Phenolic profile and biological properties of the leaves of Ficus vasta Forssk. (Moraceae) growing in Egypt.

BACKGROUND: Ficus vasta Forssk. (Moraceae) is traditionally used for the treatment of various ailments; nonetheless, this species has been poorly studied to date. This work aimed to characterize the phenolic profile and to evaluate the antioxidant and antimicrobial properties of a hydroalcoholic extract obtained from F. vasta leaves collected in Egypt. METHODS: The phenolic profile of the extract was characterized by HPLC-PDA/ESI-MS. The antioxidant properties were examined by different in vitro systems: DPPH test, reducing power and metal chelating activity assays. Moreover, the ability of the extract to protect Escherichia coli growth and survival from H2O2-induced oxidative stress was evaluated. The potential toxicity was investigated using Artemia salina lethality bioassay. Finally, the antimicrobial properties against a representative set of Gram-positive and Gram-negative bacterial strains and the yeast C. albicans were assayed by standard methods. RESULTS: By HPLC-PDA/ESI-MS analysis 12 compounds belonging to the groups of phenolic acids and flavonoids were identified. The extract exhibited strong radical scavenging activity in DPPH test (IC50 = 0.0672 ± 0.0038 mg/mL), reducing power (3.65 ± 0.48 ASE/mL) and chelating activity (IC50 = 0.801 ± 0.007 mg/mL). A total protection against H2O2-induced damage on E. coli was observed. No toxicity against A. salina was found (LC50 > 1000 µg/mL). The extract exhibited bacteriostatic activity against almost all the bacteria tested (MICs: 250-62.5 µg/mL). CONCLUSIONS: The obtained results demonstrate the potential of F. vasta leaves as safe sources of natural antioxidant and antimicrobial compounds.

Antimicrobial Activity of Selected Polyphenols and Capsaicinoids Identified in Pepper (Capsicum annuum L.) and Their Possible Mode of Interaction.

Antimicrobial activity of pepper polyphenols and capsaicinoids (Coumarin, caffeic acid, narangin, kaempferol, rutin, quercetin, capsaicin, and dihydrocapsaicin) against 13 pathogen bacteria and three beneficial strains was studied using the disk diffusion and microdilution methods. In general, phenolic compounds had the most important activity with the highest inhibition zones obtained with caffeic acid (3.5-20.5 mm), quercetin (4.75-3.5 mm), and kaempferol (7-14 mm). In the determination of the minimal inhibitory concentrations, the effects of both quercetin and kaempferol were more important than caffeic acid. The clinical strains Staphylococcus aureus (319, 14, 8, 32, and 550) were more sensitive to quercetin (0.00195-0.0078 mg L-1) whereas kaempferol was more active against the strains S. aureus (ATCC 6538, 26), S. typhimurium ATCC 13311, and Pseudomonas aeruginosa ATCC 27853 (0.0156-0.125 mg L-1). The interaction between these three polyphenols was studied against S. aureus ATCC 6538 and P. aeruginosa ATCC 27853. Different modes of interaction were observed (synergism, additive, and indifferent), but no antagonism was obtained. The best combination was quercetin and caffeic acid for S. aureus with fractional inhibitory concentration index (FICI) of 0.37, and kaempferol with quercetin for P. aeruginosa (FICI = 0.31).

Chemical Characterization and Biological Activities of Phenolic-Rich Fraction from Cauline Leaves of Isatis tinctoria L. (Brassicaceae) Growing in Sicily, Italy.

The present work focused on the evaluation of the antioxidant and cytotoxic activities of the phenolic-rich fraction (ItJ-EAF) obtained from cauline leaves collected in January from Isatis tinctoria L. (Brassicaceae) growing wild around Acireale (Sicily, Italy). The total phenolic, flavonoid, and condensed tannin contents of the fraction were determined spectrophotometrically, whereas the phenolic profile was assessed by HPLC-PDA/ESI-MS analysis. A total of 20 compounds were positively identified and twelve out of them were never previously reported in I. tinctoria leaves. The fraction exhibited good radical scavenging activity in DPPH test (IC50  = 0.6657 ± 0.0024 mg/ml) and reducing power (3.87 ± 0.71 ASE/ml), whereas, it neither showed chelating activity nor was able to counteract H2 O2 induced oxidative stress damage in Escherichia coli. The antiproliferative effect was evaluated in vitro on two human anaplastic thyroid carcinoma cell lines (CAL-62 and 8505C) by MTT assay. At the highest tested concentration ItJ-EAF significantly reduced (80%) the growth of CAL-62 cells. No cytotoxicity against Artemia salina was observed. It can be concluded that I. tinctoria cauline leaves represent a source of phenolic compounds which could be potentially used as chemopreventive or adjuvant agents against cancer.

