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1.
J Sci Food Agric ; 100(3): 1204-1212, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31696521

RESUMO

BACKGROUND: The aim of this study was to select appropriate low-toxicity degreasing solvents to degrease black soldier fly (BSF, Hermetia illucens L.) larvae to prepare high-quality protein. Aqueous ethyl acetate was chosen as the solvent to extract BSF protein, and traditional solvents, such as petroleum ether, n-hexane, and isopropanol, were chosen as controls. RESULTS: The meal degreased by aqueous ethyl acetate (the volume ratio of ethyl acetate to water is 90 to 10, EA + W10) shows a high degreasing rate (29.04%), crude protein content (562.3 g kg-1 ), essential amino acid index (EAAI, 95.57), and digestible indispensable amino acid score (DIAAS, 85). The digestibility of the degreased meal samples in the simulated in vitro intestine can reach 76.52%. Thermodynamic analysis and the apparent morphology of the protein fragments showed that the meal degreased by EA + W10 exhibited thermodynamic stability, which suggests that using aqueous ethyl acetate as the degreasing solvent did not affect the nutritional value of the degreased meal. CONCLUSION: The results suggest that aqueous ethyl acetate (EA + W10) can be used as a novel solvent in the degreasing of BSF larvae meal to prepare high-quality protein with high EAAI and DIAAS and good digestibility. © 2019 Society of Chemical Industry.


Assuntos
Acetatos/química , Manipulação de Alimentos/métodos , Larva/química , Simuliidae/química , Animais , Temperatura Alta , Valor Nutritivo
2.
Chemosphere ; 239: 124740, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31527005

RESUMO

Bromochloroacetic acid is classified as one of the typical disinfection byproducts (DBPs). In this work, supported palladium catalysts on different supports (CeO2, Al2O3, SiO2 and activated carbon (AC)) (labelled as Pd/support) were synthesized via the deposition-precipitation method (D-P method) and their activities for the complete dehalogenation of bromochloroacetic acid by liquid phase catalytic hydrogenation were evaluated. Comprehensive characterizations of the catalysts were conducted by powder X-ray diffraction (XRD), transmission electron microscopy (TEM), point of zero charge (PZC), X-ray photoelectron spectroscopy (XPS) and CO chemisorption. Results indicated that the PZCs of the supports varied with each other. The stronger Pd-support interaction and higher Pd dispersion of Pd/CeO2 and Pd/Al2O3 than those of Pd/AC and Pd/SiO2 were confirmed by X-ray photoelectron spectroscopy and CO chemisorption. Pd/CeO2 had a higher ratio of positively charged Pd to metallic Pd (Pdn+/Pd0) than Pd/Al2O3 and Pd/AC due to a stronger metal-support interaction. Accordingly, a negligible bromochloroacetic acid conversion was observed on Pd/SiO2, whereas bromochloroacetic acid was found to be readily decomposed on Pd/CeO2, Pd/Al2O3 and Pd/AC. However, the dechlorination reaction could not further proceed on Pd/Al2O3 and Pd/AC catalysts after the bromine functionality was removed from bromochloroacetic acid. A complete dehalogenation of bromochloroacetic acid occurred only on Pd/CeO2. Furthermore, the dechlorination rate constants of monochloroacetic acid and bromochloroacetic acid over Pd(1.40)/CeO2 were 0.018 and 0.031 min-1 respectively, confirming an induced synergistic effect due to the existence of bromine atoms. It was worth noting that a stepwise-concerted pathway was verified during the liquid phase catalytic hydrodehalogenation of bromochloroacetic acid.


Assuntos
Acetatos/química , Cério/química , Paládio/química , Poluentes Químicos da Água/química , Monóxido de Carbono/química , Catálise , Carvão Vegetal , Desinfetantes/química , Halogenação , Hidrogenação , Microscopia Eletrônica de Transmissão , Espectroscopia Fotoeletrônica , Dióxido de Silício/química , Difração de Raios X
3.
Acta Crystallogr C Struct Chem ; 75(Pt 12): 1658-1665, 2019 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-31802756

