Publications by authors named "Antonella Smeriglio"

55 Publications

The Hull of Ripe Pistachio Nuts (Pistacia vera L.) as a Source of New Promising Melanogenesis Inhibitors.

Plant Foods Hum Nutr 2021 Mar 26;76(1):111-117. Epub 2021 Feb 26.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Giovanni Palatucci, 98168, Messina, Italy.

In the present study an acidified methanol pistachio hull extract was investigated for antioxidant and inhibitory effects on melanin biosynthesis by in vitro and in vivo assays. The chromatographic analysis revealed that cyanidin-3-O-galactoside represents the main compound (98.37%). The pistachio hull extract efficiently inhibits the mono and diphenolase activity of mushroom tyrosinase (IC= 141.07 and 116.08 μg/mL, respectively) and it was able, thanks to its strong antioxidant and free-radical scavenging activities, to hinder the L-DOPA auto-oxidation in a concentration-dependent manner (125-500 μg/mL). Results of in vivo assay showed that the treatment with pistachio hull extract (10 μg/mL) reduced pigmentation in zebrafish embryos at early stages of development (60.01% of inhibition vs control). In conclusion, these findings suggest that the ripe pistachio hull may be considered as a promising source of antioxidant and skin whitening agents for the development of new products useful in preventing the pigmentation disorders in humans and/or to improve the food quality.
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http://dx.doi.org/10.1007/s11130-021-00883-xDOI Listing
March 2021

Antioxidant and Anti-Inflammatory Activity of Flavanones Mix and Its Stability after In Vitro Simulated Digestion.

Antioxidants (Basel) 2021 Jan 20;10(2). Epub 2021 Jan 20.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, 98168 Messina, Italy.

Recently, several studies have highlighted the role of flavanones in counteracting oxidative stress and inflammatory response in bowel diseases. The aim of study was to identify the most promising flavanones by a preliminary antioxidant and anti-inflammatory screening by in vitro cell-free assays, and then to mix the most powerful ones in equimolar ratio in order to investigate a potential synergistic activity. The obtained flavanones mix (FM) was then subjected to in vitro simulated digestion to evaluate the availability of the parent compounds at the intestinal level. Finally, the anti-inflammatory activity was investigated on a Caco-2 cell-based model stimulated with interleukin (IL)-1β. FM showed stronger antioxidant and anti-inflammatory activity with respect to the single flavanones, demonstrating the occurrence of synergistic activity. The LC-DAD-ESI-MS/MS analysis of gastric and duodenal digested FM (DFM) showed that all compounds remained unchanged at the end of digestion. As proof, a superimposable behavior was observed between FM and DFM in the anti-inflammatory assay carried out on Caco-2 cells. Indeed, it was observed that both FM and DFM decreased the IL-6, IL-8, and nitric oxide (NO) release similarly to the reference anti-inflammatory drug dexamethasone.
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http://dx.doi.org/10.3390/antiox10020140DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7908975PMC
January 2021

Antioxidant, Anti-Inflammatory and Anti-Angiogenic Properties of Juice.

Front Pharmacol 2020 3;11:593506. Epub 2020 Dec 3.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina, Italy.

juices are a rich source of bioactive compounds with various and well-known health benefits. The aim of this study was to investigate the polyphenols and ascorbic acid content as well as to investigate the antioxidant, anti-inflammatory and anti-angiogenic properties of the juice of an ancient Mediterranean species, Risso (CLJ). The antioxidant and anti-inflammatory activities were evaluated by several cell-free and cell-based assays, whereas two different models, the chick chorioallantoic membrane (CAM) and the zebrafish embryos, were used to characterize the anti-angiogenic properties. Twenty-eight polyphenols were identified by RP-LC-DAD-ESI-MS analysis (flavonoids 68.82% and phenolic acids 31.18%) with 1-caffeoyl-5-feruloylquinic acid and kaempferol 3'-rhamnoside, which represent the most abundant compounds (25.70 and 23.12%, respectively). HPLC-DAD analysis showed a high ascorbic acid content (352 mg/kg of CLJ), which contributes with polyphenols to the marked and dose-dependent antioxidant and anti-inflammatory properties observed. CLJ showed strong and dose-dependent anti-angiogenic activity as highlighted by the inhibition of blood vessel formation on CAMs and the decrease of endogenous alkaline phosphatase on zebrafish embryos. Moreover, within the concentration range tested, no dead or malformed embryos were recorded. Certainly, further studies are needed to investigate the molecular mechanisms underlying these promising biological effects, but considering the evidence of the present study, the use of CLJ as a ready-to drink safe prevention strategy for inflammatory-based diseases correlated to angiogenesis could be justified.
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http://dx.doi.org/10.3389/fphar.2020.593506DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7744484PMC
December 2020

Phytochemical Profile, Safety Assessment and Wound Healing Activity of L.

Plants (Basel) 2020 Dec 10;9(12). Epub 2020 Dec 10.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via Giovanni Palatucci, 98168 Messina, Italy.

The aim of study was to validate, by in vitro and in vivo studies, the traditional use for wound-healing activity of L. Reversed-phase liquid chromatography coupled with diode array detection and electrospray ion trap mass spectrometry (RP-LC-DAD-ESI-MS) analysis allowed to identify eleven polyphenols with chlorogenic acid as the most abundant compound (3.75 g/100 g of dry extract). After that, antibacterial activity as well as acute dermal and oral toxicity were assessed in animal models. In order to investigate the wound-healing activity of methanol extract, two ointments were formulated (MEO 5% and 10%). The ointment with the highest concentration of plant extract (10%) showed a statistically significant effect on the rats wound contraction, similar to that exerted by the reference drug Cicatryl-Bio. Moreover, methanol extract showed the best antibacterial activity against the Gram-negative ATCC 10536 (MIC 1.25-2.5 mg/mL) and the Gram-positive ATCC 6538 (0.31-0.625 mg/mL). The absence of oral and topical toxicity of the treated animals allowed to establish the safety of the ointments. Overall, data collected in the present study support and validate the use of as a wound healing agent in the Algerian traditional medicine.
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http://dx.doi.org/10.3390/plants9121744DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7763807PMC
December 2020

Understanding the Fate of Almond ( (Mill.) D.A. Webb) Oleosomes during Simulated Digestion.

