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1.
Fitoterapia ; 174: 105852, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38325587

RESUMO

Phytochemical studies on the leaves and twigs of Hypericum ascyron Linn. led to the isolation of two previously undescribed rearranged polycyclic polyprenylated acylphloroglucinols (PPAP) with a 4,5-seco-3(2H)-furanone skeleton, named hyperascone A and B (1-2). Additionally, a known PPAP tomoeone A (3) and two known xanthones 1,3,5 -trihydroxy-6-O-prenylxanthone (4) and 3,7-dihydroxy-1,6-dimethoxyxanthone (5) were also isolated. The structures of the compounds were determined by the analysis of their spectroscopic data including HRMS, NMR and ECD. All of the five isolated compounds exhibited neuroprotective effects against MPP+ and microglia activation induced damage of SH-SY5Y cells.


Assuntos
Hypericum , Neuroblastoma , Fármacos Neuroprotetores , Propilaminas , Humanos , Hypericum/química , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/química , Estrutura Molecular , Floroglucinol/farmacologia , Floroglucinol/química
2.
Int J Biol Macromol ; 258(Pt 2): 129007, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38151082

RESUMO

The excellent comprehensive properties of microfiber synthetic leathers have led to their wide application in various aspects of our lives. However, the issue of flammability remains a significant challenge that needs to be addressed. Nowadays, the bio-based chemicals used in the flame-retardant materials have extremely grabbed our eyes. Herein, we developed an ecologically friendly flame-retardant microfiber synthetic leather using phosphorus-free layer-by-layer assembly technology (LBL) based on natural polysaccharide alginate (SA) coupled with polyethyleneimine (PEI) and 3-aminopropyltriethoxysilane (APTES). The effect of different LBL coating systems on the flame retardancy of microfiber synthetic leather was investigated. The results demonstrated that the introduction of APTES can completely inhibit the melt-dripping by enhancing char formation through silica elements. Furthermore, the trinary coating system consisting of SA/APTES/PEI exhibited excellent flame retardancy by combining gas-phase action from PEI and condensed-phase function from APTES. This modified microfiber synthetic leather showed a significantly higher limiting oxygen index (LOI) value of 33.0 % with no molten droplet. Additionally, the SA-based coating slightly suppressed the heat release, resulting in a 20 % reduction in total heat release during the combustion test. Overall, this work presents a facile and environmentally-friendly approach for achieving flame-retardant and anti-dripping microfiber synthetic leather.


Assuntos
Alginatos , Retardadores de Chama , Propilaminas , Silanos , Epiderme , Olho , Fósforo , Polietilenoimina
3.
Poult Sci ; 101(10): 102096, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36055028

RESUMO

A series of experiments was designed and conducted to determine the apparent and standardized ileal phosphorus digestibility (i.e., AIDP and SIDP, respectively) of some grains and protein meals in Japanese quail at different age classes during the growing period from the hatch to 35 d of age. Experimental diets included a PFD, to measure basal endogenous P losses (EPL), corn, wheat, soybean meal (SBM), and corn gluten meal (CGM), so as to be each ingredient the sole source of P, were developed and fed to five experimental groups with 5 replicates of 30 chicks each. Titanium dioxide as an indigestible marker was added to the diets at the rate of 5 g/kg of diet. The EPL in birds fed on PFD was estimated at 201 mg/kg dry matter intake (DMI) and quail chicks fed on PFD exhibited the lowest performance compared to chicks received dietary P regardless of P sources (P = 0.001). The estimated coefficients of AIPD (P = 0.001) | SIDP (P = 0.004) for CGM, corn, SBM, and wheat were 49.2 | 51.9%, 38.8 | 44.9%, 41.4 | 45.9%, and 33.2 | 40.1%, respectively. The mean differences between AIPD and SIPD coefficients with each ingredients including CGM (P = 0.245), corn (P = 0.169), and SBM (P = 0.169) were not statistically significant, while the comparison of those estimations for wheat (P = 0.022) showed significant differences. The present work showed that the use of direct method could successfully estimate the coefficients of P digestibility in growing quail for both the cereals and protein meals that were studied. The high relative contribution of endogenous P in young quail fed on wheat during the first 2 wk posthatch makes it inevitable to correct AIDP for EPL and evoke the implementation of SIDP coefficients in the feed formulation matrix.


