Yazar "Dvoracsko, Szabolcs" seçeneğine göre listele

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    Chemical characterization, antioxidant properties, anti-inflammatory activity, and enzyme inhibition of Ipomoea batatas L. leaf extracts
    (TAYLOR & FRANCIS INC, 2017) Zengin, Gökhan; Locatelli, Marcello; Stefanucci, Azzurra; Macedonio, Giorgia; Novellino, Ettore; Mirzaie, Sako; Dvoracsko, Szabolcs
    Ipomoea batatas L. is widely used as a functional food in many countries. In this work, I. batatas leaf extracts (Soxhlet extract, microwave [MW] extract, and decoction extract) were characterized for the first time, and their total flavonoid and phenolic compound contents were measured by spectrophotometric and chromatographic analyses. These extracts were investigated for their antioxidant activities (free radical scavenging and reducing power assays), enzyme inhibitory activities (cholinesterase, tyrosinase, alpha-amylase, and alpha-glucosidase) and effects on inflammation pathways. Various bioactive secondary metabolites were identified; among them, chlorogenic acid appeared to be the most abundant. The decoction extract displayed the highest level of phenolics (89.26mg GAE/g extract) and thus exhibited stronger antioxidant ability than the Soxhlet and MW extracts. Each preparation was tested in in vitro enzymatic assays, which revealed that all three extracts exhibited interesting inhibitory activities against acetylcholinesterase, alpha-glucosidase, and alpha-amylase. Moreover, in vitro and ex vivo anti-inflammatory activities were observed for the decoction extract. Collectively, these results indicated that I. batatas leaf can be considered a potential candidate for the development of functional foods to combat the symptoms of metabolic disorders, such as type II diabetes mellitus.
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    Discovery of orexant and anorexant agents with indazole scaffold endowed with peripheral antiedema activity
    (MDPI, 2019) Dimmito, Marilisa P.; Stefanucci, Azzurra; Pieretti, Stefano; Minosi, Paola; Dvoracsko, Szabolcs; Tomboly, Csaba; Zengin, Gökhan; Mollica, Adriano
    The endocannabinoid system represents an integrated neuronal network involved in the control of several organisms' functions, such as feeding behavior. A series of hybrids of 5-(4-chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide (mimonabant), a well-known inverse agonist of the type-1 cannabinoid receptor (CB1), once used as an antiobesity drug, and the N-(2S)-substitutes of 1-[(4-fluorophenyl)methyl]indazole-3-carboxamide with 1-amino-3-methyl-1-oxobutane (AB-Fubinaca), 1-amino-3,3-dimethyl-1-oxobutane (ADB-Fubinaca), and 3-methylbutanoate (AMB-Fubinaca), endowed with potent agonistic activity towards cannabinoid receptors CB1 and CB2 were in solution as C-terminal amides, acids, methyl esters and N-methyl amides. These compounds have been studied by binding assays to cannabinoid receptors and by functional receptor assays, using rat brain membranes in vitro. The most active among them as an agonist, (S)-1-(2,4-dichlorobenzyl)-N-(3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl)-1H-indazole-3-carboxamide (LONI11), and an antagonist, (S)-2-(1-(2,4-dichlorobenzyl)-1H-indazole-3-carboxamido)-3-methylbutanoic acid (LONI4), were tested in vivo in mic, to evaluate their ability to stimulate or suppress feeding behavior after intraperitoneal (i.p.) administration. For a LONI11 formalin test and a tail flick test after an administration by the subcutaneous (s.c.) and intracerebroventricular (i.c.v.) routes, respectively, were also carried out in vivo in mice to investigate the antinociceptive property at the central and peripheral levesl. We observed a significant orexant effect for LONI11 and an intense anorexant effect for (S)-methyl 2-(1-(2,4-dichlorobenzyl)-1H-indazole-3-carboxamido)-3,3-dimethylbutanoate (LONI2) and LONI4. In zymosan-induced edema and hyperalgesia, LONI11 reduced the percent of paw volume increase and paw latency after s.c. administration, also suggesting a possible peripheral anti-inflammatory activity.