Publications by authors named "Sonia Piacente"

187 Publications

Portulaca oleracea, a rich source of polar lipids: Chemical profile by LC-ESI/LTQOrbitrap/MS/MS and in vitro preliminary anti-inflammatory activity.

Food Chem 2022 Sep 12;388:132968. Epub 2022 Apr 12.

Department of Pharmacy, Università degli Studi di Salerno, via Giovanni Paolo II n. 132, I-84084 Fisciano, SA, Italy. Electronic address:

Considering the ongoing interest in foods rich in nutrients like polyunsaturated fatty acids and bioactive polar lipids, the chemical and biological investigation of Portulaca oleracea (purslane), a herbaceous plant typically appreciated in Mediterranean and Asiatic diet, was carried out. The LC-ESI/HRMS/MS analysis of extracts and lipid enriched fractions of purslane edible parts provided a comprehensive polar lipid profile, ranging from linear and cyclic oxylipins to high molecular weight lipids including glycolipids, phospholipids and sphingolipids. The evaluation of the anti-inflammatory potential by in vitro reporter gene assays highlighted the ability of purslane lipid enriched fractions, at a concentration of 20 µg/ml, to inhibit the TNF-α-stimulated NF-kB pathway by 30-40% and to activate PPAR-ɣ and Nrf2 transcription factors to the same extent or more than the positive control, respectively. Altogether, these results encourage to revalue purslane in human nutrition as a source of bioactive polar lipids.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.foodchem.2022.132968DOI Listing
September 2022

HR-LC-ESI-Orbitrap-MS-Based Metabolic Profiling Coupled with Chemometrics for the Discrimination of Different Organs and Evaluation of Their Antioxidant Activity.

Antioxidants (Basel) 2022 Feb 24;11(3). Epub 2022 Feb 24.

Department of Life and Environmental Sciences, University of Cagliari, University Campus, S.P. Monserrato-Sestu km 0.700, 09042 Monserrato, CA, Italy.

This study aimed to assess and correlate the phenolic content and the antioxidant activity of the methanol extracts of the stems, roots, flowers, and leaves of L. from north-eastern Algeria. Qualitative analysis was performed by high-resolution mass spectrometry (HR) LC-ESI-Orbitrap-MS and (HR) LC-ESI-Orbitrap-MS/MS). Forty-five compounds were identified in the methanol extracts; some are described for the first time in Targeted phenolic compounds were quantified by HPLC-DAD and it was shown that caffeoyl quinic derivatives were the most abundant compounds. Chemometric analysis was performed using principal component analysis (PCA) and hierarchical cluster analysis (HCA) based on the qualitative and quantitative LC data. The score plot discriminates different organs into three distinct clusters, with the stems and flowers allocated in the same cluster, reflecting their resemblance in their secondary metabolites. The antioxidant activities of the methanol extracts were assessed using cupric reducing antioxidant capacity (CUPRAC), ferric reducing antioxidant assay (FRAP), diphenyl picryl hydrazyl radical-scavenging capacity assay (DPPH), and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS). The root extract exhibited the highest antioxidant activity, evidenced by 3.26 and 1.61 mmol Fe/g dried residue for CUPRAC and FRAP, respectively, and great free radical-scavenging activities estimated by 0.53 and 0.82 mmol TEAC/g dried residue for DPPH and ABTS, respectively. The methanol extract of the roots demonstrated a significant level of total phenolics (TP: 125.16 mg GAE/g dried residue) and flavonoids (TFI: 25.40 QE/g dried residue TFII: 140 CE/g dried residue). Molecular docking revealed that tricaffeoyl-altraric acid and dicaffeoyl-altraric acid exhibited the best fit within the active sites of NADPH oxidase (NO) and myeloperoxidase (MP). From ADME/TOPAKT analyses, it can be concluded that tricaffeoyl-altraric acid and dicaffeoyl-altraric acid also revealed reasonable pharmacokinetic and pharmacodynamic characteristics with a significant safety profile.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/antiox11030453DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8944760PMC
February 2022

: A Source of Diarylheptanoids With α-Glucosidase Inhibitory Activity Evaluated by and Studies.

Front Plant Sci 2022 14;13:805660. Epub 2022 Feb 14.

Dipartimento di Farmacia, Università degli Studi di Salerno, Fisciano, Italy.

hard shells, green leafy involucres, leaves, and male flowers have shown to be a source of diarylheptanoids, a class of natural products with promising biological activities. Cyclic diarylheptanoids, named giffonins, were isolated from the Italian cultivar "Tonda di Giffoni." Even if many efforts have been made to establish the chemistry of these compounds, little is known about their biological properties. Herein, the inhibitory effects of diarylheptanoids isolated from byproducts against α-glucosidase enzyme were evaluated. Molecular docking experiments disclosed the establishment of several key interactions between all the screened diarylheptanoids and the protein counterpart, whose model was built through homology modeling procedure, thus rationalizing the detected inhibitory activities. Specifically, the most active compounds giffonin J (), K (), and P () were able to make both H-bonds and π-π stacking contacts with different residues belonging to the binding site responsible for the catalytic activity of the investigated enzyme. To highlight the occurrence of the bioactive diarylheptanoids in the extracts of byproducts obtained by eco-friendly extractions, their LC-MS profiles were analyzed. LC-MS analysis showed how giffonin J (), K (), and P () occurred in the ethanol extract of the leaves, while in the extracts of shells and green leafy involucres only giffonin P () was evident. Moreover, the quantitative analysis of giffonin J (), K (), and P () in byproducts was carried out by an analytical approach based on LC-ESI/QTrap/MS, using the Multiple Reaction Monitoring (MRM) experiment. These results prompt to evaluate byproducts, especially the leaves, as a prospective source of bioactive diarylheptanoids for the development of functional ingredients for the treatment of diabetes.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3389/fpls.2022.805660DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8882611PMC
February 2022

Salviolone from Roots Impairs Cell Cycle Progression, Colony Formation, and Metalloproteinase-2 Activity in A375 Melanoma Cells: Involvement of P21(Cip1/Waf1) Expression and STAT3 Phosphorylation.

