population. Last, the selected F5 population consumed significantly more Tetranychusurticae adults than the parental population. Together, the results of this study shed light on the molecular determinants of acaricide selectivity in predatory mites, and will contribute to a better design of an integrated mite management program, including the use of pesticide resistant N. californicus in apple orchards.


Assuntos
Carbamatos , Resistência a Inseticidas , Ácaros , Pirimidinas , Tetranychidae , Acetilcolinesterase/genética , Animais , Variações do Número de Cópias de DNA , Inseticidas , Controle Biológico de Vetores
7.
Spectrochim Acta A Mol Biomol Spectrosc ; 264: 120188, 2022 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-34358782

RESUMO

Toxicity is one of the most important factors limiting the success of new drug development. In this paper, we built a fast and convenient new method (Carrier protein binding information-toxicity relationship, CPBITR) for predicting drug acute toxicity based on the perspective of binding information with carrier protein. First, we studied the binding information between carbamate pesticides and human serum albumin (HSA) through various spectroscopic methods and molecular docking. Then a total of 16 models were established to clarify the relationship between binding information with HSA and drug toxicity. The results showed that the binding information was related to toxicity. Finally we obtained the effective toxicity prediction model for carbamate pesticides. And the "Platform for Predicting Drug Toxicity Based on the Information of Binding with Carrier Protein" was established with the Back-propagation neural network model. We proposed and proved that it was feasible to predict drug toxicity from this new perspective: binding with carrier protein. According to this new perspective, toxicity prediction model of other drugs can also be established. This new method has the advantages of convenience and fast, and can be used to screen out low-toxic drugs quickly in the early stage. It is helpful for drug research and development.


Assuntos
Proteínas de Transporte , Praguicidas , Sítios de Ligação , Carbamatos/toxicidade , Humanos , Simulação de Acoplamento Molecular , Praguicidas/toxicidade , Ligação Proteica , Espectrometria de Fluorescência
8.
J Oncol Pharm Pract ; 28(1): 199-202, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34581610

RESUMO

Recently, the introduction of encorafenib in combination with cetuximab was considered as a practice changing in BRAFV600-mutated metastatic colorectal cancer. The aim of this paper was to assess the cost-effectiveness of encorafenib plus cetuximab in the second-line treatment of BRAFV600-mutated metastatic colorectal cancer. BEACON CRC Trail was considered. Incremental cost-effectiveness ratio was calculated as the ratio between the difference of the costs in the intervention and in the control groups (pharmacy costs) and the difference between the effect in the intervention and in the control groups (overall survival). Four hundred forty-one patients were included. Differences in costs between the two arms (encorafenib plus cetuximab vs FOLFIRI plus cetuximab) was 59 501 €, with a cost of 17 500 € per month of overall survival-gain. Combining pharmacological costs of drugs with the measure of efficacy represented by overall survival, at the actual prize encorafenib cannot be considered cost-effectiveness for second-line treatment of BRAFV600-mutated metastatic colorectal cancer.


Assuntos
Neoplasias Colorretais , Proteínas Proto-Oncogênicas B-raf , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Carbamatos , Cetuximab/uso terapêutico , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/genética , Análise Custo-Benefício , Humanos , Mutação , Proteínas Proto-Oncogênicas B-raf/genética , Sulfonamidas
9.
Spectrochim Acta A Mol Biomol Spectrosc ; 267(Pt 1): 120536, 2022 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-34739999

RESUMO

Velpatasvir and sofosbuvir are new drugs prescribed in a combined pharmaceutical dosage form that pose a new challenge for the treatment of chronic hepatitis C. In this work, a comparative evaluation of the classical mathematical model, simultaneous equations, and the advanced mathematical model, partial least squares, for the spectrophotometric quantitative analysis of velpatasvir and sofosbuvir in bulk powder and in the new combined pharmaceutical dosage form was presented. The mathematical simultaneous equation method was used to resolve the overlap between velpatasvir and sofosbuvir. The absorbance and absorbativity values at 255 and 244.8 were used to construct two mathematical equations required for spectrophotometric quantitative analysis of the drugs under study. Partial least squares, an advanced mathematical tool dealing with the full spectral data of velpatasvir and sofosbuvir, was also introduced. An experimental design for the calibration sets and validation sets for the binary mixture of the drugs under study were created. The model was optimized based on a five-level, two-factor experimental design. Pre-processing of the spectral data was applied and resulted in the exclusion of the spectral region from 200 to 230 nm due to noise. The described methods were successfully applied to the spectrophotometric quantitative analysis of velpatasvir and sofosbuvir in Epclusa® tablets.


