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Zengin G.,Selcuk University | Nithiyanantham S.,Tierra Seed Science Private Ltd | Locatelli M.,University of Chieti Pescara | Locatelli M.,Interuniversity Consortium of Structural and Systems Biology | And 5 more authors.
European Journal of Integrative Medicine | Year: 2016

Introduction: The importance of plants products in traditional medicine has been recognized for some time. Two plants of Turkish origin, Centranthus longiflorus subsp. longiflorus and Cerinthe minor subsp. auriculata used as traditional Turkish medicine have remained uninvestigated for Alzheimer diseases and diabetes mellitus for their in vitro biological activity despite their use for sleep disorders.The antioxidant and enzyme inhibitory properties of these plants have not been reported. The aim of this study was to determine the total phenolics, flavonoids, and antioxidant as well as their enzyme inhibitory activity (in aqueous and solvent extracts). Methods: Antioxidant assays used standard methods to assess phosphomolybdenum, free radical scavenging activity, reducing power, and metal chelating activity on ferrous ions. Additionally, the extracts were tested also for enzyme inhibitory activity (Cholinesterase, Tyrosinase, α-amylase, and α-glucosidase). Results: Organic extracts showed the highest anti-cholinesterase (AChE, and BChE) activity, while aqueous extracts showed valuable Tyrosinase inhibitory activity. Total phenolics (expressed as gallic acid equivalents) in C. longiflorus subsp. longiflorus and C. minor subsp. auriculata were 46.2 and 25.4. mg in methanolic extracts, 27.5 and 26.2. mg in ethyl acetate extracts, and 37.9 and 46.6. mg in aqueous extracts, respectively. Similarly, total flavonoids (expressed as rutin equivalents) in C. longiflorus subsp. longiflorus and C. minor subsp. auriculata were 39.9 and 27.8. mg in methanolic extracts, 17.6 and 52.4. mg in ethyl acetate extracts, and 24.35 and 24.6. mg in aqueous extracts, respectively. Conclusion: The reported results may be valuable for preparing new food supplements and can represent a good model for the development of new drug formulations. © 2015 Elsevier GmbH. Source


Zengin G.,Selcuk University | Locatelli M.,University of Chieti Pescara | Locatelli M.,Interuniversity Consortium of Structural and Systems Biology | Ceylan R.,Selcuk University | Aktumsek A.,Selcuk University
Journal of Enzyme Inhibition and Medicinal Chemistry | Year: 2015

Plant-based foods have become attractive for scientists and food producers. Beneficial effects related to their consumption as dietary supplements are due to the presence of natural occurring secondary metabolites. In this context, studies on these products are important for natural and safely food ingredients evaluation. The aim of this study was to evaluate root extract of eight Asphodeline species as antioxidants, enzyme inhibitors and phytochemical content. Spectrophotometric antioxidant and enzyme inhibitory assays were performed. Total phenolic and flavonoids contents as well as the chemical free-anthraquinones profiles were determined using routinely procedure (HPLC-PDA). Data show that Asphodeline roots can be considered as a new source of natural compounds and can be used as a valuable dietary supplement. Some differences related to biological activities can be inferred to other phytochemicals that can be considered in the future for their synergic or competitive activities. © 2015 Informa UK Ltd. All rights reserved: reproduction in whole or part not permitted Source


Locatelli M.,University of Chieti Pescara | Locatelli M.,Interuniversity Consortium of Structural and Systems Biology | Ciavarella M.T.,University of Chieti Pescara | Paolino D.,University of Catanzaro | And 10 more authors.
Journal of Chromatography A | Year: 2015