Assuntos
Glycine max , Fósforo na Dieta , Ração Animal/análise , Fenômenos Fisiológicos da Nutrição Animal/fisiologia , Animais , Galinhas/fisiologia , Coturnix/metabolismo , Dieta/veterinária , Digestão/fisiologia , Glutens/metabolismo , Refeições , Fósforo/metabolismo , Fósforo na Dieta/metabolismo , Propilaminas , Codorniz/metabolismo , Glycine max/metabolismo , Triticum/metabolismo , Zea mays/metabolismo
4.
Carbohydr Polym ; 272: 118450, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34420712

RESUMO

One of the well-recognized weaknesses of starch-based materials is their sensitivity to moisture, which limits their expanding applications. Natural materials, soyabean oils have been used as a coating for starch film, but the poor interface between hydrophilic starch and hydrophobic soyabean oil needs to be improved. In this work, (3-Aminopropyl) triethoxysilane (APTES) was used to reinforce the bonding between starch matrix and the coating of bio-based acrylated epoxidized soyabean oil (AESO). Study results show that APTES interacted effectively with both starch films via hydrogen bonding, and chemical bonds with AESO through the Michael addition reaction. Pull adhesion and cross-cutting tests demonstrated that the interfacial adhesion was significantly improved after treating their surface with APTES. The interfacial adhesion strength increased over 4 times after treating with 1.6 wt% APTES. The starch films treated with APTES and AESO coating were intact after soaking in water for more than 2 h.


Assuntos
Interações Hidrofóbicas e Hidrofílicas , Propilaminas/química , Silanos/química , Óleo de Soja/química , Amido/química , Ligação de Hidrogênio , Microscopia Eletrônica de Varredura/métodos , Permeabilidade , Espectroscopia Fotoeletrônica/métodos , Óleos de Plantas/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Água/química
5.
Chem Asian J ; 16(15): 2018-2021, 2021 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-34109742

RESUMO

In this study, we report an efficient fabrication method for the membrane of a metal-organic framework (MOF) (Kgm-OEt) which is one kind of kagomé-type MOF with a two-dimensional (2D) sheet structure having one-dimensional (1D) channels suitable for separation of H2 from other larger gases. The Kgm-OEt seed layer was created on an Al2 O3 substrate using layer-by-layer (LBL) growth, then a membrane was fabricated by secondary growth. The membrane on a 3-aminopropyltriethoxysilane (APTEs)-treated substrate obtained in this method was continuous and defect-free with the crystal orientation suitable for gas transportation, while the membrane grown on an unmodified substrate was loosely packed with unfavorable crystal orientation.


Assuntos
Óxido de Alumínio/química , Estruturas Metalorgânicas/síntese química , Propilaminas/química , Silanos/química , Estruturas Metalorgânicas/química , Estrutura Molecular , Tamanho da Partícula , Porosidade , Propriedades de Superfície
6.
Molecules ; 26(6)2021 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-33799713

RESUMO

Osteomyelitis and orthopedic infections are major clinical problems, limited by a lack of antibiotics specialized for such applications. In this paper, we describe the design and synthesis of a novel bone-binding antibiotic (BBA-1) and its subsequent structural and functional characterization. The synthesis of BBA-1 was the result of a two-step chemical conjugation of cationic selective antimicrobial-90 (CSA-90) and the bisphosphonate alendronate (ALN) via a heterobifunctional linker. This was analytically confirmed by HPLC, FT-IR, MS and NMR spectroscopy. BBA-1 showed rapid binding and high affinity to bone mineral in an in vitro hydroxyapatite binding assay. Kirby-Baur assays confirmed that BBA-1 shows a potent antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus comparable to CSA-90. Differentiation of cultured osteoblasts in media supplemented with BBA-1 led to increased alkaline phosphatase expression, which is consistent with the pro-osteogenic activity of CSA-90. Bisphosphonates, such as ALN, are inhibitors of protein prenylation, however, the amine conjugation of ALN to CSA-90 disrupted this activity in an in vitro protein prenylation assay. Overall, these findings support the antimicrobial, bone-binding, and pro-osteogenic activities of BBA-1. The compound and related agents have the potential to ensure lasting activity against osteomyelitis after systemic delivery.


