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Öğe Euphorbia denticulata Lam.: A promising source of phyto-pharmaceuticals for the development of novel functional formulations(ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2017) Zengin, Gökhan; Uysal, Ahmet; Aktümsek, Abdurrahman; Mocan, Andrei; Mollica, Adriano; Locatelli, Marcello; Custodio, LuisaIn this study, Methanolic extracts of Euphorbia denticulata parts (flowers, leaf, stem, and mix of aerial parts) were assessed for a panoply of bioactivities. Inhibitory potential against key enzymes involved in diabetes (alpha-glucosidase and alpha-amylase), obesity (pancreatic lipase), neurodegenerative diseases (cholinesterases), and hyperpigmentation (tyrosinase) was evaluated. The antioxidant and antibacterial properties were also assessed. The total phenolic, flavonoid, and phytochemical profile were established using HPLC/DAD and molecular modelling studies on specific target compounds were performed in silico. The flower extract was found to be rich in phenolics and flavonoids, (60.11 +/- 1.40 mgGAE/g and 42.04 +/- 0.16 mgRE/g respectively), which tend to correlate with the high radical scavenging activity of this extract (120.34 +/- 3.33 mgTE/g and 165.42 +/- 2.16 mgTE/g for DPPH and ABTS respectively). Catechin, epicatechin, gallic acid, p-OH-Benzoic acid, rosmarinic acid, and epigallocatechin gallate, found in significant abundance in the extracts were assessed using molecular modelling with the aim to study their docking properties on a set of six enzymes used in this study. The extracts were moderately effective with MIC values ranging between 1.56 to 6.25 mg/ml, but potent growth inhibitors of MRSA strains. Results amassed herein can be used as a stimulus for further studies geared towards the development of novel phyto-pharmaceuticals. (C) 2016 Elsevier Masson SAS. All rights reserved.Öğe Exploring the halophyte Cistanche phelypaea (L.) Cout as a source of health promoting products: In vitro antioxidant and enzyme inhibitory properties, metabolomic profile and computational studies(ELSEVIER, 2019) Trampetti, Francesca; Pereira, Catarina; Rodrigues, Maria Joao; Celaj, Odeta; D'Abrosca, Brigida; Zengin, Gökhan; Mollica, Adriano; Stefanucci, Azzurra; Custodio, LuisaIn this study, ethyl acetate, acetone, ethanol and water extracts from flowers, stems and roots of Cistanche phelypaea (L.) Cout were appraised for radical scavenging activity (RSA) towards 1,1-diphenyl-2-picrylhydrazyl,2,2-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) and superoxide free radicals, and for metal chelating activities on iron and copper ions. The water extracts had the highest antioxidant activity, especially those from roots and flowers, and were further appraised for in vitro inhibition of enzymes implicated on the onset of human ailments, namely acetyl- (AChE) and butyrylcholinesterase (BuChE) for Alzheimer's disease, alpha-glucosidase and alpha-amylase for diabetes, and tyrosinase for skin hyper-pigmentation disorders. The extracts had a higher activity towards BuChE, and the roots extract had the highest capacity to inhibit tyrosinase. Samples showed a low capacity to inhibit carbohydrate hydrolysing enzymes, except for the root extract with a good inhibition on glucosidase. Samples were then characterized by NMR (1D and 2D): the main metabolites identified in the flowers extract were iridoid glycosides, in particular gluroside and bartsioside. In stems, phenylehanoid glycosides (PhGs) and iri doids were detected, especially acteoside. In roots were detected essentially PhGs, mainly echinacoside and tubuloside A. Docking studies were performed on the identified compounds. A favorable binding energy of tubuloside A to tyrosinase was calculated, and indicated this compound as a possible competitive inhibitor of alpha-glucosidase and tyrosinase. Our results suggest that C. phelypeae is a promising source of biologically-active compounds with health promoting properties for pharmaceutical and biomedical applications. (C) 2018 Elsevier B.V. All rights reserved.