This paper reports a new, easy, cheap, and fast MEPS-HPLC-PDA method for the simultaneous analysis of ciprofloxacin and levofloxacin, two fluoroquinolones (FLQs) commonly used for the treatment of pulmonary infections in cystic fibrosis (CF) patients. The FLQs were resolved on a Discovery C8 column (250mm×4.6mm; 5μm particle size) using an isocratic elution with a run time of 15min, without further purification. The method was validated over concentrations ranging from 0.05 to 2μg/mL for both analytes in human sputum, and enrofloxacin was used as internal standard.This method was successfully tested to detect FLQs in sputum collected from CF patients. The MEPS-HPLC-PDA method was validated using biological samples collected from CF patients orally or intravenously injected with FLQs. The resultant data showed that the method is selective, sensitive and robust over range of concentrations for both FLQs. The limit of quantification of the method was 0.05. μg/mL for both analytes (comparable to more complex and expensive instrument configurations), weighted-matrix-matched standard curves showed a good linearity up to 2. μg/mL, and parallelism tests were also successfully assessed. The intra- and inter-day precision (RSD%) values were ≤10.4% and ≤11.1%, respectively, for all range of analysis. The intra- and inter-day trueness (Bias%) values are ranged from -11.8% to 7.25% for both antibiotic drugs.At the best of our knowledge, this is the first MEPS-HPLC-PDA based method that uses MEPS procedure for simultaneous determination of ciprofloxacin and levofloxacin in human sputum. The method was tested successfully on real sputum samples by following a conventional drug administration. Furthermore, the MEPS-HPLC-PDA based method provides more advantages to detect and analyze quickly the antibiotic drugs in biological matrices than other analytical procedures reported in literature. © 2015 Elsevier B.V.. Source


Pica A.,University of Naples Federico II | Russo Krauss I.,University of Naples Federico II | Merlino A.,University of Naples Federico II | Merlino A.,CNR Institute of Neuroscience | And 6 more authors.
FEBS Journal | Year: 2013

Thrombin plays a pivotal role in the coagulation cascade; therefore, it represents a primary target in the treatment of several blood diseases. The 15-mer DNA oligonucleotide 5′-GGTTGGTGTGGTTGG-3′, known as thrombin binding aptamer (TBA), is a highly potent inhibitor of the enzyme. TBA folds as an antiparallel chair-like G-quadruplex structure, with two G-tetrads surrounded by two TT loops on one side and a TGT loop on the opposite side. Previous crystallographic studies have shown that TBA binds thrombin exosite I by its TT loops, T3T4 and T12T13. In order to get a better understanding of the thrombin-TBA interaction, we have undertaken a crystallographic characterization of the complexes between thrombin and two TBA mutants, TBAΔT3 and TBAΔT12, which lack the nucleobase of T3 and T12, respectively. The structural details of the two complexes show that exosite I is actually split into two regions, which contribute differently to TBA recognition. These results provide the basis for a more rational design of new aptamers with improved therapeutic action. The X-ray structure of two mutants of thrombin binding aptamer (TBA) in complex with their target protein shed new light about the recognition process. The interaction site of thrombin (exosite I) is split into two regions differently contributing to the binding. This result suggests new TBA modifications to improve the aptamer action. © 2013 FEBS. Source


Locatelli M.,University of Chieti Pescara | Locatelli M.,Interuniversity Consortium of Structural and Systems Biology | Ferrone V.,University of Chieti Pescara | Cifelli R.,University of Chieti Pescara | And 2 more authors.
Journal of Chromatography A | Year: 2014

This paper reports a new MEPS-HPLC-PDA method for the simultaneous analysis of seven non-steroidal anti-inflammatory drugs (Furprofen, Indoprofen, Ketoprofen, Fenbufen, Flurbiprofen, Indomethacin, and Ibuprofen) in human plasma and urine. NSAIDs were resolved on a Gemini C18 column (4.6mm×250mm; 5μm particle size) using a gradient elution mode with a run time of 25min, comprising re-equilibration, without further purification. The method was validated over the concentration range from 0.1 to 10μg/mL for all the analytes both in human plasma and urine, using Benzyl 4-hydroxybenzoate as the internal standards. This method was successfully tested to NSAIDs analyses in real matrices, in order to check the method potentiality and the correct response. The results from assay validations show that the method is selective, sensitive and robust. The limit of quantification of the method was 0.1μg/mL for all analytes, and weighted-matrix-matched standard curves showed a good linearity up to 10μg/mL. In order to check the correct response for over-range samples, parallelism tests were also assessed. In the entire analytical range the intra and inter-day precision (RSD%) values were ≤7.31% and ≤13.5%, respectively. For all the analytes the intra and inter-day trueness (Bias%) values ranged from -11.3% to 10.2%. To our knowledge, this is the first MEPS-HPLC-PDA based method that uses MEPS procedure for simultaneous determination of these seven NSAIDs in plasma and urine samples. © 2014 Elsevier B.V. Source

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