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Roberta Gaziano,1,* Elena Campione,2,* Federico Iacovelli,3 Daniele Marino,1 Francesca Pica,1 Paolo Di Francesco,1 Stefano Aquaro,4 Francesco Menichini,4 Mattia Falconi,3 Luca Bianchi2 1Microbiology Section, Department of Experimental Medicine and Surgery, University of Rome ‘Tor Vergata’, Rome, Italy; 2Department of Systems Medicine, University of Rome ‘Tor Vergata’, Rome, Italy; 3Department of Biology, University of Rome ‘Tor Vergata’, Rome, Italy; 4Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende, Italy *These authors contributed equally to this work Introduction: Dermatophytosis is a superficial fungal infection limited to the stratum corneum of the epidermis, or to the hair and nails, and constitutes an important public health problem because of its high prevalence and associated morbidity. Dermatophyte fungi, especially 2 species, Trichophyton rubrum and Trichophyton mentagrophytes, are the predominant pathogens. Topical antifungal drugs, mainly azoles or allyamines, are currently used for the treatment of dermatophytoses, although in some cases, such as in nail and hair involvement, systemic treatment is required. However, therapeutic efficacy of current antifungal agents can be limited by their side effects, costs, and the emergence of drug resistance among fungi. Plant extracts represent a potential source of active antimicrobial agents, due to the presence of a variety of chemical bioactive compounds. In the present work, we evaluated in silico and in vitro the antifungal activity of an extract of the medicinal plant Cardiospermum halicacabum against T. rubrum suggesting a potential interaction with Hsp90 as playing an important role in both pathogenicity and drug susceptibility of T. rubrum. Methods: We investigated in vitro the effect of different concentrations of C. halicacabum (from 500 to 31.25 µg) against a clinical isolate of T. rubrum. Furthermore, using a computational assessment, the interaction between different C. halicacabum active compounds and the fungal Hsp90 was also investigated. Results: Our results indicate a clear-cut antifungal activity of the total plant extract at the highest concentrations (500 and 250 µg). Among all tested C. halicacabum compounds, the luteolin and rutin molecules have been identified in silico as the most important potential inhibitors of Hsp90. Based on these data, luteolin and rutin were also individually assessed for their antifungal activity. Results demonstrate that both substances display an antifungal effect, even if lower than that of the total plant extract. Conclusion: Our data indicate a strong fungistatic effect of C. halicacabum against T. rubrum, suggesting its potential therapeutic efficacy in the treatment of dermatophytoses. Additionally, C. halicacabum compounds, and particularly luteolin and rutin, are all possible Hsp90 interactors, explaining their fungistatic activity. Keywords: Trichophyton rubrum, dermatophytoses, Cardiospermum halicacabum, antifungal activity, Hsp90, molecular modeling, molecular docking, rutin, luteolin

A stabilization technique targeting the Reynolds-averaged Navier-Stokes (RANS) equations is proposed to account for the multiscale nature of turbulence and high solution gradients. The objective is effective stabilization in computations with the advection-diffusion reaction equations, which are typical of the class of turbulence scale-determining equations where reaction-dominated effects strongly influence the boundary layer prediction in the presence of nonequilibrium phenomena. The stabilization technique, which is based on a variational multiscale method, includes a discontinuity-capturing term designed to be operative when the solution gradients are high and the reactionlike terms are dominant. As test problems, we use a 2D model problem and 3D flow computation for a linear compressor cascade. [DOI: 10.1115/1.3062967]

The aim of this study was to investigate the essential oil profile ofSalvia thomasii(Southern Italy) and to assess the relationship of this taxonomic unit toS. fruticosa. The essential oil, obtained by hydrodistillation, was analysed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The main components are β-pinene, viridiflorol, 1,8-cineole, camphor, α-pinene andtrans-caryophyllene. The oil was tested for its potential antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), Ferric Reducing Ability Power (FRAP) and β-carotene bleaching test. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity assays were used to screen the neuroprotective effect of the essential oil. A clear distinction of the two taxonomic units emerge by the comparison ofS. thomasiiandS. fruticosas.l. essential oil composition. Considering the weak morphological differences and the clear-cut geographic separation we propose to treat the Italian unit at subspecies level asSalvia fruticosaMill subsp.thomasii(Lacaita) Brullo, Guglielmo, Pavone & Terrasi. [ABSTRACT FROM PUBLISHER]