Nutrients 2020 Nov 5;12(11). Epub 2020 Nov 5.

Department of Chemical, Biological, Pharmaceutical and Environmental Science, University of Messina, Via Giovanni Palatucci, 98168 Messina, Italy.

Background: Almond kernels contain phytochemicals with positive health effects in relation to heart disease, diabetes and obesity. Several studies have previously highlighted that almond cell wall encapsulation during digestion and particle size are factors associated with these benefits. In the present study, we have characterized almond oleosomes, natural oil droplets abundant in plants, and we have investigated their integrity during simulated gastrointestinal digestion.

Methods: Oleosomes were visualized on the almond seed surface by imaging mass spectrometry analysis, and then characterized in terms of droplet size distribution by dynamic light scattering and protein profile by liquid chromatography high-resolution tandem mass spectrometry analysis.

Results: The almond oleosomes' distribution remained monomodal after in vitro mastication, whereas gastric and duodenal digestion led to a bimodal distribution, albeit characterized mainly by a prevalent population with a droplet size decrease related to a rearrangement of the protein profile. Oleosins, structural proteins found in plant oil bodies, persisted unchanged during simulated mastication, with the appearance of new prunin isoforms after gastric and duodenal digestion.

Conclusions: The rearrangement of the protein profile could limit lipid bioaccessibility. The data improve our understanding of the behavior of almond lipids during gastrointestinal digestion, and may have implications for energy intake and satiety imparted by almonds.
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http://dx.doi.org/10.3390/nu12113397DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7694400PMC
November 2020

Antioxidant activity of Hydroxytyrosol and Vitamin E reduces systemic inflammation in children with paediatric NAFLD.

Dig Liver Dis 2020 Oct 12. Epub 2020 Oct 12.

Research Unit of Molecular Genetics of Complex Phenotypes, Bambino Gesù Children's Hospital, IRCCS, Rome, Italy. Electronic address:

Background: The rise in paediatric non-alcoholic fatty liver disease (NAFLD) is particularly alarming. We recently reported that Hydroxytyrosol (HXT) and Vitamin E (VitE) may improve oxidative stress, insulin resistance, and steatosis in children with biopsy-proven NAFLD.

Aim: Here, we investigated if HXT+VitE may reduce systemic inflammation in the above-mentioned patients.

Methods: This study analysed the plasma levels of IL (interleukin)-6, IL-1β, IL-10, tumour necrosis factor (TNF)-α, 4‑hydroxy-2-nonenal (4-HNE) and 8-hydroxy-2'deoxyguanosine (8-OHdG) in children enrolled in the HXT+VitE trial (ClinicalTrials.gov, NCT02842567).

Results: Changes in markers of systemic inflammation were found in both placebo (Pla) and HXT+VitE. In particular, after four months, the levels of IL-1β and TNF-α were reduced in both groups, while IL-6 decreased, and IL-10 increased significantly only in the group treated with HXT+VitE. Children treated with HXT+VitE showed a significant decrease of 4-HNE and 8-OHdG that correlated with the improvement of triglyceride levels. Noticeably, only the 8-OHdG decrease correlated with steatosis amelioration and with the increase of IL-10 levels.

Conclusion: The treatment with HXT and VitE reduced the NAFLD-related systemic inflammation in children, mainly by an increase of IL-10 circulating levels that occurred in response to DNA damage recovery, ultimately improving steatosis and hypertriglyceridemia.
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http://dx.doi.org/10.1016/j.dld.2020.09.021DOI Listing
October 2020

Antioxidant and antimicrobial activity of two standardized extracts from a new Chinese accession of non-psychotropic Cannabis sativa L.

Phytother Res 2021 Feb 9;35(2):1099-1112. Epub 2020 Oct 9.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina, Italy.

The purpose of this study was to evaluate the antioxidant and antimicrobial properties of two extracts from a new Chinese accession (G-309) of Cannabis sativa L. (Δ -tetrahydrocannabinol <0.2%) with high content of propyl side chain phytocannabinoids. Dried flowering tops, as such and after hydrodistillation of the essential oil, were extracted with acidic hexane to produce the Cannabis Chinese hexane extract 1 (CChHE1) and 2 (CChHE2), respectively. The phytochemical profile of CChHE1 and CChHE2 was investigated by gas chromatography-mass spectrometry (GC-MS) and liquid chromatography-diode array detector-electrospray ionization-tandem mass spectrometry (LC-DAD-ESI-MS/MS) analyses. The antioxidant properties were assessed by several in vitro cell-free assays. The antimicrobial activity was evaluated against Gram-positive and Gram-negative bacteria and the yeast Candida albicans. Phytochemical analyses highlighted a high content of cannabidivarinic acid (CBDVA) and tetraydrocannabivarinic acid (THCVA) in CChHE1, and cannabidivarin (CBDV) and tetraydrocannabivarin (THCV) in CChHE2. Both extracts showed remarkable antioxidant activity and strong antimicrobial properties (MIC 39.06 and MBC 39.06-78.13 μg/ml) against both ATCC and methicillin-resistant clinical strains of Staphylococcus aureus. In conclusion, standardized extracts of C. sativa Chinese accession could be promising for their possible use as novel antibacterial agents for the treatment of widespread S. aureus infections.
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http://dx.doi.org/10.1002/ptr.6891DOI Listing
February 2021

Consumption of . (Cashew Nuts) Inhibits Oxidative Stress through Modulation of the Nrf2/HO-1 and NF-kB Pathways.

Molecules 2020 Sep 26;25(19). Epub 2020 Sep 26.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina, Italy.