In vitro effect of bergamot (Citrus bergamia) juice against cagA-positive and-negative clinical isolates of Helicobacter pylori.

BACKGROUND: Helicobacter pylori infection has been associated with chronic gastritis, peptic ulcer and gastric carcinoma as over half of the world's population is colonized with this gram-negative bacterium. Due to the increasing antibiotic resistance, its eradication rates fails in a great portion of patients. A number of studies showed that molecules largely distributed in commonly consumed fruits and vegetables may have antimicrobial activity. The aim of the present study was to investigate the effect of bergamot juice (BJ) against Helicobacter pylori in vitro. The potential therapeutic combination between BJ and the antibiotics amoxicillin (AMX), clarithromycin (CLA) and metronidazole (MTZ) has also been evaluated. METHODS: The minimum inhibitory concentration (MIC) of BJ, AMX, CLA and MTZ against 2 ATCC and 32 clinical isolates of H. pylori was assayed according to CLSI. The checkerboard method was used to determine the efficacy of the association BJ with the three reference antibiotics. Killing curves were performed on the two cagA-positive ATCC strains of H. pylori (ATCC 43504 and ATCC 49503), on the clinical isolate cagA-positive HP6 strain of H. pylori and on the clinical isolate cagA-negative HP61 strain of H. pylori. RESULTS: BJ (2.5%, v/v) inhibited the growth of 50% of the H. pylori clinical isolates, whereas 5% (v/v) inhibited 90%. AMX was the most effective antibiotic against the reference strains and the clinical isolates, followed by CLA and MTZ. In the combination assays, synergism was observed between BJ and AMX and between BJ and MTZ against both the reference strains and the clinical isolates. Indifference was observed between BJ and CLA. CONCLUSIONS: BJ was effective in vitro against H. pylori and the genotype status of the clinical strains may have an impact on its susceptibility. The synergistic combination of BJ and antibiotics could be used to prevent or treat resistance.

Almond Skin Inhibits HSV-2 Replication in Peripheral Blood Mononuclear Cells by Modulating the Cytokine Network.

We have investigated the effect of almond skin extracts on the production of pro-inflammatory and anti-inflammatory cytokines in human peripheral blood mononuclear cells (PBMCs). PBMCs were either infected or not by herpes simplex virus type 2 (HSV-2), with and without prior treatment with almond skin extracts. Production of IL-17 induced by HSV-2 was inhibited by natural skins (NS) treatment. NS triggered PBMC in releasing IFN-α, IFN-γ and IL-4 in cellular supernatants. These results may explain the antiviral potential of almond skins.

3,4-DHPEA-EA from Olea Europaea L. is effective against standard and clinical isolates of Staphylococcus sp.

BACKGROUND: The aim of the present work was to evaluate the antibacterial effect of 3,4-DHPEA-EA (methyl-4-(2-(3,4-dihydroxyphenethoxy)-2-oxoethyl)-3-formyl-2-methyl-3,4-dihydro-2H-pyran-5-carboxylate), a derivate of oleuropein, against a range of Gram-positive bacteria, including ATCC strains, food and clinical isolates. METHODS: The minimum inhibitory concentrations (MICs) of 3,4-DHPEA-EA were determined by the broth microdilution method and the Bioscreen C. RESULTS: 3,4-DHPEA-EA was effective against ATCC and clinical isolates of Staphylococcus aureus (MIC values between 125 and 250 µg/ml) and ATCC and clinical isolates of Staphylococcus epidermidis (MIC values between 7.81 and 62.5 µg/ml). No significant differences were observed between the two solvents (methanol and DMSO) used to dissolve 3,4-DHPEA-EA. CONCLUSIONS: The results obtained could be used to develop novel therapies for the treatment of skin infections. Further studies need to be performed to elucidate the formation of 3,4-DHPEA-EA by acid hydrolysis of oleuropein in the human stomach.