RESUMO

Because of its versatile coordination modes and strong coordination ability, the mercaptoacetic acid substituted 1,2,4-triazole 2-{[5-(pyridin-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl}acetic acid (H2L) was synthesized and characterized. Treatment of H2L with cobalt and nickel acetate afforded the dinuclear complexes {µ-3-[(carboxylatomethyl)sulfanyl]-5-(pyridin-2-yl)-4H-1,2,4-triazol-4-ido-κ2N1,N5:N2,O}bis[aqua(methanol-κO)cobalt(II)] methanol disolvate, [Co2(C9H6N4O2S)2(CH3OH)2(H2O)2]·2CH3OH (1), and {µ-3-[(carboxylatomethyl)sulfanyl]-5-(pyridin-2-yl)-4H-1,2,4-triazol-4-ido-κ2N1,N5:N2,O}bis[diaquanickel(II)] methanol disolvate dihydrate, [Ni2(C9H6N4O2S)2(H2O)4]·2CH3OH·2H2O (2), respectively. Complex 1 crystallized in the monoclinic space group P21/c, while 2 crystallized in the tetragonal space group I41/a. Single-crystal X-ray diffraction studies revealed that H2L is doubly deprotonated and acts as a tetradentate bridging ligand in complexes 1 and 2. For both of the obtained complexes, extensive hydrogen-bond interactions contribute to the formation of their three-dimensional supermolecular structures. Hirshfeld surface analysis was used to illustrate the intermolecular interactions. Additionally, the urease inhibitory activities of 1, 2 and H2L were investigated against jack bean urease, where the two complexes revealed strong urease inhibition activities.


Assuntos
Acetatos/química , Cobalto/farmacologia , Complexos de Coordenação/química , Níquel/farmacologia , Compostos Organometálicos/química , Tioglicolatos/farmacologia , Urease/antagonistas & inibidores , Urease/química , Cobalto/química , Cristalografia por Raios X , Ligações de Hidrogênio , Ligantes , Modelos Moleculares , Níquel/química , Tioglicolatos/química
4.
Phys Chem Chem Phys ; 21(41): 22849-22856, 2019 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-31612167

RESUMO

Hyperpolarized metabolites are very attractive contrast agents for in vivo magnetic resonance imaging studies enabling early diagnosis of cancer, for example. Real-time production of concentrated solutions of metabolites is a desired goal that will enable new applications such as the continuous investigation of metabolic changes. To this end, we are introducing two NMR experiments that allow us to deliver high levels of polarization at high concentrations (50 mM) of an acetate precursor (55% 13C polarization) and acetate (17% 13C polarization) utilizing 83% para-state enriched hydrogen within seconds at high magnetic field (7 T). Furthermore, we have translated these experiments to a portable low-field spectrometer with a permanent magnet operating at 1 T. The presented developments pave the way for a rapid and affordable production of hyperpolarized metabolites that can be implemented in e.g. metabolomics labs and for medical diagnosis.


Assuntos
Técnicas de Química Analítica/métodos , Meios de Contraste/síntese química , Campos Magnéticos , Acetatos/química , Acetatos/metabolismo , Meios de Contraste/química , Hidrogênio/química , Imagem por Ressonância Magnética/instrumentação
5.
J Mass Spectrom ; 54(10): 791-801, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31652381

RESUMO

Supercritical fluid chromatography (SFC) has experienced a particular revival in recent years thanks to the development of robust and efficient commercial systems. Because of its physico-chemical properties, supercritical carbon dioxide (CO2 ) mixed with cosolvents and additives is particularly suitable for SFC to allow the elution of compounds of different polarities and more particularly complex lipids. Hyphenation with mass spectrometry (MS) is increasingly described in the literature but still requires many further developments in order to be as user-friendly as coupling with liquid chromatography. The basic concepts of SFC and MS hyphenation will be first considered. Then a representative example of method development in lipidomics will be introduced. In conclusion, the challenges and future needs in this field of research will be discussed.


Assuntos
Cromatografia com Fluido Supercrítico/métodos , Lipídeos/análise , Espectrometria de Massas em Tandem/métodos , Acetatos/química , Técnicas Biossensoriais , Dióxido de Carbono/química , Limite de Detecção , Reprodutibilidade dos Testes , Solventes/química
6.
Chem Commun (Camb) ; 55(82): 12348-12351, 2019 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-31559401

RESUMO

A multimeric MRI contrast agent based on the closo-borane motif is reported. Twelve copies of a modified AAZTA chelate with an alkyne end group are appended on an azide-functionalized closo-borane motif using Cu(i) catalyzed click chemistry. The presence of two water molecules on the Gd-bound AAZTA chelate results in high relaxivity for the closomer in vitro/in vivo.