During the last decades, different natural compounds have been demonstrated to modulate inflammatory pathways. In this study, methanolic extract ofEchinophora tenuifoliaL. inflorescences was investigated for its chemical composition andin vitroantioxidant and anti-inflammatory properties. Phytochemical profile was investigated by means of high-performance thin layer chromatography (HPTLC) and gas chromatography–mass spectrometry analyses. Myristic acid and palmitic acid were found to be the major constituents. Six terpenes were identified: α-phellandrene, o-cymene, dihydroactinidiolide, neophytadiene, phytol and β-amyrin, and two phenolic compounds: carvacrol and ferulic acid. HPTLC analysis of the ethyl acetate fraction highlighted the presence of the flavonoid glycosides rutin and quercitrin. This sample showed the best diphenylpicrylhydrazyl scavenging capacity, with an IC50value equal to 40.39 μg/ml, and the strongest capacity to protect linoleic acid from peroxidation, as assessed by the β-carotene bleaching test (IC50 = 16.31 μg/ml). All samples inhibited nitric oxide production in cell supernatants in a dose-dependent manner, being the two apolar fractions (n-hexane and dichloromethane) even more active than the positive control indomethacin. A relevant biological activity was observed for dichloromethane fraction (IC50value equal to 39.97 μg/ml). Obtained results indicate that this sample could be an excellent candidate for further investigations aimed at the development of new antioxidant and anti-inflammatory drugs. [ABSTRACT FROM PUBLISHER]

Tyrosinase (EC 1.14.18.1), a copper-containing enzyme, can cause enzymatic browning in raw fruits, vegetables, and beverages. Browning is an undesirable reaction that is responsible for less attractive appearance and loss in nutritional quality. These phenomena have encouraged researchers to seek new potent tyrosinase inhibitors for use in the food industry. This article reviews recent studies on tyrosinase inhibitors of natural and synthetic origins. The information offered here should help food industry in developing and using potential tyrosinase inhibitors desirable efficacy and safety, and for improving food quality. [ABSTRACT FROM AUTHOR]

This study aimed to evaluate the influence of collection zone on total phenol, flavonoid and glucosinolate contents and antioxidant and anti-inflammatory activities of caper (Capparis sicula ssp. sicula). This species has been characterized through the detection, isolation and quantitative evaluation of chemical markers (polyphenols, flavonoids and glucosinolates). The chemical investigation showed a different composition between the two collection zones. While the total amounts of phenolics and flavonoids of the two samples were quite the same, their high-performance liquid chromatography profiles were very different. In both samples, the most abundant aglycone was quercetin which accounted for 60% of total flavonoids. Nuclear magnetic resonance data analysis allowed the identification of two compounds: 3,5-dicaffeoylquinic and 4,5-dicaffeoylquinic acids which represented 6.67% and 15.94%, respectively, of the total amount of flavonoids in sample 1. In sample 2, these two acids were still present, but their percentages were much less (2.20% and 1.71%, respectively). As far as we know, this is the first report about the presence of dicaffeoylquinic acids in Capparis. With regard to glucosinolate content, sample 1 showed a higher content of glucosinolates. In both samples, glucocapparin was the most abundant compound. Antioxidant activity of the methanolic C. sicula extracts using diphenyl picrylhydrazyl, β-carotene bleaching test and oxygen radical absorbance capacity showed that the sample 2 was more active than 1. As regards the inhibition of NO production, the extracts from sample 2 were more active than those from sample 1. [ABSTRACT FROM AUTHOR]

