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Öğe 4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis(TAYLOR & FRANCIS LTD, 2019) Secci, Daniela; Carradori, Simone; Petzer, Anel; Guglielmi, Paolo; D'Ascenzio, Melissa; Chimenti, Paola; Bagetta, Donatella; Alcaro, Stefano; Zengin, Gökhan; Petzer, Jacobus P.; Ortuso, FrancescoA new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure-activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.Öğe Anti-diabetic and anti-hyperlipidemic properties of Capparis spinosa L.: In vivo and in vitro evaluation of its nutraceutical potential(ELSEVIER SCIENCE BV, 2017) Mollica, Adriano; Zengin, Gökhan; Locatelli, Marcello; Stefanucci, Azzurra; Mocan, Andrei; Macedonio, Giorgia; Carradori, SimoneIn this study, the nutraceutical potential of Capparis spinosa L for the treatment of hyperglycemic states has been thoroughly investigated. A series of in vivo and in vitro tests have been conducted on fresh leaf, buds and salty buds (24 h desalted) processed to dry powder. 60% MeOH/H2O extracts were obtained for HPLC analysis and for alpha-amylase and alpha-glucosidase inhibition tests. To estimate the in vivo anti-diabetic effect, dry powders of C spinosa leaf and buds were orally administered to streptozocin-induced diabetic rats over a period of 28 days. At the end of the experiment, animals were sacrificed, blood taken for assessment of lipid profile and liver/kidney biochemistry while section of the pancreas, liver and kidneys were processed for general histology. Results showed that the regular administration of C. spinosa leaf or buds normalized all the biochemical parameters and reversed the liver/kidney injury with variable degrees of organ protection. (C) 2017 Elsevier Ltd. All rights reserved.Öğe Chromatographic analyses, in vitro biological activities, and cytotoxicity of cannabis sativa l. essential oil: a multidisciplinary study(MDPI, 2018) Zengin, Gökhan; Menghini, Luigi; Sotto, Antonella Di; Mancinelli, Romina; Sisto, Francesca; Carradori, Simone; Cesa, Stefania; Fraschetti, Caterina; Filippi, Antonello; Angiolella, Letizia; Locatelli, Marcello; Mannina, Luisa; Ingallina, Cinzia; Puca, Valentina; D’Antonio, Marianna; Grande, RossellaDue to renewed interest in the cultivation and production of Italian Cannabis sativa L., we proposed a multi-methodological approach to explore chemically and biologically both the essential oil and the aromatic water of this plant. We reported the chemical composition in terms of cannabinoid content, volatile component, phenolic and flavonoid pattern, and color characteristics. Then, we demonstrated the ethnopharmacological relevance of this plant cultivated in Italy as a source of antioxidant compounds toward a large panel of enzymes (pancreatic lipase, -amylase, -glucosidase, and cholinesterases) and selected clinically relevant, multidrug-sensible, and multidrug-resistant microbial strains (Staphylococcus aureus, Helicobacter pylori, Candida, and Malassezia spp.), evaluating the cytotoxic effects against normal and malignant cell lines. Preliminary in vivo cytotoxicity was also performed on Galleria mellonella larvae. The results corroborate the use of this natural product as a rich source of important biologically active molecules with particular emphasis on the role exerted by naringenin, one of the most important secondary metabolites.Öğe A comparative assessment of biological effects and chemical profile of Italian asphodeline lutea extracts(MDPI, 2018) Melucci, Dora; Locatelli, Marcello; Locatelli, Clinio; Zappi, Alessandro; De laurentiis, Francesco; Carradori, Simone; Campestre, Cristina; Leporini, Lidia; Zengin, Gökhan; Picot, Carene Marie Nancy; Menghini, Luigi; Mahomoodally, Mohamad FawziThe present study aims to highlight the therapeutic potential of Asphodeline lutea (AL), a wild edible plant of the Mediterranean diet. Roots, aerial parts, and flowers of AL at two different phenological stages were collected from three locations in Italy. The inhibitory activities of extracts on strategic enzymes linked to human diseases were assessed. The antioxidant properties were evaluated in vitro, using six standard bioassays. The phenolic and anthraquinone profiles were also established using HPLC-PDA. Zinc, cadmium, lead, and copper