Ischemia/reperfusion injury is a severe disorder associated with a high mortality. Several antioxidant and pharmacological properties of cashew nuts () and its metabolites from different countries have recently been described. It is a medicinal plant with important therapeutic effects. This study aimed to verify the effect of an oral administration of cashew nuts in a rat model of ischemia/reperfusion (I/R). Adult male rats were subjected to intestinal I/R injury by clamping the superior mesenteric artery for 30 min and then allowing animals to 1 h of reperfusion. Rats subjected to I/R of the gut showed a significant increase in different biochemical markers. In particular, we evaluated lipid peroxidation, tissue myeloperoxidase activity, protein carbonyl content, reactive oxygen species generation and decreased antioxidant enzyme activities. Western blot analysis showed the activation of the NRF2 and NF-kB pathways. Increased immunoreactivity to nitrotyrosine, PARP, P-selectin, and ICAM-1 was observed in the ileum of rats subjected to I/R. Administration of cashew nuts (100 mg/kg) significantly reduced the mortality rate, the fall in arterial blood pressure, and oxidative stress and restored the antioxidant enzyme activities by a mechanism involving both NRF2 and NF-kB pathways. Cashew nuts treatments reduced cytokines plasma levels, nitrotyrosine, and PARP expression as well as adhesion molecules expressions. Additionally, cashew nuts decreased the intestinal barrier dysfunction and mucosal damage, the translocation of toxins and bacteria, which leads to systemic inflammation and associated organs injuries in particular of liver and kidney. Our study demonstrates that cashew nuts administration exerts antioxidant and pharmacological protective effects in superior mesenteric artery occlusion-reperfusion shock.
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http://dx.doi.org/10.3390/molecules25194426DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7582295PMC
September 2020

In vitro intestinal transport and anti-inflammatory properties of ideain across Caco-2 transwell model.

Fitoterapia 2020 Oct 17;146:104723. Epub 2020 Sep 17.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via Giovanni Palatucci, 98168 Messina, Italy. Electronic address:

The aim of the study was to investigate the absorption and transport mechanisms as well as the anti-inflammatory properties of ideain on Caco-2 transwell model. A concentration and time-dependent bidirectional transport was highlighted; despite this, a clear saturation of the transepithelial absorption in the A-B direction was observed at ideain concentration > 10 μM, suggesting an involvement of membrane transporters. Comparing Papp and PDR values of ideain (10 μM) to reference drugs with a low to a high apparent permeability, it is possible to predict a low in vivo absorption, with a transport efficiency of 1.03%. Co-treatments with several EDTA-Na concentrations (1-5 mM) and P-gp inhibition studies with verapamil 100 μM ruled out a passive diffusion of this molecule as well the possibility that P-gp could affect ideain absorption. Inhibition studies using 2 mM phloridzin (SGLT1 inhibitor) and 2 mM phloretin (GLUT2 inhibitor), showed a clear SGLT1 and GLUT2 involvement in the ideain absorption, with SGLT1, which plays the pivotal role. Finally, preliminary anti-inflammatory studies showed that ideain is able to modulate, at a pharmanutritional dose, and with a comparable activity in respect to the reference drug dexamethasone (10 μM), the LPS-induced inflammation in Caco-2 transwell model, which makes it a potentially useful molecule for nutraceutical purpose.
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http://dx.doi.org/10.1016/j.fitote.2020.104723DOI Listing
October 2020

Evaluation of Anthocyanin Profile, Antioxidant, Cytoprotective, and Anti-Angiogenic Properties of Flowers.

Plants (Basel) 2020 Aug 17;9(8). Epub 2020 Aug 17.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via G. Palatucci, 98168 Messina, Italy.

Lemon bottlebrush ( (Curtis) Skeels) is one of the most common ornamental plants, diffused worldwide, and characterized by the presence of flowers with an intense red/purple coloration. There is increasing interest in the use and application of anthocyanins for their unique structural/chemical features in both food and pharmaceutical applications. RP-HPLC-DAD-ESI-MS/MS analysis of an enriched fraction of acidified methanolic extract of flowers allow the possibility of identifying, for the first time, the presence of four anthocyanins: cyanidin-3,5--diglucoside (cyanin), peonidin-3,5--diglucoside (peonin), cyanidin-3--glucoside, and cyanidin-coumaroylglucoside-pyruvic acid. Moreover, the evaluation of antioxidant and biological potential showed a remarkable activity of this fraction, able to actively scavenge DPPH, AAPH, and ABTS radicals, and to counteract the β-carotene-bleaching. In addition, it protects human mononuclear cells from oxidative injuries and prevents angiogenesis (acting in the range of few μg/ml); furthermore, it does not show significant iron-chelating ability (up to 200 µg/mL). The easy way of cultivation, robustness, and adaptability to different environments make the flowers of this plant a useful source of anthocyanins, with remarkable health promoting properties.
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http://dx.doi.org/10.3390/plants9081045DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7465370PMC
August 2020

Comparative and Functional Screening of Three Species Traditionally used as Antidepressants: L., Jones ex Roxb. and (D.Don) DC.

Plants (Basel) 2020 Aug 5;9(8). Epub 2020 Aug 5.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via Giovanni Palatucci, 98168 Messina, Italy.

The essential oils (EOs) of three Caprifoliaceae species, the Eurasiatic (Vo), the Himalayan (Vj) and (Nj), are traditionally used to treat neurological disorders. Roots/rhizomes micromorphology, DNA barcoding and EOs phytochemical characterization were carried out, while biological effects on the nervous system were assessed by acetylcholinesterase (AChE) inhibitory activity and microelectrode arrays (MEA). Nj showed the highest inhibitory activity on AChE (IC 67.15 μg/mL) followed by Vo (IC 127.30 μg/mL) and Vj (IC 246.84 μg/mL). MEA analyses on rat cortical neurons, carried out by recording mean firing rate (MFR) and mean bursting rate (MBR), revealed stronger inhibition by Nj (IC 18.8 and 11.1 μg/mL) and Vo (16.5 and 22.5 μg/mL), compared with Vj (68.5 and 89.3 μg/mL). These results could be related to different EO compositions, since sesquiterpenes and monoterpenes significantly contribute to the observed effects, but the presence of oxygenated compounds such as aldehydes and ketones is a discriminating factor in determining the order of potency. Our multidisciplinary approach represents an important tool to avoid the adulteration of herbal drugs and permits the evaluation of the effectiveness of EOs that could be used for a wide range of therapeutic applications.
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http://dx.doi.org/10.3390/plants9080994DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7464919PMC
August 2020

Modulatory Activities of Plant Extracts on Jellyfish Cytotoxicity.