Total water extract, ethyl acetate, and aqueous fractions from the leaves of Artocarpus heterophyllus were evaluated for phenolic content, antioxidant, and antibacterial activities against some foodborne pathogens such as E. coli, Listeria monocytogenes, Salmonella typhimurium, Salmonella enterica, Bacillus cereus, Enterococcus faecalis, and Staphylococcus aureus. The minimum inhibitory concentration (MICs) of extract and fractions determined by the agar dilution method were ranged from 221.9 μg/mL for ethyl acetate fraction to 488.1 μg/mL for total extract. In the agar diffusion method the diameters of inhibition were 12.2 for the total extract, 10.7 and 11.5 for ethyl acetate and aqueous fractions, respectively. A. heterophyllus showed significant antioxidant activity tested in different in vitro systems (DPPH, ABTS, FRAP, and Fe2+ chelating activity assay). In particular, in DPPH assay A. heterophyllus total extract exhibited a strong antiradical activity with an IC50 value of 73.5 μg/mL while aqueous fraction exerted the highest activity in FRAP assay (IC50 value of 72.0 μg/mL). The total phenols content by Folin–Ciocalteau method was determined with the purpose of testing its relationship with the antioxidant and antibacterial activities. Practical Application: The appearance of food is one of the major determinants of its appeal to consumers and consequently, sales of the product. Microbial contamination and lipid oxidation are the main factors that determine food quality loss and shelf-life reduction. Therefore, preventing microbial contamination and delaying lipid oxidation are highly relevant to food processors. The growth of microorganisms in food products may cause spoilage or foodborne diseases. Oxidative processes in food products lead to the degradation of lipids and proteins which, in turn, contribute to the deterioration in flavor, texture, and color of the products. A. heterophyllus leaves extracts demonstrated interesting biological properties that suggest its use as a new potential source of natural antioxidant and antimicrobial agent. [ABSTRACT FROM AUTHOR]

Abstract The aim of this work was to examine the chemical composition and antiproliferative activity of Salvia leriifolia Benth. and Salvia acetabulosa L. oils. S. leriifolia oil was characterized by 50 components, whereas 19 components were identified in S. acetabulosa. S. leriifolia oil was characterized by camphor (10.5%), 1,8-cineole (8.6%), camphene (6.2%), and alpha-pinene (4.7%). alpha-Pinene (52.3%), 1,8-cineole (27.7%), and camphor (6.7%) were the major components in S. acetabulosa oil. Both oils exerted a strong antiproliferative activity comparing with vinblastine against COR-L23 with 50% inhibitory concentration (IC(50)) values of 7.5 and 6.5 mug/mL for S. leriifolia and S. acetabulosa, respectively. Salvia oils showed an interesting activity also on C32 (IC(50) = 6.3 and 9.1 mug/mL for S. acetabulosa and S. leriifolia, respectively). S. acetabulosa was also found to possess cytotoxic activity against renal adenocarcinoma (IC(50) = 6.8 mug/mL). The results clearly showed that for both Salvia species the antiproliferative activity could not be related to the major abundant compounds. Consequently, the minor components may be involved in some type of synergism with the other active compounds. [ABSTRACT FROM AUTHOR]

Ethanolic extract from the fruits of Pimpinella anisoides, an aromatic plant and a spice, exhibited activity against AChE and BChE, with IC(50) values of 227.5 and 362.1 microg/ml, respectively. The most abundant constituents of the extract were trans-anethole, (+)-limonene and (+)-sabinene. trans-Anethole exhibited the highest activity against AChE and BChE with IC(50) values of 134.7 and 209.6 microg/ml, respectively. The bicyclic monoterpene (+)-sabinene exhibited a promising activity against AChE (IC(50) of 176.5 microg/ml) and BChE (IC(50) of 218.6 microg/ml). [ABSTRACT FROM AUTHOR]

