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1.
Shanghai Kou Qiang Yi Xue ; 33(3): 245-249, 2024 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-39104337

RESUMO

PURPOSE: To investigate the effects of erbium laser pretreatment on the bond strength of dentin and enamel,as well as microleakage at the edge of tooth defects repaired with computer-aided design (CAD) and computer-assisted manufacturing (CAM) glass-ceramic restorations for repairing dental defects. METHODS: A total of 62 fresh, nondecayed, nondiscoloration and noncracked wisdom teeth were collected from the Oral Surgery Clinic between January 2020 and January 2023. According to different pretreatment methods, they were randomly divided into two groups, erbium laser group and phosphoric acid group, with 31 teeth in each group. Each group was further divided into two subsets for bond strength testing (16 teeth) and microleakage testing (15 teeth).The shear bond strength between enamel and dentin of both groups was compared, as well as the degree and distribution of microleakage.Statistical analysis was performed with SPSS 17.0 software package. RESULTS: The shear bond strength between enamel and dentin of the erbium laser group was significantly higher than that of the phosphoric acid group (P<0.05); the degree and distribution of microleakage at the lateral walls and gumline of the erbium laser group were significantly lower than those of the phosphoric acid group (P<0.05). The scores of microleakage at the lateral walls of the erbium laser group mainly concentrated in grade 1 and 2, whereas those of the phosphoric acid group mainly concentrated in grade 2. There was significant difference in the distribution of lateral wall microleakage scores between the two groups (P<0.05). The scores of microleakage at the gumline of the erbium laser group mainly concentrated in grade 1 and 2, whereas those of the phosphoric acid group mainly concentrated in grade 2 and 3. There was significant difference in the distribution of gumline microleakage scores between the two groups (P<0.05). CONCLUSIONS: Erbium laser pretreatment can improve bonding strength between glass ionomer cement and dentin and enamel, reduce microleakage at the edge of CAD/CAM glass ionomer cement restorations, and enhance marginal fit.


Assuntos
Desenho Assistido por Computador , Colagem Dentária , Esmalte Dentário , Dentina , Cimentos de Ionômeros de Vidro , Esmalte Dentário/efeitos da radiação , Humanos , Dentina/química , Cimentos de Ionômeros de Vidro/química , Colagem Dentária/métodos , Ácidos Fosfóricos/química , Lasers de Estado Sólido/uso terapêutico , Resistência ao Cisalhamento , Infiltração Dentária/etiologia , Restauração Dentária Permanente/métodos , Érbio/química
2.
Chemosphere ; 362: 142655, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38908444

RESUMO

Lead is used in many industries such as refining, mining, battery manufacturing, smelting. Releases of lead from these industries is one of the major public health concerns due to widespread persistence in the environment and its resulting poisoning character. In this work, the castor seed shell (CSS) waste was exploited for preparing a beneficial bio-adsorbent for removal of Pb(II) ions from water. The raw CSS was modified with H3PO4 at different acid concentrations, impregnation ratios, activation times, and temperatures. An optimum adsorption capacity was observed for CSS modified with 2 M acid, 5 mL g-1 solid to liquid ratio, treated at 95 °C for 160 min. Exploiting acid modification, the SEM, XRD, and FTIR analyses show some alterations in functional groups and the surface morphology of the biomass. The impacts of physiochemical variables (initial lead ions concentration, pH, adsorbent dose and adsorption time) on the lead removal percentage were investigated, using response surface methodology (RSM). Maximum removal of 72.26% for raw CSS and 97.62% for modified CSS were obtained at an initial lead concentration (50 mg L-1), pH (5.7), adsorption time (123 min) and adsorbent dosage (1.1 g/100 mL). Isothermal and kinetics models were fitted to adsorption equilibrium data and kinetics data for the modified CSS and the adsorption system was evaluated thermodynamically and from the energy point of view. Isothermal scrutinization indicated the mono-layer nature of adsorption, and the kinetics experimental outcomes best fitted with the pseudo-second-order, implying that the interaction of lead ions and hot acid-treated CSS was the rate-controlling phenomenon of process. Overall, results illustrated that the hot acid-treated biomass-based adsorbent can be considered as an alternative bio-adsorbent for removing lead from water media.