Int J Mol Sci 2022 Jan 20;23(3). Epub 2022 Jan 20.

Department of Neurosciences, Biomedicine and Movement Sciences, Biochemistry Section, University of Verona, Strada Le Grazie, 8, I-37134 Verona, Italy.

Melanoma is a highly malignant solid tumor characterized by an elevated growth and propagation rate. Since, often, melanoma treatment cannot prevent recurrences and the appearance of metastasis, new anti-melanoma agents need to be discovered. roots are a source of diterpenoid derivatives, natural compounds with several biological activities, including antiproliferative and anticancer effects. Seven diterpenoid derivatives were purified from   roots and identified by NMR and MS analysis. Tanshinone IIA and cryptotanshinone were detected as the main components of   root ethanol extract. Although their antitumor activity is already known, they have been confirmed to induce a reduction in A375 and MeWo melanoma cell growth. Likewise, salviolone has been shown to impair the viability of melanoma cells without affecting the growth of normal melanocytes. The underlying anticancer activity of salviolone has been investigated and compared to that of cryptotanshinone in A375 cells, showing an increased P21 protein expression in a P53-dependent manner. In that way, salviolone, even more than cryptotanshinone, displays a multitarget effect on cell-cycle-related proteins. Besides, it modulates the phosphorylation level of the signal transducer and activator of transcription (STAT)3. Unexpectedly, salviolone and cryptotanshinone induce sustained activation of the extracellular signal-regulated kinases (ERK)1/2 and the protein kinase B (Akt). However, the blockage of ERK1/2 or Akt activities suggests that kinase activation does not hinder their ability to inhibit A375 cell growth. Finally, salviolone and cryptotanshinone inhibit to a comparable extent some crucial malignancy features of A375 melanoma cells, such as colony formation in soft agar and metalloproteinase-2 activity. In conclusion, it has been shown for the first time that salviolone, harboring a different molecular structure than tanshinone IIA and cryptotanshinone, exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/ijms23031121DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8835475PMC
January 2022

Mangostanin, a Xanthone Derived from Fruit, Exerts Protective and Reparative Effects on Oxidative Damage in Human Keratinocytes.

Pharmaceuticals (Basel) 2022 Jan 11;15(1). Epub 2022 Jan 11.

Department of Molecular Medicine and Medical Biotechnology, University of Naples "Federico II", 80131 Naples, Italy.

The fruit of (mangosteen) is known in ancient traditional Asian medicine for its antioxidant, anti-inflammatory, immunomodulatory and anticancer activities. These effects are mainly due to the action of polyphenols known as xanthones, which are contained in the pericarp of the fruit. In recent years, there has been a growing interest from pharmaceutical companies in formulating new topicals based on mangosteen full extracts to prevent skin aging. However, the molecules responsible for these effects and the mechanisms involved have not been investigated so far. Here, the arils and shells of were extracted with chloroform and methanol, and the extracts were further purified to yield 12 xanthone derivatives. Their effects were evaluated using in vitro cultures of human epidermal keratinocytes. After confirming the absence of cytotoxicity, we evaluated the antioxidant potential of these compounds, identifying mangostanin as capable of both protecting and restoring oxidative damage induced by HO. We showed how mangostanin, by reducing the generation of intracellular reactive oxygen species (ROS), prevents the activation of AKT (protein kinase B), ERK (extracellular signal-regulated kinase), p53, and other cellular pathways underlying cell damage and apoptosis activation. In conclusion, our study is the first to demonstrate that mangostanin is effective in protecting the skin from the action of free radicals, thus preventing skin aging, confirming a potential toward its development in the nutraceutical and cosmeceutical fields.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/ph15010084DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8780152PMC
January 2022

Metabolite Profiling of Derived Food Supplements by H-NMR-Based Metabolomics.

Molecules 2021 Oct 31;26(21). Epub 2021 Oct 31.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II n. 132, 84084 Fisciano, SA, Italy.

is a medicinal plant from the Mediterranean area, widely used in traditional medicine for its anti-inflammatory, antibacterial and antioxidant properties and for its preventive effects on microcirculation diseases. Due to these properties, it finds large applications in cosmetic, food and pharmaceutical fields. Additionally, hydroalcoholic extracts and mother tinctures based on represent products with a high commercial value, widely distributed not only in drug stores but also on on-line markets. The different extraction procedures used can greatly affect the fingerprints of the extracts, resulting in a different qualitative or quantitative profile of the chemical constituents responsible for biological activity. The aim of the present study was to characterize the composition of bioactive compounds present in water-ethanol and glycerol extracts of derived food supplements. Metabolite profiles of the extracts were obtained by H NMR experiments and data were processed by multivariate statistical analysis to highlight differences in the extracts and to evidence the extracts with the highest concentrations of bioactive metabolites. In detail, this work highlights how derived food supplements of obtained using ethanol-water mixtures ranging from 45% to 20% of ethanol represent the products with the highest amount of both primary (amino acids) and secondary metabolites including 3,4-dicaffeoylquinic acid (), chlorogenic acid (), 3,5-dicaffeoylquinic acid (), and kaempferol 3--glucopyranoside (). Moreover, it is evident that the use of an ethanol-water mixture 20:80 is the most suitable method to afford the highest number of phenolic compounds, while food-derived supplements obtained by glycerol extraction are characterized by a high amount of β-glucose and α-glucose and a low content of phenolic compounds.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/molecules26216619DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8588389PMC
October 2021

Conversion of Organic Dyes into Pigments: Extraction of Flavonoids from Blackberries () and Stabilization.

Molecules 2021 Oct 17;26(20). Epub 2021 Oct 17.

Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Viale delle Scienze, 90128 Palermo, Italy.

The blackberry's color is composed mainly of natural dyes called anthocyanins. Their color is red-purple, and they can be used as a natural colorant. Anthocyanins are flavonoids, which are products of plants, and their colors range from orange and red to various shades of blue, purple and green, according to pH. In this study, the chemical composition of an extract obtained from blackberries was defined by LC-ESI/LTQOrbitrap/MS in positive and negative ionization mode. Furthermore, we investigated the adsorption process of blackberry extract using several inorganic fillers, such as metakaolin, silica, Lipari pumice, white pozzolan and alumina. The pigments exhibit different colors as a function of their interactions with the fillers. The analysis of the absorption data allowed the estimation of the maximum adsorbing capacity of each individual filler tested. Through thermogravimetric measurements (TGA), the thermal stability and the real adsorption of the organic extract were determined.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/molecules26206278DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8538118PMC
October 2021

Pulp and Skin: In Depth Chemical Profile and Evaluation of Antioxidant Activity.