Assuntos
Compostos Heterocíclicos de 4 ou mais Anéis , Sofosbuvir , Antivirais , Carbamatos , Análise dos Mínimos Quadrados , Modelos Teóricos , Espectrofotometria
10.
Food Chem ; 372: 131267, 2022 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-34638065

RESUMO

In this study, reduced graphene oxide (rGO) was prepared using a green ultrasonic microwave assisted method and investigated rGO based non-enzymatic electrochemical sensor for detecting a synthetic fungicide as a propamocarb (PM) pesticide. The rGO-based sensor exhibited rapid response within 1 min, low detection limit of 0.6 µM and wide linear range of (1-5) µM with a high sensitivity of 101.1 µAµM-1 cm-2 for PM. Besides this, the sensor detected the propamocarb pesticide on the real cucumber sample with high sensitivity in the concentration range of (1-5) µM within a 1-minute cycle. The sensor is highly selective against propamocarb pesticide. The prepared non-enzymatic electrochemical sensor exhibited high sensitivity, high selectivity, reproducibility, and rapid response.


Assuntos
Fungicidas Industriais , Grafite , Praguicidas , Carbamatos , Técnicas Eletroquímicas , Eletrodos , Reprodutibilidade dos Testes
11.
Food Chem ; 370: 131360, 2022 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-34662796

RESUMO

A novel deep eutectic solvent-based extraction and sulfur-doped carbon quantum dots (S-CQDs) serving as fluorescence probes to detect pirimicarb in cereals were established. The deep eutectic solvent was synthesized using choline chloride and butanediol, achieving direct and efficient extraction of pirimicarb residue in the cereals. The fluorescence quenching of S-CQDs was caused by the electrostatic interaction between the negatively charged S-CQDs and positively charged thiocholine, which was the hydrolysate of acetylthiocholine. The fluorescence of S-CQDs was enhanced as the activity of acetylcholinesterase (AChE) was inhibited by pirimicarb, achieving the detection of pirimicarb in the cereal samples. The limit of detection (LOD) was 0.006 µg mL-1. The recovery ranged from 96.6% to 108.2%. This extraction and detection method of pirimicarb based on an environmentally friendly DES and S-CQD fluorescent sensor maintains good stability and convenience, offering a promising strategy for extracting and testing harmful substances in food samples.


Assuntos
Grão Comestível , Pontos Quânticos , Acetilcolinesterase , Carbamatos , Pirimidinas , Solventes
12.
Talanta ; 237: 122909, 2022 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-34736646

RESUMO

In this work, we propose a two-step coating method, combining C-ZIF67@Ni with molecular imprinting polymer (MIP), to develop a high-sensitivity and high-selectivity Carbendazim (CBD) electrochemical sensor. ZIF67@Ni was prepared by a simple chemical bath method, and C-ZIF67@Ni was obtained by high-temperature carbonization of ZIF67@Ni. Then, MIP layer was prepared by electrochemical in-situ polymerization, with O-aminophenol as functional monomers, CBD acting as template on the surface of the C-ZIF67@Ni-modified glassy carbon electrode (GCE). During the preparation process, the types of functional monomers, the polymerization solution pH, the ratio of functional monomers to template molecules, and the incubation time are optimized. The morphological characteristics, composition information and electrochemical properties of MIP/C-ZIF67@Ni/GCE were investigated in detail under optimal conditions. Physical characterization and electrochemical tests revealed that ZIF67@Ni significantly improves the electron transmission capacity and surface area of the sensor after high-temperature carbonization. C-ZIF67@ Ni has a good synergistic effect on MIP, allowing rapid and specific identification of the test substance. MIP/C-ZIF67@Ni/GCE showed a good linear relationship with CBD in the concentration range from 4 × 10-13 M to 1 × 10-9 M, the lowest detection limit was 1.35 × 10-13 M (S/N = 3) R2 = 0.9983 and RSD = 2.34. Additionally, the sensor showed good repeatability, stability, and selectivity, and can be used for the detection of carbendazim in soil and water with a recovery of 98% above.