Assuntos
Chumbo , Ácidos Fosfóricos , Sementes , Poluentes Químicos da Água , Adsorção , Chumbo/química , Chumbo/isolamento & purificação , Sementes/química , Ácidos Fosfóricos/química , Poluentes Químicos da Água/química , Cinética , Purificação da Água/métodos , Ricinus communis/química , Concentração de Íons de Hidrogênio
3.
J Prosthet Dent ; 131(4): 743.e1-743.e6, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38368144

RESUMO

STATEMENT OF PROBLEM: Phosphoric acid is commonly used in dentistry as an etchant but can result in excessive demineralization of dentin, a major contributor to the instability of dentin-bonded restorations. Nevertheless, research on the development of etchants that can reduce acid damage is sparse. PURPOSE: The purpose of this in vitro study was to investigate the effects of polyvinylpyrrolidone-modified phosphoric acid on the dentin bonding of an etch-and-rinse adhesive. MATERIAL AND METHODS: Protective etchants were prepared by adding polyvinylpyrrolidone to 35% phosphoric acid aqueous solutions: the 3 concentrations were 0.5% (P0.5% group), 1% (P1% group), and 2% (P2% group) w/v. The treatment agent of the control group (C) was 35% phosphoric acid gel. Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), microhardness, microtensile bonding strength (µTBS), nanoleakage, and in situ zymography were used to evaluate the appearance of the protective etchant on dentin bonding. The results were analyzed with a 1-way ANOVA test (α=.05). RESULTS: SEM showed no obviously exposed collagen fiber in the P1% and P2% groups. FTIR showed less demineralization of the dentin surface, and microhardness was higher after treatment with the protective etchant (P<.05). The µTBS of P1% (70 ±9.2 MPa) was the highest, and group C (44 ±5.8 MPa) was the lowest in all groups (P<.05). Moreover, there was weaker MMP activity in the P1% and P2% groups (P<.05). CONCLUSIONS: This study demonstrated that the protective etchant effectively reduced demineralization, enhanced bond strength, and reduced nanoleakage and enzyme activity within the hybrid layer.


Assuntos
Colagem Dentária , Desmineralização do Dente , Humanos , Povidona , Ácidos Fosfóricos/química , Ácidos Fosfóricos/farmacologia , Microscopia Eletrônica de Varredura , Dentina , Resistência à Tração , Adesivos Dentinários/química , Teste de Materiais , Cimentos de Resina/química
4.
J Oleo Sci ; 71(2): 177-185, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35110462

RESUMO

Phosphoric acid is used in the refining of palm oil for the removal of phosphatides. The high concentration of phosphorus in solvent extracted palm-pressed mesocarp fiber oil hinders palm oil mills to recover this phytonutrients-rich residual oil in pressed fiber which typically contains 0.1 to 0.2% of total oil yield. This study aimed to refine the palm-pressed mesocarp fiber oil and determine the optimum dosage of phosphoric acid for acid-degumming of palm-pressed mesocarp fiber oil while retaining its phytonutrients. The refining process was carried out with combination of wet degumming, acid degumming, neutralisation, bleaching and deodorization. The optimum dose of phosphoric acid was identified as 0.05 wt.% by incorporating the wet degumming process. The refined palm-pressed mesocarp fiber oil showed a reduction in phosphorus content by 97% (from 901 ppm to 20 ppm) and 97% free fatty acid content removal (from 6.36% to 0.17%), while the Deterioration of Bleachability Index increased from 1.76 to 2.48, which showed an increment of 41%. The refined oil retained the key phytonutrients such as carotenoids (1,150 ppm) and vitamin E (1,540 ppm) that can be further developed into high-value products. The oil meets the quality specification of refined, bleached, and deodorized palm oil while preserving the heat-sensitive phytonutrients, which in turn provides a new resource of nutritious oil.


Assuntos
Manipulação de Alimentos/métodos , Extração Líquido-Líquido/métodos , Óleo de Palmeira/química , Fosfolipídeos/isolamento & purificação , Fósforo/isolamento & purificação , Compostos Fitoquímicos/análise , Carotenoides/análise , Qualidade dos Alimentos , Óleo de Palmeira/análise , Fosfolipídeos/análise , Ácidos Fosfóricos/química , Fósforo/análise , Solventes , Vitamina E/análise
5.
Rev. Fac. Odontol. (B.Aires) ; 37(87): 35-46, 2022. ilus, tab
Artigo em Espanhol | LILACS | ID: biblio-1537969