Wilderness Environ Med 2020 Sep 15;31(3):266-272. Epub 2020 Jul 15.

Biophysics Institute, National Research Council (CNR), Genova, Italy; Department of Pharmacy (DIFAR), University of Genova, Genova, Italy.

Introduction: The potential efficacy of selected plant extracts to counteract the dermal toxicity of jellyfish envenomation was investigated using an in vitro cell culture model.

Methods: We studied plant extracts from Carica papaya, Ananas comosus, and Bouvardia ternifolia, known for their antivenom properties, in pairwise combinations with tissue homogenates of the jellyfish Pelagia noctiluca, Phyllorhiza punctata, and Cassiopea andromeda, to evaluate modulations of jellyfish cytotoxic effects. L929 mouse fibroblasts were incubated with pairwise jellyfish/plant extract combinations and examined by MTT assay (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide).

Results: C papaya and A comosus significantly lowered the cytotoxicity of P noctiluca and P punctata but induced a slight worsening of C andromeda cytotoxicity. Conversely, B ternifolia was protective against P punctata, ineffective against P noctiluca, and worsened C andromeda cytotoxicity.

Conclusions: Data showed species-specific and contrasting effects of plant extracts, suggesting that those containing protease activities, namely A comosus and C papaya, are more effective in lowering the cytotoxicity of jellyfish venom containing toxic peptidic factors such as phospholipase A. However, all examined plants require further investigation in vivo to evaluate their ability to counteract jellyfish injury to the skin.
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http://dx.doi.org/10.1016/j.wem.2020.03.004DOI Listing
September 2020

Chemical Composition and Biological Activities of the Essential Oils of and .

Front Microbiol 2020 15;11:409. Epub 2020 Apr 15.

Institute of Food Sciences, CNR-ISA, Italian National Research Council, Avellino, Italy.

The aim of this study was to characterize the chemical composition and to evaluate the antimicrobial and phytotoxic properties of the essential oils (EOs) obtained from leaves of chemotype "Variety B" and , native to Australia. Geranyl acetate, γ-terpinene, geraniol, terpinolene, α-pinene, -cimene, and linalool were the main components in EO, confirming also the existence of several chemotypes in such taxa; on the other hand, 1,8-cineole, -sabinene hydrate acetate, globulol, longicyclene, terpinolene, and camphene were present in major amounts in the EO. Chemical analysis of revealed that it belongs to the variety "B." EO showed good antibacterial activity, with an MIC of 0.5 and 2 μg/mL against , and , respectively. The activity of EO was stronger than EO, whose maximum MIC reached 5 μg/mL. and EOs were particularly effective in inhibiting the biofilm formation by , already at a concentration of 0.01 μg/mL. The other strains were resistant to both EOs up to a dose of 0.05 μg/mL. The maximum inhibition on biofilm formed by was recorded for EO, reaching a value of 93.12% at 1.0 μg/mL. This is the first manuscript which studies the biofilm inhibition by EOs and evaluates their effects on biofilm metabolism. Both EOs were more effective against . In addition, even though EO 0.1 μg/mL was unable to inhibit biofilm formation by , it decreased the metabolic activity of the biofilm to 78.55% compared to control; furthermore, despite it inducing a relatively low inhibition (66.67%) on biofilm formation, it markedly affected metabolic activity, which decreased to 16.09% with respect to the control. On the contrary, EO 0.5 μg/mL induced a 79.88% inhibition of biofilm, maintaining a high metabolic activity (90.89%) compared to the control. Moreover, this EO showed inhibitory activity against radical elongation of and the germination of radish. On the contrary, EO showed no phytotoxic activity.
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http://dx.doi.org/10.3389/fmicb.2020.00409DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7174609PMC
April 2020

Chemical Composition and Biological Activities of Essential Oils from Peels of Three Species.

Molecules 2020 Apr 19;25(8). Epub 2020 Apr 19.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, 98168 Messina, Italy.

Background: Fruit peels are generally underutilized byproducts of the food industry, although they are valuable sources of bioactive compounds. The aim of this study is to evaluate a new application for three peel EOs as bio-herbicides.

Methods: After a micro-morphological evaluation of peels by SEM analysis, the phytochemical composition of the EOs of Risso & Poit., Raf., and (L.) Osbeck was characterized by GC/FID and GC/MS analyses. The in vitro phytotoxicity against germination and initial radical elongation of several crop and weed species was evaluated. Furthermore, the eco-compatibility of these EOs has been assessed by the brine shrimp () lethality assay.

Results: SEM analysis highlighted the morphometric differences of the schizolysigenous pockets among the peels of the three species. Oxygenated monoterpenes are the main constituents in (51.09%), whereas monoterpene hydrocarbons represent the most abundant compounds in (82.15%) and (80.33%) EOs. They showed marked and selective phytotoxic activity in vitro, often at very low concentration (0.1 μg/mL) against all plant species investigated, without showing any toxicity on , opening the perspective of their use as safe bio-herbicides.
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http://dx.doi.org/10.3390/molecules25081890DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7221518PMC
April 2020

Promising in vitro antioxidant, anti-acetylcholinesterase and neuroactive effects of essential oil from two non-psychotropic Cannabis sativa L. biotypes.

Phytother Res 2020 Sep 20;34(9):2287-2302. Epub 2020 Apr 20.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina, Italy.

