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Öğe Innovative perspectives on Pulicaria dysenterica extracts: phyto-pharmaceutical properties, chemical characterization and multivariate analysis(WILEY, 2019) de la Luz Cadiz-Gurrea, Maria; Zengin, Gökhan; Kayacık, Özlem; Lobine, Devina; Mahomoodally, Mohamad Fawzi; Javier Leyva-Jimenez, Francisco; Segura-Carretero, AntonioBACKGROUND In this study, we aimed to evaluate the influence of different extraction procedures [decoction, homogenizer-assisted extraction (HAE), infusion, maceration, Soxhlet and ultrasound-assisted extraction (UAE)] on the chemical profiling and biological properties of methanol and water extracts of Pulicaria dysenterica (L.) Bernh. The chemical profiles of the extracts were evaluated by high-performance liquid chromatography coupled to electrospray ionization and time-of-flight mass spectrometry (HPLC-ESI-TOF-MS). The antioxidant properties and enzymes (lipase, alpha-amylase, alpha-glucosidase, tyrosinase and cholinesterases) inhibitory potential of the extracts were evaluated. RESULTS The chemical profiles were dependent on the type of extraction methods as well as on the type of solvent. The methanolic extracts showed higher levels of total phenolic, flavonoid, and phenolic acid content, while the highest total flavonol content was observed in the HAE-water extract. Forty different compounds were identified from P. dysenterica. In relation to the potential in vitro anti-diabetic effects, the highest activity against the studied key enzymes was observed for the macerated extract (alpha-amylase: 0.58 +/- 0.03 and alpha- glucosidase: 1.65 +/- 0.03 mmol ACAE g(-1)). The HAE-methanol extract was the most potent inhibitor of cholisterases, whereas the highest activities against tyrosinase were observed for UAE-methanol extract, followed by macerated and Soxhlet. The inhibitory activity of the studied extracts against lipase were in the order: soxhlet > macerated> HAE-methanol > UAE-methanol. CONCLUSION This study has established scientific baseline data on the therapeutic properties of P. dysentrica, thereby advocating the need for further investigations in an endeavour to develop novel pharmaceuticals from this plant. (c) 2019 Society of Chemical IndustryÖğe Marine algae: A potential resource of anti-HSV molecules(MDPI, 2019) Mahomoodally, Mohamad Fawzi; Lobine, Devina; Rengasamy, Kannan R. R.; Gowrishankar, Shanmugaraj; Tewari, Devesh; Zengin, Gökhan; Kim, Doo Hwan; Sivanesan, IyyakkannuHerpes simplex viruses (HSVs) are common human pathogens belonging to the subfamily alpha-herpesvirinae that trigger severe infections in neonates and immunocompromised patients. After primary infection, the HSVs establish a lifelong latent infection in the vegetative neural ganglia of their hosts. HSV infections contribute to substantial disease burden in humans as well as in newborns. Despite a fair number of drugs being available for the treatment of HSV infections, new, effective, and safe antiviral agents, exerting different mechanisms of action, are urgently required, mainly due to the increasing number of resistant strains. Accumulating pieces of evidence have suggested that structurally diverse compounds from marine algae possess promising anti-HSV potentials. Several studies have documented a variety of algal polysaccharides possessing anti-HSV activity, including carrageenan and fucan. This review aimed to compile previous anti-HSV studies on marine algae-derived compounds, especially sulfated polysaccharides, along with their mode of action, toward their development as novel natural anti-HSV agents for future investigations.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 Phytochemical characterization, in vitro and in silico approaches for three Hypericum species(ROYAL SOC CHEMISTRY, 2018) Llorent-Martinez, Eulogio J.; Zengin, Gökhan; Lobine, Devina; Molina-Garcia, Lucia; Mollica, Adriano; Mahomoodally, Mohamad FawziMembers of the Hypericum genus are spread throughout the world and have a long history of use in traditional systems of medicines. In this present investigation, the methanolic extracts of aerial parts of three Hypericum species (H. olympicum (HO), H. pruinatum (HP), and H. scabrum (HS)) growing in Turkey were investigated for their key enzyme inhibitory potential. The chemical profiles were evaluated using HPLC-ESI-MSn, and their total phenolic and flavonoid contents were established. Also, relevant bioactive compounds observed in the extracts were subjected to molecular docking experiments to provide insights into their interactions with the tested enzymes. HPLC-ESI-MSn analysis revealed that the extract of HO, followed by the HS extract, has the highest total phenolic content (38 +/- 1.0 mg g(-1) DE), with flavonoids as major components. The extracts showed remarkable enzyme inhibitory effects against cholinesterases (AChE and BChE - 0.56-2.03 mgGALAE per g extract), tyrosinase, and alpha-glucosidase. Only HO (61.32 +/- 3.27 mgQE per g) and HP (39.88 +/- 2.51 mgQE per g) extracts showed notable inhibitory potency against lipase, while all the tested extracts exhibited modest activity against alpha-amylase. The phytochemicals with the most favourable interactions in the enzymatic cavity of alpha-glucosidase were found to be hyperoside, myricetin, and neo-chlorogenic acid, each with a docking score of -7.7. From these results, the three Hypericum species can be classified as potent sources of biologically active secondary metabolites, which warrant further investigations as novel medicinal products.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 Untargeted metabolomic profiling of three Crataegus species (hawthorn) and their in vitro biological activities(WILEY, 2019) Rocchetti, Gabriele; Senizza, Biancamaria; Zengin, Gökhan; Mahomodally, Mohamad Fawzi; Senkardes, Ismail; Lobine, Devina; Lucini, LuigiBACKGROUND In this investigation, the chemical and biological profiles of three Turkish Crataegus species (Crataegus orientalis, Crataegus szovitsii and Crataegus tanacetifolia) were studied in order to provide the first comprehensive characterization and their health-promoting potential. In this respect, polyphenolic profiles were evaluated using ultrahigh-performance liquid chromatography-quadrupole time-of-flight mass spectrometry. The in vitro antioxidant activities of the Crataegus samples were evaluated by using free-radical scavenging, phosphomolybdenum, ferrous-ion chelating, and reducing power assays. The inhibitory activities against alpha-glucosidase, amylase, cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), and tyrosinase were also established. RESULTS The untargeted metabolomic approach highlighted the effect of both extraction types and species on the phenolic profiles of different Crateagus tissues (i.e. leaves and twigs). The methanolic extracts showed the maximum radical scavenging and reducing activity in all test systems, whereas for ferrous-ion chelating assays the decocted and infused extracts showed the highest activity. Only the methanolic extracts were effective against AChE and BChE. The extract tested showed remarkable inhibitory effects against tyrosinase and alpha-glucosidase, whereas all the extracts exhibited modest inhibition against alpha-amylase. Overall, the twig extracts of the three species studied showed superior antioxidant and enzyme inhibitory activities. CONCLUSION On the basis of these results, the three Crataegus species can be classified as potent bioresources for high-value phytochemicals, which warrant further investigations for developing novel nutraceuticals. (c) 2019 Society of Chemical Industry