RESUMO

La adhesión a dentina con sistemas adhesivos polimé-ricos representa un desafío que surge de la necesi-dad de vincular un sustrato dentario heterogéneo y variable con materiales que presentan todavía cier-tos aspectos a atender para poder conseguir el máxi-mo desempeño. El propósito del presente artículo es evaluar algunas de las estrategias propuestas para mejorar la adhesión a dentina, y sugerir un protocolo de trabajo con los diferentes tipos de sistemas adhesivos (AU)


Dentin bonding with polymeric adhesive systems represents a challenge that arises from the need to link a heterogeneous and variable dental substrate with materials that still have certain aspects to be addressed in order to achieve maximum performance. The aim of this article is to evaluate some of the proposed strategies to improve dentin bonding and to suggest a protocol for each different type of bonding systems (AU)


Assuntos
Protocolos Clínicos , Adesivos Dentinários/uso terapêutico , Dentina/efeitos dos fármacos , Ácidos Fosfóricos/química , Condicionamento Ácido do Dente/métodos , Camada de Esfregaço , Resinas Compostas/química , Esmalte Dentário/efeitos dos fármacos , Polimerização
6.
J Nanobiotechnology ; 19(1): 445, 2021 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-34949196

RESUMO

Phosphomolybdate-based nanoparticles (PMo12-based NPs) have been commonly applied in nanomedicine. However, upon contact with biofluids, proteins are quickly adsorbed onto the NPs surface to form a protein corona, which induces the opsonization and facilitates the rapid clearance of the NPs by macrophage uptake. Herein, we introduce a family of structurally homologous PMo12-based NPs (CDS-PMo12@PVPx(x = 0 ~ 1) NPs) capping diverse content of zwitterionic polymer poly (N-vinylpyrrolidone) (PVP) to regulate the protein corona formation on PMo12-based NPs. The fluorescence quenching data indicate that the introduction of PVP effectively reduces the number of binding sites of proteins on PMo12-based NPs. Molecular docking simulations results show that the contact surface area and binding energy of proteins to CDS-PMo12@PVP1 NPs are smaller than the CDS-PMo12@PVP0 NPs. The liquid chromatography-tandem mass spectrometry (LC-MS/MS) is further applied to analyze and quantify the compositions of the human plasma corona formation on CDS-PMo12@PVPx(x = 0 ~ 1) NPs. The number of plasma protein groups adsorption on CDS-PMo12@PVP1 NPs, compared to CDS-PMo12@PVP0 NPs, decreases from 372 to 271. In addition, 76 differentially adsorption proteins are identified between CDS-PMo12@PVP0 and CDS-PMo12@PVP1 NPs, in which apolipoprotein is up-regulated in CDS-PMo12@PVP1 NPs. The apolipoprotein adsorption onto the NPs is proposed to have dysoponic activity and enhance the circulation time of NPs. Our findings demonstrate that PVP grafting on PMo12-based NPs is a promising strategy to improve the anti-biofouling property for PMo12-based nanodrug design.


Assuntos
Molibdênio/química , Nanopartículas/química , Ácidos Fosfóricos/química , Povidona/química , Coroa de Proteína/química , Adsorção , Apolipoproteínas/análise , Apolipoproteínas/química , Apolipoproteínas/metabolismo , Proteínas Sanguíneas/análise , Proteínas Sanguíneas/química , Proteínas Sanguíneas/metabolismo , Cromatografia Líquida de Alta Pressão , Humanos , Simulação de Acoplamento Molecular , Propriedades de Superfície , Tensoativos/química , Espectrometria de Massas em Tandem
7.
J Chromatogr A ; 1650: 462247, 2021 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-34087520

RESUMO

The adsorptive loss of acidic analytes in liquid chromatography was investigated using metal frits. Repetitive injections of acidic small molecules or an oligonucleotide were made on individual 2.1 or 4.6 mm i.d. column frits. Losses were observed for adenosine 5'-(α,ß-methylene) diphosphate, 2-pyridinol 1-oxide and the 25-mer phosphorothioate oligonucleotide Trecovirsen (GEM91) on stainless steel and titanium frits. Analyte adsorption was greatest at acidic pH due to the positive charge on the metal oxide surface. Analyte recovery increased when a series of injections was performed; this effect is known as sample conditioning. Nearly complete recovery was achieved when the metal adsorptive sites were saturated with the analyte. A similar effect was achieved by conditioning the frits with phosphoric, citric or etidronic acids, or their buffered solutions. These procedures can be utilized to mitigate analyte loss. However, the effect is temporary, as the conditioning agent is gradually removed by the running mobile phase. Metal frits modified with hybrid organic/inorganic surface technology were shown to mitigate analyte-to-metal surface interactions and improve recovery of acidic analytes. Quantitative recovery of a 15-35 mer oligodeoxythymidine mixture was achieved using column hardware modified with hybrid surface technology, without a need for column conditioning prior to analysis.