Assuntos
Alendronato/química , Antibacterianos/síntese química , Osteomielite/tratamento farmacológico , Pregnanos/química , Propilaminas/química , Células 3T3 , Alendronato/farmacologia , Animais , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Osso e Ossos/efeitos dos fármacos , Calcificação Fisiológica/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Células Cultivadas , Difosfonatos/química , Difosfonatos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Camundongos , Osteoblastos/efeitos dos fármacos , Osteogênese/efeitos dos fármacos , Pregnanos/farmacologia , Propilaminas/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/efeitos dos fármacos
7.
Sci Total Environ ; 771: 144764, 2021 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-33736157

RESUMO

Heavy metals like Cr (VI), when released into the environment, pose a serious threat to animal and human health. In this study, iron and (3-Aminopropyl)triethoxysilane (APTES) biochar composites were prepared from the biochar, which was produced through the pyrolysis of rice straw at 400 and 600 °C, using the chemical processes with an aim that the doping of pristine biochar structure with the Fe and NH2 radicals would enhance the removal of Cr (VI) and Zn (II) adsorption in both aqueous solution and soil. Both biochar composites were mixed at a rate of 3% (w/w) with the mine soil for the soil incubation test, and after completion of the test, a soil fertility index (SFI) was calculated. Results showed that both iron and APTES biochar composites followed the Langmuir-Freundlich isotherm showing the maximum removal capacity of 100.59 mg/g for Cr (VI) by APTES/SiBC 600 and maximum adsorption capacity of 83.92 mg/g for Zn2+ by Fe/BC 400. The SFI of the mine-soil amended with both Fe and APTES biochar composites were 16.67 and 13.04%, respectively higher than the controlled study. The mitotic index of the A. cepa cells that grew up in the soil amended with Fe/BC and APTES/SiBC were 40.47 and 44.45%, respectively, higher than the controlled study. The results indicated that the incorporation of the Fe and APTES biochar composites in the soil effectively reduced the metal toxicity and improved the soil physicochemical properties. This study opens up the prospects of using biochar composites in contaminated soil and water treatments.


Assuntos
Metais Pesados , Oryza , Poluentes do Solo , Adsorção , Carvão Vegetal , Humanos , Ferro , Metais Pesados/análise , Extratos Vegetais , Propilaminas , Silanos , Solo , Poluentes do Solo/análise , Zinco
8.
Mikrochim Acta ; 187(9): 535, 2020 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-32870397

RESUMO

An innovative ultrasensitive electrochemical aptamer-based sensor was developed for ochratoxin A (OTA) detection in cold brew coffee through revolutionary combination of nanofibers, electrochemical method, and aptamer technologies. The assembly of the aptasensor was based on the activation of silanized cellulose nanofibrous membranes as a supporting matrix for methylene blue (MB) redox probe-labeled aptamer tethering. Cellulose nanofibrous membranes were regenerated by deacetylating electrospun cellulose acetate nanofibrous membranes with deacetylation efficacy of 97%, followed by silanization of the nanofiber surfaces by using (3-aminopropyl)triethoxysilane (APTES). A replacement of conventionally casted membranes by the nanofibrous membranes increased the active surface area on the working electrode of a screen-printed three-electrode sensor by more than two times, consequently enhancing the fabricated aptasensor performance. The developed aptasensor demonstrated high sensitivity and specificity toward OTA in a range 0.002-2 ng mL-1, with a detection limit of 0.81 pg mL-1. Moreover, the assembled aptamer-based sensor successfully detected OTA in cold brew coffee samples without any pretreatment. The aptasensor exhibited good reusability and stability over long storage time. Graphical abstract.


Assuntos
Aptâmeros de Nucleotídeos/química , Técnicas Biossensoriais/métodos , Celulose/química , Técnicas Eletroquímicas/métodos , Nanofibras/química , Ocratoxinas/análise , Café/química , Contaminação de Alimentos/análise , Ácidos Nucleicos Imobilizados/química , Limite de Detecção , Azul de Metileno/química , Ocratoxinas/química , Oxirredução , Propilaminas/química , Silanos/química
9.
Int J Biol Macromol ; 157: 170-176, 2020 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-32348857

RESUMO

The 3-aminopropyltriethoxysilane modified nano-carbon sphere (MNCS) was added into pectin-Ca2+ film to improve the controlled release properties of the pectin-based oral colon-specific drug delivery system (OCDDS). The FT-IR measurements indicated the successful modification of nano-carbon sphere via silylation reaction and the electrostatic interaction between the pectin molecules and MNCS in the composite film. The FE-SEM showed the pore structure when the MNCS was mingled with the pectin. The 5-fluorouracil (5-FU) was employed as the drug model and the controlled release properties of the corresponding OCDDSs were determined. The values of the encapsulation efficiency ranged from 30.1% to 52.6%. All composite film based OCDDSs presented higher encapsulation efficiency than single pectin-Ca2+ based OCDDS. The drug release studies emerged that almost all the OCDDSs from composite films presented better release properties than single pectin-Ca2+ based OCDDS. The sample C revealed best release performance with the cumulative release rate of 32.17%, 22.77% and 63.89% in the simulated gastric fluid, small intestinal fluid and colon fluid, respectively. In addition, the kinetics studies were performed to analyze the release data. The cytotoxicity assay indicated good biocompatibility of the composite carriers.


