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Öğe Comprehensive Chemical Profiling and Multidirectional Biological Investigation of Two Wild Anthemis Species (Anthemis tinctoria var. Pallida and A. cretica subsp. tenuiloba): Focus on Neuroprotective Effects(MDPI, 2019) Orlando, Giustino; Zengin, Gökhan; Ferrante, Claudio; Ronci, Maurizio; Recinella, Lucia; Şenkardeş, İsmail; Gevrenova, Reneta; Zheleva-Dimitrova, Dimitrina; Chiavaroli, Annalisa; Leone, Sheila; Di Simone, Simonetta; Brunetti, Luigi; Picot-Allain, Carene Marie Nancy; Mahomoodally, Mohamad Fawzi; Sinan, Kouadio Ibrahime; Menghini, LuigiEthyl acetate (EA), methanol (MeOH), and aqueous extracts of aerial parts of Anthemis tinctoria var. pallida (ATP) and A. cretica subsp. tenuiloba (ACT) were investigated for their phenol and flavonoid content, antioxidant, and key enzyme inhibitory potentials. All extracts displayed antiradical effects, with MeOH and aqueous extracts being a superior source of antioxidants. On the other hand, EA and MeOH extracts were potent against AChE and BChE. Enzyme inhibitory effects against tyrosinase and alpha-glucosidase were observed, as well. We also studied Anthemis extracts in an ex vivo experimental neurotoxicity paradigm. We assayed extract influence on oxidative stress and neurotransmission biomarkers, including lactate dehydrogenase (LDH) and serotonin (5-HT), in isolated rat cortex challenged with K+ 60 mM Krebs-Ringer buffer (excitotoxicity stimulus). An untargeted proteomic analysis was finally performed in order to explore the putative mechanism in the brain. The pharmacological study highlighted the capability of ACT water extract to blunt K+ 60 mM increase in LDH level and 5-HT turnover, and restore physiological activity of specific proteins involved in neuron morphology and neurotransmission, including NEFMs, VAMP-2, and PKC gamma, thus further supporting the neuroprotective role of ACT water extract.Öğe Influence of different extraction techniques on the chemical profile and biological properties of Anthemis cotula L.: Multifunctional aspects for potential pharmaceutical applications(ELSEVIER SCIENCE BV, 2019) Sut, Stefania; Dall'Acqua, Stefano; Zengin, Gökhan; Şenkardeş, İsmail; Bulut, Gizem; Cvetanovic, Aleksandra; Stupar, Alena; Mandić, Anamarija; Picot-Allain, Carene; Doğan, Ahmet; Sinan, Kouadio Ibrahime; Mahomoodally, FawziThe phytochemical composition of different extracts obtained from stinking chamomile (Anthemis cotula L) was investigated. Ethanol was used as solvent and accelerated solvent extraction (ASE), microwave assisted extraction (MAE), maceration, soxhlet extraction (SE), and ultrasound assisted extraction (UAE) were applied on plant material. Comparison of the phytochemical contents, antioxidant, and enzyme inhibitory properties were performed. The most abundant sesquiterpene in the extracts was anthecotuloide, while the most present phenolics were caffeoyl quinic acid, quercetin, and kaempferol derivatives. UAE extract was the most efficient in the extraction of sesquiterpenoids and polyphenols. Considering the assays on antioxidant activity and enzyme inhibition, ASE extract showed highest phenolic content (62.92 mg gallic acid equivalent/g extract). Likewise, this extract showed highest radical scavenging (103.44 mg trolox equivalent [TE]/g extract and 155.70 mg TE/g extract, for DPPH and ABTS assays respectively) and reducing power potential (435.32 and 317.89 mg TE/g extract, for CUPRAC and FRAP assays, respectively). The different extracts showed similar results in the enzyme inhibition assays suggesting that the extraction methods used have no effect on observed enzyme activities. Novelty of our findings are the inhibitory action of the ethanol extract of A. cotula aerial parts on key enzymes associated with Alzheimer's disease (acetyl cholinesterase, butyryl cholinesterase), type 2 diabetes (alpha-amylase, alpha-glucosidase), and skin hyperpigmentation disorders (tyrosinase). Data collected from the present work further appraises the multiple potential biological properties of stinking chamomile suggesting the need for further investigation on its constituents. (C) 2019 Elsevier B.V. All rights reserved.