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1.
Arch Environ Contam Toxicol ; 82(4): 569-580, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35460350

RESUMO

The fungicide fludioxonil, given its physicochemical properties, potentially accumulates and persists in sediments. Fludioxonil has a widespread agricultural use to control various fungal diseases. Its residues may cause toxic effects to benthic aquatic fauna, thereby impacting ecosystem service functions of aquatic ecosystems. To assess the potential environmental effects of fludioxonil in the sediment compartment of edge-of-field surface waters, sediment-spiked single-species toxicity tests with benthic macroinvertebrates were performed. In all experiments artificial sediment was used with an organic carbon content of 2.43% on dry weight basis. The single-species tests were conducted with 8 benthic macroinvertebrates covering different taxonomic groups typical for the Yangtze River Delta, China. The 28d-EC10 and 28-LC10 values thus obtained were used to construct species sensitivity distributions (SSDs). In addition, our dataset was supplemented with 28d-EC10 and 28-LC10 values for 8 different benthic invertebrates from a study in the Netherlands that used field-collected sediment. Based on SSDs constructed with 28d-EC10 or 28d-LC10 values hazardous concentrations to 5% of the species tested (HC5's) were obtained. The HC5 values based on the toxicity tests from China were lower than those from the Netherlands, although 95% confidence bands overlapped. The HC5 values derived from the separate datasets from China and the Netherlands, as well as from the combined dataset, were compared to the Tier-3 Regulatory Acceptable Concentrations (RAC) for fludioxonil and the benthic invertebrate community derived from a sediment-spiked outdoor microcosm experiment conducted in the Netherlands. The HC5 values obtained appeared to be lower than this Tier-3 RAC when expressed in terms of total sediment concentration, but not always when expressed in terms of pore water concentrations.


Assuntos
Sedimentos Geológicos , Poluentes Químicos da Água , Animais , Dioxóis , Ecossistema , Sedimentos Geológicos/química , Invertebrados , Pirróis , Testes de Toxicidade , Poluentes Químicos da Água/análise , Poluentes Químicos da Água/toxicidade
2.
J Cell Mol Med ; 24(2): 1332-1344, 2020 01.
Artigo em Inglês | MEDLINE | ID: mdl-31811750

RESUMO

Fuziline, an aminoalcohol-diterpenoid alkaloid derived from Aconiti lateralis radix preparata, has been reported to have a cardioprotective activity in vitro. However, the potential mechanism of fuziline on myocardial protection remains unknown. In this study, we aimed to explore the efficacy and mechanism of fuziline on isoproterenol (ISO)-induced myocardial injury in vitro and in vivo. As a result, fuziline effectively increased cell viability and alleviated ISO-induced apoptosis. Meanwhile, fuziline significantly decreased the production of ROS, maintained mitochondrial membrane potential (MMP) and blocked the release of cytochrome C, suggesting that fuziline could play the cardioprotective role through restoring the mitochondrial function. Fuziline also could suppress ISO-induced endoplasmic reticulum (ER) stress via the PERK/eIF2α/ATF4/Chop pathway. In addition, using ROS scavenger NAC could decrease ISO-induced apoptosis and block ISO-induced ER stress, while PERK inhibitor GSK2606414 did not reduce the production of ROS, indicating that excess production of ROS induced by ISO triggered ER stress. And fuziline protected against ISO-induced myocardial injury by inhibiting ROS-triggered ER stress. Furthermore, fuziline effectively improved cardiac function on ISO-induced myocardial injury in rats. Western blot analysis also showed that fuziline reduced ER stress-induced apoptosis in vivo. Above these results demonstrated that fuziline could reduce ISO-induced myocardial injury in vitro and in vivo by inhibiting ROS-triggered ER stress via the PERK/eIF2α/ATF4/Chop pathway.


Assuntos
Alcaloides/farmacologia , Diterpenos/farmacologia , Estresse do Retículo Endoplasmático , Regulação da Expressão Gênica/efeitos dos fármacos , Isoproterenol/toxicidade , Traumatismo por Reperfusão Miocárdica/tratamento farmacológico , Espécies Reativas de Oxigênio/metabolismo , Aconitum/química , Fator 4 Ativador da Transcrição/genética , Fator 4 Ativador da Transcrição/metabolismo , Agonistas Adrenérgicos beta/toxicidade , Animais , Apoptose , Masculino , Traumatismo por Reperfusão Miocárdica/induzido quimicamente , Traumatismo por Reperfusão Miocárdica/metabolismo , Traumatismo por Reperfusão Miocárdica/patologia , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-Dawley , Transdução de Sinais , Fator de Transcrição CHOP/genética , Fator de Transcrição CHOP/metabolismo , eIF-2 Quinase/genética , eIF-2 Quinase/metabolismo
3.
Chin Med Sci J ; 35(2): 179-185, 2020 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-32684238