Assuntos
Carbono/química , Colo/metabolismo , Portadores de Fármacos/química , Nanocompostos/química , Nanosferas/química , Pectinas/química , Administração Oral , Fluoruracila/administração & dosagem , Fluoruracila/química , Géis , Especificidade de Órgãos , Propilaminas/química , Silanos/química
10.
Artigo em Inglês | MEDLINE | ID: mdl-32222675

RESUMO

C60-based magnetic nanospheres were synthesized by coating Fe3O4 nanospheres with silica, then modifying with 3-aminopropyltriethoxysilane as a linker and a C60 fullerene stationary phase. The morphologies, magnetic properties, infrared absorption and carbon content of magnetic nanospheres were studied by TEM, VSM, FTIR and carbon and sulfur analyzer. The magnetic nanospheres were employed for the magnetic solid-phase extraction (MSPE) of 16 polycyclic aromatic hydrocarbons (PAHs) in nine Chinese herbal medicines. The analyses were conducted by isotope dilution gas chromatography-mass spectrometry. The main parameters influencing the extraction, including extraction solvent, adsorbent amount, and extraction time were optimized. Method validation showed that the limit of detection (LOD) was 0.02-0.11 µg/kg, and the limit of quantification (LOQ) was 0.07-0.36 µg/kg. The spiked recoveries rates for 16 PAHs in white peony root were 84.7-107.2%. The relative standard deviation (RSD) was 1.7-8.4%. The established method was further used for the determination 16 PAHs in nine Chinese herbal medicines. Total content of 16 PAHs varied from 73.6 µg/kg (fructus lycii) to 2172.6 µg/kg (astragalus root). The results indicate that the pollution of PAHs in Chinese herbal medicines is serious. The established method can effective detect PAHs contamination in Chinese herbal medicines.


Assuntos
Medicamentos de Ervas Chinesas/análise , Fulerenos/química , Isótopos/química , Nanopartículas de Magnetita/química , Nanosferas/química , Hidrocarbonetos Policíclicos Aromáticos/análise , Adsorção , Cromatografia Gasosa-Espectrometria de Massas , Limite de Detecção , Fenômenos Magnéticos , Propilaminas/química , Silanos/química , Dióxido de Silício/química , Extração em Fase Sólida/métodos , Propriedades de Superfície
11.
Mol Reprod Dev ; 87(5): 598-606, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32017318

RESUMO

Extracellular calcium is required for intracellular Ca2+ oscillations needed for egg activation, but the regulatory mechanism is still poorly understood. The present study was designed to demonstrate the function of calcium-sensing receptor (CASR), which could recognize extracellular calcium as first messenger, during porcine egg activation. CASR expression was markedly upregulated following egg activation. Functionally, the addition of CASR agonist NPS R-568 significantly enhanced pronuclear formation rate, while supplementation of CASR antagonist NPS2390 compromised egg activation. There was no change in NPS R-568 group compared with control group when the egg activation was performed without extracellular calcium addition. The addition of NPS2390 precluded the activation-dependent [Ca2+ ]i rise. When egg activation was conducted in intracellular Ca2+ chelator BAPTA-AM and NPS R-568 containing medium, CASR function was abolished. Meanwhile, CASR activation increased the level of the [Ca2+ ]i effector p-CAMKII, and the presence of KN-93, an inhibitor of CAMKII, significantly reduced the CASR-mediated increasement of pronuclear formation rate. Furthermore, the increase of CASR expression following activation was reversed by inhibiting CAMKII activity, supporting a positive feedback loop between CAMKII and CASR. Altogether, these findings provide a new pathway of egg activation about CASR, as the extracellular Ca2+ effector, promotes egg activation via its downstream effector and upstream regulator CAMKII.


Assuntos
Proteína Quinase Tipo 2 Dependente de Cálcio-Calmodulina/fisiologia , Fertilização/fisiologia , Receptores de Detecção de Cálcio/fisiologia , Suínos/fisiologia , Adamantano/análogos & derivados , Adamantano/farmacologia , Animais , Benzilaminas/farmacologia , Sinalização do Cálcio/efeitos dos fármacos , Sinalização do Cálcio/fisiologia , Proteína Quinase Tipo 2 Dependente de Cálcio-Calmodulina/metabolismo , Células Cultivadas , Ácido Egtázico/análogos & derivados , Ácido Egtázico/farmacologia , Feminino , Fertilização/efeitos dos fármacos , Masculino , Fenetilaminas/farmacologia , Propilaminas/farmacologia , Quinoxalinas/farmacologia , Receptores de Detecção de Cálcio/antagonistas & inibidores , Transdução de Sinais/efeitos dos fármacos , Interações Espermatozoide-Óvulo/efeitos dos fármacos , Sulfonamidas/farmacologia
12.
J Chromatogr Sci ; 58(1): 75-82, 2019 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-31879774