Öğe Metabolomics-based profiling with chemometric approach to delineate the bio-pharmaceutical properties of fruit extracts from Ligustrum vulgare L(ELSEVIER, 2019) Rocchetti, Gabriele; Senizza, Biancamaria; Zengin, Gökhan; Şenkardeş, İsmail; Sadeer, Nabeelah Bibi; Mahomoodally, Mohamad Fawzi; Lucini, LuigiLigustrum vulgare L. (Family: Oleaceae) is an evergreen shrub native to North-west Africa, Europe and Western Asia. In the present work, infusion (water), ethyl acetate, methanol and n-hexane extracts of the fruits of L. vulgare L. were studied for their in vitro antioxidant and enzyme inhibitory properties along with their untargeted polyphenolic profile (using an ultra-high-performance liquid chromatography-quadrupole time-of-flight (UHPLC-QTOF) mass spectrometry approach). Untargeted metabolomics coupled to multivariate statistics showed that Ligustrum fruit extracts were very abundant in polyphenols, such as flavonoids, tyrosols and lignans, with ethyl acetate allowing the highest recovery among the extraction solvents tested. The methanolic extract inhibited the highest acetylcholinesterase (AChE), tyrosinase and glucosidase activity (4.23 mg galatamine equivalent (GALAE)/g, 132.85 mg kojic acid equivalent (KAE)/g and 1.94 mmol acarbose equivalent (ACAE)/g respectively) while the ethyl acetate extract inhibited the highest butyrylcholinesterase (BChE) and amylase activity (4.92 mg GALAE/g and 0.73 mmol ACAE/g, respectively). However, the infusion showed the weakest activity against all the enzymes studied. However, the extract showed highest antioxidant property in'the antioxidant assays (except for phosphomolybdenum). The present paper is the first comprehensive report on L. vulgare fruits and thus our findings are of considerable interest to design new bioproducts for the pharmaceutical and cosmeceutical industry in the future.Öğe New insights into the in vitro biological effects, in silico docking and chemical profile of clary sage - Salvia sclarea L.(ELSEVIER SCI LTD, 2018) Zengin, Gökhan; Şenkardeş, İsmail; Mollica, Adriano; Picot-Allain, Carene Marie Nancy; Bulut, Gizem; Doğan, Ahmet; Mahomoodally, M. FawziSalvia sclarea L. is traditionally used to manage common human ailments and is consumed as a food product. This study aimed to establish the phytochemical profile and antioxidant potential of ethyl acetate, methanol, and water extracts of Salvia sclarea. The inhibitory action of the extracts against alpha-amylase, alpha-glucosidase, acetyicholinesterase, butyrylcholinesterase, and tyrosinase was also investigated. Methanol extract showed the highest phenolic and fiavonoid contents (81.78 mg GAE/g extract and 40.59 mg RE/g extract, respectively). Reversed phase high performance liquid chromatography with diode array detector analysis revealed that S. sclarea was rich in rosmarinic acid. The water extract exhibited the lowest inhibitory activity against alpha-amylase but the upmost activity against alpha-glucosidase (0.19 and 18.24 mmol ACAE/g extract, respectively). Experimental data showed that only the water extract (8.86 mg KAE/g extract) significantly inhibited tyrosinase. Docking studies showed that quercetin binds to tyrosinase by two hydrogen and a pi-pi bonds. Salvia sclarea showed interesting biological activity against key enzymes involved in the pathogenesis of common ailments. (C) 2018 Elsevier Ltd. All rights reserved.Öğe Qualitative fingerprint analysis and multidirectional assessment of different crude extracts and essential oil from wild Artemisia santonicum L.(MDPI, 2019) Ferrante, Claudio; Zengin, Gökhan; Menghini, Luigi; Diuzheva, Alina; Jeko, Jozsef; Cziaky, Zoltan; Recinella, Lucia; Chiavaroli, Annalisa; Leone, Sheila; Brunetti, Luigi; Lobine, Devina; Şenkardeş, İsmail; Mahomoodally, Mohamad Fawzi; Orlando, GiustinoArtemisia species are used as folk medicines in several countries. This work was aimed to shed more light on the effect of methanol, water, ethyl acetate extracts, and essential oil (EO) of A. santonicum on selected enzymes (cholinesterase, tyrosinase alpha-amylase, and alpha-glucosidase) as well of their antioxidant and pharmacological effects. The chemical profile of the essential oil was determined using gas chromatography coupled to mass spectrometry (GC-MS) analysis, while the extracts were chemically characterized by high performance liquid chromatography coupled to mass spectrometry (HPLC-MS). Forty-nine constituents were identified and camphor (36.6%), 1,8-cineole (10.2%), alpha-thujone (10.1%), borneol (4.5%), and beta-thujone (3.6%) were the major components. Overall, 45, 74, and 67 components were identified from the ethyl acetate, methanol, and water extracts, respectively. The EO and extracts showed significant antioxidant properties, in a cell-free model; particularly, methanol and water extracts revealed promising sources of antioxidant compounds. Additionally, we evaluated protective effects of EO and extracts in isolated rat colon tissue challenged with lipopolysaccharide (LPS), as an ex vivo model of colon inflammation, and human colon cancer HCT116 cell line. Particularly, we observed that, among all tested samples, A. santonicum ethyl acetate displayed the best pharmacological profile, being able to blunt LPS-induced levels of all tested biomarkers of inflammation and oxidative stress, including colon nitrites, lactate dehydrogenase, prostaglandin E-2, and serotonin. Additionally, this extract was also able to reduce HCT116 cell viability, thus suggesting potential antiproliferative effects against colon cancer cells. Based on our results, A. santonicum has great potential for developing novel functional agents including pharmaceuticals, cosmeceuticals, and nutraceuticals.