Öğe Insight into the biological properties and phytochemical composition of Ballota macrodonta Boiss. et Balansa, - an endemic medicinal plant from Turkey(ELSEVIER SCIENCE BV, 2018) Uysal, Şengül; Aumeeruddy-Elalfi, Zaahira; Zengin, Gökhan; Aktümsek, Abdurrahman; Mocan, Andrei; Custodio, Luisa; Neng, Nuno R.Ballota macrodonta Boiss. et Balansa., is a traditionally used endemic medicinal plant used to manage a plethora of diseases in Turkey. Nonetheless, few studies have endeavoured to highlight its therapeutic potential and its phytochemical profile. We hypothesized that B. macrodonta would possess multi-pharmacological propensities and bioactive compounds that would justify its use as a folk remedy. Aerial part of B. macrodonta was assessed for its antioxidant, antimicrobial, and enzymatic inhibitory potential using different extraction solvents. The total bioactive components determination and compound identification using High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) method were used to correlate the biological properties. HPLC-DAD profile showed the presence of 19 components (e.g. hydroxybenzoic acid, catechin hydrate, vanillic acid, caffeic acid, syringic acid, epicatechin, coumaric acid, ferulic acid, luteolin-7-O-glucoside, rutin, and quercetin). The water and methanolic extracts showed high total phenolic and flavonoid contents, respectively. The overall antioxidant capacity of the water extract was higher than the one of the methanol extract. The extracts showed inhibitory activity against cholinesterases, tyrosinase, alpha-amylase and alpha-glucosidase. The extracts also presented antimicrobial activity against eight Gram positive/negative bacteria (MIC - 0.05-0.15 mg/mL) and eight fungi (MIC - 0.0125-0.20 mg/mL). The presence of active biomolecules with multi-pharmacological properties makes B. macrodonta a potential source of health-promoting compounds that can be exploited as a novel medicinal herbal product.Öğe Juncaceae species as sources of innovative bioactive compounds for the food industry: In vitro antioxidant activity, neuroprotective properties and in silico studies(PERGAMON-ELSEVIER SCIENCE LTD, 2017) Rodrigues, Maria Joao; Gangadhar, Katkam N.; Zengin, Gökhan; Mollica, Adriano; Varela, Joao; Barreira, Luisa; Custodio, LuisaSeveral Juncus species are traditionally used as sedative and to treat health problems like insomnia. This work was based on the hypothesis that Juncus acutus, J. maritimus and J. inflexus may have molecules with bioactivities relevant for the improvement of cognitive functions and thus with potential use as food additives and/or nutraceuticals. Therefore leaves and roots extracts of those species were evaluated for radical scavenging (RSA) and metal chelating activities, and for in vitro inhibition of acetyl-(AChE) and butyrylcholinesterase (BuChE). The bioactive compound was isolated and identified by HPLC-DAD, and its anticholinesterase capacity was determined by different assays. Docking studies were performed to elucidate its inhibitory mechanism. The dichloromethane root extract of J. acutus had the highest RSA against DPPH and ABTS radicals, and the dichloromethane extract of J. maritimus leaves had the uppermost FRAP. The dichloromethane extract from J. acutus leaves had the strongest BuChE inhibition. Juncunol was the bioactive compound, exhibiting dual anticholinesterase capacity on enzyme-based assays and AChE inhibition in neuronal and glial cells in vitro. Molecular docking studies indicate juncunol as a competitive reversible inhibitor. Our results suggest that Juncus spp. can be sources of bioactive compounds with application in the food industry as cognitive-enhancer nutraceuticals. (C) 2017 Elsevier Ltd. All rights reserved.Öğe New insights into the chemical profiling, cytotoxicity and bioactivity of four Bunion species(ELSEVIER, 2019) Zengin, Gökhan; Paksoy, Mehmet Yavuz; Aumeeruddy, Muhammad Zakariyyah; Glamocilja, Jasmina; Sokovic, Marina; Diuzheva, Alina; Jeko, Jozsef; Cziáky, Zoltán; Rodrigues, Maria João; Custodio, Luisa; Mahomoodally, Mohamad FawziBunium species have been reported to be used both as food and in traditional medicines. The scientific community has attempted to probe into the pharmacological and chemical profiles of this genus. Nonetheless, many species have not been investigated fully to date. In this study, we determined the phenolic components, antimicrobial, antioxidant, and enzyme inhibitory activities of aerial parts of four Bunium species (B. sayai, B. pinnatifolium, B. brachyactis