Assuntos
Técnicas Biossensoriais , Impressão Molecular , Benzimidazóis , Carbamatos , Técnicas Eletroquímicas , Eletrodos , Limite de Detecção , Polímeros Molecularmente Impressos
13.
Food Chem ; 370: 131284, 2022 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-34788953

RESUMO

Propamocarb is a carbamate fungicide used to control Phytophthora disease. Frequent and large-scale use of propamocarb means that it poses a potential threat to the health of consumers. Monoclonal antibodies against propamocarb were prepared using a hapten of propamocarb that was generated by introducing a benzene ring and a carboxyl group into the structure of propamocarb. A lateral flow immunoassay strip was developed for the detection of propamocarb in tomato and cucumber samples using the gold nanoparticle-labeled antibody. The immunoassay strip was found to provide a visible limit of detection was 5 ng/g and the cut-off value was 250 ng/g for propamocarb in food samples. For quantitative analysis, the calculated limits of detection (LODs) of the immunoassay strip were 1.43 ng/g and 0.44 ng/g in cucumber and tomato, respectively. Using the immunoassay strip, the average recoveries ranged from 95.5 ± 5.4% to 108.8 ± 6.8%, with CVs of 3.1-6.2% for the cucumber, and the average recoveries were 95.1 ± 6.5%-111.9 ± 4.2%, with CVs ranging from 3.7% to 6.8% for tomato samples. All the results demonstrated that the immunoassay strip was suitable for the detection of propamocarb in fruits and vegetables.


Assuntos
Ouro , Nanopartículas Metálicas , Anticorpos Monoclonais , Carbamatos , Imunoensaio , Limite de Detecção
14.
Cells ; 10(12)2021 12 08.
Artigo em Inglês | MEDLINE | ID: mdl-34943962

RESUMO

Modulation of the endocannabinoid system has emerged as an effective approach for the treatment of many neurodegenerative and neuropsychological diseases. However, the underlying mechanisms are still uncertain. Using a repetitive mild traumatic brain injury (mTBI) mouse model, we found that there was an impairment in locomotor function and working memory within two weeks post-injury, and that treatment with MJN110, a novel inhibitor of the principal 2-arachidononyl glycerol (2-AG) hydrolytic enzyme monoacylglycerol lipase dose-dependently ameliorated those behavioral changes. Spatial learning and memory deficits examined by Morris water maze between three and four weeks post-TBI were also reversed in the drug treated animals. Administration of MJN110 selectively elevated the levels of 2-AG and reduced the production of arachidonic acid (AA) and prostaglandin E2 (PGE2) in the TBI mouse brain. The increased production of proinflammatory cytokines, accumulation of astrocytes and microglia in the TBI mouse ipsilateral cerebral cortex and hippocampus were significantly reduced by MJN110 treatment. Neuronal cell death was also attenuated in the drug treated animals. MJN110 treatment normalized the expression of the NMDA receptor subunits NR2A and NR2B, the AMPA receptor subunits GluR1 and GluR2, and the GABAA receptor subunits α1, ß2,3 and γ2, which were all reduced at 1, 2 and 4 weeks post-injury. The reduced inflammatory response and restored glutamate and GABA receptor expression likely contribute to the improved motor function, learning and memory in the MJN110 treated animals. The therapeutic effects of MJN110 were partially mediated by activation of CB1 and CB2 cannabinoid receptors and were eliminated when it was co-administered with DO34, a novel inhibitor of the 2-AG biosynthetic enzymes. Our results suggest that augmentation of the endogenous levels of 2-AG can be therapeutically useful in the treatment of TBI by suppressing neuroinflammation and maintaining the balance between excitatory and inhibitory neurotransmission.


Assuntos
Lesões Encefálicas Traumáticas/tratamento farmacológico , Carbamatos/farmacologia , Monoacilglicerol Lipases/genética , Succinimidas/farmacologia , Animais , Comportamento Animal/efeitos dos fármacos , Lesões Encefálicas Traumáticas/genética , Lesões Encefálicas Traumáticas/patologia , Modelos Animais de Doenças , Endocanabinoides/genética , Endocanabinoides/metabolismo , Inibidores Enzimáticos/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Camundongos , /patologia , Neurônios/efeitos dos fármacos , Receptores de AMPA/genética , Receptores de N-Metil-D-Aspartato/genética , Sinapses/efeitos dos fármacos , Sinapses/genética
15.
Zhonghua Gan Zang Bing Za Zhi ; 29(11): 1046-1052, 2021 Nov 20.
Artigo em Chinês | MEDLINE | ID: mdl-34933421