Assuntos
Acetatos/química , Azepinas/química , Boranos/química , Quelantes/química , Meios de Contraste/química , Complexos de Coordenação/química , Imagem por Ressonância Magnética , Acetatos/síntese química , Azepinas/síntese química , Boranos/síntese química , Quelantes/síntese química , Meios de Contraste/síntese química , Complexos de Coordenação/síntese química , Estrutura Molecular
7.
Cell Mol Biol (Noisy-le-grand) ; 65(6): 6-11, 2019 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-31472041

RESUMO

In traditional medicine, Ficus carica (also known as fig) latex is recognized as a remedy with various therapeutic effects. In the present study we investigated the antitumor activity of Ficus carica extracts and latex. We evaluated the effects of increasing concentrations of Ficus carica extracts and latex on HCT-116 and HT-29 human colorectal cell proliferation using MTT assay and apoptosis induction by evaluating PARP cleavage by Western blot analysis. Peel, pulp, leaves, whole fruit and latex extracts of Ficus carica exerted significant antiproliferative effects on HCT-116 (IC50 values 239, 343, 177, 299, 206 µg/ml) and HT-29 cells (IC50 values 207, 249, 230, 261, 182 µg/ml) after 48h of treatment. Furthermore, treatment with different extracts of Ficus carica induced apoptosis in both HT-29 and HCT-116 cancer cells. Leaves and latex extracts of Ficus carica showed the strongest antiproliferative activities. Overall, our results showed that these natural products are strong apoptosis inducers which suggest their use of for therapeutic purposes.


Assuntos
Antineoplásicos/farmacologia , Neoplasias Colorretais/patologia , Ficus/química , Acetatos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Extratos Vegetais/farmacologia , Folhas de Planta/química
8.
Artigo em Inglês | MEDLINE | ID: mdl-31479387

RESUMO

An extraction method based on metal-organic framework has been developed and applied to acetanilide herbicides, including metazachlor, propanil, pretilachlor, and butachlor, in black beans, red beans, and kidney beans. The acetanilide herbicides are extracted with a mixture of ethyl acetate and n-hexane. The extract solution is absorbed and purified with metal-organic framework MIL-101 (Zn). The separation and determination of four acetanilide herbicides were implemented by high-performance liquid chromatography. The experimental parameters were evaluated by a univariate method and orthogonal experiments. The presented method can obtain effective extraction and purification. The detection limits for metazachlor, propanil, pretilachlor, and butachlor were 0.58, 0.90, 1.78 and 1.18 µg/kg, respectively. The average recoveries of the acetanilide herbicides at spiked concentrations of 10, 50, and 100 µg/kg ranged from 86.9% to 119.0%, and relative standard deviations were equal to or lower than 2.80%.


Assuntos
Acetanilidas/isolamento & purificação , Herbicidas/isolamento & purificação , Estruturas Metalorgânicas/química , Acetanilidas/química , Acetatos/química , Adsorção , Animais , Canavalia/química , Herbicidas/química , Hexanos/química , Tamanho da Partícula , Phaseolus/química
9.
Microb Cell Fact ; 18(1): 151, 2019 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-31484572