The aim of this study was to compare the micro-morphological features of two different non-drug Cannabis sativa L. biotypes (Chinese accession G-309 and one fibrante variety) and to evaluate the phytochemical profile as well as some biological properties of the essential oils (EOs) obtained by hydrodistillation of dried flowering tops. After a micro-morphological evaluation by scanning electron microscopy, the phytochemical composition was analysed by GC-FID and GC-MS analyses. Antioxidant and anti-acetylcholinesterase properties were investigated by several in vitro cell-free assays, while neuroactive effects were evaluated on mouse cortical neuronal as well as human iPS cell-derived central nervous system cells grown on MEA chips. Both EOs showed strong antioxidant properties mainly attributable to the high content of hydroxylated compounds as well as significant anti-acetylcholinesterase activities (IC 74.64 and 57.31 μg/ml for Chinese accession and fibrante variety, respectively). Furthermore, they showed a concentration-dependent inhibition of spontaneous electrical activity of human and mouse neuronal networks, with the fibrante variety, which showed the best activity (MFR, IC 0.71 and 10.60 μg/ml, respectively). The observed biological activities could be due to a synergic effect between terpenes and phytocannabinoids, although in vivo studies, which clarify the molecular mechanism, are still lacking.
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http://dx.doi.org/10.1002/ptr.6678DOI Listing
September 2020

The Antioxidant and Anti-Inflammatory Properties of L. Cashew Nuts in a Mouse Model of Colitis.

Nutrients 2020 Mar 20;12(3). Epub 2020 Mar 20.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina, Italy.

Background: L. is a tropical plant used for the treatment of inflammatory diseases. The goal of the present work was to investigate the anti-inflammatory and anti-oxidant potential of oral administration of cashew nuts (from L.) in a mouse model of colitis.

Methods: Induction of colitis was performed by intrarectally injection of dinitrobenzene sulfonic acid (DNBS). Cashew nuts were administered daily orally (100 mg/kg) in DNBS-injected mice.

Results: Four days after DNBS, histological and macroscopic colon alterations as well as marked clinical signs and increased cytokine production were observed. Neutrophil infiltration, measured by myeloperoxidase (MPO) positive immunostaining, was correlated with up-regulation of adhesion molecules ICAM-1 and P-selectin in colons. Oxidative stress was detected with increased malondialdehyde (MDA) levels, nitrotyrosine, and poly ADP-ribose polymerase (PARP) positive staining in inflamed colons. Oral treatment with cashew nuts reduced histological, macroscopic damage, neutrophil infiltration, pro-inflammatory cytokines and MDA levels, as well as nitrotyrosine, PARP and ICAM-1, and P-selectin expressions. Colon inflammation could be related to nuclear factor (NF)-kB pathway activation and reduced manganese superoxide dismutase (MnSOD) antioxidant activity. Cashew nuts administration inhibited NF-kB and increased MnSOD antioxidant expressions.

Conclusions: The results suggested that oral assumption of cashew nuts may be beneficial for the management of colitis.
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http://dx.doi.org/10.3390/nu12030834DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7146548PMC
March 2020

Flavones: An Update on Sources, Biological Functions, and Health Promoting Properties.

Plants (Basel) 2020 Feb 26;9(3). Epub 2020 Feb 26.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale F. Stagno d'Alcontres 31, 98166, Messina, Italy.

spp. are among the most widespread plants cultivated worldwide and every year millions of tons of fruit, juices, or processed compounds are produced and consumed, representing one of the main sources of nutrients in human diet. Among these, the flavonoids play a key role in providing a wide range of health beneficial effects. Apigenin, diosmetin, luteolin, acacetin, chrysoeriol, and their respective glycosides, that occur in concentrations up to 60 mg/L, are the most common flavones found in fruits and juices. The unique characteristics of their basic skeleton and the nature and position of the substituents have attracted and stimulated vigorous investigations as a consequence of an enormous biological potential, that manifests itself as (among other properties) antioxidant, anti-inflammatory, antiviral, antimicrobial, and anticancer activities. This review analyzes the biochemical, pharmacological, and biological properties of flavones, emphasizing their occurrence in spp. fruits and juices, on their bioavailability, and their ability to modulate signal cascades and key metabolic enzymes both in vitro and in vivo. Electronic databases including PubMed, Scopus, Web of Science, and SciFinder were used to investigate recent published articles on spp. in terms of components and bioactivity potentials.
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http://dx.doi.org/10.3390/plants9030288DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7154817PMC
February 2020

In Vitro Anti-HSV-1 Activity of Polyphenol-Rich Extracts and Pure Polyphenol Compounds Derived from Pistachios Kernels ( L.).

Plants (Basel) 2020 Feb 18;9(2). Epub 2020 Feb 18.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale SS. Annunziata, 98168 Messina, Italy.

Natural compounds are a prominent source of novel antiviral drugs. Several reports have previously shown the antimicrobial activity of pistachio polyphenol extracts. Therefore, the aim of our research was to investigate the activity of polyphenol-rich extracts of natural shelled (NPRE) pistachios kernels ( L.) on herpes simplex virus type 1 (HSV-1) replication. The Vero cell line was used to assess the cytotoxicity and antiviral activity. The cell viability was calculated by detection of cellular ATP after treatment with various concentrations of NPRE. For antiviral studies, five nontoxic-concentrations (0.1, 0.2, 0.4, 0.6, 0.8 mg/mL) were tested. Our study demonstrated that treatment with NPRE (0.4, 0.6, 0.8 mg/mL) reduced the expression of the viral proteins ICP8 (infected cell polypeptide 8), UL42 (unique long UL42 DNA polymerase processivity factor) , and US11 (unique short US11 protein), and resulted in a decrease of viral DNA synthesis. The 50% cytotoxic concentration (CC), 50% inhibitory concentration (EC), and the selectivity index (SI) values for NPRE were 1.2 mg/mL, 0.4mg/mL, and 3, respectively. Furthermore, we assessed the anti-herpetic effect of a mix of pure polyphenol compounds (NS MIX) present in NPRE. In conclusion, our findings indicate that natural shelled pistachio kernels have remarkable inhibitory activity against HSV-1.
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http://dx.doi.org/10.3390/plants9020267DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076519PMC
February 2020

Antiviral activity of plants and their isolated bioactive compounds: An update.

Phytother Res 2020 Apr 19;34(4):742-768. Epub 2019 Dec 19.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina, Italy.