RESUMO

The hybrid monomer synthesized with 3-aminopropyltriethoxysilanes and acrylamide was applied for synthesis of molecularly imprinting polymers, and the obtained polymers were used as sorbent in solid-phase extraction for purification of theophylline (THP) in green tea. The static adsorption curves showed better molecular recognition ability and binding capability of the polymers for the target. On the optimized condition, a method was developed for increasing extraction of THP with satisfactory recovery of 93.7%. Good calibration linearity obtained in a range of 5-500 µg·mL-1. The recoveries at three spiked levels ranged from 86.7% to 100.7% with relative standard deviations ≤6.6% (n = 3). The result showed that the obtained polymers exhibited highly selective imprinting recognition to the analyte, and the number of templates was an important factor affecting the selective recognition ability of polymers. The proposed method with hybrid monomer imprinting polymers was successfully applied for purification of THP in green tea.


Assuntos
Acrilamida/química , Propilaminas/química , Silanos/química , Teofilina/química , Impressão Molecular , Polímeros/química , Extração em Fase Sólida , Chá/química
13.
J Photochem Photobiol B ; 201: 111648, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31710924

RESUMO

Superparamagnetic iron oxide nanoparticles (SPIONs) have been recently recognized as highly efficient photothermal therapy (PTT) agents. Here, we demonstrate, for the first time to our knowledge, dose and laser intensity dependent PTT potential of small, spherical, 3-aminopropyltrimethoxysilane coated cationic superparamagnetic iron oxide nanoparticles (APTMS@SPIONs) in aqueous solutions upon irradiation at 795 nm. Indocyanine green (ICG) which has been recently used for photodynamic therapy (PDT), was loaded to APTMS@SPIONs to improve the stability of ICG and to achieve an effective mild PTT and PDT (dual therapy) combination for synergistic therapeutic effect on cancer cells via a single laser treatment in the near infrared (NIR). Neither APTMS@SPIONs nor ICG-APTMS@SPIONs showed dark toxicity on MCF7 breast and HT29 colon cancer cell lines. A safe laser procedure was determined as 10 min irradiation at 795 nm with 1.8 W/cm2 of laser intensity, at which APTMS@SPION did not cause a significant cell death. However, free ICG reduced cell viability at and above 10 µg/ml under these conditions along with generation of reactive oxygen species (ROS), more effectively in MCF7. ICG-APTMS@SPION treated cells showed 2-fold increase in ROS generation and near complete cell death at and below 5 µg/ml ICG dose, even in less sensitive HT29 cells after a single laser treatment at NIR, which would be safe for the healthy tissue and provide a longer penetration depth. Besides, both components can be utilized for diagnosis and the overall composition may be used for optical-image guided phototherapy in the NIR region.


Assuntos
Verde de Indocianina/química , Nanopartículas de Magnetita/toxicidade , Propilaminas/química , Silanos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Verde de Indocianina/farmacologia , Raios Infravermelhos , Nanopartículas de Magnetita/química , Nanopartículas de Magnetita/uso terapêutico , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Neoplasias/terapia , Fotoquimioterapia , Fototerapia , Espécies Reativas de Oxigênio/metabolismo , Temperatura
14.
J AOAC Int ; 102(3): 761-766, 2019 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-30388968

RESUMO

Background: Aflatoxins (AFs) have attracted increasing amounts of attention in recent years for their high toxicity. Previously, AF-polluted Chinese Patent Medicines (CPMs) were ignored, but their quality, safety, and efficacy might be influenced by the toxic compounds. Objective: The objective is to develop a simple, low-cost, and efficient method for quantitative analysis of aflatoxins B1 (AFB1) and B2 (AFB2) in CPMs to ensure their safe use. Methods: A simple, modified, magnetic nanoparticle-based solid-phase extraction (SPE) combined with HPLC-fluorescence detection for the determination of trace amounts of AFB1 and AFB2 was established. The main parameters affecting the efficiency of modified magnetic nanoparticle-based SPE, such as pH of sample solution, adsorbent amount, adsorption time, and desorption condition, were investigated. Results: Under the optimum conditions, AFB1 and AFB2 were linear in the ranges of 0.3-10 and 0.04-3 ng/mL with the correlation coefficient (R) of 0.9998 and 0.9999, respectively. Their intraday precisions were 1.16 and 2.30% and the interday precisions were 1.28 and 1.87% for AFB1 and AFB2, respectively. The developed SPE was applied for AFB1 and AFB2 extraction in three commercially available Fupuganmao granule samples, and the results were compared with the official immunoaffinity column chromatography method. Conclusions: The method provided a preferable candidate for the determination approach of AF measurement in CPMs. Highlights: Amine-functionalized magnetic nanoparticles were successfully applied to SPE for adsorbing AFB1 and AFB2 in CPMs for the first time.