RESUMO

Objective: To study the real-world outcome of China FDA-approved Sofosbuvir (SOF)/Velpatasvir (VEL) in Northwest China. Methods: In this multicenter, prospective, real-world cohort study, we recruited patients from 10 sites from Northwest China, who were chronically infected with HCV GTs 1-6 from 06/2018 to 09/2019. Patients received SOF (400mg)/VEL (100mg) for 12 weeks, and with ribavirin 900-1200 mg for GT3 cirrhosis and for any genotype decompensated cirrhosis. The primary endpoint was sustained virological response at 12-weeks post-treatment (SVR12) and safety. The secondary endpoint was the change of liver function after the achievement of SVR12. Results: Totally, 143 patients were enrolled in the study, four patients were lost to follow-up and one died during the follow-up, 138 patients were included in per-protocol analysis. Of the 138 patients, the mean age 53 years, 53.6% male, 94.2% Han nationality, 53.6% liver cirrhosis, 10.1% HBsAg(+), 6.5% renal dysfunction, 5.1% treatment-experienced, and 16.7% patients received ribavirin treatment. The genotype distribution was as follows: 35.5% GT1, 42.8% GT2, 15.9% GT3, and 5.8% un-typed. The SVR12 rate was 96.5% (138/143, 95%CI: 93.5%-99.6%) for intention-to-treat analysis, and in per-protocol analysis, all 138 patients obtained SVR12 (100%). Compared with baseline, the serum total bilirubin, ALT and AFP levels decreased (all P < 0.05), as well as increased ALB and platelet count (all P < 0.001) at post-treatment 12-weeks. Overall adverse events (AEs) rate is 29.0%, and the most common AEs were anemia (14.5%) and fatigue (8.0%). Severe side effects (edema and fatigue) occurred in 2 patients, one of whom needed a short-term interruption of treatment due to fatigue. Conclusion: In this real-world cohort study, 12-week SOF/VEL regimen with or without ribavirin achieved high SVR12 rates (96.5%-100% overall) with excellent safety profile among patients with HCV GT1/2/3 infection including patients with GT3 and cirrhosis, and led to improvement of liver function.


Assuntos
Hepatite C Crônica , Sofosbuvir , Antivirais/uso terapêutico , Carbamatos , Estudos de Coortes , Quimioterapia Combinada , Feminino , Genótipo , Hepacivirus/genética , Hepatite C Crônica/tratamento farmacológico , Compostos Heterocíclicos de 4 ou mais Anéis , Humanos , Cirrose Hepática/tratamento farmacológico , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Ribavirina/uso terapêutico , Sofosbuvir/uso terapêutico , Resultado do Tratamento
16.
Environ Monit Assess ; 194(1): 23, 2021 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-34904192

RESUMO

Activities like agriculture contribute to the pollution of aquatic systems by fungicides, such as benomyl/carbendazim. This chemical inhibits the activity of acetylcholinesterase (AChE), having teratogenic, oncogenic, reproductive, and hepatic effects on aquatic and soil organisms. This paper presents the results of a study conducted in the Tenango dam, Mexico, aimed at detecting and determining the spatial and temporal variability of benomyl/carbendazim fungicide in the dam's water and its possible impact on Nile tilapia (Oreochromis niloticus), farmed and commercialized in the site. Five site visits were made during 2015. Benomyl/carbendazim was quantified at 34 georeferenced stations. Thirty O. niloticus specimens were collected per visit. The quality of water and O. niloticus specimens was evaluated according to the Mexican standards. The fungicide concentrations in the O. niloticus muscle and the AChE activity were measured. Seasonal and spatial variations of benomyl/carbendazim were determined using geostatistical methods (ordinary kriging [OK] and universal kriging [UK]). Geostatistical analyses demonstrated that agriculture contributes to the increased amounts of the chemical in specific areas. Even though the fungicide levels in water varied over time, they did not represent a risk to O. niloticus according to the current standards. The specimens met the quality criteria for their commercialization; however, they had low weights and small sizes. The benomyl/carbendazim concentration in the muscle increased with the size and exhibited a negative correlation with the AChE activity, thus indicating a potential harmful effect.


Assuntos
Benomilo , Ciclídeos , Acetilcolinesterase , Animais , Benzimidazóis , Carbamatos , Monitoramento Ambiental , México , Análise Espacial , Água
17.
Pharm Nanotechnol ; 9(5): 326-338, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34939558

RESUMO

Repaglinide is an antidiabetic drug that works by stimulating insulin secretion from pancreatic beta cells. Repaglinide is practically insoluble in water with a water solubility of 34 µg/mL at 37°C, and it has a high absorption rate from the gastrointestinal tract following oral administration since the log P value of repaglinide is 3.97. The low aqueous solubility and the high permeability of repaglinide represent a typical behavior for drugs that belong to class II Biopharmaceutical Classification System (BCS II). Managing type-2 diabetes mellitus with repaglinide is considered a burdensome therapy, as it requires frequent dosing of repaglinide before each meal to maintain its therapeutic plasma concentration due to its short plasma half-life of approximately one hour. Hence the present review aims to discuss thoroughly the various approaches investigated in recent years to develop drug delivery systems that improve oral delivery of repaglinide, including nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, sustained-release hydrophilic matrix, floating microspheres, and nanocomposites.