Viral infections represent one of the main causes of disease worldwide, especially today due to the increase of migration, global travel, and urbanization. The several side effects of the conventional drugs and the growing phenomenon of resistance have led researchers to turn to the plant kingdom as a source of potential new antiviral drugs. The aim of this work is to summarize the updated evidence for antiviral activity of different plants and their isolated bioactive compounds, evaluating also the potential interactions, which can occur in cotreatment with conventional antiviral drugs. The plant complexes have proved to be usually more active than their most abundant isolated compounds by hypothesizing synergistic mechanisms. In addition to cellular and molecular investigations, molecular docking studies have proved essential in highlighting the interaction mechanisms of bioactive compounds with target molecules. However, the use of nonstandardized extracts, or too high concentrations in vitro, which do not reproduce their bioavailability in vivo, are often limiting factors. Moreover, the lack of studies concerning the safety profile of plant extracts and their isolated compounds, alone or in combination with conventional antiviral drugs, is the most worrying aspect. In light of this, further studies are needed to validate their possible therapeutic use.
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http://dx.doi.org/10.1002/ptr.6575DOI Listing
April 2020

Antiangiogenic Effects of Coumarins against Cancer: From Chemistry to Medicine.

Molecules 2019 Nov 24;24(23). Epub 2019 Nov 24.

Lake Erie College of Osteopathic Medicine, Bradenton, FL 34211, USA.

Angiogenesis, the process of formation and recruitment of new blood vessels from pre-existing vessels, plays an important role in the development of cancer. Therefore, the use of antiangiogenic agents is one of the most critical strategies for the treatment of cancer. In addition, the complexity of cancer pathogenicity raises the need for multi-targeting agents. Coumarins are multi-targeting natural agents belonging to the class of benzopyrones. Coumarins have several biological and pharmacological effects, including antimicrobial, antioxidant, anti-inflammation, anticoagulant, anxiolytic, analgesic, and anticancer properties. Several reports have shown that the anticancer effect of coumarins and their derivatives are mediated through targeting angiogenesis by modulating the functions of vascular endothelial growth factor as well as vascular endothelial growth factor receptor 2, which are involved in cancer pathogenesis. In the present review, we focus on the antiangiogenic effects of coumarins and related structure-activity relationships with particular emphasis on cancer.
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http://dx.doi.org/10.3390/molecules24234278DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6930449PMC
November 2019

Polyphenol Characterization and Skin-Preserving Properties of Hydroalcoholic Flower Extract from (Orchidaceae).

Plants (Basel) 2019 Nov 14;8(11). Epub 2019 Nov 14.

Department of Earth, Environment and Life Sciences, University of Genova, 16132 Genova, Italy.

(Loisel.) P. Delforge is a Mediterranean orchid whose propagation in vitro has been achieved, making it eligible as a source of bioactive substances. Flowers were analyzed by light and SEM microscopy and used to obtain a polyphenol-rich, hydroalcoholic flower extract (HFE). HFE was characterized for total phenols, flavonoids and proanthocyanidins, and for polyphenol profile by RP-LC-DAD. Antioxidant assays, in vitro collagenase and elastase inhibition, and MTT and cell motility assays on HaCaT keratinocytes were done. Microscopy showed epidermal cells containing anthocyanins in the flower labellum. Flavonoids (flavones and flavan-3-ols) represented the most abundant compounds (42.91%), followed by scopoletin (33.79%), and phenolic acids (23.3%). Antioxidant assays showed strong activities, rating ORAC > FRAP > TEAC > β-carotene bleaching > DPPH > iron-chelation. Biological assays showed elastase and collagenase inhibition (up to 42% and 78%, respectively), improvement of HaCaT cell viability after treatment with 500 μM HO (from 30% to 84% of control), and stimulation of cell migration rate up to 210% of control. In summary, HFE counteracted different free radicals, while protective properties were shown by cell-free and cell-based bioassays, suggesting the possible use of flowers for skin-preserving, repair, and anti-aging applications.
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http://dx.doi.org/10.3390/plants8110502DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6918203PMC
November 2019

The Antimicrobial and Antiviral Activity of Polyphenols from Almond ( L.) Skin.

Nutrients 2019 Oct 3;11(10). Epub 2019 Oct 3.

Department of Chemical, Biological, Pharmaceutical and Environmental Science, University of Messina, Viale SS. Annunziata, 98168 Messina, Italy.

Due to their antimicrobial and antiviral activity potential in vitro, polyphenols are gaining a lot of attention from the pharmaceutical and healthcare industries. A novel antiviral and antimicrobial approach could be based on the use of polyphenols obtained from natural sources. Here, we tested the antibacterial and antiviral effect of a mix of polyphenols present in natural almond skin (NS MIX). The antimicrobial potential was evaluated against the standard American Type Culture Collection (ATCC) and clinical strains of , including methicillin-resistant (MRSA) strains, by minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Herpes simplex virus type I was used for the antiviral assessment of NS MIX by plaque assay. Furthermore, we evaluated the expression of viral cascade antigens. NS MIX exhibited antimicrobial (MIC values of 0.31-1.25 mg/ml) and antiviral activity (decrease in the viral titer ** < 0.01, and viral DNA accumulation * < 0.05) against and HSV-1, respectively. Amongst the isolated compounds, the aglycones epicatechin and catechin showed the greatest activity against ATCC 6538P (MIC values of 0.078-0.15 and 0.15 mg/ml, respectively), but were not active against all the other strains. These results could be used to develop novel products for topical use.
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http://dx.doi.org/10.3390/nu11102355DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836111PMC
October 2019

Nitrogen Headspace Improves the Extra Virgin Olive Oil Shelf-Life, Preserving Its Functional Properties.

Antioxidants (Basel) 2019 Aug 22;8(9). Epub 2019 Aug 22.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, 98168 Messina, Italy.