Molecules 2021 Aug 29;26(17). Epub 2021 Aug 29.

Dipartimento di Farmacia, Università degli Studi di Salerno, via Giovanni Paolo II n. 132, 84084 Fisciano, SA, Italy.

Ruiz and Pav., known as the 'Gold of the Incas' or 'lucuma', is a subtropical fruit belonging to the Sapotaceae family, with a very sweet flavor, used to prepare cakes, ice creams as well as in the baking and dairy industries. To date, the content of primary metabolites is known, but little information is reported about the composition in specialized metabolites. Moreover, no study is reported on skin which represent an important agricultural waste due to the high demand for lucuma. In order to have a preliminary metabolite profile of , the extracts of pulp and skin have been analyzed by LC-ESI/LTQOrbitrap/MS/MS in negative ion mode. The careful analysis of the accurate masses, of the molecular formulas and of the ESI/MS spectra allowed to identify specialized metabolites belonging to phenolic, flavonoid and polar lipid classes. The LC-MS/MS analysis guided the isolation of compounds occurring in the pulp extract whose structures have been characterized by spectroscopic methods including 1D- and 2D-NMR experiments and ESI-MS analysis. Furthermore, the phenolic content of the extracts along with the antioxidant activity of extracts and isolated compounds was evaluated.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/molecules26175236DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8434328PMC
August 2021

Metabolite Profile and In Vitro Beneficial Effects of Black Garlic ( L.) Polar Extract.

Nutrients 2021 Aug 13;13(8). Epub 2021 Aug 13.

Department of Pharmacy, University of Naples Federico II, Via Domenico Montesano 49, 80131 Naples, Italy.

Over the centuries, humans have traditionally used garlic ( L.) as a food ingredient (spice) and remedy for many diseases. To confirm this, many extensive studies recognized the therapeutic effects of garlic bulbs. More recently, black garlic (BG), made by heat-ageing white garlic bulbs, has increased its popularity in cuisine and traditional medicine around the world, but there is still limited information on its composition and potential beneficial effects. In this study, the metabolite profile of methanol extract of BG (BGE) was determined by high-performance liquid chromatography coupled to tandem mass spectrometry in high-resolution mode. Results allowed to establish that BGE major components were sulfur derivatives, saccharides, peptides, organic acids, a phenylpropanoid derivative, saponins, and compounds typical of glycerophospholipid metabolism. Characterization of the BGE action in cancer cells revealed that antioxidant, metabolic, and hepatoprotective effects occur upon treatment as well as induction of maturation of acute myeloid leukemia cells. These results are interesting from the impact point of view of BG consumption as a functional food for potential prevention of metabolic and tumor diseases.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/nu13082771DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8398518PMC
August 2021

LC-ESI/LTQOrbitrap/MS Metabolomic Analysis of Fennel Waste ( Mill.) as a Byproduct Rich in Bioactive Compounds.

Foods 2021 Aug 15;10(8). Epub 2021 Aug 15.

Dipartimento di Farmacia, Università Degli Studi di Salerno, via Giovanni Paolo II n. 132, I-84084 Fisciano, SA, Italy.

Food industries produce a high amount of waste every year. These wastes represent a source of bioactive compounds to be used to produce cosmetic and nutraceutical products. In this study, the possibility to retrain food waste as a potential source of bioactive metabolites is evaluated. In particular, metabolite profiles of different parts (bulb, leaves, stems and little stems) of fennel waste were investigated by liquid chromatography coupled with mass spectrometry (LC-ESI/LTQ Orbitrap MS). To discriminate the different plant parts, a Multivariate Data Analysis approach was developed. Metabolomic analysis allowed the identification of different metabolites mainly belonging to hydroxycinnamic acid derivatives, flavonoid glycosides, flavonoid aglycons, phenolic acids, iridoid derivatives and lignans. The identification of compounds was based on retention times, accurate mass measurements, MS/MS data, exploration on specific metabolites database and comparison with data reported in the literature for . Moreover, the presence of different oxylipins was relieved; these metabolites for the first time were identified in fennel. Most of the metabolites identified in possess anti-inflammatory, antioxidant and/or immunomodulatory properties. Considering that polyphenols are described to possess antioxidant activity, spectrophotometric tests were performed to evaluate the antioxidant activity of each part of the fennel.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/foods10081893DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8392248PMC
August 2021

Almond ( cv. Casteltermini) Skin Confectionery By-Products: New Opportunity for the Development of a Functional Blackberry ( Schott) Jam.

Antioxidants (Basel) 2021 Jul 29;10(8). Epub 2021 Jul 29.

Interdepartmental Research Center "Bio-Based Reuse of Waste from Agri-Food Matrices" (RIVIVE), University of Palermo, Viale delle Scienze, Parco d'Orleans II, 90128 Palermo, Italy.

This work proposes for the first time a model for reusing almond ( cv. Casteltermini from Sicily, Southern Italy) skin to formulate a new functional blackberry ( Schott) jam. For this purpose, blackberries were analysed fresh and as jam, traditionally prepared with a minimum fruit amount of 80%. Different percentages of almond skin (20, 15, and 10% /) were added to jam. The phytochemical profile of enriched jam was investigated by LC-ESI/LTQOrbitrap/MS analyses. Anthocyanins, hydrolysable tannins, and triterpenoids were identified in a blackberry extract, while proanthocyanidins, flavonoids, and oxylipins were identified in an almond extract. The -hexane extract of skin, investigated by GC-MS, evidenced linoleic, palmitic, and oleic acids as the main abundant compounds. Samples were investigated for their antioxidant activity using DPPH, ABTS, β-carotene, and FRAP tests. The hypoglycaemic and hypolipidemic effects were studied by α-amylase, α-glucosidase, and lipase inhibitory assays. In order to evaluate the effect of thermal process on enriched jam bioactivity, pasteurisation was applied. An increase in activities for all samples was observed, in particular for jam enriched with 20% / of almond skin. Based on obtained data, and supported by sensory analysis, we propose enriched jam as a promising source of compounds useful for preventing diseases associated with oxidative stress.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/antiox10081218DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8388876PMC
July 2021

LC-ESI/HRMS analysis of glucosinolates, oxylipins and phenols in Italian rocket salad (Diplotaxis erucoides subsp. erucoides (L.) DC.) and evaluation of its healthy potential.