RESUMO

BACKGROUND: Escherichia coli (E. coli) is a bacteria that is widely employed in many industries for the production of high interest bio-products such as recombinant proteins. Nevertheless, the use of E. coli for recombinant protein production may entail some disadvantages such as acetate overflow. Acetate is accumulated under some culture conditions, involves a decrease in biomass and recombinant protein production, and its metabolism is related to protein lysine acetylation. Thereby, the carbon and nitrogen sources employed are relevant factors in cell host metabolism, and the study of the central metabolism of E. coli and its regulation is essential for optimizing the production of biomass and recombinant proteins. In this study, our aim was to find the most favourable conditions for carrying out recombinant protein production in E. coli BL21 using two different approaches, namely, manipulation of the culture media composition and the deletion of genes involved in acetate metabolism and Nε-lysine acetylation. RESULTS: We evaluated protein overexpression in E. coli BL21 wt and five mutant strains involved in acetate metabolism (Δacs, ΔackA and Δpta) and lysine acetylation (ΔpatZ and ΔcobB) grown in minimal medium M9 (inorganic ammonium nitrogen source) and in complex TB7 medium (peptide-based nitrogen source) supplemented with glucose (PTS carbon source) or glycerol (non-PTS carbon source). We observed a dependence of recombinant protein production on acetate metabolism and the carbon and nitrogen source employed. The use of complex medium supplemented with glycerol as a carbon source entails an increase in protein production and an efficient use of resources, since is a sub-product of biodiesel synthesis. Furthermore, the deletion of the ackA gene results in a fivefold increase in protein production with respect to the wt strain and a reduction in acetate accumulation. CONCLUSION: The results showed that the use of diverse carbon and nitrogen sources and acetate metabolism knockout strains can redirect E. coli carbon fluxes to different pathways and affect the final yield of the recombinant protein bioprocess. Thereby, we obtained a fivefold increase in protein production and an efficient use of the resources employing the most suitable strain and culture conditions.


Assuntos
Acetatos/metabolismo , Carbono/metabolismo , Escherichia coli/crescimento & desenvolvimento , Escherichia coli/metabolismo , Nitrogênio/metabolismo , Proteínas Recombinantes/biossíntese , Acetatos/química , Acetilação , Carbono/química , Meios de Cultura/química , Proteínas de Escherichia coli/biossíntese , Lisina/metabolismo , Nitrogênio/química , Engenharia de Proteínas , Processamento de Proteína Pós-Traducional
10.
Med Sci Monit Basic Res ; 25: 179-186, 2019 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-31451678

RESUMO

BACKGROUND With the continued demand for new, effective, and safe endodontic therapies, the aim of this study was assessment of efficiency of the ethyl acetate (EthOAc) extract of Tanacetum vulgare (L.) against Candida albicans. MATERIAL AND METHODS The antifungal effectiveness of the EthOAc extract of T. vulgare was determined using the agar disk diffusion method. The inhibition zones induced by the EthOAc extract were compared after 5 minutes, 60 minutes, and 24 hours to those induced by standard solutions (2% chlorhexidine, saturated calcium hydroxide, and 2% sodium hypochlorite). Statistical analysis of the results was performed using the Kruskal-Wallis test and one-way ANOVA. RESULTS The inhibition zone of chlorhexidine against C. albicans was 30.3-19.3 mm, but in combination with EthOAc extract (100 mg/mL) of T. vulgare, this inhibition was from 32.7-30 mm, indicating that this combination exerted a marked synergistic effect against C. albicans. The inhibition zone of sodium hypochlorite (69.7-65 mm) was higher than the inhibition zone of EthOAc extract and chlorhexidine. The combination of EthOAc extract with sodium hypochlorite resulted in a loss of antifungal activity. Furthermore, the activity of the EthOAc extract against C. albicans was decreased after mixing the extract with dentine at a concentration of 25 mg/50 µL (30.3-20.7 mm). The EthOAc extract did not show a genotoxic effect on lymphocyte cells. CONCLUSIONS The EthOAc extract of T. vulgare may be a useful tool to discover natural bioactive agents that have antifungal activity against C. albicans and could be used as endodontic therapies.


Assuntos
Acetatos/química , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Extratos Vegetais/farmacologia , Tanacetum/química , Candida albicans/crescimento & desenvolvimento , Dentina/metabolismo , Sinergismo Farmacológico , Humanos , Linfócitos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Mutagênicos/toxicidade
11.
Int J Pharm ; 569: 118583, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31376468

RESUMO

Nanoparticles are being developed for a wide range of medical applications such as, controlled release, drug delivery systems or imagery, theranostics, implants…. For the moment, there is no legal definition of nanoparticles or nanomaterials for therapeutic use. The specific case of gold nanoparticles is not an exception: their current definition as nanoparticle material does not correspond to classic pharmaceutical ingredients as described in Pharmacopoeias. In this study, more than 30 different batches of citrate stabilized gold nanoparticles (AuNP) were synthesized and analyzed thanks to both classical approaches (UV-Vis spectrophotometry, dynamic light scattering coupled or not to electrophoresis …) and capillary zone electrophoresis (CZE) coupled to diode array detection to assess their purity and impurity profiles. These techniques led to the beginning of defined specifications, a key step for the use of gold nanoparticles as pharmaceutical ingredients. CZE was demonstrated suitable to evaluate a batch-to-batch quality control, to monitor the purification processes and to follow the stability of 18 different batches for 20 days. Finally, commercially available AuNP samples were tested and the results compared to the provided certificates of analysis.


