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Öğe Chemical Composition and Biological Activity of Capparis spinosa L. from Lipari Island(ELSEVIER SCIENCE BV, 2019) Mollica, A.; Stefanucci, A.; Macedonio, G.; Locatelli, M.; Luisi, G.; Novellino, E.; Zengin, GökhanSeveral plants belonging to the genus Capparis are the focus of growing interest due to their singular nutritional and medicinal properties. In the present study, flower bud samples from C. spinosa L. (Lipari Island, Italy) were subjected to decoction, Soxhlet, and microwave extraction techniques and the individual extracts investigated to better characterize the phytochemical and antioxidant profiles of the plant. Total phenolic and flavonoid amounts, phenolic composition, radical scavenging as well as reductive and metal chelating properties were determinated by well-established chemical and analytical procedures. Furthermore, cholinesterase inhibitory effects were evaluated by Ellman's method. Fatty acid percentage and essential oil composition were also detected by GC and GC-MS techniques respectively. Rutin was found to be the major component in the studied extracts. The Soxhlet extract exhibited the strongest radical scavenging and reductive activities as compared to the other extracts, most probably due to the highest concentration of phenolics, especially rutin. The best cholinesterase inhibitory effect was observed in the microwave extract. Palmitic acid was the most abundant fatty acid in the studied oil, whereas docosane was the major volatile compound in the essential oil. Present data corroborate the multipurpose potential of C. spinosa for designing bio-based drug formulations or functional applications. (c) 2018 SAAB. Published by Elsevier B.V. All rights reserved.Öğe Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin(American Chemical Society, 2020) Stefanucci, A.; Dimmito, M. P.; Molnar, G.; Streicher, J. M.; Novellino, E.; Zengin, Gökhan; Mollica, A.The development of bioconjugates is of pivotal importance in medicinal chemistry due to their potential applications as therapeutic agents to improve the targeting of specific diseases, decrease toxicity, or control drug release. In this work we achieved the synthesis and characterization of three novel opioid peptides fluorescently labeled, analogues of cyclic biphalin derivatives, namely 1D, 1C, and 2C. Among them, compound 1D, containing a dansyl-maleimide motif, exhibited an excellent binding affinity and functional potency for the ?-opioid receptor (DOR). 1D also demonstrated a strong fluorescence emission spectrum ranging from 300 to 700 nm. These features could be highly desirable for medical and biological applications needed for targeting the DOR, including in vivo imaging, and as a lead for the design of fluorescent probes. © 2020 American Chemical Society.Öğe Natural occurring ?-peptides: A fascinating world of bioactive molecules(Bentham Science Publishers B.V., 2018) Stefanucci, A.; Uysal, Şengül; Ceylan, Ramazan; Zengin, GökhanBackground: Living organisms are a natural source of ?-amino acids and peptides containing them. Many marine organisms and plants are able to produce by themselves such compounds, e.g. depsi-peptides and macrocyclic molecules, which possess different biological activities, mostly concerned to the treatment of human diseases. Methods: Literature has been collected ranging from 1980 until now; both reviews and research articles have been carefully considered and cited in our paper. Results: Literature revealed an increased interest in natural bioactive peptides incorporating ?-amino acids. Several papers focused their attention on structural characteristics of depsipeptides and cyclic compounds incorporating them in marine organisms, which may influence and determine the specific biological activity in vivo. Conclusion: In this brief review, we collect a series of naturally occurring peptides incorporating ?-amino acids, with the aim to update the arsenal of bioactive compounds available, highlighting the significant structural modifications which are the base of the exerting biological properties. © 2018 Bentham Science Publishers.Öğe Phenolic profile, toxicity, enzyme inhibition, in silico studies, and antioxidant properties of cakile maritima scop. (brassicaceae) from Southern Portugal(MDPI AG, 2020) Placines, C.; Castañeda-Loaiza, V.; Rodrigues, M. J.; Pereira, C. G.; Stefanucci, A.; Mollica, A.; Zengin, GökhanCakile maritima Scop. (sea rocket) is an edible halophyte plant with several ethnomedicinal uses. This work reports the chemical profile and bioactivities of food grade extracts from sea rocket organs. Toxicity was determined on mammalian cells, and phenolic profiling and the quantitation of the main metabolites were made by high-performance liquid chromatography coupled to mass spectrometry (HPLC-MS). Enzymatic inhibition was determined towards acetyl-and butyrylcholinesterase (AChE, BuChE), ?-glucosidase, ?-amylase, and tyrosinase. Docking studies were performed to tyrosinase, on the major metabolites, and samples were tested for antioxidant properties. Extracts were not toxic, were constituted mainly by flavonoids, and some compounds (roseoside and oleuropein) are here described for the first time in the species. The aerial organs’ ethanol extract had relevant activity towards 2,2-diphenyl-1-picrylhydrazyl [DPPH, half maximal inhibitory concentration (IC50) = 0.59 mg/mL], and ferric-reducing activity power (FRAP, IC50 = 0.99 mg/mL). All samples were more active towards AChE than on BuChE. The ethanol fruits’ extract inhibited ?-glucosidase [2.19 mmol of equivalent of acarbose (ACAE)/g]. Samples were active against tyrosinase, especially the aerial organs’ ethanol extracts [25.9 mg of equivalent of kojic acid (KAE)/g]. Quercetin and kaempferol glycosides fit well into the enzymatic pocket of tyrosinase. Our results suggest sea rocket as a candidate to be further explored as a source of bioactive products. © 2020 by the authors. Licensee MDPI, Basel, Switzerland.