J Sci Food Agric 2021 Nov 14;101(14):5872-5879. Epub 2021 Apr 14.

Department of Pharmacy, University of Salerno, Fisciano, Italy.

Background: This study investigated the chemical profile and biological activity of Diplotaxis erucoides subsp. erucoides (L.) DC. (Brassicaceae) collected in Sicily (Italy).

Results: Liquid chromatography coupled with electrospray ionization and high-resolution mass spectrometry (LC-ESI/HRMS) analysis of the ethanol extract revealed the presence of 42 compounds - glucosinolates, hydroxycinnamic acids, flavonoids, and oxylipins. The extract was tested for its antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS), ferric reducing ability power (FRAP), and β-carotene bleaching tests. Promising protection from lipid peroxidation was observed after 30 min of incubation in a β-carotene bleaching test (IC of 3.32 μg mL ). The inhibition of carbohydrates-hydrolyzing enzymes resulted in IC values of 85.18 and 92.36 μg mL for α-amylase and α-glucosidase, respectively. Significant inhibition against lipase enzyme was observed (IC of 61.27 μg mL ).

Conclusion: Diplotaxis erucoides can be considered a potential source of antioxidant, hypoglycemic, and hypolipidemic bioactives. © 2021 Society of Chemical Industry.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1002/jsfa.11239DOI Listing
November 2021

Antioxidant and In Vitro Preliminary Anti-Inflammatory Activity of (Italian Cultivar "Marrone di Roccadaspide" PGI) Burs, Leaves, and Chestnuts Extracts and Their Metabolite Profiles by LC-ESI/LTQOrbitrap/MS/MS.

Antioxidants (Basel) 2021 Feb 11;10(2). Epub 2021 Feb 11.

Dipartimento di Farmacia, Università degli Studi di Salerno, via Giovanni Paolo II n. 132, I-84084 Fisciano, SA, Italy.

The Italian "Marrone di Roccadaspide" (), a labeled Protected Geographical Indication (PGI) product, represents an important economic resource for the Italian market. With the aim to give an interesting opportunity to use chestnuts by-products for the development of nutraceutical and/or cosmetic formulations, the investigation of burs and leaves along with chestnuts of , cultivar "Marrone di Roccadaspide", has been performed. The phenolic, tannin, and flavonoid content of the MeOH extracts of "Marrone di Roccadaspide" burs, leaves, and chestnuts as well as their antioxidant activity by spectrophotometric methods (1,1-diphenyl-2-picrylhydrazyl (DPPH), Trolox Equivalent Antioxidant Capacity (TEAC), and Ferric Reducing Antioxidant Power (FRAP) have been evaluated. Furthermore, a cell-based antioxidant in vitro test along with in vitro assays for the evaluation of the ability to reduce nuclear factor-kappa B (NF-κB) activation and nitric oxide (NO) production have been carried out. In order to identify the secondary metabolites responsible for the high phenolic content and the strong antioxidant activity shown by leaves and burs extracts, and to highlight the differences between their chemical composition, the analysis of the metabolite profile of the MeOH extracts obtained from both by-products and chestnuts by liquid chromatography coupled to electrospray ionization and multiple-stage linear ion-trap and Orbitrap high-resolution mass spectrometry (LC-(-)ESI/LTQOrbitrap/MS/MS) has been performed. LC-MS analysis allowed the identification of different classes of specialized metabolites including hydrolyzable tannins, flavonoids, ellagic acid and phenol glucoside derivatives, and triterpenoids as well as polar lipids. Our results show how the antioxidant activity of the extracts can be correlated to their high tannins and flavonoids content while polar lipids occurring in the MeOH extract of the leaves could contribute to determining its higher anti-inflammatory activity.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/antiox10020278DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7917746PMC
February 2021

Giffonins, Antioxidant Diarylheptanoids from , and Their Ability to Prevent Oxidative Changes in Human Plasma Proteins.

J Nat Prod 2021 03 22;84(3):646-653. Epub 2021 Feb 22.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II no. 132, 84084 Fisciano (SA), Italy.

With the aim to explore the ability of diarylheptanoids to reduce oxidative changes in human plasma proteins, a phytochemical investigation of the MeOH extract of leaves was perfomed. Analysis by LC-ESI/LTQOrbitrap/MS/MS guided the isolation of two new diarylheptanoid derivatives, giffonins W () and X (). The structures and were assigned by analysis of NMR data combined with a QM (quantum mechanical)/NMR approach. The absolute configurations of and were established by analysis of electronic circular dichroism (ECD) spectra compared with the TDDFT-simulated curves. The antioxidant activity of the new and known giffonins was evaluated by inhibition of human plasma lipid peroxidation. Giffonins with the highest inhibitory activity were tested for their ability to reduce oxidation of thiol groups and carbonylation in plasma proteins, and some of them exhibited higher antioxidant activity than curcumin.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jnatprod.0c01251DOI Listing
March 2021

Effects of bio-fertilizers on the production of specialized metabolites in Salvia officinalis L. leaves: An analytical approach based on LC-ESI/LTQ-Orbitrap/MS and multivariate data analysis.

J Pharm Biomed Anal 2021 Apr 3;197:113951. Epub 2021 Feb 3.