The present study showed for the first time the biological properties of different fractions from Cardamine battagliae Cesca & Peruzzi, an apoendemic Calabrian (southern Italy) plant that belongs to the Cruciferae family. The antioxidant activities of the different fractions of C. battagliae were carried out using two different in vitro assays (β-carotene bleaching test and lipid peroxidation of liposomes assay) while radical scavenging activity was carried out using DPPH test. AcOEt fraction showed the highest activity on DPPH inhibition (IC50 of 0.162 mg mL-1) while dichloromethane fraction showed the highest activity on β-carotene bleaching (IC50 of 0.004 mg mL-1). The assay for α-amylase inhibition showed that n-hexane fraction showed the highest activity with an IC50 of 0.055 mg mL-1. [ABSTRACT FROM AUTHOR]

This study reports on the α-amylase inhibitory and antimicrobial activities of Senecio leucanthemifolius Poiret. Extracts of S. leucanthemifolius were tested for their antimicrobial and antifungal activities against seven different pathogenic microorganisms using the microdilution technique. The ethyl acetate extract exhibited a strong antibiotic activity against Staphylococcus aureus with a MIC value of 31.25 µg mL-1, while the n-hexane extract showed a significant activity against dermatophytic fungi. S. leucanthemifolius extracts were tested also for their potential hypoglycemic activity through the in vitro inhibition of α-amylase. The dichloromethane extract inhibited α-amylase with a value of 56.6% at 0.05 mg mL-1 and the n-butanol extract showed a value of 89.2% at 1 mg mL-1. [ABSTRACT FROM AUTHOR]

The Sulforodamine B (SRB) assay was used to test cytotoxicity against four human cancer cell lines and one normal cell line of antioxidant constituents isolated from Hypericum triquetrifolium Turra. Methanolic extract and pure compounds were tested against the large cell lung carcinoma cell line COR-L23, the hepatocellular carcinoma cell line HepG-2, renal cell adenocarcinoma ACHN, the amelanotic melanoma cell line C32 and normal human foetal lung MRC5. The results showed that I3-II8-biapigenin exhibited strong cytotoxic activity (IC50 = 5.73 µg mL-1) showing a certain degree of selectivity against the different cell types. [ABSTRACT FROM AUTHOR]

In our screening program for antihypertensive properties of plants, the leaves of Ailanthus excelsa (Roxb), a plant used in Egyptian traditional medicine, were analysed. Chromatographic separation of A. excelsa MeOH extract yielded six flavonoids for the first time from this species, namely apigenin, luteolin, kaempferol-3-O-alpha-arabinopyranoside, kaempferol-3-O-beta-galactopyranoside, quercetin-3-O-alpha-arabinopyranoside and luteolin-7-O-beta-glucopyranoside. The in vitro hypotensive activities of the MeOH extract and the isolated compounds were elucidated. All the flavonoids tested exhibited ACE inhibitory activity, in particular the most active compound was kaempferol-3-O-beta-galactopyranoside with an IC(50) value of 260 microm. [ABSTRACT FROM AUTHOR]

The aim of this study was to evaluate the in vitro antioxidant and cytotoxic activities of the methanolic extract and fractions of Senecio gibbosus subsp. gibbosus aerial parts. The antioxidant activity was assessed by means of two different tests: (1) bleaching of the stable 2,2-diphenyl-1-picrylhydrazil (DPPH) radical; and (2) lipid peroxidation of liposomes which were prepared from bovine brain extract. In both tests used methanolic extract and AcOEt fraction showed a significant antioxidant effect. The cytotoxic activity of the methanolic extract and fractions was carried out using the SRB assay. The methanolic extract demonstrated a good cytotoxic activity against human breast cancer cell line (MCF-7) and human prostate cancer cell line (LNCaP). Dichloromethane and AcOEt fractions showed the greatest cytotoxic activity, particularly on LNCaP cell line. [ABSTRACT FROM AUTHOR]