and B. macrocatpum). Results showed that B. microcarpum and B. pinnatifolium were strong antioxidants as evidenced in the DPPH, ABTS, CUPRAC, and FRAP assays. B. brachyactis was the most effective metal chelator, and displayed high enzyme inhibition against cholinesterase, tyrosinase, amylase, glucosidase, and lipase. The four species showed varied antimicrobial activity against each microorganism. Overall, they showed high activity against P. mirabilis and E. call (MIC and MBC < 1 mg(-1)). B. brachyactis was more effective against Aspergillus versicolor compared to the standard drug ketoconazole. B. brachyactis was also more effective than both ketoconazole and bifonazole against Trichoderma viride. B. sayai was more effective than ketoconazole in inhibiting A. fumigates. B. sayai was most non-toxic to HEK 293 (cellular viability = 117%) and HepG2 (cellular viability = 104%). The highest level of TPC was observed in B. pinnatifolium (35.94 mg GAE g(-1)) while B. microcarpum possessed the highest TFC (39.21 mg RE g(-1)). Seventy four compounds were detected in B. microcarpum, 70 in B. brachyactis, 66 in B. sayai, and 51 in B. pinnatifolium. Quinic acid, chlorogenic acid, pantothenic acid, esculin, isoquercitrin, rutin, apigenin, and scopoletin were present in all the four species. This study showed that the four Bunium species are good sources of biologically active compounds with pharmaceutical and nutraceutical potential.Öğe Novel in vitro and in silico insights of the multi-biological activities and chemical composition of Bidens tripartita L.(PERGAMON-ELSEVIER SCIENCE LTD, 2018) Uysal, Şengül; Uğurlu, Aslı; Zengin, Gökhan; Baloğlu, Mehmet Cengiz; Altunoğlu, Yasemin Çelik; Mollica, Adriano; Custodio, LuisaBidens tripartita L. is a traditional phyto-remedy used in several countries, yet there is still a paucity of data on its biological potential. We aimed to provide new insights on the pharmacological potential of extracts prepared from B. tripartita via highlighting its antioxidant, key enzymes inhibitory potency, and DNA protecting effects. Phytochemical profile was established using High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) and bioactive compound(s) docked against target enzymes using in silica methods. Cytotoxicity against three cancer cell lines was assessed using the methylthiazolyldiphenyl-tetrazolium bromide (MTT) cell viability test. The main compounds were luteolin-7-glucoside (cynaroside), chlorogenic acid, and epicatechin in the extracts. The methanol extract exhibited the highest radical scavenging activity. Ethyl acetate extract showed strongest a-amylase inhibitory activity, while the best a-glucosidase inhibitory effect recorded for the methanol extract. Molecular docking showed that cynaroside strongly interact to a-glucosidase cavity by establishing six hydrogen bonds. B. tripartita extracts were found to protect supercoiled form of pUC19 plasmid (>70%) and also showed anti-proliferative properties. Results amassed in the present study add on to a growing body of literature on the multi-pharmacological potency of B. tripartita which can be applied to bio-products development geared towards management of common diseases.Öğe Phytochemical characterization and bioactivities of five Apiaceae species: Natural sources for novel ingredients(ELSEVIER SCIENCE BV, 2019) Zengin, Gökhan; Mahomoodally, Mohamad Fawzi; Paksoy, Mehmet Yavuz; Picot-Allain, Carene; Glamocilja, Jasmina; Sokovic, Marina; Diuzheva, Alina; Jeko, Jozsef; Cziáky, Zoltán; Rodrigues, Maria João; Sinan, Kouadio Ibrahime; Custodio, LuisaSeveral species of the Apiaceae family have been employed in traditional cultures for their curative virtues. The present study focused on five Apiaceae species, (Falcaria vulgaris (FV), Smyrniopsis aucher( (SA), Smyrniopsis mtutzurdagensis (SM), Smyrnium cordifolium (SC), and Actinolema macrolema (AM)). The antioxidant, enzyme inhibitory (alpha-amylase, alpha-glucosidase, acetyl- and butyrylcholinesterase, lipase, and tyrosinase), antimicrobial, phytochemical, and cytotoxicity profiles of the methanol extracts of the selected Apiaceae species were determined. SC extract (35.68 mg gallic acid equivalent/g extract) possessed the highest phenolic content while the AM extract (56.79 mg rutin equivalent/g