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 84084, Fisciano, SA, Italy. Electronic address:

In recent years, the use of organic substances has been increased to improve the production of specialized metabolites in aromatic and medicinal plants. Salvia officinalis L., known as sage, is an important medicinal and aromatic plant, whose leaves are commonly used as a condiment in food but mainly as a raw material in pharmaceutical and perfumery industries. In this work to define the effects of bio-fertilizers and foliar applications of l-phenylalanine on specialized metabolites production and biochemical characteristics of S. officinalis leaves, an experimental field in 2 years (2016 and 2017) was developed in semiarid climate, South-western, Iran. Experimental treatments included foliar spraying of l-phenylalanine in diverse concentration (0-250 and 500 mg/mL) and different bio-fertilizers [Arbuscular mycorrhizal fungi (AMF), Pseudomonas fluorescens (Pf), both fungi and bacteria (AMF + Pf)]. A metabolomics approach was carried out on the ethanolic extracts of sage leaves obtained by different treatments using Liquid Chromatography coupled with High-Resolution Mass Spectrometry (LC-ESI/LTQ-Orbitrap/MS) followed by multivariate data analysis. A total of 41 specialized metabolites were detected, and 35 of them were identified based on their accurate mass and mass fragmentation, as belonging to organic acids, phenylpropanoids, flavonoids, diterpenes, salvianolic acids and oxylipins. This work highlighted that the foliar application of l-phenylalanine along with the inoculation of Arbuscular mycorrhizal fungi and P. fluorescens can improve the yields of specific metabolites of pharmaceutical interest.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jpba.2021.113951DOI Listing
April 2021

Terpenoid Constituents of Aerial Parts with Inhibitory Effects on Bacterial Biofilm Growth.

J Nat Prod 2021 01 30;84(1):26-36. Epub 2020 Dec 30.

Dipartimento di Farmacia, Università degli Studi di Salerno, via Giovanni Paolo II n. 132, Fisciano, 84084 SA, Italy.

is a perennial and aromatic plant distributed in the Baluchestan region of Iran. In the present work, an -hexane extract of aerial parts showed excellent capabilities to both inhibit the formation of biofilms by different Gram-positive and Gram-negative pathogens and block the cell metabolism within microbial biofilms. To correlate the activity of the extract with the biologically active compounds present, first an analytical approach based on LC-HRMS/MS was carried out. The metabolite profile obtained guided the isolation of 21 compounds, among which two sesquiterpenes ( and ) and one diterpene () were found to be new. The antimicrobial activity of the isolated compounds was evaluated by determining how they were able not only to reduce the growth of different Gram-positive and Gram-negative human bacteria and phytopathogens but also to inhibit the formation of biofilms by these bacteria and affect the metabolism of microbial cells present within the biofilms. With the aim of correlating the activity exhibited by the extract with the concentration levels of the constituent compounds, a quantitative determination was carried out by an analytical approach based on LC-ESI/QTrap/MS.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jnatprod.0c00832DOI Listing
January 2021

Okra fruit: LC-ESI/LTQOrbitrap/MS/MS based deep insight on polar lipids and specialized metabolites with evaluation of anti-oxidant and anti-hyperglycemic activity.

Food Funct 2020 Sep;11(9):7856-7865

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.

Okra is a vegetable crop very popular in tropical, subtropical, and warm temperate regions of the world for its edible fruit. Nowadays, this species can be easily found in European local markets, as a basic ingredient in many local and traditional dishes. Considering the extensive and spread use of okra fruits, to achieve deep insight on its chemical composition the analysis of the polar extract by high-performance liquid chromatography coupled to multiple-stage linear ion-trap and orbitrap high-resolution mass spectrometry in negative electrospray ionization mode was carried out. By this approach, 39 metabolites belonging to different polar lipid classes, such as oxylipins, phospholipids, glycolipids, and sphingolipids, were putatively identified for the first time in A. esculentus. Moreover, LC-HRMS/MS analyses guided the isolation and characterization by NMR experiments of 19 specialized metabolites belonging to phenolic acid and flavonoid classes, 8 of them never reported before in A. esculentus. Finally, antioxidant activity and inhibition of α-glucosidase activity were assayed, suggesting a good anti-oxidant anti-hyperglycemic activity for okra fruit.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1039/d0fo00867bDOI Listing
September 2020

Metabolite profiling and antioxidant activity of the polar fraction of Italian almonds (Toritto and Avola): Analysis of seeds, skins, and blanching water.

J Pharm Biomed Anal 2020 Oct 3;190:113518. Epub 2020 Aug 3.

Dipartimento di Farmacia, University of Salerno, Via Giovanni Paolo II n. 132, 84084, Fisciano, SA, Italy. Electronic address:

The health benefits of almonds along with their ability to prevent atheroschlerosis as well as cardiovascular and diabetes risks are well known. Previous works were focused mainly on the lipid fraction, thus a lack of information about the polar constituents still persists. In order to provide deeper insight into the chemical composition of almond, the polar fraction of Italian almond cultivars (Toritto and Avola) was investigated. The MeOH extract of the Toritto cultivar was submitted to LC-ESI-(HR)MS/MS experiments, highlighting the occurrence of several compounds, mainly cyanogenic glycosides, glycosylated flavonoids, proanthocyanidins, and a diterpene glycoside. EtOH and EtOH:HO solution were also employed for extractions, resulting selective for flavonoids and proanthocyanidins, while cyanogenic glycosides were mainly detected in EtOH:HO extract. Almonds were also blanched to afford skins and blanching water which were analyzed by LC-ESI-(HR)MS/MS experiments in order to establish the source of the identified compounds. Cyanogenic glycosides were detected in the peeled almonds, while flavonoids and proanthocyanidins were detected in almond skins and blanching water. The LC-ESI-(HR)MS/MS analyses of the almonds of the Avola cvs (Fascionello, Pizzuta and Romana) were compared with those of the Toritto cv., showing clear differences in their metabolome, probably due to the different growing conditions. Finally, total phenolic content and radical scavenging activity of the extracts and blanching waters were evaluated by Folin-Ciocalteu assay and by DPPH and ABTS assays, highlighting interesting antioxidant properties possessed by almond skins and blanching water, suggesting their potential employment in pharmaceutical, cosmetic and nutraceutical formulations.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jpba.2020.113518DOI Listing
October 2020

Chemical profiling and biological screening with potential anti-inflammatory activity of grown in Egypt.