RESUMO

Chinese scientists have been actively engaged in biotechnology research since the mid-20th century. However, biotechnology education, especially biomedical laboratory technology education, is relatively scarce in China. More and more cutting-edge equipment and techniques have been introduced into biomedical laboratories in China, but there is a lack of high-quality technicians to apply these advancements to scientific research. In addition, the traditional education and apprenticeship systems have been demonstrated little progress. To address this gap, West China Hospital of Sichuan University established a 2-year educational program for laboratory technology in 2006 based on the residency training program. The project integrates scientific methods into the research laboratory technician training in relevant disciplines, and has developed a systematic, scientific, and effective standardized training system to cultivate high-level and stable experimental technician team for the need of advanced laboratories, which has been demonstrated greatly improve the efficiency of biomedical researchers and laboratory facilities. In this article, we introduce the practical experience in establishment and development of a standardized training system for biomedical laboratory technicians to ensure the sustainable development of medical researches.


Assuntos
Biotecnologia/educação , China , Pessoal de Laboratório/educação
4.
Acta Pharmacol Sin ; 37(8): 1020-30, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27374488

RESUMO

AIM: The continuous presence of an agonist drives its receptor into a refractory state, termed desensitization. In this study, we tested the hypothesis that a competitive antagonist, SR95531, could facilitate the recovery of α1ß2γ2 GABAA receptor from functional desensitization. METHODS: α1ß2γ2 GABAA receptors were expressed in Xenopus oocytes. GABA-evoked currents were recorded using two-electrode voltage-clamp technique. Drugs were applied through perfusion. RESULTS: Long application of GABA (100 µmol/L) evoked a large peak current followed by a small amplitude steady-state current (desensitization). Co-application of SR95531 during the desensitization caused a larger rebound of GABA current after removal of SR95531. Furthermore, application of SR95531 after removal of GABA increased the rate of receptor recovery from desensitization, and the recovery time constant was decreased from 59±3.2 s to 33±1.6 s. SR95531-facilitated receptor recovery from desensitization was dependent on the perfusion duration of SR95531. It was also dependent on the concentration of SR95531, and the curve fitting with Hill equation revealed two potency components, which were similar to the two potency components in inhibition of the steady-state current by SR95531. Bicuculline caused similar facilitation of desensitization recovery. CONCLUSION: SR95531 facilitates α1ß2γ2 GABAA receptor recovery from desensitization, possibly through two mechanisms: binding to the desensitized receptor and converting it to the non-desensitized state, and binding to the resting state receptor and preventing re-desensitization.


Assuntos
Antagonistas de Receptores de GABA-A/farmacologia , Oócitos/metabolismo , Piridazinas/farmacologia , Receptores de GABA-A/metabolismo , Animais , Bicuculina/farmacologia , Células Cultivadas , Interações Medicamentosas , Agonistas de Receptores de GABA-A/farmacologia , Potenciais da Membrana/efeitos dos fármacos , Oócitos/efeitos dos fármacos , Receptores de GABA-A/genética , Recuperação de Função Fisiológica/efeitos dos fármacos , Xenopus laevis , Ácido gama-Aminobutírico/farmacologia
5.
J Asian Nat Prod Res ; 17(1): 47-55, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25290081

RESUMO

In an attempt to discover more potential antifungal agents, in this study, 21 novel trichodermin derivatives containing conjugated oxime ester (5a-5u) were designed and synthesized and were screened for in vitro antifungal activity. The bioassay tests showed that some of them exhibited good inhibitory activity against the tested pathogenic fungi. Compound 5a exhibited better activity against Pyricularia oryzae and Sclerotonia sclerotiorum than trichodermin, and compound 5j showed particular activity against P.oryzae and Botrytis cinerea. The quantitative structure-activity relationship (QSAR) indicated that log P and hardness were two critical parameters for the biological activities. The result suggested that these would be potential lead compounds for the development of fungicides with further structure modification.


Assuntos
Antifúngicos/síntese química , Antifúngicos/farmacologia , Fungicidas Industriais/síntese química , Fungicidas Industriais/farmacologia , Oximas/síntese química , Oximas/farmacologia , Tricodermina/síntese química , Tricodermina/farmacologia , Antifúngicos/química , Botrytis/efeitos dos fármacos , Fungicidas Industriais/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Oximas/química , Relação Quantitativa Estrutura-Atividade , Tricodermina/química
6.
Bioorg Med Chem Lett ; 24(15): 3565-8, 2014 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-24908609

RESUMO

To discover more potential antifungal agents, 17 novel trichodermin derivatives were designed and synthesized by modification of 3 and 4a. The structures of all the synthesized compounds were confirmed by (1)H NMR, ESI-MS and HRMS. Their antifungal activities against Ustilaginoidea oryzae and Pyricularia oryzae were evaluated. Most of the target compounds showed potent inhibitory activity, in which 4g showed superior inhibitory effects than 4a and commercial fungicide prochloraz. Furthermore, 4h demonstrated comparable inhibitory activity to 4a. Moreover, 4i and 4l exhibited excellent inhibitory activity for Pyricularia oryzae. Additionally, compound 9 was found to be more active against all tested fungal strains than 3, with EC50 values of 0.47 and 3.71 mg L(-1), respectively.