Antibacterial activities of almond skins on cagA-positive and-negative clinical isolates of Helicobacter pylori.

BACKGROUND: Helicobacter pylori is known to be a gastric pathogen of humans. Eradication regimens for H. pylori infection have some side effects, compliance problems, relapses, and antibiotic resistance. Therefore, the need for alternative therapies for H. pylori infections is of special interest. We have previously shown that polyphenols from almond skins are active against a range of food-borne pathogens. The aim of this study was to evaluate the antibacterial effects of natural almond skins before and after simulated human digestion and the pure flavonoid compounds epicatechin, naringenin and protocatechuic acid against H. pylori. RESULTS: H. pylori strains were isolated from gastric biopsy samples following standard microbiology procedures. Also, cagA and vacA genes were identified using PCR. Susceptibility studies on 34 strains of H. pylori, including two reference strains (ATCC 43504, ATCC 49503), were performed by the standard agar dilution method. CONCLUSIONS: Polyphenols from almond skins were effective in vitro against H. pylori, irrespective of genotype status and could therefore be used in combination with antibiotics as a novel strategy for antibiotic resistance.

Qualitative Differences in Attribution of Mental States to Other People in Autism and Schizophrenia: What are the Tools for Differential Diagnosis?

The differential diagnosis between schizophrenia spectrum disorders (SSD) and autism spectrum disorders (ASD) remains an important clinical question, because they have overlap in clinical diagnosis. This study explored the differences between ASD (n = 44) and SSD patients (n = 59), compared to typically developing peers (n = 63), in completing an advanced Theory of Mind (ToM) task. The outcome found several differences between groups. The SSD patients showed greater difficulty in understanding social scenarios, while ASD individuals understood the stories, but did not correctly identify the protagonist's intention. The interesting aspect of the results is that some ToM stories are more informative about the mentalistic reasoning of the two clinical groups, namely, the stories that investigate pretend, persuasion, double bluff and ironic joke constructs.

Contribution of the Glucosinolate Fraction to the Overall Antioxidant Potential, Cytoprotection against Oxidative Insult and Antimicrobial Activity of Eruca sativa Mill. Leaves Extract.

BACKGROUND: Eruca sativa Mill. (Brassicaceae) is commonly utilized as an ingredient in salads and also as a folk remedy to treat various diseases. OBJECTIVE: The objective of this study was to establish the contribution of the glucosinolate (GLS) fraction to the overall antioxidant, cytoprotection against oxidative insult and antimicrobial properties of the hydro-alcoholic extract of E. sativa leaves from Sicily (Italy), characterized phytochemically. MATERIALS AND METHODS: The antioxidant activity was evaluated by different in vitro systems. The cytoprotective effect against hydrogen peroxide (H2O2)-induced oxidative stress was tested in human peripheral blood mononuclear cells (PBMCs). The antimicrobial potential against bacteria and fungi was assayed by standard methods. RESULTS: E. sativa extract exhibited both radical scavenging (50% inhibitory concentration [IC50] 1.04 ± 0.04 mg/mL) and ferrous ions-chelating activity (IC50 0.327 ± 0.0032 mg/mL) and mild reducing power; the GLS fraction showed chelating ability only (IC50 0.225 ± 0.009 mg/mL). In the experimental model of H2O2-induced oxidative stress in human PBMCs, a significant cytoprotective effect and a suppression of reactive oxygen species production by both extract and GLS fraction were observed (P < 0.001). E. sativa extract displayed moderate antimicrobial activity against Gram-positive bacteria, and Staphylococcus aureus was the most sensitive strain (minimum inhibitory concentration 0.125 mg/mL), whereas the GLS fraction was not active. CONCLUSION: GLSs are not involved in the primary antioxidant activity of E. sativa leaf extract but they are, almost in part, responsible for its ferrous ion-chelating properties. Iron-chelating compounds in E. sativa extract may protect cells under conditions of oxidative stress, and GLSs might play a chief role in this effect. SUMMARY: Eruca sativa Mill. leaf extract exhibited antioxidant activity in different in vitro systems, whereas the glucosinolate (GLS) fraction showed Fe2+-chelating ability onlyA significant cytoprotective effect and a suppression of intracellular reactive oxygen species production by both extract and GLS fraction were observed in human peripheral blood mononuclear cellsE. sativa extract displayed moderate antimicrobial activity against Gram-positive bacteria, whereas the GLS fraction was not active. Abbreviations used: GLS: Glucosinolate; H2O2: Hydrogen peroxide; PBMCs: Peripheral blood mononuclear cells; IC50: 50% inhibitory concentration; MIC: Minimum inhibitory concentration.