Assuntos
Cromatografia Líquida , Metais , Adsorção , Soluções Tampão , Cromatografia Líquida/métodos , Cromatografia Líquida/normas , Ácido Cítrico/química , Ácido Etidrônico/química , Indicadores e Reagentes , Metais/química , Ácidos Fosfóricos/química , Aço Inoxidável/química , Propriedades de Superfície , Titânio/química
8.
Rev. Círc. Argent. Odontol ; 79(229): 9-17, abr. 2021. ilus, tab
Artigo em Espanhol | LILACS | ID: biblio-1253242

RESUMO

La aparición de aparatología preadjustada ha colaborado en la efectividad de los tratamientos de ortodoncia, pero para que la expresión de esta aparatología se logre, es necesario una correcta colocación de los brackets y la permanencia de estos en boca durante todo el tratamiento. La precisión en la colocación mejora con la técnica de cementado indirecta, ya que permite el acceso a las zonas posteriores, a lugares donde se ve disminuida la visión y además disminuye la condensación de aliento y contaminación salival. Si bien esta técnica requiere tiempo extra de laboratorio, es más rápida en la etapa clínica (AU)


Assuntos
Humanos , Masculino , Feminino , Adolescente , Adulto , Elastômeros de Silicone , Cimentação/métodos , Braquetes Ortodônticos , Ácidos Fosfóricos/química , Projetos de Pesquisa , Faculdades de Odontologia , Condicionamento Ácido do Dente/instrumentação , Eficácia , Técnica de Moldagem Odontológica , Colagem Dentária/instrumentação , Resinas Compostas , Modelos Dentários
9.
Anal Biochem ; 623: 114170, 2021 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-33736971

RESUMO

Colorimetric methods are convenient for the determination of inorganic phosphate. However, the acidic conditions required can complicate measurement of ATPase through non-enzymatic ATP hydrolysis. Here we present an optimized antimony-phosphomolybdate microassay for the simple and rapid detection of ATPase activity, with micromolar sensitivity. The low acidity of the color reagent results in no interference for samples containing up to 0.5-5 mM ATP, dependent on the sample volume. The assay is compatible with common assay conditions and was similar in accuracy to an established continuous method. The simplicity of this method makes it ideal for medium to high throughput applications.


Assuntos
Adenosina Trifosfatases/análise , Adenosina Trifosfatases/química , Antimônio/química , Ensaios de Triagem em Larga Escala/métodos , Microquímica/métodos , Molibdênio/química , Fosfatos/análise , Ácidos Fosfóricos/química , Adenosina Trifosfatases/metabolismo , Colorimetria/métodos
10.
Angew Chem Int Ed Engl ; 60(22): 12279-12283, 2021 05 25.
Artigo em Inglês | MEDLINE | ID: mdl-33651459

RESUMO

An unprecedented example of a chiral phosphoric acid-catalyzed atroposelective Pictet-Spengler reaction of N-arylindoles is reported. Highly enantioenriched N-aryl-tetrahydro-ß-carbolines with C-N bond axial chirality are obtained via dynamic kinetic resolution. The hydrogen bond donor introduced on the bottom aromatic ring, forming a secondary interaction with the phosphoryl oxygen, is essential to achieving high enantioselectivity. A wide variety of substituents are tolerable with this transformation to provide up to 98 % ee. The application of electron-withdrawing group-substituted benzaldehydes enables the control of both axial and point stereogenicity. Biological evaluation of this new and unique scaffold shows promising antiproliferative activity and emphasizes the significance of atroposelective synthesis.