Nat Prod Res 2021 Dec 10;35(23):5521-5524. Epub 2020 Jul 10.

Department of Pharmacognosy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

The ethanolic extract of aerial parts showed a significant strong anti-inflammatory and antioxidant activities with a high gastrointestinal safety profile and a very low cytotoxicity on peripheral blood mononuclear cells (PBMCs) with an IC > 1000 μg/ml. The alcoholic extract of has been analysed by HPLC coupled to multiple-stage Linear Ion-Trap and Orbitrap High-Resolution mass spectrometry in negative electrospray ionisation mode (LC-ESI/LTQOrbitrap/MS/MSn). By this approach, it was possible to putatively identify 13 compounds, mainly organic acids, flavonoids, one steroid and one hydroxy-coumarin. Luteolin 6--glucopyranosyl-7--glucopyranoside, luteolin-8--glucopyranosyl-7--rhamnopyranoside, luteolin-6-C-glucoside and isoorientin 7--[6''-feruloyl]-glucoside were detected for the first time in and family Commelinaceae.[Figure: see text].
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/14786419.2020.1791113DOI Listing
December 2021

LC-ESI-FT-MS Metabolite Profiling of L. Roots Leads to Isolation of Comfreyn A, an Unusual Arylnaphthalene Lignan.

Int J Mol Sci 2020 Jun 30;21(13). Epub 2020 Jun 30.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II, 84084 Salerno, Italy.

Preparations of comfrey ( L.) roots are used topically to reduce inflammation. Comfrey anti-inflammatory and analgesic properties have been proven in clinical studies. However, the bioactive compounds associated with these therapeutic activities are yet to be identified. An LC-ESI-Orbitrap-MS metabolite profile of a hydroalcoholic extract of comfrey root guided the identification of 20 compounds, including a new arylnaphthalene lignan bearing a rare δ-lactone ring, named comfreyn A. Its structure was determined using extensive 2D NMR and ESI-MS experiments. Additionally, the occurrence of malaxinic acid, caffeic acid ethyl ester, along with the lignans ternifoliuslignan D, 3-carboxy-6,7-dihydroxy-1-(3',4'-dihydroxyphenyl) -naphthalene, globoidnan A and B, and rabdosiin was reported in for the first time. These results helped to redefine the metabolite profile of this medicinal plant. Finally, caffeic acid ethyl ester and comfreyn A were found to significantly inhibit E-selectin expression in IL-1β stimulated human umbilical vein endothelial cells (HUVEC), with EC values of 64 and 50 µM, respectively.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/ijms21134671DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7370062PMC
June 2020

Cardenolide-rich fraction of Pergularia tomentosa as a novel Antiangiogenic agent mainly targeting endothelial cell migration.

Daru 2020 Dec 1;28(2):533-543. Epub 2020 Jul 1.

Department of Stem Cells and Developmental Biology, Cell Science Research Center, Royan Institute for Stem Cell Biology and Technology, ACECR, Banihashem Sq., Banihashem St., Resalat Highway, P.O. Box: 16635-148, Tehran, Iran.

Purpose: Angiogenesis related abnormalities underlie several life-threatening disorders. Despite approved therapies, scientists have yet to develop highly efficient, low cost approaches with minimal side effects.

Methods: We evaluated the antiangiogenic activity of 50% hydroalcoholic extracts of Pergularia tomentosa L. root and aerial parts along with their EtOAc and water fractions, in vivo and in vitro. Transgenic zebrafish line Tg(fli1:EGFP) was used for in vivo assay and human umbilical vein endothelial cell (HUVEC) migration test along with possibility of tube formation were performed as in vitro tests. Furthermore, microvasculature in chicken chorioallantoic membrane (CAM) was assessed under P. tomentosa treatment. The fractionation of the 50% hydroalcoholic extracts was led to the identification of the best active fraction in this study. The metabolite profiling of the active fraction was also carried out using LC-HRESIMS analysis.

Results: Pergularia tomentosa markedly inhibited intersegmental vessel (ISV) formation at 48 h post-fertilization (hpf) embryos in zebrafish. The water fraction of root hydroalcoholic extract (PtR2), showed strong antiangiogenic effect with minimal adverse viability impacts. Over 80% of embryos showed more than 50% inhibition in their ISV development at 20 and 40 μg/mL. PtR2 at 20 μg/mL substantially reduced human umbilical vein endothelial cell (HUVEC) migration up to 40%, considerable destruction of the formed tubes in the tube formation and microvasculature in CAM assays. Immunocytochemistry showed a marked reduction in vascular endothelial cadherin (VE-cadherin) abundance at cell junctions concurrent with substantial reduction of phospho-Akt (p-Akt) and β-catenin protein expressions. Phytochemical profile of PtR2 showed a rich source of cardenolide structures, including ghalakinoside, calactin and calotropin derivatives.

Conclusion: Thus, the P. tomentosa cardenolide-rich fraction (PtR2) may hold a considerable promise for an antiangiogenic impact by impairment of endothelial cell (EC) migration and viability. Graphical abstract.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-020-00356-7DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7704873PMC
December 2020

Triterpene glycosides from Silene odontopetala.

Phytochemistry 2020 Aug 22;176:112404. Epub 2020 May 22.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II, 84084, Salerno, Italy.

Silene species are known for their use in traditional medicine in treating several diseases. To the authors' knowledge there is no report on the chemical composition of S. odontopetala. Therefore, the phytochemical investigation of the methanol extract of S. odontopetala was carried out, leading to the isolation of six undescribed oleanane-type glycosides along with the known saponin azukisaponin IV. Their structures were elucidated by the analysis of 1D and 2D-NMR experiments, along with mass spectrometry analysis. The cytotoxic activity of oleanane-type saponins was evaluated against a small panel of cancer cell lines, including PC-3 (prostate carcinoma cells), MCF-7 (breast cancer cells), A549 (alveolar basal carcinoma cells), and HeLa (cervical carcinoma cells). Furthermore, the activity of isolated compounds against a normal cell line HEK-293, used for assessing their cytotoxicity, was evaluated.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.phytochem.2020.112404DOI Listing
August 2020

Phytochemical investigation of Scabiosa sicula guided by a preliminary HPLC-ESIMS profiling.

