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    Chemical characterization, antioxidant properties, anti-inflammatory activity, and enzyme inhibition of Ipomoea batatas L. leaf extracts
    (TAYLOR & FRANCIS INC, 2017) Zengin, Gökhan; Locatelli, Marcello; Stefanucci, Azzurra; Macedonio, Giorgia; Novellino, Ettore; Mirzaie, Sako; Dvoracsko, Szabolcs
    Ipomoea batatas L. is widely used as a functional food in many countries. In this work, I. batatas leaf extracts (Soxhlet extract, microwave [MW] extract, and decoction extract) were characterized for the first time, and their total flavonoid and phenolic compound contents were measured by spectrophotometric and chromatographic analyses. These extracts were investigated for their antioxidant activities (free radical scavenging and reducing power assays), enzyme inhibitory activities (cholinesterase, tyrosinase, alpha-amylase, and alpha-glucosidase) and effects on inflammation pathways. Various bioactive secondary metabolites were identified; among them, chlorogenic acid appeared to be the most abundant. The decoction extract displayed the highest level of phenolics (89.26mg GAE/g extract) and thus exhibited stronger antioxidant ability than the Soxhlet and MW extracts. Each preparation was tested in in vitro enzymatic assays, which revealed that all three extracts exhibited interesting inhibitory activities against acetylcholinesterase, alpha-glucosidase, and alpha-amylase. Moreover, in vitro and ex vivo anti-inflammatory activities were observed for the decoction extract. Collectively, these results indicated that I. batatas leaf can be considered a potential candidate for the development of functional foods to combat the symptoms of metabolic disorders, such as type II diabetes mellitus.
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    Combinatorial peptide library screening for discovery of diverse alpha-glucosidase inhibitors using molecular dynamics simulations and binary QSAR models
    (TAYLOR & FRANCIS INC, 2019) Mollica, Adriano; Zengin, Gökhan; Durdağı, Serdar; Salmas, Ramin Ekhteiari; Macedonio, Giorgia; Stefanucci, Azzurra; Dimmito, Marilisa Pia; Novellino, Ettore
    Human alpha-glucosidase is an enzyme involved in the catalytic cleavage of the glucoside bond and involved in numerous functionalities of the organism, as well as in the insurgence of diabetes mellitus 2 and obesity. Thus, developing chemicals that inhibit this enzyme is a promising approach for the treatment of several pathologies. Small peptides such as di- and tri-peptides may be in natural organism as well as in the GI tract in high concentration, coming from the digestive process of meat, wheat and milk proteins. In this work, we reported the first tentative hierarchical structure-based virtual screening of peptides for human alpha-glucosidase. The goal of this work is to discover novel and diverse lead compounds that my act as inhibitors of alpha-glucosidase such as small peptides by performing a computer aided virtual screening and to find novel scaffolds for further development. Thus, in order to select novel candidates with original structure we performed molecular dynamics (MD) simulations among the 12 top-ranked peptides taking as comparison the MD simulations performed on crystallographic inhibitor acarbose. The compounds with the lower RMSD variability during the MD, were reserved for in vitro biological assay. The selected 4 promising structures were prepared on solid phase peptide synthesis and used for the inhibitory assay, among them compound 2 showed good inhibitory activity, which validated our method as an original strategy to discover novel peptide inhibitors. Moreover, pharmacokinetic profile predictions of these 4 peptides were also carried out with binary QSAR models using MetaCore/MetaDrug applications.
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    Exogenous opioid peptides derived from food proteins and their possible uses as dietary supplements: A critical review
    (TAYLOR & FRANCIS INC, 2018) Stefanucci, Azzurra; Mollica, Adriano; Macedonio, Giorgia; Zengin, Gökhan; Ahmed, Abdelkareem A.; Novellino, Ettore
    Endogenous opioid peptides are neuro-hormones and neurotransmitters involved in several physiological actions such as stress reactions, nociception control, sedation, breathing tone, depression, hypotension, appetite, digestion, etc. It is now clear that hydrolysis by the digestion of certain food-proteins can lead to the production of bioactive peptides. Commonly diffused foods like milk, wheat, meat, and spinach may produce after enzymatic digestion a variable amount of opioid peptides. The aim of this review is to provide arising perspectives on opioid peptides, focusing on their production from milk, their potential benefits, drawbacks, and safety issues related to infants' feeding.