Assuntos
Aflatoxina B1/análise , Aflatoxinas/análise , Medicamentos de Ervas Chinesas/análise , Nanopartículas de Magnetita/química , Extração em Fase Sólida/métodos , Adsorção , Cromatografia Líquida de Alta Pressão/métodos , Contaminação de Medicamentos , Concentração de Íons de Hidrogênio , Limite de Detecção , Medicamentos sem Prescrição/análise , Propilaminas/química , Silanos/química , Silicatos/química , Espectroscopia de Infravermelho com Transformada de Fourier/métodos
15.
Biomed Pharmacother ; 110: 431-439, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30530045

RESUMO

The SUR2B/Kir6.1 channel openers iptakalim and natakalim reverse cardiac remodeling and ameliorate endothelial dysfunction by re-establishing the balance between the nitric oxide and endothelin systems. In this study, we investigated the microRNAs (miRs) involved in the molecular mechanisms of SUR2B/Kir6.1 channel opening in chronic heart failure. Both iptakalim and natakalim significantly upregulated the expression of miR-1-3p, suggesting that this miR is closely associated with the therapeutic effects against chronic heart failure. Bioinformatic analysis showed that many of the 183 target genes of miR-1-3p are involved in cardiovascular diseases, suggesting that miR-1-3p plays a vital role in such diseases and vascular remodeling. Target gene prediction showed that miR-1-3p combines with the 3' untranslated region (UTR) of endothelin-1 (ET-1) mRNA. Iptakalim and natakalim upregulated miR-1-3p expression and downregulated ET-1 mRNA expression in vitro. The dual luciferase assay confirmed that there is a complementary binding sequence between miR-1-3p and the 3' UTR 158-165 sequence of ET-1 mRNA. To verify the effect of miR-1-3p on ET-1, lentiviral vectors overexpressing or inhibiting miR-1-3p were constructed for the transduction of rat primary cardiac microvascular endothelial cells. The results showed that natakalim enhanced the miR-1-3p level. miR-1-3p overexpression downregulated the expression of ET-1, whereas miR-1-3p inhibition had the opposite effect. Therefore, we verified that SUR2B/Kir6.1 channel openers could correct endothelial imbalance and ameliorate chronic heart failure through the miR-1-3p/ET-1 pathway in endothelial cells. Our study provides comprehensive insights into the molecular mechanisms behind the SUR2B/Kir6.1 channel's activity against chronic heart failure.


Assuntos
Endotelina-1/metabolismo , Endotélio Vascular/metabolismo , Insuficiência Cardíaca/metabolismo , Canais KATP/metabolismo , MicroRNAs/metabolismo , Receptores de Sulfonilureias/metabolismo , Compostos Alílicos/farmacologia , Compostos Alílicos/uso terapêutico , Animais , Células Cultivadas , Relação Dose-Resposta a Droga , Endotelina-1/antagonistas & inibidores , Endotélio Vascular/efeitos dos fármacos , Endotélio Vascular/patologia , Células HEK293 , Insuficiência Cardíaca/tratamento farmacológico , Insuficiência Cardíaca/patologia , Humanos , Canais KATP/agonistas , MicroRNAs/antagonistas & inibidores , Propilaminas/farmacologia , Propilaminas/uso terapêutico , Ratos , Ratos Wistar , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia , Receptores de Sulfonilureias/agonistas
16.
ACS Sens ; 3(11): 2351-2358, 2018 11 26.
Artigo em Inglês | MEDLINE | ID: mdl-30350590