Phytochemistry 2020 Jun 21;174:112350. Epub 2020 Mar 21.

Dipartimento di Farmacia, Università Degli Studi di Salerno, Via Giovanni Paolo II, 84084, Salerno, Italy. Electronic address:

The genus Scabiosa (Caprifoliaceae) is represented by 80 species, widely used as medicinal plants for their positive effects on human diseases. On the basis of the interesting biological activity shown by Scabiosa spp., the phytochemical investigation of Scabiosa sicula L., never investigated before, was carried out. An initial LC-MS profile of the MeOH extract of S. sicula whole plant guided the isolation of 34 compounds, of which the structures were unambiguously elucidated by NMR analysis as phenolic compounds and triterpene saponins, among which eight undescribed compounds. Moreover, the total phenolic content of S. sicula methanol extract has been evaluated. On the basis of the pharmacological activities reported for Scabiosa species the antioxidant activity of the methanol extract was tested by TEAC and DPPH assays. Finally, the α-glucosidase inhibitory activity of the methanol extract was assayed, showing an IC value (49 μg/mL) comparable to that exerted by acarbose (90 μg/mL), used as positive control.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.phytochem.2020.112350DOI Listing
June 2020

Natural Products Targeting ER Stress, and the Functional Link to Mitochondria.

Int J Mol Sci 2020 Mar 11;21(6). Epub 2020 Mar 11.

Dipartimento di Farmacia, Università degli Studi di Salerno, Via Giovanni Paolo II 132, 84084 Fisciano (Salerno), Italy.

The endoplasmic reticulum (ER) is a dynamic organelle essential for intracellular homeostasis maintenance, controlling synthesis, the folding of secreted and membrane-bound proteins, and transport of Ca. During cellular stress, ER dysfunction leads to the activation of unfolded protein response (UPR) due to accumulated misfolded proteins in the ER. This condition is referred as ER stress. Mitochondria and ER form a site of close contact (the mitochondria-associated membrane, MAM) which is a major platform exerting important physiological roles in the regulation of intracellular Ca homeostasis, lipid metabolism, mitochondrial fission, autophagosome formation, and apoptosis progression. Natural products have been receiving increasing attention for their ability to interfere with ER stress. Research works have focused on the capacity of these bioactive compounds to induce apoptosis by activating ER stress through the ER stress-mediated mitochondrial apoptotic pathway. In this review we discuss the role of natural products in the signaling communication between ER and mitochondria, focusing on the effects induced by ER stress including Ca permeability transition and UPR signaling (protein kinase R-like ER kinase/mitofusin 2).
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/ijms21061905DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7139827PMC
March 2020

Chestnut shells (Italian cultivar "Marrone di Roccadaspide" PGI): Antioxidant activity and chemical investigation with in depth LC-HRMS/MS rationalization of tannins.

Food Res Int 2020 03 20;129:108787. Epub 2019 Nov 20.

Dipartimento di Farmacia, Università degli Studi di Salerno, via Giovanni Paolo II n. 132, I-84084 Fisciano (SA), Italy. Electronic address:

In Italy a particularly valuable chestnut is "Marrone di Roccadaspide", a protected geographical indication (PGI) product, deriving from a Castanea sativa cultivar, typical of Salerno province in Campania region. As chestnut industrial processes yield a large amount of shell by-products, in this study the possibility to retrain this waste food as potential source of bioactives was investigated. The ability of "Marrone di Roccadaspide" shell MeOH extract to modulate the pro-inflammatory transcriptional factor NF-κB after LPS stimulation, along with the antioxidant activity by a cell-based in vitro test, were evaluated. To correlate the NF-κB inhibition (67.67% at 5 μg/mL) and the strong antioxidant activity to the chemical composition, an analytical approach based on LC-ESI/LTQOrbitrap/MS/MS along with NMR characterization of isolated compounds was developed. The identification of hydrolysable and condensed tannins, along with flavonoids, phenol glucosides, ellagic acid derivatives, and triterpenoids was accomplished. The most representative compounds were quantitatively analyzed by LC-ESI/QTrap/MS/MS, showing bartogenic acid as the compound occurring in the highest amount (103.08 mg/100 g shells). With the aim to explore the possibility to employ chestnut shells as suitable source of bioactives for the preparation of functional ingredients, the chemical composition and the antioxidant activity of "eco-friendly" extracts (EtOH and EtOH:HO 7:3) was finally evaluated, showing a high superimposability of the EtOH:HO (7:3) extract to the MeOH extract.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.foodres.2019.108787DOI Listing
March 2020

Comparative Phytochemical Characterization, Genetic Profile, and Antiproliferative Activity of Polyphenol-Rich Extracts from Pigmented Tubers of Different Varieties.

Molecules 2020 Jan 6;25(1). Epub 2020 Jan 6.

Department of Precision Medicine, University of Campania "Luigi Vanvitelli", Via L. De Crecchio 7, 80138 Naples, Italy.

Plants produce a vast array of biomolecules with beneficial effects for human health. In this study, polyphenol and anthocyanin-rich extracts (PAE) from pigmented tubers of L. varieties "Blue Star", "Magenta Love", and "Double Fun" in comparison with the more extensively studied "Vitelotte" were evaluated and compared for antiproliferative effects in human leukemia cells, and their phytochemical and genetic profiles were determined. In U937 cells, upon treatment with PAE, it was possible to reveal the expression of specific apoptotic players, such as caspase 8, 9, 3, and poly (ADP-ribose) polymerase (PARP), as well as the induction of monocyte and granulocyte differentiation. A liquid chromatography/electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) investigation revealed the presence of polyphenolic compounds in all the varieties of potatoes analyzed, among which caffeoyl and feruloyl quinic acid derivatives were the most abundant, as well as several acylated anthocyanins. Each pigmented variety was genotyped by DNA-based molecular markers, and flavonoid-related transcription factors were profiled in tubers in order to better characterize these outstanding resources and contribute to their exploitation in breeding. Interesting biological activities were observed for "Blue Star" and "Vitelotte" varieties with respect to the minor or no effect of the "Double Fun" variety.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/molecules25010233DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6983029PMC
January 2020

Detection and comparison of phenolic compounds in different extracts of black currant leaves by liquid chromatography coupled with high-resolution ESI-LTQ-Orbitrap MS and high-sensitivity ESI-Qtrap MS.