extract) had the highest flavonoid content. HPLC-ESI-MS (High performance liquid chromatography-electrospray tandem mass spectrometry) analyses showed presence of ferulic acid in all the five species. SC extract exhibited high radical scavenging (59.28 and 94.31 mg Trolox equivalent [TE]/g extract, DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid), respectively) and reducing activity (161.44 and 113.62 mg TE/g extract, for CUPRAC (cupric reducing antioxidant capacity) and FRAP (ferric reducing antioxidant power), respectively). SM extract exhibited the highest cholinesterase's inhibitory action (3.82 and 4.76 mg galantamine equivalent/g extract, for acetyland butyrylcholinesterase, respectively). The extracts showed higher inhibition against alpha-glucosidase (7.32-11.99 mmol acarbose equivalent [ACAE]/g extract) compared to alpha-amylase (0.51-0.55 mmol ACAE/g extract). SC extract was the most active (137.54 mg kojic acid equivalent/g extract) tyrosinase inhibitor and FV extract (113.75 mg Orlistat equivalent/g) the best lipase inhibitor. SM extract showed potent antibacterial effect against B. cereus (MIC (minimum inhibitory concentration) 0.180 mg/mL), P. mirabilis (MIC 0.180 mg/mL), M. flavus (MIC 0.560 mg/mL), P. aeruginosa (MIC 0.275 mg/mL), and S. typhimurium (MIC 1.500 mg/mL). FV extract (MIC 0.140 mg/mL) suppressed A. fumigates growth. Cytotoxicity was assessed on murine macrophage (RAW 264.7), human embryonic kidney (HEK 293), and human hepatocellular carcinoma (HepG2) cell lines. FV (60.3%) and SM (57.4%) showed the highest reduction on RAW 264.7 cellular viability, whereas SM (74.1%) showed toxicity against HepG2. This study supports that the Apiaceae species could be considered as promising candidates for the development of novel pharmacophores for the management of several human ailments.Öğe Scrophularia Lucida L. As A Valuable Source Of Bioactive Compounds For Pharmaceutical Applications: In Vitro Antioxidant, Anti-İnflammatory, Enzyme İnhibitory Properties, İn Silico Studies, And HPLC Profiles(ELSEVIER SCIENCE BV, 2019) Zengin, Gökhan; Stefanucci, Azzurra; Rodrigues, Maria Joao; Mollica, Adriano; Custodio, Luisa; Aumeeruddy, Muhammad Zakariyyah; Mahomoodally, Mohamad FawziThe genus Scrophularia has received much interest with regards to its traditional uses against eczema, psoriasis, and mastitis. Yet, the medicinal properties of some species still need to be scientifically validated. The present study was designed to investigate into the biological properties of various solvent extracts (ethyl acetate, methanol, and aqueous) of the roots and aerial parts of Scrophularia lucida based on its antioxidant, anti-inflammatory, and enzyme inhibitory activities together with phytochemical screening. Our results revealed that the solvent extracts differed in their biological effectiveness. The root ethyl acetate extract showed the highest ABTS scavenging, FRAP, CUPRAC, and inhibitory activity against AChE and alpha-glucosidase. The ethyl acetate extract of the aerial parts displayed the highest BChE and alpha-amylase inhibition and antioxidant effect in the phosphomolybdenum assay, while the methanol extracts of both parts were the most effective DPPH center dot scavengers and tyrosinase inhibitors. The methanol extracts of the root and aerial parts also inhibited NO production in lipopolysaccharide (LPS)-stimulated murine leukemic monocyte-macrophage cell (4.99% and 10.77%, respectively), at 31.25 mu g/mL concentration. The highest TPC (34.98 mg GAE/g extract) and TFC (48.33 mg RE/g extract) were observed in the ethyl acetate extract of the root and aerial parts, respectively. The most abundant compounds in the root ethyl acetate extract were luteolin (852 mu g/g extract), rosmarinic acid (522 mu g/g extract), and hesperidin (394 mu g/g extract) while kaempferol was most abundant in the ethyl acetate extract of the aerial parts (628 mu g/g extract). In silico experiments were conducted on tyrosinase and the higher docking values were observed for rosmarinic acid and hesperidin. The present findings provide base line information which tend to support the potential use of S. lucida in the management of several chronic diseases, including Alzheimer's disease and diabetes mellitus. (C) 2018 Elsevier B.V. All rights reserved.