Assuntos
Antineoplásicos/química , Ácidos Fosfóricos/química , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Benzaldeídos/química , Carbolinas/química , Carbono/química , Catálise , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Ligação de Hidrogênio , Nitrogênio/química , Estereoisomerismo
11.
Science ; 371(6530): 702-707, 2021 02 12.
Artigo em Inglês | MEDLINE | ID: mdl-33574208

RESUMO

We report the catalytic stereocontrolled synthesis of dinucleotides. We have demonstrated, for the first time to our knowledge, that chiral phosphoric acid (CPA) catalysts control the formation of stereogenic phosphorous centers during phosphoramidite transfer. Unprecedented levels of diastereodivergence have also been demonstrated, enabling access to either phosphite diastereomer. Two different CPA scaffolds have proven to be essential for achieving stereodivergence: peptide-embedded phosphothreonine-derived CPAs, which reinforce and amplify the inherent substrate preference, and C2-symmetric BINOL-derived CPAs, which completely overturn this stereochemical preference. The presently reported catalytic method does not require stoichiometric activators or chiral auxiliaries and enables asymmetric catalysis with readily available phosphoramidites. The method was applied to the stereocontrolled synthesis of diastereomeric dinucleotides as well as cyclic dinucleotides, which are of broad interest in immuno-oncology as agonists of the stimulator of interferon genes (STING) pathway.


Assuntos
Nucleotídeos Cíclicos/síntese química , Oligonucleotídeos/síntese química , Catálise , Estrutura Molecular , Nucleotídeos Cíclicos/química , Oligonucleotídeos/química , Compostos Organofosforados/química , Ácidos Fosfóricos/química , Oligonucleotídeos Fosforotioatos/química , Estereoisomerismo
12.
Chem Soc Rev ; 50(3): 1522-1586, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33496291

RESUMO

The efficacy and synthetic versatility of asymmetric organocatalysis have contributed enormously to the field of organic synthesis since the early 2000s. As asymmetric organocatalytic methods mature, they have extended beyond the academia and undergone scale-up for the production of chiral drugs, natural products, and enantiomerically enriched bioactive molecules. This review provides a comprehensive overview of the applications of asymmetric organocatalysis in medicinal chemistry. A general picture of asymmetric organocatalytic strategies in medicinal chemistry is firstly presented, and the specific applications of these strategies in pharmaceutical synthesis are systematically described, with a focus on the preparation of antiviral, anticancer, neuroprotective, cardiovascular, antibacterial, and antiparasitic agents, as well as several miscellaneous bioactive agents. The review concludes with a discussion of the challenges, limitations and future prospects for organocatalytic asymmetric synthesis of medicinally valuable compounds.


Assuntos
Produtos Biológicos/química , Química Farmacêutica , Compostos Orgânicos/química , Aminas/química , Antineoplásicos/síntese química , Antineoplásicos/química , Antivirais/síntese química , Antivirais/química , Produtos Biológicos/síntese química , Catálise , Química Farmacêutica/métodos , Metano/análogos & derivados , Metano/química , Ácidos Fosfóricos/química , Estereoisomerismo
13.
Int J Biol Macromol ; 166: 117-126, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-33096172

RESUMO

Polyvinyl alcohol and phosphoric acid were used as primary raw materials to synthesize a polyvinyl alcohol/ammonium phosphate flame retardant (PVAAP) for cotton fabrics. The limiting oxygen index of the cotton fabric treated with 24% PVAAP was 42.1. After 50 standard laundry cycles, the limiting oxygen index remained relatively high (26.3), suggesting that the 24% PVAAP can be used as a durable flame retardant. The vertical flammability test of the cotton fabric treated with PVAAP exhibited no afterflame and afterglow. The cone calorimetry test indicated that the peak of the heat release rate and total heat release of the cotton fabric treated with 24% PVAAP were significantly lower than those of the control cotton. Thermogravimetric and thermogravimetric-infrared spectroscopy revealed that the initial decomposition temperature of the PVAAP-treated fabric was substantially lower than that of the control fabric, and more residual carbon was generated. The PVAAP altered the thermal decomposition pathway of the treated cotton. The X-ray diffraction patterns and scanning electron microscopy images suggested that the PVAAP treatment did not change the structure of the fibers.