contents were also determined. All the samples inhibited acetylcholinesterase (from 1.51 to 2.20 mg GALAEs/g extract), tyrosinase (from 7.50 to 25.3 mg KAEs/g extract), and alpha-amylase (from 0.37 to 0.51 mmol ACAEs/g extract). Aloe-emodin and physcion were present in all parts, while rhein was not detected. The phenolic profile and the heavy metals composition of specimens gathered from three different regions of Italy were different. It can be argued that samples collected near the street can contain higher concentrations of heavy metals. The experimental data confirm that the A. lutea species could be considered as a potential source of bioactive metabolites, and its consumption could play a positive and safe role in human health maintenance.Öğe Crocus Sativus, Serenoa Repens and Pinus Massoniana Extracts Modulate Inflammatory Response in Isolated Rat Prostate Challenged with LPS(BIOLIFE SAS, 2017) Chiavaroli, Annalisa; Recinella, Lucia; Ferrante, Claudio; Locatelli, Marcello; Carradori, Simone; Macchione, Nicola; Zengin, Gökhan; Leporini, Lidia; Leone, Sheila; Martinotti, S.; Brunetti, L.; Vacca, M.; Menghini, Luigi; Orlando, GiuliaProstatitis is a common prostate disease that could be promoted by bacterial or non-bacterial infectious agents. In addition, inflammatory pathways involved in prostatitis have been increasingly studied, and herbal extracts endowed with anti-inflammatory effects are under investigation, individually or in combination, for their efficacy in alleviating the burden of inflammation, with possible improvements in symptoms. Serenoa repens (Serenoa), in combination with Crocus sativus (Crocus) and Pinus massoniana (Pinus), has previously shown to improve sexual function and limit urinary symptoms in patients suffering from concomitant erectile dysfunction and lower urinary tract symptoms. In this context, the aim of the present study is to evaluate the efficacy of Serenoa, Crocus and Pinus extracts, either alone or in combination, on immortalized prostate cells (PC3) and in an experimental model of bacterial prostatitis constituted by ex vivo prostate specimens challenged with lipopolysaccharide (LPS). We found that the tested extracts were able to reduce ROS production by PC3 cells and NF kappa B and PGE(2) activity in prostate specimens challenged with LPS. In addition, the pharmacological association of the extracts displayed synergistic effects indicating a rational use of the mixture of the tested extracts as a novel anti-oxidant and anti-inflammatory formulation in bacterial prostatitis. Finally, we performed analytical and in vitro evaluation to better characterize the phytochemical profile and the mechanism of action of selected secondary metabolites.Öğe Graminex Pollen: Phenolic Pattern, Colorimetric Analysis and Protective Effects in Immortalized Prostate Cells (PC3) and Rat Prostate Challenged with LPS(MDPI, 2018) Locatelli, Marcello; Macchione, Nicola; Ferrante, Claudio; Chiavaroli, Annalisa; Recinella, Lucia; Carradori, Simone; Zengin, GökhanProstatitis, a general term describing prostate inflammation, is a common disease that could be sustained by bacterial or non-bacterial infectious agents. The efficacy of herbal extracts with antioxidant and anti-inflammatory effects for blunting the burden of inflammation and oxidative stress, with possible improvements in clinical symptoms, is under investigation. Pollen extracts have been previously reported as promising agents in managing clinical symptoms related to prostatitis. The aim of the present work was to evaluate the protective effects of Graminex pollen (Graminex(TM), Deshler, OH, USA), a commercially available product based on standardized pollen extracts, in rat prostate specimens, ex vivo. In this context, we studied the putative mechanism of action of pollen on multiple inflammatory pathways, including the reduction of prostaglandin E-2 (PGE(2)), nuclear factor kappa-light-chain-enhancer of activated B cells (NFB), and malondialdehyde (MDA), whose activities were significantly increased by inflammatory stimuli. We characterized by means of chromatographic and colorimetric studies the composition of Graminex pollen to better correlate the activity of pollen on immortalized prostate cells (PC3), and in rat prostate specimens challenged with Escherichia coli lipopolysaccharide (LPS). We found that Graminex pollen was able to reduce radical oxygen species (ROS) production by PC3 cells and MDA, NFB mRNA, and PGE(2) levels, in rat prostate specimens. According to our experimental evidence, Graminex pollen appears to be a promising natural product for the management of the inflammatory components in the prostate.