Öğe UHPLC-QTOF-MS phytochemical profiling and in vitro biological properties of Rhamnus petiolaris (Rhamnaceae)(ELSEVIER, 2019) Rocchetti, Gabriele; Miras-Moreno, Maria Begona; Zengin, Gökhan; Şenkardeş, İsmail; Sadeer, Nabeelah Bibi; Mahomoodally, Mohamad Fawzi; Lucini, LuigiThe genus Rhanmus has a great attention as source of bioactive compounds. So, this work aimed to investigate phytochemical profile and biological activity of water and methanolic extracts of different parts of Rhamnus petiolaris Boiss. & Balansa, namely twigs, leaves, mature and unmature fruits. The in vitro antioxidant activity, enzyme inhibitory properties, along with their polyphenol and anthraquinone profiles were determined by untargeted metabolomics. Results showed that methanolic and aqueous unmature fruit extracts were the most effective 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) scavenger (470.96 mg trolox equivalent (TE)/g and 394.96 mg TE/g, respectively). The aqueous unmature fruit extract displayed the most potent cupric and ferric reducing power and showed the highest total phenolic contents (TPC) (137.17 mg gallic acid equivalent (GAE)/g). The methanolic twig extract showed the highest enzymatic inhibitory property against of alpha-glucosidase, tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). On the basis of the correlation coefficients calculated separately for all experimental parameter pairs, flavonols and anthocyanins highly correlated with DPPH, whereas tyrosols correlated with BChE activity. Multivariate statistics following untargeted metabolomics allowed to describe the differences in polyphenols and anthraquinones, as affected by the extraction solvent used. Mature and unmature fruits were substantially comparable and were affected in a similar way by the extraction conditions, while different profiles were recorded for Rhamnus leaves and twigs. These findings indicate that the recovery efficiencies of specific subclasses of compounds (above all when considering flavonoids, phenolic acids and anthraquinones) as a function of the matrix and extraction chosen, significantly affect the phytochemical profile and biological activity of Rhamnus.Öğe Utilisation of Rhododendron luteum Sweet bioactive compounds as valuable source of enzymes inhibitors, antioxidant, and anticancer agents(PERGAMON-ELSEVIER SCIENCE LTD, 2020) Mahomoodally, Mohamad Fawzi; Sieniawska, Elwira; Sinan, Kouadio Ibrahime; Picot-Allain, Marie Carene Nancy; Yerlikaya, Şerife; Baloğlu, Mehmet Cengiz; Altunoğlu, Yasemin Çelik; Şenkardeş, İsmail; Rengasamy, Kannan R. R.; Zengin, GökhanEthnobotanical evidences report the use of Rhododendron luteum Sweet (Ericaceae) in traditional medicinal systems. However, R. luteum has been associated to the occurrence of 'mad honey' poisoning. In the present study, the ethyl acetate, methanol, and water extracts of R. luteum were investigated for their in vitro antioxidant, enzyme inhibition, and cytotoxic properties. The cytotoxicity of R. luteum extracts on A549 lung cancer cell line was evaluated using MTT cell viability assay. Besides, HPLC-ESI-MSn approach was employed to elucidate the secondary metabolite profiles of R. luteum in order to establish any structure-activity relationship. Methanol and water extracts of R. luteum possessed highest radical scavenging and reducing properties while the ethyl acetate extract showed highest metal chelating properties. In terms of enzyme inhibition, the methanol and ethyl acetate extracts of R. luteum, possessing epigallocatechin, were active inhibitors of cholinesterase enzymes, a-glucosidase, and tyrosinase. Water extract caused growth inhibition of A549 cells with 207.2 mu g/ml IC50 value. Though R. luteum has received little scientific attention due to the occurrence of grayanotoxins in the plant, however, data presented in this work shows promising biological activity of R. luteum and highlighted its role as a potential source of antioxidant and key enzyme inhibitors.