Assuntos
Ácido Cítrico/química , Ouro/química , Nanopartículas Metálicas/química , Acetatos/química , Estabilidade de Medicamentos , Eletroforese Capilar , Poliaminas/química , Controle de Qualidade
12.
Talanta ; 205: 120107, 2019 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-31450415

RESUMO

A comprehensive structural characterization of the complex family of isomeric forms related to Oleuropein aglycone (OA) detected in virgin olive oil (VOO) was performed by reverse phase liquid chromatography with electrospray ionization and Fourier-transform mass spectrometry (RPLC-ESI-FTMS), integrated by enzymatic/chemical reactions performed on Oleuropein, the natural precursor of OA. First, some of the OA-related isomers typically observed in VOO extracts were generated upon enzymatic hydrolysis of the glycosidic linkage of Oleuropein. This step mimicked the process occurring during olive drupes crushing in the first stage of oil production. The incubation of the enzymatic reaction mixture at a more acidic pH was subsequently performed, to simulate the conditions of olive paste malaxation during oil production. As a result, further isomeric forms were generated and the complex chromatographic profile typically observed for OA in olive oil extracts, including at least 13 different peaks/bands/groups of peaks, was carefully reproduced. Each of those chromatographic features could be subsequently assigned to specific types of OA-related isomers, belonging to one of four structurally different classes. Specifically, diastereoisomers/geometrical isomers corresponding to two different types of open-structure forms and to as many types of closed-structure, di-hydropyranic forms of OA, characterized by the presence of one or two carbonyl groups, according to the case, were evidenced. In addition, the presence of stable enolic/dienolic tautomers, providing an indirect structural confirmation for some OA isomers, was ascertained through RPLC-ESI-FTMS analyses performed under H/D exchange conditions, i.e. in the presence of deuterated water as one of the mobile phase solvents.


Assuntos
Acetatos/análise , Azeite de Oliva/análise , Piranos/análise , Acetatos/química , Acetatos/isolamento & purificação , Cromatografia de Fase Reversa/métodos , /isolamento & purificação , Deutério , Análise de Fourier , Hidrólise , Iridoides/química , Isomerismo , Extração Líquido-Líquido , Olea/química , Piranos/química , Piranos/isolamento & purificação , Espectrometria de Massas em Tandem/métodos , beta-Glucosidase/química
13.
Mol Cell Biochem ; 460(1-2): 175-193, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31367889

RESUMO

The upsurge of marine-derived therapeutics for cancer treatment is evident, with many drugs in clinical use and in clinical trials. Seaweeds harbor large amounts of polyphenols and their anti-cancer benefit is linear to their anti-oxidant activity. Our studies identified three superlative anti-cancer seaweed polyphenol drug candidates (SW-PD). We investigated the acquisition of oncogenic burden in radiation-resilient pancreatic cancer (PC) that could drive tumor relapse, and elucidated the efficacy of SW-PD candidates as adjuvants in genetically diverse in vitro systems and a mouse model of radiation-residual disease. QPCR profiling of 88 oncogenes in therapy-resilient PC cells identified a 'shared' activation of 40 oncogenes. SW-PD pretreatment inflicted a significant mitigation of acquired (shared) oncogenic burden, in addition to drug- and cell-line-specific repression signatures. Tissue microarray with IHC of radiation-residual tumors in mice signified acquired cellular localization of key oncoproteins and other critical architects. Conversely, SW-PD treatment inhibited the acquisition of these critical drivers of tumor genesis, dissemination, and evolution. Heightened death of resilient PC cells with SW-PD treatment validated the translation aspects. The results defined the acquisition of oncogenic burden in resilient PC and demonstrated that the marine polyphenols effectively target the acquired oncogenic burden and could serve as adjuvant(s) for PC treatment.