Öğe In vitro and in silico Studies of Mangiferin from Aphloia theiformis on Key Enzymes Linked to Diabetes Type 2 and Associated Complications(BENTHAM SCIENCE PUBL LTD, 2017) Picot, Marie C. N.; Zengin, Gökhan; Mollica, Adriano; Stefanucci, Azzurra; Carradori, Simone; Mahomoodally, Mohamad F.Background: Mangiferin, was identified in the crude methanol extract, ethyl acetate, and n-butanol fractions of Aphloia theiformis (Vahl.) Benn. Objective: This study aimed to analyze the plausible binding modes of mangiferin to key enzymes linked to diabetes type 2 (DT2), obesity, hypertension, Alzheimer's disease, and urolithiasis using molecular docking. Method: Crystallographic structures of alpha-amylase, alpha-glucosidase, glycogen phosphorylase (GP), pancreatic lipase, cholesterol esterase (CEase), angiotensin-I-converting enzyme (ACE), acetyl cholinesterase (AChE), and urease available on the Protein Databank database were docked to mangiferin using Gold 6.0 software. Results: We showed that mangiferin bound to all enzymes by pi-pi and hydrogen bonds mostly. Mangiferin was docked to both allosteric and orthosteric sites of a-glucosidase by pi-pi interactions. However, several hydrogen bonds were observed at the orthosteric position, suggesting a preference for this site. The docking of mangiferin on AChE with the catalytic pocket occupied by paraoxon could be attributed to pi-pi stacking involving amino acid residues, Trp341 and Trp124. Conclusion: This study provided an insight of the molecular interaction of mangiferin with the studied enzymes and can be considered as a valuable tool for designing new drugs for better management of these diseases.Öğe Microwave-assisted extraction, HPLC analysis, and inhibitory effects on carbonic anhydrase I, II, VA, and VII isoforms of 14 blueberry Italian cultivars(TAYLOR & FRANCIS LTD, 2016) Mollica, Adriano; Locatelli, Marcello; Macedonio, Giorgia; Carradori, Simone; Sobolev, Anatoly P.; De Salvador, Roberto F.; Monti, Simona M.The multi-component fingerprint and the biological evaluation of plant-derived material are indispensable for the pharmaceutical field, in food quality control procedures, and in all plant based products. We investigated the quantitative content of biologically active compounds (anthocyanins and chlorogenic acid) of microwave-assisted blueberry extracts from 14 different Italian cultivars, using validated high-performance liquid chromatography-photodiode array detector (HPLC-PDA) method and routinely instrument configuration. The carbonic anhydrase (CA, EC 4.2.1.1) inhibition profiles against several pharmacologically relevant CA isoforms of blueberry extracts and some bioactive compounds were also investigated. The various cultivars showed a highly variable content in anthocyanins and chlorogenic acid, and their CA inhibitory effects were also highly variable. Overall these data prove that antioxidant natural products found in blueberries may be useful for designing pharmacological agents in which various CAs are involved, e.g., antiobesity, antitumor, or anticonvulsants agents.Öğe Multicomponent pattern and biological activities of seven Asphodeline taxa: potential sources of natural-functional ingredients for bioactive formulations(TAYLOR & FRANCIS LTD, 2017) Locatelli, Marcello; Zengin, Gökhan; Uysal, Ahmet; Carradori, Simone; De Luca, Elisa; Bellagamba, Giuseppe; Aktümsek, AbdurrahmanThe 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, alpha-amylase and alpha-glucosidase. From the herein reported results, Asphodeline could be valuable for the production of bioactive products or food supplements for cosmetic and pharmaceutical industries.