The antimicrobial and cytotoxic activities of extracts from Senecio samnitum Huet are reported. Extracts from S. samnitum were able to inhibit the in vitro proliferation of four human tumor cell lines. The dichloromethane extract demonstrated effective cytotoxic activity with IC50 of 22.89  µg  mL -1 on the Caco-2 cell line and the EtOAc extract had IC50 value of 11.91  µg  mL -1 against the COR-L23 cell line. The n -hexane extract displayed the best antibacterial activity against Gram positive bacteria, particularly Staphylococcus aureus . The antifungal activity of all extracts was also seen, particularly against the dermatophytes Trichophyton tonsurans and Microsporum gypseum for the methanol and n -hexane extracts. [ABSTRACT FROM AUTHOR]

Extracts of Senecio samnitum Huet and derived methyl ester of chlorogenic acid have been shown to inhibit angiotensin-converting enzyme (ACE) by using an in vitro bioassay based on the enzymatic cleavage of the chromophore-fluorophore labeled substrate dansyltriglycine into dansylglycine, which is quantitatively measured by high-performance liquid chromatography (HPLC). GC/MS and NMR identified compounds present within the studied S. samnitum extracts. The most effective fraction was obtained in ethyl acetate, which gave 52.56 ± 0.23% (SD) inhibition at 300 µg/ml. The major constituent of this fraction, the methyl ester of chlorogenic acid, showed significant ACE inhibition of 56.78 ± 0.25% at a concentration of 82.5 µg/ml. [ABSTRACT FROM AUTHOR]

The biovariability of Helichrysum italicum (Roth) Don grown wild in Calabria and Sardinia (Italy) was reported. This species has been characterized through the detection, isolation and quantitative evaluation of chemical markers (a-terpinolene, trans -cariophyllene and neryl acetate) by GC and GC-MS. Antioxidant activity of the methanolic H. italicum extracts using DPPH and ß-carotene bleaching test showed that the Calabrian samples were more active than those from Sardinia. The antibacterial activity of all extracts evidenced the best performance on the Gram positive bacteria particularly on Micrococcus luteus . Moreover, antifungal activity of all extracts was also tested evidencing important results particularly on the phytopathogene fungus Pythium ultimum . In general, as regards the antifungal activity, the extracts from Sardinia were more active than those from Calabria. The phytochemical analysis and the biological activity data suggested a possible use of these plant matrices in alimentary, cosmetic and pharmaceutical fields. [ABSTRACT FROM AUTHOR]

The biovariability of Hypericum perforatum L. (St. John's Wort) grown wild in Calabria and Sardinia (Italy) was reported with the aim to characterize the species through the isolation, detection, and quantitative evaluations of chemical markers (hypericin, quercetin, rutin) by HPLC analysis. Antioxidant activity of the methanolic H. perforatum extracts showed that the Calabrian samples were more active than those from Sardinia. The antibacterial activity evidenced the best performance on the gram positive bacteria with a MIC value of 50 µg/mL. Moreover, antifungal activity of all the extracts was also tested which showed interesting results particularly on the phytopathogene fungus P. ultimum . The variability shown by the samples could be attributed to environmental factors such as chemical-physical properties, composition of the soil, geographical coordinate, altitude, and solar exposure. The phytochemical analysis and the biological activity data suggested a possible use of H. perforatum extracts in the alimentary, cosmetic, and pharmaceutical fields. [ABSTRACT FROM AUTHOR]

The aim of this study was to evaluate the in vitro antioxidant and cytotoxic activities of the methanol extracts of Retama raetam subsp. gussonei leaves and seeds. The antioxidant activity of the extracts was assessed by means of two different tests: (1) bleaching of the stable 2,2-diphenyl-1-picrylhydrazil (DPPH) radical; and (2) lipid peroxidation of liposomes which were prepared from bovine brain extract. In both tests used leaves extract showed a significant antioxidant effect. The extract of leaves also demonstrated a good cytotoxic activity against COR-L23 (large cell carcinoma) cell line. [ABSTRACT FROM AUTHOR]

The inhibitory activity of alpha-amylase and the phytochemical composition of Cedrus libani essential oils obtained from wood, leaves and cones were investigated. The C. libani woods oil exhibit an IC(50) value of 0.14 mg/ml, whereas the leaves and cones oils were devoid of any significant activity. [ABSTRACT FROM AUTHOR]