Assuntos
Antifúngicos/farmacologia , Magnaporthe/efeitos dos fármacos , Tricodermina/farmacologia , Ustilaginales/efeitos dos fármacos , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Modelos Moleculares , Estrutura Molecular , Relação Estrutura-Atividade , Tricodermina/síntese química , Tricodermina/química
7.
J Sep Sci ; 37(9-10): 1134-40, 2014 May.
Artigo em Inglês | MEDLINE | ID: mdl-24610829

RESUMO

This study developed an improved analytical method for the simultaneous quantification of 13 quinolones in cosmetics by ultra high performance liquid chromatography combined with ESI triple quadrupole MS/MS under the multiple reaction monitoring mode. The analytes were extracted and purified by using an SPE cartridge. The limits of quantification ranged from 0.03 to 3.02 µg/kg. The precision for determining the quinolones was <19.39%. The proposed method was successfully developed for the determination of quinolones in real cosmetic samples.


Assuntos
Cosméticos/química , Quinolonas/análise , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas em Tandem
8.
Anal Biochem ; 389(1): 32-9, 2009 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-19303861

RESUMO

Using a simple test for rapid identification and quantification of pesticide multiresidues in food and environmental samples is a long-cherished approach for practical monitoring purposes. Here two gold-based lateral-flow strips (strip A and strip B) were investigated for simultaneous detection of carbofuran and triazophos. For the strip A format, a bispecific monoclonal antibody (BsMcAb) against both carbofuran and triazophos was employed to prepare the immunogold probe. For the strip B format, anti-carbofuran monoclonal antibody (McAb) and anti-triazophos McAb separately labeled with colloidal gold were combined as detector reagents. By comparison of visual results from pesticide standard tests between the two formats, the strip B assay manifested higher sensitivities for both pesticides. Analysis of spiked water samples by the preferable strip indicated that the detection limits for carbofuran and triazophos were 32 and 4 microg/L, respectively. The strength of the portable one-step strip assay was in the simultaneous screening for two pesticides within a short time (8-10 min) without any equipment.


Assuntos
Anticorpos Monoclonais/imunologia , Carbofurano/análise , Imuno-Histoquímica/métodos , Organotiofosfatos/análise , Praguicidas/análise , Triazóis/análise , Poluentes Químicos da Água/análise , Água/análise , Carbofurano/imunologia , Organotiofosfatos/imunologia , Praguicidas/imunologia , Triazóis/imunologia , Poluentes Químicos da Água/imunologia
9.
Anal Biochem ; 393(1): 88-94, 2009 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-19538934

RESUMO

A heterologous direct competitive enzyme-linked immunosorbent assay (ELISA) for parathion residue determination is described based on a monoclonal antibody and a new competitor. The effects of several physicochemical factors, such as methanol concentration, ionic strength, pH value, and sample matrix, on the performance of the ELISA were optimized for the sake of obtaining a satisfactory assay sensitivity. Results showed that when the assay medium was in the optimized condition (phosphate buffer solution [PBS] containing 10% [v/v] methanol and 0.2 mol/L NaCl at a pH value of 5.0), the sensitivity (estimated as the IC(50) value) and the limit of detection (LOD, estimated as the IC(10) value) were 1.19 and 0.08 ng/ml, respectively. The precision investigation indicated that the intraassay precision values all were below 10% and that the interassay precision values ranged from 4.89 to 19.12%. In addition, the developed ELISA showed a good linear correlation (r(2)=0.9962) to gas chromatography within the analyte's concentration range of 0.1 to 16 ng/ml. When applied to the fortified samples (parathion adding level: 5-15 microg/kg), the developed ELISA presented mean recoveries of 127.46, 122.52, 91.92, 124.01, 129.72, 99.37, and 87.17% for tomato, cucumber, banana, apple, orange, pear, and sugarcane, respectively. Results indicated that the established ELISA is a potential tool for parathion residue determination.


Assuntos
Ensaio de Imunoadsorção Enzimática/métodos , Análise de Alimentos/métodos , Inseticidas/análise , Paration/análise , Ensaio de Imunoadsorção Enzimática/instrumentação , Análise de Alimentos/instrumentação , Frutas/química , Concentração de Íons de Hidrogênio , Inseticidas/química , Metanol , Estrutura Molecular , Concentração Osmolar , Paration/química , Verduras/química
10.
Acta Crystallogr Sect E Struct Rep Online ; 65(Pt 12): o2992, 2009 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-21578732

RESUMO

In the title spiro-diclofen derivative, C(22)H(17)Cl(3)O(4), the cyclo-hexane ring adopts a chair conformation [four C atoms are planar with a mean deviation of 0.018 Šand the two C atoms at the flap positions deviate by 0.613 (4) and -0.668 (5) Šfrom the plane]. The dihedral angles between the furan ring and the two benzene rings are 55.78 (3) and 49.92 (3)°. Weak inter-molecular C-H⋯Cl inter-actions are observed in the crystal structure.

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