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1.
J Enzyme Inhib Med Chem ; 32(1): 1-11, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28776447

RESUMO

This paper reports the MEPS-HPLC-DAD method for the simultaneous determination of 12 azole drugs (bifonazole, butoconazole, clotrimazole, econazole, itraconazole, ketoconazole, miconazole, posaconazole, ravuconazole, terconazole, tioconazole and voriconazole) administered to treat different systemic and topical fungal infections, in biological samples. Azole drugs separation was performed in 36 min. The analytical method was validated in the ranges as follows: 0.02-5 µg mL-1 for ravuconazole; 0.2-5 µg mL-1 for terconazole; 0.05-5 µg mL-1 for the other compounds. Human plasma and urine were used as biological samples during the analysis, while benzyl-4-hydroxybenzoate was used as an internal standard. The precision (RSD%) and trueness (Bias%) values fulfill with International Guidelines requirements. To the best of our knowledge, this is the first HPLC-DAD procedure coupled to MEPS, which provides the simultaneous analysis of 12 azole drugs, available in the market, in human plasma and urine. Moreover, the method was successfully applied for the quantitative determination of two model drugs (itraconazole and miconazole) after oral administration in real samples.


Assuntos
Imidazóis/análise , Microextração em Fase Sólida , Triazóis/análise , Adsorção , Cromatografia Líquida de Alta Pressão , Estrutura Molecular
2.
Front Pharmacol ; 8: 290, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28588492

RESUMO

In this work, the biological and chemical fingerprints of three extracts (ethyl acetate, methanol, and water) from two Potentilla species (Potentilla reptans and P. speciosa) were investigated. Antioxidant, enzyme inhibitory, and cytotoxic activities were performed for the biological fingerprint. For the chemical characterization, total bioactive components, and individual phenolic components were determined using photometric and HPLC methods, respectively. The main identified phenolic compounds in these extracts were rutin and catechin. Methanol and water extracts contained the highest total phenolic and flavonoid content. The results of antioxidant assays showed that methanol and water extracts displayed higher antioxidant activity compared to the ethyl acetate extract. Generally, methanol and water extracts exhibited higher biological activities correlated with higher levels the bioactive components. For P. speciosa, the methanol extract exhibited the highest enzyme inhibitory activity (except BChE inhibitory activity). P. reptans exhibited also high antiproliferative activity against MCF-7 cells whilst P. speciosa had weak to moderate activity against both of A549 and MCF-7 cell lines. The results suggest that Potentilla species could be potential candidates for developing new phyto-pharmaceuticals and functional ingredients.

3.
Food Chem ; 232: 114-123, 2017 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-28490054

RESUMO

Colour is the first organoleptic property that consumers appreciate of a foodstuff. In blueberry (Vaccinium spp.) fruits, the anthocyanins are the principal pigments determining the colour as well as many of the beneficial effects attributed to this functional food. Commercial blueberry-derived products represent important sources of these healthy molecules all year round. In this study, blueberries were produced into purees comparing two homogenization methods and further heated following different thermal treatments. All the supernatants of the homogenates were monitored for pH. Then, the hydroalcoholic extracts of the same samples were characterized by CIELAB and HPLC-DAD analyses. These analytical techniques provide complementary information on fruit pigments content as a whole and on quali-quantitative profile of the single bioactive colorants. These data could be very interesting to know the best manufacturing procedure to prepare blueberry-derived products, well accepted by the consumers, while maintaining their healthy properties unaltered.


Assuntos
Antocianinas , Mirtilos Azuis (Planta) , Extratos Vegetais , Cromatografia Líquida de Alta Pressão , Cor , Frutas , Vaccinium
4.
Food Chem Toxicol ; 107(Pt B): 554-564, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28366844

RESUMO

In this study, we evaluated the nutraceutical potential of Juglans regia L. (a dietary supplement and food-additive) by evaluating the in-vitro anti-diabetic potential and by assessing the in-vivo anti-hyperglycaemic, anti-hyperlipidaemic, and organ-protective effects of freshly-dried and powdered leaves of J. regia L. in diabetic rats. In the in-vivo experiments, dry powder of J. regia L. leaf (25, 50 and 100 mg/kg) was administered orally, twice daily (9.00 a.m. and 5 p.m.) to streptozocin-induced diabetic rats over a period of 28 days, during which body weight and blood glucose were monitored weekly. At the end of the experimental period, animals were sacrificed, blood was taken for assessment of lipid profile, antioxidant activity and liver/kidney biochemistry; while samples of the pancreas, liver and kidneys were fixed, processed, sectioned, and stained for general histology. Phytochemical evaluations of three extracts were carried out using HPLC-PDA validated procedures, while enzyme-inhibitory potentials were tested against α-amylase and α-glucosidase. In-vivo assays showed that twice-daily administration of J. regia L. leaf resulted in weight gain, glycaemic control, reversal of dyslipidaemia and biochemical evidences of liver/kidney injury, and protection against pancreas, liver and kidney tissue injury.