Assuntos
Organismos Aquáticos/química , Carcinogênese/patologia , Neoplasias Pancreáticas/patologia , Polifenóis/farmacologia , Acetatos/química , Animais , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Progressão da Doença , Humanos , Camundongos Nus , Proteínas de Neoplasias/metabolismo , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/radioterapia , Polifenóis/uso terapêutico , Alga Marinha/química
14.
Chemosphere ; 237: 124439, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31376693

RESUMO

Dielectric barrier discharge (DBD) has been widely used as end-of-pipe technology to degrade low-concentration volatile organic compound (VOC) emissions. In this work, the influence of DBD conditions including discharge voltage, VOC residence time in DBD plasma, VOC initial concentration and synergistic effect of multiple VOC mixing on the decomposition efficiency of three VOCs (toluene, ethyl acetate and acetone) were investigated systematically. One focus of this work was to investigate size distribution and chemical composition of aerosol by-products. The results suggested that high discharge voltage, long residence time and low VOC initial concentration would increase VOC removal ratio and their conversion to CO2. Among the three VOCs, toluene was easiest to form particles with a mode diameter between 40 and 100 nm and most difficult to be decomposed completely to CO2. Maximum aerosol yield from toluene was observed to account for 13.1 ±â€¯1.0% of initial concentration (400 ppm) in the condition of discharge voltage 6 kV and residence time 0.52 s. Gas chromatography-mass spectrometry analysis showed that non-nitrogen containing benzene derivatives, nitrophenol derivatives and amines were the main components of toluene aerosol by-products. For ethyl acetate and acetone, aerosols could only be produced in the condition of high discharge voltages (>7.5 kV) and long gas residence time (≥0.95 s) with a bimodal distribution below 20 nm. When the mixture of three VOCs was fed into the plasma, we observed a strong synergistic effect that led to higher VOC removal ratio, but lower conversion of decomposed VOCs to CO2 and aerosols.


Assuntos
Acetatos/química , Acetona/química , Aerossóis/química , Tolueno/química , Compostos Orgânicos Voláteis/química , Dióxido de Carbono/química , Recuperação e Remediação Ambiental/métodos , Cromatografia Gasosa-Espectrometria de Massas , Tamanho da Partícula , Tolueno/análise , Compostos Orgânicos Voláteis/análise
15.
J Pharm Biomed Anal ; 175: 112793, 2019 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-31377652

RESUMO

A simple and sensitive method was developed for separation and characterization of seventeen impurities from commercial latamoxef sodium for injection by liquid chromatography combined with electrospray ionization and QTOF mass spectrometer (LC-ESI-QTOF MS). The chromatographic separation was performed on a Boston Green ODS-AQ C18 column (250 mm × 4.6 mm, 5 µm) under gradient mode using binary mobile phase: (A) ammonium acetate (10 mM)-methanol (99:1, v/v) and (B) ammonium acetate (10 mM)-methanol (70:30, v/v). Based on tandem multistage MS and high resolution MS data, the molecular formulas and structures of unknown impurities were inferred. A plausible formation mechanism of impurities was also proposed. In addition, the fragmentation regularity of degraded impurities in positive-ion mode was summarized.


Assuntos
Íons/química , Moxalactam/química , Sódio/química , Acetatos/química , Cromatografia Líquida/métodos , Contaminação de Medicamentos , Metanol/química , Espectrometria de Massas por Ionização por Electrospray/métodos
16.
Oxid Med Cell Longev ; 2019: 6764756, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31379989

RESUMO

Hyperactivation of microglia, the resident innate immune cells of the central nervous system, exacerbates various neurodegenerative disorders, including Parkinson's disease (PD). Parkinson's disease is generally characterized by a severe loss of dopaminergic neurons in the nigrostriatal pathway, with substantial neuroinflammation and motor deficits. This was experimentally replicated in animal models, using neurotoxins, i.e., LPS (lipopolysaccharides) and MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine). Salicornia europaea L. (SE) has been used as a dietary supplement in Korea and Europe for several years, due to its nutritional and therapeutic value. In this study, we intend to investigate the antineuroinflammatory and anti-PD-like effects of the bioactive fraction/candidate of the SE extract. Initially, we screened various fractions of SE extract using an in vitro antioxidant assay. The optimal fraction was investigated for its in vitro antineuroinflammatory potential in LPS-stimulated BV-2 microglial cells and in vivo anti-PD-like potential in MPTP-intoxicated mice. Subsequently, to identify the potential candidate responsible for the elite therapeutic potential of the optimal fraction, we conducted antioxidant activity-guided isolation and purification; the bioactive candidate was structurally characterized using nuclear magnetic resonance spectroscopy and chromatographic techniques and further investigated for its in vitro antioxidative and antineuroinflammatory potential. The results of our study indicate that SE-EA and its bioactive candidate, Irilin B, effectively alleviate the deleterious effect of microglia-mediated neuroinflammation and promote antioxidative effects. Thus, they exhibit potential as therapeutic candidates against neuroinflammatory and oxidative stress-mediated PD-like neurodegenerative complications.