Assuntos
Celulose/química , Fibra de Algodão , Retardadores de Chama/síntese química , Álcool de Polivinil/química , Formaldeído/química , Fosfatos/química , Ácidos Fosfóricos/química
14.
Molecules ; 25(23)2020 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-33287431

RESUMO

Research advances in electropolishing, with respect to the field of metalworking, have afforded significant improvements in the surface roughness and conductivity properties of aluminum polished surfaces in ways that machine polishing and simple chemical polishing cannot. The effects of a deep eutectic medium as an acid-free electrolyte were tested to determine the potential energy thresholds during electropolishing treatments based upon temperature, experiment duration, current, and voltage. Using voltammetry and chronoamperometry tests during electropolishing to supplement representative recordings via atomic force microscopy (AFM), surface morphology comparisons were performed regarding the electropolishing efficiency of phosphoric acid and acid-free ionic liquid treatments for aluminum. This eco-friendly solution produced polished surfaces superior to those surfaces treated with industry standard acid electrochemistry treatments of 1 M phosphoric acid. The roughness average of the as-received sample became 6.11 times smoother, improving from 159 nm to 26 nm when electropolished with the deep eutectic solvent. This result was accompanied by a mass loss of 0.039 g and a 7.2 µm change in step height along the edge of the electropolishing interface, whereas the acid treatment resulted in a slight improvement in surface roughness, becoming 1.63 times smoother with an average post-electropolishing roughness of 97.7 nm, yielding a mass loss of 0.0458 g and a step height of 8.1 µm.


Assuntos
Alumínio/química , Eletroquímica/métodos , Eletrólitos/química , Condutividade Elétrica , Líquidos Iônicos/química , Teste de Materiais/métodos , Microscopia de Força Atômica/métodos , Ácidos Fosfóricos/química , Solventes/química , Propriedades de Superfície , Temperatura
15.
Proc Natl Acad Sci U S A ; 117(51): 32370-32379, 2020 12 22.
Artigo em Inglês | MEDLINE | ID: mdl-33288723

RESUMO

The design of modified oligonucleotides that combine in one molecule several therapeutically beneficial properties still poses a major challenge. Recently a new type of modified mesyl phosphoramidate (or µ-) oligonucleotide was described that demonstrates high affinity to RNA, exceptional nuclease resistance, efficient recruitment of RNase H, and potent inhibition of key carcinogenesis processes in vitro. Herein, using a xenograft mouse tumor model, it was demonstrated that microRNA miR-21-targeted µ-oligonucleotides administered in complex with folate-containing liposomes dramatically inhibit primary tumor growth via long-term down-regulation of miR-21 in tumors and increase in biosynthesis of miR-21-regulated tumor suppressor proteins. This antitumoral effect is superior to the effect of the corresponding phosphorothioate. Peritumoral administration of µ-oligonucleotide results in its rapid distribution and efficient accumulation in the tumor. Blood biochemistry and morphometric studies of internal organs revealed no pronounced toxicity of µ-oligonucleotides. This new oligonucleotide class provides a powerful tool for antisense technology.


Assuntos
Amidas/química , Antineoplásicos/farmacologia , MicroRNAs/genética , Oligonucleotídeos Antissenso/química , Oligonucleotídeos Antissenso/farmacologia , Ácidos Fosfóricos/química , Animais , Antineoplásicos/química , Antineoplásicos/farmacocinética , Linhagem Celular Tumoral , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Masculino , Melanoma/genética , Melanoma/patologia , Camundongos SCID , Terapia de Alvo Molecular , Oligonucleotídeos Antissenso/farmacocinética , Distribuição Tecidual , Ensaios Antitumorais Modelo de Xenoenxerto
16.
Angew Chem Int Ed Engl ; 59(45): 20154-20160, 2020 11 02.
Artigo em Inglês | MEDLINE | ID: mdl-32757352

RESUMO

Phosphoramidates composed of an amino acid and a nucleotide analogue are critical metabolites of prodrugs, such as remdesivir. Hydrolysis of the phosphoramidate liberates the nucleotide, which can then be phosphorylated to become the pharmacologically active triphosphate. Enzymatic hydrolysis has been demonstrated, but a spontaneous chemical process may also occur. We measured the rate of enzyme-free hydrolysis for 17 phosphoramidates of ribonucleotides with amino acids or related compounds at pH 7.5. Phosphoramidates of proline hydrolyzed fast, with a half-life time as short as 2.4 h for Pro-AMP in ethylimidazole-containing buffer at 37 °C; 45-fold faster than Ala-AMP and 120-fold faster than Phe-AMP. Crystal structures of Gly-AMP, Pro-AMP, ßPro-AMP and Phe-AMP bound to RNase A as crystallization chaperone showed how well the carboxylate is poised to attack the phosphoramidate, helping to explain this reactivity. Our results are significant for the design of new antiviral prodrugs.