Öğe Multiple pharmacological approaches on Fibigia eriocarpa extracts by in vitro and computational assays(WILEY, 2018) Zengin, Gökhan; Lobine, Devina; Mollica, Adriano; Locatelli, Marcello; Carradori, Simone; Mahomoodally, Mohamad FawziThe ethyl acetate, methanolic, and water extracts of Fibigia eriocarpa were assessed for a panoply of bioactivities. Total phenolic and flavonoid content were quantified as well as individual phenolic compounds by HPLC-DAD. The invitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, -amylase, and -glucosidase) inhibitory potential of the extracts were evaluated. In silico molecular docking was used to investigate possible interaction between dominant compounds and selected enzymes. Vanillin (303g/g extract), apigenin (270g/g extract), and kaempferol (180g/g extract) were the main compounds in the ethyl acetate extract, while the methanolic extract was characterized by the presence of vanillin, rutin, and apigenin (616, 616 and 252g/g extract, respectively). (+)-catechin (1422g/g extract) was the main compound in the water extracts. The ethyl acetate extract was found to be a superior source of antioxidant compounds and enzyme inhibitors against above-mentioned enzymes. Docking studies revealed that p-hydroxybenzoic and (+)-catechin have the best scores for tyrosinase, while kaempferol and apigenin showed the best binding pose for -glucosidase, AChE, and BChE. Results amassed herein are the first report on the phytochemical and biological attributes of F.eriocarpa, which tend to validate the pharmacological uses of this plant as an alternative medicine.Öğe Novel 1,3-thiazolidin-4-one derivatives as promising anti-Candida agents endowed with anti-oxidant and chelating properties(ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2016) Secci, Daniela; Carradori, Simone; Bizzarri, Bruna; Chimenti, Paola; De Monte, Celeste; Mollica, Adriano; Rivanera, DanielaPursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nitrogen with differently substituted (NO2, NH2, Cl and F) benzyl groups. These compounds were tested to evaluate their minimum inhibitory concentration (MIC) against several clinical Candida spp. with respect to topical and systemic reference drugs (clotrimazole, fluconazole, ketoconazole, miconazole, tioconazole, amphotericin B). Moreover, anti-oxidant properties were also evaluated by using different protocols including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelating and phosphomolybdenum assays. Moreover, for the most active derivatives we assessed the toxicity (CC50) against Hep2 human cells in order to characterize them as multi-target agents for fungal infections. (C) 2016 Elsevier Masson SAS. All rights reserved.Öğe Total Phenolics, Flavonoids, Condensed Tannins Content of Eight Centaurea Species and Their Broad Inhibitory Activities against Cholinesterase, Tyrosinase, alpha-Amylase and alpha-Glucosidase(UNIV AGR SCI & VETERINARY MED CLUJ-NAPOCA, 2016) Zengin, Gökhan; Locatelli, Marcello; Carradori, Simone; Mocan, Andrei M.; Aktümsek, AbdurrahmanSeveral bioactive compounds originate from natural sources and their uses are generally related with traditional or folk medicine. Synthetic drugs can have adverse side effects and, for this reason, the investigation of novel, safe, and natural-occurring products can account for the development of new drugs. The genus Centaurea L. is one of the most important genera of the Asteraceae family, containing more than 200 species in the Turkish flora, about 140 of which are endemic. The aim of the present work was to determine enzyme inhibitory potentials of two extracts (chloroform and ethyl acetate) from eight Centaurea species against cholinesterase, tyrosinase, amylase, and glucosidase. The total phenolics, flavonoids and condensed tannin contents were also reported for each extract. These components in the extracts varied according to species and extraction solvents as well as enzyme inhibitory effects. The highest level of phenolics was found to be in the chloroform extract of C. pulchella (119.23 mg GAEs/g extract). Generally, chloroform extracts exhibited stronger enzyme inhibitory effects as compared to ethyl acetate. Additionally, possible correlations with total phenolics, flavonoids, and condensed tannins content were also highlighted. This paper is the first report of the inhibitory capacities of the eight Centaurea species on the selected enzymes. The present results may be a valuable starting point in the development of new bioactive formulations.