Assuntos
Chenopodiaceae/química , Isoflavonas/farmacologia , Intoxicação por MPTP/prevenção & controle , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/química , Acetatos/química , Animais , Antioxidantes/metabolismo , Chenopodiaceae/metabolismo , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Modelos Animais de Doenças , Isoflavonas/uso terapêutico , Lipopolissacarídeos/farmacologia , Intoxicação por MPTP/metabolismo , Intoxicação por MPTP/patologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Microglia/citologia , Microglia/efeitos dos fármacos , Microglia/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/uso terapêutico , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Espécies Reativas de Oxigênio/metabolismo
17.
Environ Sci Pollut Res Int ; 26(27): 27761-27768, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31342350

RESUMO

Ozone (O3) is an adverse environmental factor posing damage to ornamental plants. Thus, it is important to seek an effective way of enhancing plant tolerance to O3-induced damage. Methyl jasmonate (MJ) and melatonin (MT) are plant growth regulators (PGRs) involved in plant abiotic stress responses. In this study, compared with the control group of plants without ozone, the influence of exogenous MJ (0, 10, 50, 100, and 150 µM) and MT (0, 0.1, 0.5, 2.5, and 12.5 µM) on the resistance of Malus crabapple 'Hong Jiu' was evaluated under O3 stress (100 ± 10 nL/L for 3 h). Our data revealed that levels of MDA were significantly enhanced following O3 treatment compared with plants without O3. O3 induced the activities of antioxidant enzymes and the accumulation of non-enzymatic antioxidants. While lower malondialdehyde (MDA) content, greater activities of antioxidant enzymes, and higher levels of soluble protein and non-enzymatic antioxidants were observed in PGRs-pretreated plants than in non-PGRs-pretreated plants under O3 stress. Based on the above results and air pollution tolerance index (APTI), an exogenous supply of MJ and MT to Malus crabapple 'Hong Jiu' seedlings was protective for O3-induced toxicity. The present study provides new insights into the mechanisms of MJ and MT amelioration of O3-induced oxidative stress damages in Malus crabapple 'Hong Jiu.'


Assuntos
Acetatos/química , Antioxidantes/química , Ciclopentanos/química , Malus/metabolismo , Melatonina/química , Oxilipinas/química , Ozônio/toxicidade , Acetatos/metabolismo , Antioxidantes/metabolismo , Ciclopentanos/metabolismo , Malondialdeído/metabolismo , Malus/química , Melatonina/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Oxilipinas/metabolismo , Plântula/efeitos dos fármacos , Estresse Fisiológico/efeitos dos fármacos
18.
Eur J Med Chem ; 179: 608-622, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31279294

RESUMO

Based on an old phenoxyacetic acid scaffold, CPU014 (compound 14) has been identified as a superior agonist by comprehensive exploration of structure-activity relationship. In vitro toxicity study suggested that CPU014 has lower risk of hepatotoxicity than TAK-875. During acute toxicity study (5-500 mg/kg), a favorable therapeutic window of CPU014 was observed by evaluation of plasma profiles and liver slices. Moreover, CPU014 promotes insulin secretion in a glucose-dependent manner, while no GLP-1 secretion has been enhanced. Other than good pharmacokinetic properties, CPU014 significantly improved glucose tolerance both in normal and diabetic models without the risk of hypoglycemia. These subversive findings provided a safer candidate CPU014, which is currently in preclinical study to assess its potential for the treatment of diabetes.