Antimicrobial activities, toxicity and phenolic composition of Asphodeline anatolica E. Tuzlaci leaf extracts from Turkey.

The antimicrobial activity of acetone, methanol and aqueous extracts of Asphodeline anatolica E. Tuzlaci leaves was evaluated against American type culture collection, food and clinical isolates (Listeria monocytogenes and Staphylococcus aureus including methicillin-resistant strains-MRSA). Biofilm formation, toxicity and characterisation of the polyphenolic content were analysed. The acetone extract demonstrated a higher antibacterial activity against S. aureus including MRSA strains, L. monocytogenes and Pseudomonas aeruginosa than against other extracts. No effect was observed in biofilm formation. The extracts resulted non-toxic against Artemia salina Leach. The phytochemical screening of extracts indicated that they mainly contained six polyphenols identified as catechin 3-O-gallate, protocatechuic acid, diosmin, rutin, cirsimaritin and kaempferol glucoside. This study is the first report on antimicrobial activity and phenolic content of A. anatolica and contributes to enrich the literature data on the biological properties of this plant. A. anatolica leaves have a potential as source of natural antimicrobial compounds.

In Vitro Antimicrobial Activity and Effect on Biofilm Production of a White Grape Juice (Vitis vinifera) Extract.

Background. The aim of the present study was to evaluate the antimicrobial effect of a white grape juice extract (WGJe) against a range of Gram-positive and Gram-negative bacteria, yeasts, and the fungus Aspergillus niger. WGJe was also tested on the production of bacterial biofilms in vitro. Results. WGJe inhibited in vitro most Gram-positive bacteria tested, Staphylococcus aureus ATCC 6538P being the most sensitive strain (MIC values of 3.9 µg/mL). The effect was bactericidal at the concentration of 500 µg/mL. Amongst the Gram-negative bacteria, Escherichia coli was the only susceptible strain (MIC and MBC of 2000 µg/mL). No effect on the growth of Candida sp. and the fungus Aspergillus niger was detected (MIC values > 2000 µg/mL). WGJe inhibited the biofilms formation of E. coli and Pseudomonas aeruginosa with a dose-dependent effect. Conclusions. WGJe exerted both bacteriostatic and bactericidal activity in vitro. The presented results could be used to develop novel strategies for the treatment of skin infections and against potential respiratory pathogens.

In vitro antimicrobial activity of pistachio (Pistacia vera L.) polyphenols.

We investigated the antimicrobial properties of polyphenol-rich fractions derived from raw shelled and roasted salted pistachios. American Type Culture Collection (ATCC), food and clinical isolates, of Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Pseudomonas mirabilis), Gram-positive bacteria (Listeria monocytogenes, Enterococcus hirae, Enterococcus faecium, Bacillus subtilis, Staphylococcus epidermidis, Staphylococcus aureus), the yeasts Candida albicans and Candida parapsilosis and the fungus Aspergillus niger were used. Pistachio extracts were active against Gram-positive bacteria with a bactericidal effect observed against L. monocytogenes (ATCC strains and food isolates), S. aureus and MRSA clinical isolates. Extracts from raw shelled pistachios were more active than those from roasted salted pistachios. The bactericidal activity of pistachio extracts could be used to help control the growth of some microorganisms in foods to improve safety and may find application as a topical treatment for S. aureus.

Bioaccessibility of pistachio polyphenols, xanthophylls, and tocopherols during simulated human digestion.