Assuntos
Diabetes Mellitus/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Juglans/química , Extratos Vegetais/administração & dosagem , Animais , Glicemia/metabolismo , Diabetes Mellitus/enzimologia , Diabetes Mellitus/metabolismo , Suplementos Nutricionais/análise , Avaliação Pré-Clínica de Medicamentos , Humanos , Masculino , Folhas de Planta/química , Ratos , Ratos Wistar , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
5.
J Enzyme Inhib Med Chem ; 32(1): 60-67, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27774819

RESUMO

The current study was carried out to evaluate multicomponent pattern, biological and enzymatic activities of seven Asphodeline taxa root extracts as useful ingredients, due to the fact that these plants are commonly used as traditional food supplements in Turkish regions. The extracts were characterized for free anthraquinones and phenolics to obtain a specific chemical fingerprint useful for quality control. These analyzes were coupled to biological and enzymatic activities in order to obtain comprehensive information of the natural product. Free anthraquinones and phenolics were determined using validated HPLC-PDA methods. Antioxidant properties were determined by different procedures including free radical scavenging, reducing power, phosphomolybdenum and metal chelating assays. Ames assay was performed to evaluate mutagenic/antimutagenic properties. Enzyme inhibitory activities were tested against cholinesterase, tyrosinase, α-amylase and α-glucosidase. From the herein reported results, Asphodeline could be valuable for the production of bioactive products or food supplements for cosmetic and pharmaceutical industries.


Assuntos
Asparagales/química , Asparagales/classificação , Cromatografia Líquida de Alta Pressão , alfa-Amilases/antagonistas & inibidores
6.
J Enzyme Inhib Med Chem ; 31(sup3): 110-116, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27444953

RESUMO

We developed and validated an analytical method based on microextraction packed sorbent (MEPS) and high-performance liquid chromatography (HPLC) coupled to photodiode array (PDA) detector to simultaneously quantify multiple nonsteroidal anti-inflammatory drugs (NSAIDs) and fluoroquinolones (FLQs), which may provide as combination several adverse reactions in nephrology and neurology. The linearity range from LOQs (0.1 µg/mL) to 10 µg/mL, and LODs values were 0.03 µg/mL for both NSAIDs and FLQs. The validation was performed according to international guidelines and the accuracy was tested measuring the precision, intermediate precision and trueness. The drugs stability was tested under different storage conditions (+4 °C and -20 °C) and after three different cycles of freezing and thawing. The method can be a suitable tool to simultaneously detect a possible association of drugs in human biological samples and provide several potentialities for clinical applications, bioequivalence studies, pharmacodynamics and toxicodynamics of different pharmaceutical dosage forms showing NSAIDs and FLQs.


Assuntos
Anti-Inflamatórios não Esteroides/sangue , Anti-Inflamatórios não Esteroides/urina , Fluoroquinolonas/sangue , Fluoroquinolonas/urina , Microextração em Fase Líquida , Anti-Inflamatórios não Esteroides/administração & dosagem , Cromatografia Líquida de Alta Pressão , Fluoroquinolonas/administração & dosagem , Voluntários Saudáveis , Humanos , Estrutura Molecular
7.
J Enzyme Inhib Med Chem ; 31(sup1): 203-208, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27143199

RESUMO

The multicomponent pattern and biological characterization of plant material are essential for pharmaceutical field, in the food supplements quality control procedures and to all plant-based products. These nutrients often show valuable effects related to their consumption due to the occurrence of secondary metabolites that show useful properties on health. In this framework, researches performed on this topic play a central role for human health and drug development process. The aim of this study was to compare phenolics and free anthraquinones multicomponent pattern of two wild Turkish species: Asphodeline anatolica and Potentilla speciosa using validated high-performance liquid chromatography-photogiode array (HPLC-PDA) assays, coupled to biological evaluation. Even if some variances related to biological and enzymatic inhibition activities can be ascribed to other phytochemicals, the reported data support traditional use of Asphodeline anatolica and Potentilla speciosa roots as valuable natural font for the development of novel natural-derived drug formulations and/or food supplements with health and nutritional benefits.


Assuntos
Antraquinonas/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Liliaceae/química , Fenóis/farmacologia , Potentilla/química , Antraquinonas/química , Antraquinonas/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Colinesterases/metabolismo , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Fenóis/química , Fenóis/isolamento & purificação , Relação Estrutura-Atividade , Turquia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
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