Assuntos
Acetatos/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Desenho de Drogas , Hipoglicemiantes/farmacologia , Receptores Acoplados a Proteínas-G/agonistas , Acetatos/síntese química , Acetatos/química , Animais , Diabetes Mellitus Tipo 2/metabolismo , Relação Dose-Resposta a Droga , Teste de Tolerância a Glucose , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos ICR , Estrutura Molecular , Ratos , Ratos Sprague-Dawley , Receptores Acoplados a Proteínas-G/metabolismo , Relação Estrutura-Atividade
19.
Int J Mol Sci ; 20(13)2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31266224

RESUMO

Extracts from the Nepenthes plant have anti-microorganism and anti-inflammation effects. However, the anticancer effect of the Nepenthes plant is rarely reported, especially for breast cancer cells. Here, we evaluate the antitumor effects of the ethyl acetate extract of Nepenthes thorellii x (ventricosa x maxima) (EANT) against breast cancer cells. Cell viability and flow cytometric analyses were used to analyze apoptosis, oxidative stress, and DNA damage. EANT exhibits a higher antiproliferation ability to two breast cancer cell lines (MCF7 and SKBR3) as compared to normal breast cells (M10). A mechanistic study demonstrates that EANT induces apoptosis in breast cancer cells with evidence of subG1 accumulation and annexin V increment. EANT also induces glutathione (GSH) depletion, resulting in dramatic accumulations of reactive oxygen species (ROS) and mitochondrial superoxide (MitoSOX), as well as the depletion of mitochondrial membrane potential (MMP). These oxidative stresses attack DNA, respectively leading to DNA double strand breaks and oxidative DNA damage in γH2AX and 8-oxo-2'deoxyguanosine (8-oxodG) assays. Overall these findings clearly revealed that EANT induced changes were suppressed by the ROS inhibitor. In conclusion, our results have shown that the ROS-modulating natural product (EANT) has antiproliferation activity against breast cancer cells through apoptosis, oxidative stress, and DNA damage.


Assuntos
Acetatos/química , Antineoplásicos Fitogênicos/farmacologia , Neoplasias da Mama/metabolismo , Caryophyllales/química , Espécies Reativas de Oxigênio/metabolismo , Anexina A5/metabolismo , Antineoplásicos Fitogênicos/química , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Dano ao DNA , Feminino , Humanos , Células MCF-7 , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos
20.
Curr Pharm Biotechnol ; 20(11): 934-944, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31264545

RESUMO

OBJECTIVE: Calcium acetate (Ca(CH3COO)2) is commonly used in calcium supplement for medicine, which is used as an auxiliary agent to treat osteoporosis. An effervescent granule is widely used in medical industry due to its palatability. The purpose of this study is to develop a new preparation of compound effervescent granule of the biological calcium acetate (Ca(CH3COO)2 effervescent granule), overcoming the disadvantages of the previous other dosage forms of calcium and thus enhancing the therapeutic efficacy. METHODS: The biological Ca(CH3COO)2 effervescent granule was prepared by the wet granulation method. The formulation was optimized by the orthogonal experiment. The effervescent base was comprised of various amounts of citric acid and sodium bicarbonate. Other ingredients were added for optimal performance of effervescent granule. The performed Ca(CH3COO)2 effervescent granule was evaluated for the particle size, repose angle, pH value of solution, calcium acetate content and effervescence time. The in vivo effects of Ca(CH3COO)2 effervescent granule on the bone microarchitecture were investigated via Micro-CT detection, and the serum calcium level was also investigated. RESULTS: The optimized formulation of the biological Ca(CH3COO)2 effervescent granules was composed of calcium acetate, citric acid, sodium bicarbonate, PEG6000, aspartame, PVP ethanol solution, lactose and vitamin D. Our findings reveal that this biological Ca(CH3COO)2 effervescent granule exhibited prominent effect on preventing the bone-mass loss and did better in enhancing the bone microarchitecture compared to the other calcium preparations. CONCLUSION: The biological Ca(CH3COO)2 effervescent granule is a novel dosage form among so many kinds of calcium preparations. It may perform better functions in the dairy calcium supplement.


Assuntos
Acetatos/química , Suplementos Nutricionais , Composição de Medicamentos/métodos , Disponibilidade Biológica , Compostos de Cálcio/química , Ácido Cítrico/química , Formas de Dosagem , Tamanho da Partícula , Polietilenoglicóis/química , Bicarbonato de Sódio/química
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