The functional foods field has recently evolved due to new research being carried out in the food area and greater regulations; these factors have contributed to the creation of health claims, and to the increasing attention that consumers give to health-promoting food products. The aim of this research was to improve the shelf-life of a typical functional food of the Mediterranean diet, the Extra Virgin Olive Oil (EVOO). We focused our attention on the standardization and validation of a production process, starting from the cultivation and harvesting of the olives, which would guarantee a product of quality in terms of bioactive compound content. Furthermore, a methodology/procedure to preserve them in the best way over a long period of time, in order to guarantee the consumer receives a product that retains its functional and organoleptic native properties, was evaluated. The monitoring of biological cultivations, harvesting, milling process, and storage, as well as careful quality control of the analytical parameters (e.g., contents of polyphenols, α-tocopherol, fatty acids, acidity, peroxides, dienes, trienes, ΔK, and antioxidant power) showed that, under the same conditions, a nitrogen headspace is a discriminating factor for the maintenance of the functional properties of EVOO.
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http://dx.doi.org/10.3390/antiox8090331DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6769529PMC
August 2019

Feijoa Fruit Peel: Micro-morphological Features, Evaluation of Phytochemical Profile, and Biological Properties of Its Essential Oil.

Antioxidants (Basel) 2019 Aug 19;8(8). Epub 2019 Aug 19.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, 98168 Messina, Italy.

(O. Berg) Burret (Feijoa) is an evergreen shrub, belonging to the Mirtaceae family. The aim of this study was to investigate the micromorphological features of the feijoa fruit peel and to evaluate the phytochemical profile, as well as the antioxidant, cytoprotective, and antimicrobial properties of its essential oil (EO), by several in vitro cell-free and cell-based assays. The micromorphological analysis showed several schizogenic secretory cavities, immediately below the epidermal layer. Forty compounds were identified and quantified by GC-FID and GC-MS analyses. Sesquiterpenes were the most abundant ones (76.89%), followed by monoterpene hydrocarbons (3.26%), and oxygenated monoterpenes (0.34%). The main compounds were γ-Selinene (17.39%), α-Cariophyllene (16.74%), β-Cariophyllene (10.37%), and Germacene D (5.32%). The EO showed a strong and dose-dependent antioxidant, and free-radical scavenging activity. Furthermore, it showed cytoprotective activity on the lymphocytes, that have been pre-treated with 100 μM tert-butyl-hydroperoxide (t-BOOH), as well as a decrease in intracellular reactive oxygen species (ROS), induced by t-BOOH on erythrocytes. A preliminary antimicrobial screening against GRAM+ and GRAM- bacteria, as well as on fungi highlighted that EO showed the best activity against and (MIC 2.7 mg/mL). In light of these results, feijoa fruit EO could find various applications, especially in the food, nutraceutical, and pharmaceutical fields.
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http://dx.doi.org/10.3390/antiox8080320DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6720543PMC
August 2019

Characterization and Phytotoxicity Assessment of Essential Oils from Plant Byproducts.

Molecules 2019 Aug 14;24(16). Epub 2019 Aug 14.

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

The present work describes the chemical characterization and the phytotoxicity assessment of essential oils (EOs) obtained from spent materials or pruning waste of four plant species: Roscoe used in the juicing industry, L. var. used in the food industry, discarded material of industrial hemp ( L. var. ), and pruning waste from L. The phytochemical profile of the EOs was evaluated by gas chromatographic flame ionization detection (GC-FID) and GC-MS analyses, which highlighted the presence of several compounds with a wide range of biological activities. Among them, application possibilities in agriculture were evaluated by studying the phytotoxic activity against germination and initial radical growth of several seeds such as L., L., L., L., Lam., and L.
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http://dx.doi.org/10.3390/molecules24162941DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6721104PMC
August 2019

Polyphenol Characterization, Antioxidant and Skin Whitening Properties of Alnus cordata Stem Bark.

Chem Biodivers 2019 Sep 28;16(9):e1900314. Epub 2019 Aug 28.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via Giovanni Palatucci, 98168, Messina, Italy.

In this study, we investigated the phenolic composition of the crude extract (MeOH 80 %) of Alnus cordata (Loisel.) Duby stem bark (ACE) and its antioxidant and skin whitening properties. RP-LC-DAD analysis showed a high content of hydroxycinnamic acids (47.64 %), flavanones (26.74 %) and diarylheptanoids (17.69 %). Furthermore, ACE exhibited a dose-dependent antioxidant and free-radical scavenging activity, expressed as half-maximal inhibitory concentration (IC ): Oxygen radical absorbance capacity (ORAC, IC 1.78 μg mL )>Trolox equivalent antioxidant capacity (TEAC, IC 3.47 μg mL )>2,2-Diphenyl-1-picrylhydrazyl (DPPH, IC 5.83 μg mL )>β-carotene bleaching (IC 11.58 μg mL )>Ferric reducing antioxidant power (FRAP, IC 17.28 μg mL ). Moreover, ACE was able to inhibit in vitro tyrosinase activity (IC 77.44 μg mL ), l-DOPA auto-oxidation (IC 39.58 μg mL ) and in an in vivo model it exhibited bleaching effects on the pigmentation of zebrafish embryos (72 h post fertilization) without affecting their development and survival. In conclusion, results show that A. cordata stem bark may be considered a potential source of agents for the treatment of skin disorders due to its bleaching properties and favorable safety profiles, associated to a good antioxidant power.
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http://dx.doi.org/10.1002/cbdv.201900314DOI Listing
September 2019

Safety and efficacy of hydroxytyrosol-based formulation on skin inflammation: in vitro evaluation on reconstructed human epidermis model.

Daru 2019 Jun 26;27(1):283-293. Epub 2019 May 26.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Via Ferdinando Stagno d'Alcontres, 31, Viale SS. Annunziata, 98166, Messina, ME, Italy.

Background: Atopic dermatitis is a multifactorial immune-mediated skin disorder characterized by an alteration of epidermal barrier function and onset of skin lesions, which range from mild erythema to severe lichenification. Treatment consists in hydration with possible use of topical or immunomodulatory corticosteroids, which, however sometimes showed side effects. Recently, the interest in natural compounds has grown significantly and among these, hydroxytyrosol (HT) plays a pivotal role due to its strong and well-known anti-inflammatory activity.

Objectives: The aim of this study was to investigate the safety and efficacy of Fenolia® Eudermal Cream 15 (HT-based formulation) on epidermal barrier impaired as consequence of skin injury.