J Pharm Biomed Anal 2020 Feb 28;179:112926. Epub 2019 Oct 28.

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 84084, Fisciano, SA, Italy.

Liquid preparations such as tinctures and infusion derived from Ribes nigrum L. (black currant) leaves are widely used in Europe. Despite the various uses reported for the infusion and hydroalcoholic extracts of the leaves of this species, their chemical profile has not yet been defined. In the present study, the infusion, hydroalcholic and methanolic extracts prepared from R. nigrum leaves were analyzed. LC-MS analyses of these extracts allowed the characterization of 31 phenolic compounds mainly belonging to organic acids, flavonoids, catechins and its oligomers. Quantitative results proved that these preparations are a rich source of polyphenols and flavonoids and among them the infusion presented the highest polyphenol levels. A metabolomics approach was also used for the comparison and evaluation of the chemical composition of the different extracts obtained from R. nigrum leaves.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jpba.2019.112926DOI Listing
February 2020

Garcinol and Related Polyisoprenylated Benzophenones as Topoisomerase II Inhibitors: Biochemical and Molecular Modeling Studies.

J Nat Prod 2019 10 16;82(10):2768-2779. Epub 2019 Oct 16.

Dipartimento di Farmacia , Università degli Studi di Salerno , Via Giovanni Paolo II 132 , 84084 Fisciano (SA) , Italy.

Garcinol, a polyisoprenylated benzophenone isolated from genus, has been reported to inhibit eukaryotic topoisomerase I and topoisomerase II at concentrations comparable to that of etoposide (∼25-100 μM). With the aim to clarify the underlying molecular mechanisms by which garcinol inhibits human topoisomerase IIα and topoisomerase IIβ, biochemical assays along with molecular docking and molecular dynamics studies were carried out on garcinol and six congeners. The biochemical results revealed that garcinol derivatives appear to act as catalytic inhibitors of topoisomerase II and to inhibit ATP hydrolysis by topoisomerase II via some form of mixed inhibition. The computational investigation identified the structural elements responsible for binding to the biological target and also provided information for the eventual design of more selective and potent analogues. Collectively, our data suggest that garcinol-type agents may bind to the DNA binding surface and/or ATP domain of type II topoisomerases to antagonize function.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jnatprod.9b00382DOI Listing
October 2019

Plant Specialized Metabolites in Hazelnut (Corylus avellana) Kernel and Byproducts: An Update on Chemistry, Biological Activity, and Analytical Aspects.

Planta Med 2019 Aug 27;85(11-12):840-855. Epub 2019 Jun 27.

Dipartimento di Farmacia, Università degli Studi di Salerno, Fisciano (SA), Italy.

(hazelnut) is one of the most popular tree nuts on a worldwide basis. The main products of are kernels, a nutritious food, with a high content of healthy lipids, contained in a hard shell. In recent years, along with the ongoing research carried out on hazelnut kernels, a growing interest has been addressed to the hazelnut byproducts including hazelnut skin, hazelnut hard shell, and hazelnut green leafy cover as well as hazelnut tree leaf. These byproducts deriving from the roasting, cracking, shelling/hulling, and harvesting processes have been found as a source of "phytochemicals" with biological activity. The aim of this review is to provide a comprehensive and critical update on the chemistry and biological activity of specialized metabolites occurring in hazelnut kernels and byproducts. Phenolics are the most abundant phytochemicals not only in the kernels, but also in other processing byproducts. Attention has been also devoted to taxane derivatives isolated from leaves. An overview on the biological activity, mainly antioxidant, antiproliferative, and antimicrobial along with less common biological effects, has been provided, contributing to highlight as a source of bioactive phytochemicals with the potential to exert beneficial effects on human health. Finally, analytical techniques for the quali-quantitative analysis of specialized metabolites occurring in the different parts of have been reviewed.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1055/a-0947-5725DOI Listing
August 2019

Cytotoxicity of cucurbitacin E from Citrullus colocynthis against multidrug-resistant cancer cells.

Phytomedicine 2019 Sep 2;62:152945. Epub 2019 May 2.

Department of Pharmaceutical Biology, Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany. Electronic address:

Background: Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad.

Purpose: This study outlines CuE's cytotoxic activity against drug-resistant tumor cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR).

Methods: Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towards multidrug resistant cancer cells. Molecular docking (In silico) has been carried out to explore the CuE's mode of binding to ABC transporters (P-gp, BCRP and ABCB5). The visualization of doxorubicin uptake was done by a Spinning Disc Confocal Microscope. The assessment of proteins expression was done by western blotting analysis. COMPARE and hierarchical cluster analyses were applied to identify, which genes correlate with sensitivity or resistance to cucurbitacins (CuA, CuB, CuE, CuD, CuI, and CuK).

Results: Multidrug-resistant cells overexpressing P-gp or BCRP were cross-resistant to CuE. By contrast, TP53 knock-out cells were sensitive to CuE. Remarkably, resistant cells transfected with oncogenic ΔEGFR or ABCB5 were hypersensitive (collateral sensitive) to CuE. In silico analyses demonstrated that CuE is a substrate for P-gp and BCRP. Immunoblot analyses highlighted that CuE targeted EGFR and silenced its downstream signaling cascades. The most striking result that emerged from the doxorubicin uptake by ABCB5 overexpressing cells is that CuE is an effective inhibitor for ABCB5 transporter when compared with verapamil. The COMPARE analyses of transcriptome-wide expression profiles of tumor cell lines of the NCI identified common genes involved in cell cycle regulation, cellular adhesion and intracellular communication for different cucurbitacins.

Conclusion: CuE represents a potential therapeutic candidate for the treatment of certain types of refractory tumors. To best of our knowledge, this is the first time to identify CuE and verapamil as inhibitors for ABCB5 transporter.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.phymed.2019.152945DOI Listing
September 2019
-->