RESUMO

In this work, we developed an innovative closed bipolar electrode (BPE)-electrochemiluminescence (ECL) sensing strategy with generality for target detection. Based on charge balance and 100% current efficiency between the closed BPE poles and the driving electrodes, one of the driving electrodes in one cell of the closed BPE system was employed as ECL sensing surface to reflect the target on the BPE pole in the opposite cell. Compared with traditional BPE-ECL sensing method, which in general adopted the anodic ECL reagents such as Ru(bpy)32+ and its coreactant on one pole (anode) to reflect the target (occurring reduction reaction) on the other pole (cathode), the difference was that the targets occurring oxidation reaction could be detected by the anodic ECL reagents based on this strategy. To verify the feasibility of this strategy, the detection principle was stated first, and Fe(CN)64- as model target at anodic BPE pole were detected by anodic ECL reagents (Ru(bpy)32+ and TprA) on the driving electrode first. The ECL signals showed good performance for target detection. By changing the size and the material of the BPE pole where the targets were located, the detection of l-ascorbic acid (AA), uric acid (UA), and dopamine (DA) as other model targets with higher detection limit were accomplished. Visual and high-throughput detection of AA, UA, and DA were also successfully realized by an array of the closed BPE system. This closed BPE (array) system is an effective supplement of traditional BPE-ECL sensing and could greatly expand the scope of the detection target.


Assuntos
Ácido Ascórbico/análise , Dopamina/análise , Técnicas Eletroquímicas/métodos , Ferrocianetos/análise , Medições Luminescentes/métodos , Ácido Úrico/análise , Ácido Ascórbico/química , Complexos de Coordenação/química , Dopamina/química , Técnicas Eletroquímicas/instrumentação , Eletrodos , Ferrocianetos/química , Limite de Detecção , Luminescência , Oxirredução , Propilaminas/química , Ácido Úrico/química
17.
J Chromatogr A ; 1564: 145-154, 2018 Aug 24.
Artigo em Inglês | MEDLINE | ID: mdl-29895409

RESUMO

Prostate cancer (PCa) is a common and fatal cancer for men and effective treatment options are still not enough for patients. Radix et Rhizoma Rhei had been applied to treat PCa long-termly and effectively when combined with surgical treatment and chemotherapy. However, its active components and target proteins are still not quite clear. As membrane receptors play a vital role in PCa, in this study, a novel strategy that combines comprehensive 2D 3-aminopropyltriethoxysilane-decorated prostate cancer cell (DU145) membrane chromatographic (CMC) system with network pharmacology approach was developed to characterize membrane binding active components proteins from Radix et Rhizoma Rhei and their targets. Thirteen active components were screened out by CMC system, among which emodin and rhapontigrnin with good membrane binding behaviors were validated to show ideal inhibitory effects on DU145 cells by cell viability and cell apoptosis assays. Five membrane proteins were predicted as the potential targets by the a specific network pharmacology approach, among which mast/stem cell growth factor receptor Kit (KIT) was identified as the most possible target by network data mining. Surface plasmon resonance analysis verified that the dissociation constant (KD) of rhapontigrnin and emodin with KIT was 6.06 × 10-5 M and 8.82 × 10-5 M, respectively. Our results showed that the combination of comprehensive 2D CMC system and network pharmacology based target identification could not only rapidly identify the membrane binding components but also find the potential membrane protein targets with high confidence, which could broaden the range of application scope of CMC, especially for the screening of active compounds from complex chemical samples using primary pathologic cell lines.


Assuntos
Membrana Celular/metabolismo , Medicamentos de Ervas Chinesas/química , Neoplasias da Próstata/patologia , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Masculino , Simulação de Acoplamento Molecular , Propilaminas/química , Neoplasias da Próstata/tratamento farmacológico , Reprodutibilidade dos Testes , Silanos/química , Ressonância de Plasmônio de Superfície
18.
J Food Drug Anal ; 26(2): 823-833, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29567254

RESUMO

Rhizoma corydalis and Radix Angelicae Dahurica (Yuanhu-Baizhi) herbal medicine pair has been used for thousands of years and has been reported to be potentially active in recent cancer therapy. But the exact active components or fractions remain unclear. In this study, a new comprehensive two-dimensional (2D) 3-aminopropyltriethoxysilane (APTES)-decorated MCF7-cell membrane chromatography (CMC)/capcell-C18 column/time-of-flight mass spectrometry system was established for screening potential active components and clarifying the active fraction of Yuanhu-Baizhi pair. APTES was modified on the surface of silica, which can provide an amino group to covalently link cell membrane fragments with the help of glutaraldehyde in order to improve the stability and column life span of the MCF7 CMC column. The comprehensive 2D MCF7-CMC system showed good separation and identification abilities. Our screen results showed that the retention components are mainly from the alkaloids in Yuanhu (12 compounds) and the coumarins (10 compounds) in Baizhi, revealing the active fractions of Yuanhu-Baizhi herbal medicine pair. Oxoglaucine, protopine, berberine, osthole, isopimpinellin and palmitic acid were selected as typical components to test the effects on cell proliferation and their IC50 were calculated as 38.17 µM, 29.45 µM, 45.42 µM, 132.7 µM, 156.8 µM and 90.5 µM respectively. Cell apoptosis assay showed that the drug efficacy was obtained mainly through inducing cell apoptosis. Furthermore, a synergistic assay results demonstrated that oxoglaucine (representative of alkaloids from Yuanhu) and isopimpinellin (representative of coumarins from Baizhi) showed significant synergistic efficacy with GFT, indicating that these components may act on other membrane receptors. The proposed 2D CMC system could also be equipped with other cells for further applications. Besides, the follow-up in-vitro experimental strategy using cell proliferation assay, cell apoptosis assay and synergistic assay proved to be a practical way to confirm the active fractions of herbal medicine.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Membrana Celular/efeitos dos fármacos , Cromatografia/métodos , Corydalis/química , Medicamentos de Ervas Chinesas/farmacologia , Antineoplásicos Fitogênicos/química , Neoplasias da Mama/fisiopatologia , Membrana Celular/química , Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/química , Feminino , Humanos , Células MCF-7 , Espectrometria de Massas , Plantas Medicinais/química , Propilaminas/química , Rizoma/química , Silanos/química
19.
J Environ Sci Health B ; 53(4): 229-236, 2018 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-29319411