Methods: Whit this purpose, morphologic and structural as well as anti-inflammatory evaluations, after treatment with pro-inflammatory mediators (PBS 1 X and LPS) and HT-based formulation on reconstructed human epidermis (RHE) were carried out by qualitative (hematoxylin/eosin- and immunostaining) and quantitative (MTT assay, IL-1α and IL-8 release by ELISA) techniques. Furthermore, HT absorption through the epidermal barrier was evaluated by RP-LC-DAD analysis.

Results: A rise in the thickness of the epidermis as well as an appropriate maturation and protein expression (Loricrin, Fillagrin, E-Cadherin and Cytokeratins 5&6) were detected in treated RHE samples. In particular, the HT-based formulation was found to stimulate cell proliferation, as evidenced by the significant increase in Ki67 expression, which suggests the involvement of repair mechanisms, increasing epithelial regeneration and differentiation and improving the epidermal barrier effect. Furthermore, HT-based formulation showed a statistically significant anti-inflammatory activity by reducing both IL-1α and IL-8 release by RHE tissues, greater than the reference drug dexamethasone. Finally, excellent transcutaneous absorption values were found for HT, demonstrating how this new formulation increases the availability of the bioactive compound.

Conclusions: In light of these results, Fenolia® Eudermal Cream 15 could be an effective agent to counteract atopic dermatitis. Graphical abstract Safety and efficacy of hydroxytyrosol-based formulation on skin inflammation: in vitro evaluation on reconstructed human epidermis model.
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http://dx.doi.org/10.1007/s40199-019-00274-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6593001PMC
June 2019

Simulated human digestion of N1-aryl-2-arylthioacetamidobenzimidazoles and their activity against Herpes-simplex virus 1 in vitro.

PLoS One 2019 2;14(5):e0216384. Epub 2019 May 2.

Department of Chemical, Biological, Pharmaceutical and Environmental Science, University of Messina, Messina, Italy.

Drug performance in the gastrointestinal tract (GIT) plays a crucial role in determining release and absorption. In the present work, we assessed the in vitro digestion of two synthetic N1-aryl-2-arylthioacetamidobenzimidazoles (NAABs), NAAB-496 and NAAB-503, using bio-relevant models of the human stomach and small intestine. The activity of NAAB-496 and NAAB-503 against herpes simplex virus (HSV-1) replication was also investigated. NAAB-496 was resistant to pepsin in the gastric environment, with a virtual 100% recovery, which decreased to 43.2% in the small intestine. NAAB-503 was sensitive to pepsin, with 65.7% degradation after 120 min gastric phase. 1H Nuclear magnetic resonance (NMR) post in vitro digestion highlighted an alteration of NAAB-496 after the gastric phase, whereas NAAB-503 appeared comparable to the original spectral data. Both NAAB-496 and NAAB-503 revealed some antiviral activity anti-HSV-1. The 50% effective concentration (EC50) of the compounds was 0.058 mg/mL for NAAB-496 and 0.066 for NAAB-503. Future studies will evaluate the behavior of NAAB-496 within pharmaceutical formulations.
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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0216384PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6497310PMC
January 2020

Study of the Lipid Profile of ATCC and Clinical Strains of in Relation to Their Antibiotic Resistance.

Molecules 2019 Apr 2;24(7). Epub 2019 Apr 2.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, I-98168 Messina, Italy.

A number of reports have indicated a relationship between bacterial resistance to antibiotics and their lipid composition. In the present study, we characterized the lipid profiles of American Type Culture Collection (ATCC) and clinical strains of and its correlation with antibiotic resistance and hydrophobicity. The following strains were used: ATCC 6538P, ATCC 43300 (MRSA), seven clinical strains from the pharynges, two strains from duodenal ulcers, four strains from hip prostheses, and one strain from the conjunctiva. Lipid-related differentiation was observed across the strains: the higher abundance of -pentadecanoic acid (-C) and -heptadecanoic acid (-C), followed by -pentadecanoic acid (-C), suggested that these were common lipids. -tridecanoic acid (-C) and -tridecanoic acid (-C), -hexadecanoic acid (-C) and -hexadecanoic acid (-C), and all forms of octadecanoic acid (C) were usually detected in low abundance. Strains isolated from pharynges showed the highest ratio of branched/straight chains. A distinction in two clusters based on the amount and type of bacterial lipids identified was obtained, which correlated to the antibiotic resistance, the strains origin, and the cell-surface hydrophobicity. We report a potential correlation between the lipid profile of strains, site of infection, antibiotic resistance, and cell-surface hydrophobicity. These results, which still need further insights, could be a first step to identifying antibiotic resistance in response to environmental adaptation.
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http://dx.doi.org/10.3390/molecules24071276DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6480324PMC
April 2019

Opuntia ficus-indica (L.) Mill. fruit as source of betalains with antioxidant, cytoprotective, and anti-angiogenic properties.

Phytother Res 2019 May 24;33(5):1526-1537. Epub 2019 Mar 24.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina, Italy.

The aim of this work was to investigate the phytochemical profile and biological properties of different colours of betalain cactus pear extracts, evaluating their antioxidant, cytoprotective, and anti-angiogenic properties by cell-free, cell-based, and in vivo assays. A QuEChERS extraction method followed by RP-LC-DAD-MS/MS analysis showed that indicaxanthin and betanin were the main compounds (≥94.32% and ≥96.95%, respectively). Orange cactus pear extracts exert the best antioxidant activity in all assays carried out, in particular into ORAC (17,352.55 ± 987.407 mg trolox equivalents/100 g dry weight) and β-carotene bleaching (60.35%) assays. The red ones, instead, showed the best cytoprotective activity decreasing the cell mortality, LDH, and Caspase-3 release ranging from 4.0 to 55%. According to antioxidant results, the orange cactus pear extracts showing also the highest anti-angiogenic activity (IC 19.31 μg/ml), followed by the red (IC 23.55 μg/ml) and the yellow ones (IC 33.97 μg/ml). In light of the results and correlation analysis, the behaviour of these molecules varies a lot according to their structure and physicochemical features and synergistic activity between betalain classes may be postulated; so the plant complex could be of greater interest compared with the isolated molecules for potential nutraceutical and pharmaceutical uses.
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http://dx.doi.org/10.1002/ptr.6345DOI Listing
May 2019