Assuntos
Carbamatos , Sistemas de Liberação de Medicamentos , Preparações de Ação Retardada , Lipossomos , Nanopartículas , Piperidinas
18.
Se Pu ; 39(12): 1324-1330, 2021 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-34812004

RESUMO

Carbamate pesticides are a class of synthetic pesticides having wide antimicrobial spectrum, good insecticidal efficacy, and a short residual period. These pesticides are used in agriculture, forestry, and animal husbandry. Their widespread use in the last two decades has led to the existence of drug residues in the environment, which are transferred to food, thereby raising concerns regarding the potential threat to human health. Rapid and accurate detection of carbamate pesticide residues in food is of great significance for food safety, and this requires pretreatment to purify the target components and maximize the accuracy and precision of the analysis. A rapid and accurate analytical method based on online solid phase extraction/purification-high performance liquid chromatography-tandem mass spectrometry (online SPE-HPLC-MS/MS) was established for the determination of eight carbamate pesticides in tomato, rice, and cabbage. About 5.0 g of tomato (without water), 2.0 g of cabbage, and 2.0 g of rice (mixed with 3 mL of water) were vortexed at 1000 r/min for 1 min. After adding 2 g of sodium chloride and 10 mL of acetonitrile containing 0.5% (v/v) formic acid, the samples were extracted and centrifuged. The supernatants were combined after the samples were extracted again. The reconstituted solutions were then purified on a CAPCELL PAK C18 column (50 mm×2.0 mm, 15 µm). When the volume ratio of 0.1% (v/v) formic acid aqueous solution and acetonitrile (used as the mobile phases) was 90∶10 and 35∶65, the eight carbamate pesticides could be completely adsorbed and eluted. The carbamate pesticides were separated on an ACQUITY UPLC CSH C18 column (100 mm×2.1 mm, 1.7 µm) under gradient elution and analyzed in the multiple reaction monitoring (MRM) mode with positive electrospray ionization (ESI+). Under the optimum conditions, the calibration curves of the eight carbamate pesticide residues showed good linearity (r>0.995) within their respective linear ranges. The limits of quantification (LOQs) and limits of detection (LODs) were in the range of 0.05-1.0 ng/mL (S/N=10) and 0.01-0.3 ng/mL (S/N=3). The recoveries were in the range of 73.76%-112.32% at three spiked levels (2, 10, and 20 ng/mL), with relative standard deviations of 1.28%-13.14% (n=6). The online purification method showed better enrichment and purification ability for the target substances than did the offline purification method and greatly improved the pretreatment efficiency. The loading and purification could be completed within 12 min. The developed method has the advantages of high recovery rate, good reproducibility, accuracy, rapidness, sensitivity, and environment friendliness. It can be used for the determination of the eight carbamate pesticides in plant foods, such as tomato, rice, and cabbage.


Assuntos
Brassica , Lycopersicon esculentum , Oryza , Resíduos de Praguicidas , Animais , Carbamatos , Cromatografia Líquida de Alta Pressão , Contaminação de Alimentos/análise , Humanos , Resíduos de Praguicidas/análise , Reprodutibilidade dos Testes , Extração em Fase Sólida , Espectrometria de Massas em Tandem
19.
Pestic Biochem Physiol ; 179: 104975, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34802525

RESUMO

Pesticides are one of the main causes of colony losses globally, posing a huge threat to the beekeeping industry. The fungicide carbendazim is commonly used on many crops worldwide, but the effects of fungicides on honey bees have received less attention than those of insecticides. Previous studies have shown that sublethal doses of carbendazim hinder growth and development and may destabilize and impede the development of honey bee colonies. The metabolome closely reflects brain activity at the functional level, allowing the effects of compounds such as fungicides to be investigated. Here, we established a model of carbendazim-treated honey bees, Apis mellifera, and used metabolomic approaches to better understand the effect of carbendazim on bee metabolic profiles. The results showed that 112 metabolites were significantly affected in carbendazim-treated bees compared to the control. Metabolites associated with energy and amino acid metabolism showed high abundance and were enriched for a wide range of pathways. In addition, the down-regulation of Aflatoxin B1exo-8,9-epoxide-GSH and glycerol diphosphate showed that carbenazim may affect the detoxification and immune system of honey bees. These results provide new insights into the interaction between fungicides and honey bees.


Assuntos
Inseticidas , Espectrometria de Massas em Tandem , Animais , Abelhas , Benzimidazóis , Carbamatos/toxicidade , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Inseticidas/toxicidade
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...