RESUMO

The aim of this study was to develop a cantilever nanobiosensor for atrazine detection in liquid medium by immobilising the biological recognition element (tyrosinase vegetal extract) on its surface with self-assembled monolayers using gold, 16-mercaptohexadecanoic acid, 1-ethyl-3-[3-dimethylaminopropyl] carbodiimide hydrochloride/n-hydroxysuccinimide. Cantilever nanobiosensors presented a surface compression tension increase when atrazine concentrations were increased, with a limit of detection and limit of quantification of 7.754 ppb (parts per billion) and 22.792 ppb, respectively. From the voltage results obtained, the evaluation of atrazine contamination in river and drinking water were very close to those of the reference sample and ultrapure water, demonstrating the ability of the cantilever nanobiosensor to distinguish different water samples and different concentrations of atrazine. Cantilever nanosensor surface functionalization was characterised by combining polarisation modulation infrared reflection-absorption spectroscopy and atomic force microscopy and indicating film thickness in nanometric scale (80.2 ± 0.4 nm). Thus, the cantilever nanobiosensor developed for this study using low cost tyrosinase vegetal extract was adequate for atrazine detection, a potential tool in the environmental field.


Assuntos
Atrazina/análise , Técnicas Biossensoriais , Monofenol Mono-Oxigenase/metabolismo , Nanotecnologia , Água Potável/química , Contaminação de Alimentos/análise , Ouro/química , Herbicidas/análise , Imidas/química , Limite de Detecção , Musa/química , Musa/enzimologia , Ácidos Palmíticos/química , Extratos Vegetais/química , Propilaminas/química , Rios/química , Propriedades de Superfície
20.
Colloids Surf B Biointerfaces ; 163: 275-283, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29329073

RESUMO

The functionalization of alumina nanoparticles of specific morphology with antimicrobial peptides (AMP) can be a promising strategy for modeling medical devices and packaging materials for cosmetics, medicines or food, since the contamination by pathogens could be reduced. In this paper, we show the synthesis of a fibrous-like alumina nanobiostructure, as well as its functionalization with the peptide EAAA-BP100, an analog of the antimicrobial peptide BP100. The antibacterial activity of the obtained material against some bacterial strains is also investigated. The covalent binding of the peptide to the nanoparticles was promoted by a reaction between the carboxyl group of the glutamate side chain (E1) of the peptide and the amino groups of the alumina nanoparticles, previously modified by reaction with 3-aminopropyltrietoxysilane (APTES). The functionalized nanoparticles were characterized by zeta potential measurements, Fourier transform infrared spectroscopy, and other physicochemical techniques. Although the obtained alumina nanobiostructure shows a relatively low degree of substitution with EAAA-BP100, antibacterial activities against Escherichia coli and Salmonella typhimurium strains are appreciably higher than the activities of the free peptide. The obtained results can affect the design of new hybrid nanobiomaterials based on nanoparticles functionalized with AMP.


Assuntos
Óxido de Alumínio/química , Nanoestruturas/química , Oligopeptídeos/química , Oligopeptídeos/síntese química , Sequência de Aminoácidos , Antibacterianos/química , Antibacterianos/farmacologia , Fluoresceínas/química , Testes de Sensibilidade Microbiana , Nanoestruturas/ultraestrutura , Oligopeptídeos/farmacologia , Propilaminas/química , Silanos/química , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática , Temperatura , Difração de Raios X
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