Assuntos
Amidas/metabolismo , Aminoácidos/química , Nucleotídeos/metabolismo , Ácidos Fosfóricos/metabolismo , Monofosfato de Adenosina/análogos & derivados , Monofosfato de Adenosina/química , Monofosfato de Adenosina/metabolismo , Alanina/análogos & derivados , Alanina/química , Alanina/metabolismo , Amidas/química , Antivirais/química , Antivirais/metabolismo , Antivirais/farmacologia , COVID-19/patologia , COVID-19/virologia , Domínio Catalítico , Cristalografia por Raios X , Meia-Vida , Concentração de Íons de Hidrogênio , Hidrólise , Cinética , Simulação de Dinâmica Molecular , Nucleotídeos/química , Ácidos Fosfóricos/química , Ribonuclease Pancreático/química , Ribonuclease Pancreático/metabolismo , SARS-CoV-2/efeitos dos fármacos , SARS-CoV-2/isolamento & purificação , Tratamento Farmacológico da COVID-19
17.
Assay Drug Dev Technol ; 18(6): 274-281, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32608988

RESUMO

Fisetin (FS) is a polyphenolic phytoconstituent reported to have various pharmacological activities such as antioxidant, antiparkinsonian, and antidepressant. An analytical method was developed and validated for the estimation of FS by ultrafast liquid chromatography using C-18 reverse phase column. Acetonitrile and orthophosphoric acid (0.2% v/v) in the ratio of 30:70 v/v was used as mobile phase. Flow rate was set at 1 mL/min. Chromatogram of FS was detected at wavelength of 362 nm. Retention time for FS was found to be 7.06 min. The developed method was found to be linear in the range of 2-10 µg/mL with regression coefficient of 0.9985. The method was validated as per the International Conference on Harmonization (ICH) Q2 (R1) guidelines. The percentage recovery was in the range of 95%-105%, which indicated the accuracy of the method. The percentage relative standard deviation (RSD) was found to be <2%, which indicates the precision of the method. Limit of detection (LOD) and limit of quantification (LOQ) were found to be 0.46 and 1.41 µg/mL, respectively. The developed method was found to be robust as there was no significant change in response with change in flow rate, ratio of mobile phase, and pH. The method was successfully applied for estimation of drug loading and drug release from self-nanoemulsifying drug delivery system (SNEDDS). The % drug loading of FS in prepared liquid SNEDDS formulation was found to be 101.95%. The results of dissolution studies indicated 67.78% FS release in water at the end of 60 min.


Assuntos
Sistemas de Liberação de Medicamentos , Flavonóis/análise , Acetonitrilas/química , Cromatografia Líquida de Alta Pressão , Cromatografia de Fase Reversa , Ácidos Fosfóricos/química
18.
J Histochem Cytochem ; 68(9): 621-634, 2020 09.
Artigo em Inglês | MEDLINE | ID: mdl-32674674

RESUMO

Picrosirius red (PSR) staining is generally used to evaluate liver fibrosis; however, PSR sometimes causes nonspecific nuclear staining. In this study, we evaluated the ability of phosphomolybdic acid (PMA) pretreatment to prevent nonspecific nuclear staining by PSR. In a manual evaluation of 27 non-tumor samples from patients with hepatocellular carcinoma, nonspecific nuclear staining was observed in 3.7% of PMA-treated specimens, compared with 85.2% of untreated specimens. Conversely, computer-assisted image analysis (CAIA) identified nonspecific nuclear staining in 0% of PMA-treated samples, vs 44.4% of untreated samples. Surprisingly, after mounting, PMA-treated specimens exhibited a blue tinge because of molybdenum blue (MB) production following sunlight exposure or virtual slide scanning. Using UV cut film, MB production induced by sunlight exposure was prevented; however, the film did not prevent MB production during virtual slide scanning. Moreover, only blue light-emitting diode exposure resulted in a blue tinge in PMA solution. Our data indicated that PMA pretreatment is effective for evaluating liver fibrosis using CAIA. Meanwhile, improvements in virtual slide scanning protocols would directly improve the quality of PMA-pretreated specimens subjected to CAIA.