OBJECTIVE: The bioaccessibility of bioactives from pistachios has not been previously evaluated. In the present study we quantified the release of polyphenols, xanthophylls (lutein), and tocopherols from pistachios (raw pistachios, roasted salted pistachios, and muffins made with raw pistachios) during simulated human digestion. METHODS: A dynamic gastric model of digestion that provides a realistic and predictive simulation of the physical and chemical processing and accurately mimics the residence time and the luminal environment within the human stomach was used for the digestion studies. RESULTS: More than 90% of the polyphenols were released in the gastric compartment, with virtually total release in the duodenal phase. No significant differences were observed between raw shelled and roasted salted pistachio. The presence of a food matrix (muffin) decreased the bioaccessibility of protocatechuic acid (78%) and luteolin (36%). Almost 100% bioaccessibility of lutein and tocopherols was found after duodenal digestion, with no difference among the three samples. CONCLUSION: The rapid release of the assayed bioactives in the stomach maximizes the potential for absorption in the duodenum and contributes to the beneficial relation between pistachio consumption and health-related outcomes.

Effect of garlic powder on the growth of commensal bacteria from the gastrointestinal tract.

Garlic (Allium sativum) is considered one of the best disease-preventive foods. We evaluated in vitro the effect of a commercial garlic powder (GP), at concentrations of 0.1% and 1% (w/v), upon the viability of representative gut bacteria. In pure culture studies, Lactobacillus casei DSMZ 20011 was essentially found to be resistant to GP whereas a rapid killing effect of between 1 and 3 log CFU/ml reduction in cell numbers was observed with Bacteroides ovatus, Bifidobacterium longum DSMZ 20090 and Clostridium nexile A2-232. After 6h incubation, bacterial numbers increased steadily and once the strains became resistant they retained their resistant phenotype upon sub-culturing. A colonic model was also used to evaluate the effect of GP on a mixed bacterial population representing the microbiota of the distal colon. Lactic acid bacteria were found to be more resistant to GP compared to the clostridial members of the gut microbiota. While for most bacteria the antimicrobial effect was transient, the lactobacilli showed a degree of resistance to garlic, indicating that its consumption may favour the growth of these beneficial bacterial species in the gut. Garlic intake has the potential to temporarily modulate the gut microbiota.

Antimicrobial activity and phenolic content of natural site and micropropagated Limonium avei (De Not.) Brullo & Erben plant extracts.

This study reported the antimicrobial activity and phenolic content of natural site and micropropagated Limonium avei (De Not.) Brullo & Erben inflorescences. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of ethanolic extracts were determined according to the Clinical Laboratory Standards Institute guidelines. Individual phenolic acids and flavonoids were detected by a high performance liquid chromatography (HPLC-DAD) method. The samples showed a comparable antimicrobial activity, although the natural site extract possessed the lower MIC values. The best activity was detected against Gram-positive bacteria, such as Staphylococcus aureus including methicillin resistant strains (MIC and MBC values ranging from 7.81 to 62.50 µg mL(-1) and from 500 to 2000 µg mL(-1) respectively). In contrast, a low activity was found on Gram-negative bacteria and Candida albicans. The HPLC-DAD analysis revealed ten phenolic acids and four flavonoids with a major amount of m-coumaric acid, naringin and quercetin in the natural site extract.

In vitro and in vivo properties of a fully human IgG1 monoclonal antibody that combats multidrug resistant Pseudomonas aeruginosa.

The development of an anti-bacterial drug in the form of a monoclonal antibody (mAb) targeting an exposed virulence factor, represents an innovative therapeutic strategy. Consequently, a fully human IgG1 mAb (LST-007) targeting Pseudomonas aeruginosa (PA) flagellin type b was recombinantly expressed and characterized in vitro and in an infection model driven by a multidrug resistant (MDR) PA strain. LST-007 demonstrated a highly specific binding towards whole PA bacteria harboring flagellin type b and its recombinant counterpart, with a K(D) of 7.4x10(-10) M. In bioactivity assays, LST-007 or titers of Cmax sera derived from pharmacokinetic studies, markedly attenuated PA motility in an equipotent manner. In vivo, parenteral LST-007 (20 mg/kg) given as a single or double-dosing paradigm post-infection, afforded survival (up to 75% at Day 7) in a lethal model of pneumonia driven by the intratracheal (i.t.) instillation of an LD(80) of the MDR PA isolate. This protective effect was markedly superior to that of imipenem (30% survival at Day 7) and totally devoid with an irrelevant, human isotype mAb. These data lay credence that LST-007 may be a valuable adjunct to the limited list of anti-bacterials that can tackle MDR PA strains, thereby warranting its continued development for eventual clinical evaluation.