Assuntos
Compostos Azo/química , Núcleo Celular/química , Luz , Molibdênio/química , Ácidos Fosfóricos/química , Coloração e Rotulagem , Idoso , Feminino , Humanos , Processamento de Imagem Assistida por Computador , Masculino
19.
Food Chem ; 328: 127147, 2020 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-32497897

RESUMO

The reduction of the 3-monochloropropane-1,2-diol esters (3-MCPDE) and glycidyl esters (GE) was successfully achieved by the optimization of four processing parameters: phosphoric acid dosage, degumming temperature, bleaching earth dosage, and deodorization temperature by response surface methodology without the need for additional processing steps. The optimized processing conditions were 0.31% phosphoric acid dosage, 50 °C degumming temperature, 3% bleaching earth dosage, and 240 °C deodorization temperature. The optimization resulted in more than 80% and 65% reduction of 3-MCPDE and GE levels, respectively with color and FFA contents maintained in the acceptable range specified by Palm Oil Refiners Association of Malaysia. The optimized refining condition was transferred to macro scale refining units of 1 kg and 3 kg capacities to investigate its successful application during scale-up process.


Assuntos
Indústria de Processamento de Alimentos/métodos , Óleo de Palmeira/química , alfa-Cloridrina/química , Cor , Compostos de Epóxi/química , Ésteres , Qualidade dos Alimentos , Laboratórios , Malásia , Ácidos Fosfóricos/química , Propanóis/química , Temperatura , alfa-Cloridrina/análise
20.
Mikrochim Acta ; 187(6): 361, 2020 05 29.
Artigo em Inglês | MEDLINE | ID: mdl-32468206

RESUMO

A magnetic bead (MB)-based sandwich biorecognition reactions is combined with a gold nanoprobe-induced homogenous synthesis of molybdophosphate to develop a novel bioassay method for the electrochemical detection of the tumor biomarker of carcinoembryonic antigen (CEA). The nanoprobe is prepared through the specific loading of numerous alkaline phosphatase (ALP)-functionalized gold nanoparticles (Au NPs) on a double-stranded DNA (dsDNA) produced by the CEA aptamer-triggered hybridization chain reaction (HCR). Both the large amounts of PO43- produced by the ALP catalytic hydrolysis of pyrophosphate and the phosphate backbones of dsDNA can react with the added MoO42- to generate electroactive molybdophosphates. So, the gold nanoprobe was used for signal tracing of the sandwich bioassay of CEA at a constructed antibody-functionalized MB platform. The sensitive electrochemical measurement of molybdophosphate produced from the quantitatively captured nanoprobes at a carbon nanotube-modified electrode (measured at about 0.12 V vs. Ag/AgCl, 3 M KCl) enabled the convenient signal transduction of the method. Due to the dually enhanced synthesis of molybdophosphate by the HCR and multi-enzyme Au NP nanotags, this method shows a wide linear range from 0.05 pg mL-1 to 10 ng mL-1 along with a low detection limit of 0.027 pg mL-1. In addition, the MB-based biorecognition reaction and the homogeneous synthesis of molybdophosphate are much convenient in manipulations. These excellent performances decide the extensive application potentials of the method. Graphical abstract A magnetic bead-based bioassay method was simply developed for the electrochemical detection of carcinoembryonic antigen. The dually enhanced homogenous synthesis of molybdophosphate by hybridization chain reaction (HCR) and enzyme nanotags and the sensitive electrochemical measurement of molybdophosphate at a carbon nanotube (CNT)-electrode enable ultrasensitive signal transduction of the method.


Assuntos
Fosfatase Alcalina/química , Antígeno Carcinoembrionário/sangue , Técnicas Eletroquímicas/métodos , Molibdênio/química , Ácidos Fosfóricos/química , Anticorpos Imobilizados/imunologia , Aptâmeros de Nucleotídeos/química , Biomarcadores Tumorais/análise , Biomarcadores Tumorais/química , Antígeno Carcinoembrionário/química , Antígeno Carcinoembrionário/imunologia , DNA/química , Enzimas Imobilizadas/química , Ouro/química , Humanos , Imunoensaio/métodos , Separação Imunomagnética , Limite de Detecção , Nanopartículas Metálicas/química , Técnicas de Amplificação de Ácido Nucleico , Ácidos Fosfóricos/síntese química
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