The synthesis of derivatives of three nonspecific COX-1 and COX-2 inhibitors, ibuprofen, ketoprofen, naproxen is presented. These acids were connected via an amide bond with an amino acid (L-proline, ...L-tyrosine, and beta-alanine) used as a linker. The amino acid carboxylic group was esterified with 3,4,5 trimethoxybenzyl alcohol. The activity of the novel derivatives was examined in vivo on carrageenan-induced inflammation, and in vitro, as cyclooxygenase and lipoxygenase inhibitors. It was found that the new compounds were more potent anti-inflammatory agents than the parent drugs. Thus, the ibuprofen (
) and ketoprofen (
) derivatives reduced rat paw edema by 67 and 91% (the reduction by the relevant NSAIDs was 36 and 47%, respectively). They inhibited COX-2 more than the starting drugs (
by 67%, ibuprofen 46%,
by 94%, ketoprofen 49%). Docking of compounds on the active sites of COX-1 and COX-2 reflects their in vitro activity. Thus,
adopts an unfavorable orientation for COX-1 inhibition, but it binds effectively in the binding pocket of COX-2, in agreement with the absence of activity for COX-1 and the high inhibition of COX-2. In conclusion, the performed structural modifications result in the enhancement of the anti-inflammatory activity, compared with the parent NSAIDs.
Sideritis
species are recognized as important medicinal plants and their commercial demand is continuously on the rise both in the European and in the global market. Consequently, the cultivation of
...Sideritis
species has been occurred to successfully meet the need for mass production of high-quality plant material. The present study was undertaken in order to investigate the chemical composition of cultivated
S. cypria
. Infusions of flowers and leaves were prepared separately, according to the European Medicine Agency (EMA) monograph. The infusion of the flowers revealed the presence of four flavones, isoscutellarein-7-O-6′″-O-acetyl-β-D-allopyranosyl-(1→2)-β-D-glucopyranoside, its 4′-O-methyl-derivative, 4′-O-methyl-hypolaetin-7-O-6′″-O-acetyl-β-D-allopyranosyl-(1→2)-β-D-glucopyranoside, and isoscutellarein-7-O-6′″-O-acetyl-β-D-allopyranosyl-(1→2)-6″-O-acetyl-β-D-glucopyranoside; four phenylethanoid glucosides, acteoside, leucosceptoside A, lamalboside, and leonoside A; one iridoid, melittoside, and one phenolic acid, chlorogenic acid, while the infusion of the leaves of the same population afforded the same first two flavones; five phenylethanoid glucosides, acteoside, leucosceptoside A, lavandulifolioside, leonoside A, and lamalboside; melittoside and chlorogenic acid. The structural elucidation of the isolated compounds was undertaken by high-field NMR spectroscopy. Moreover, the essential oils of the flowers and leaves were studied by GC-MS, separately. In addition, the mineral, bioactive compounds, protein and carbohydrate contents were evaluated for both plant materials.
The application of chemometrics, a widely used science in food studies (and not only food studies) has begun to increase in importance with chemometrics being a very powerful tool in analyzing large ...numbers of results. In the case of honey, chemometrics is usually used for assessing honey authenticity and quality control, combined with well-established analytical methods. Research related to investigation of the quality changes in honey due to modifications after processing and storage is rare, with a visibly increasing tendency in the last decade (and concentrated on investigating novel methods to preserve the honey quality, such as ultrasound or high-pressure treatment). This review presents the evolution in the last few years in using chemometrics in analyzing honey quality during processing and storage. The advantages of using chemometrics in assessing honey quality during storage and processing are presented, together with the main characteristics of some well-known chemometric methods. Chemometrics prove to be a successful tool to differentiate honey samples based on changes of characteristics during storage and processing.
A Blatter radical is oxidized to benzotriazin-7(H)-one which after amination and subsequent acyl- and aroylation gives N-(benzotriazin-6-yl)carboxamides that undergo ring closure with P2S5 to afford ...the corresponding thiazolo5′,4′:4,5benzo1,2-e1,2,4triazin-4-yls. These highly delocalized radicals are air stable and show good reversible electrochemical behavior.
Thirty-four honey samples donated by beekeepers and purchased from supermarkets were collected during harvesting years 2010–2014 from Cyprus, Greece, and Egypt. The aims of this study were to ...characterize honey samples and, if possible, to differentiate honeys according to the honey type on the basis of physicochemical parameter values, mineral content, and their combination using supervised statistical techniques (linear discriminant analysis (LDA)). Physicochemical parameters (colour, pH, free acidity, total dissolved solids, salinity, electrical conductivity, and moisture content) were determined according to official methods, while minerals (Al, As, B, Ba, Be, Ca, Cd, Co, Cr, Cu, Fe, Hg, Mg, Mn, Mo, Ni, P, Pb, Sb, Si, Ti, Tl, V, and Zn) using inductively coupled plasma optical emission spectrometry. The majority of honey samples analyzed met the quality criteria set by the European directive and national decision related to honey. Implementation of multivariate analysis of variance (MANOVA) and LDA on specific physicochemical parameters, minerals, or their combination provided a satisfactory classification of honeys according to floral type. The overall correct classification rate (based on the cross-validation method) was 79.4% using 7 minerals and 91.2% using 8 physicochemical parameters. When the 15 parameters were combined, the classification rate of Egyptian honeys was improved by 25%.
A new biocatalyst was prepared by immobilization of
Saccharomyces cerevisiae AXAZ-1 yeast cells on whole wheat grains. This biocatalyst was used for 30 repeated batch fermentations of glucose and ...grape must at various temperatures. The biocatalyst retained its operational stability for a long period and it was proved capable to produce dry wines of fine clarity even at extremely low temperatures (5
°C). After the completion of these fermentations the new biocatalyst was used in a scale-up system of 80
L for wine making at ambient (20
°C) and extremely low temperatures (2
°C). The scale-up process did not affect the fermentative ability of biocatalyst, even at low temperatures, while the produced wines had almost the same improved aromatic profile compare to free cells as revealed by GC and GC–MS analyses. More specifically the results showed that both systems with immobilized cells (laboratory scale and 80
L bioreactor) increased the formation of esters and produced wines with improved aromatic profile compared to those with free cells. Finally an increase in the percentages of total esters and a decrease in those of higher alcohols was observed in lower fermentation temperatures.
Novel vitamin E chelate siderophore derivatives and their VV and FeIII complexes have been synthesised and the chemical and biological properties have been evaluated. In particular, the α- and ...δ-tocopherol derivatives with bis-methyldroxylamino triazine (α-tocTHMA) and (δ-tocDPA) as well their VV complexes, V2VO3(α-tocTHMA)2 and V2IVO3(δ-tocTHMA)2, have been synthesised and characterised by infrared (IR), nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR) and ultra violet-visible (UV-Vis) spectroscopies. The dimeric vanadium complexes in solution are in equilibrium with their respefrctive monomers, H2O + V2VO2(μ-O)4+ = 2 VVO(OH)2+. The two amphiphilic vanadium complexes exhibit enhanced hydrolytic stability. EPR shows that the complexes in lipophilic matrix are mild radical initiators. Evaluation of their biological activity shows that the compounds do not exhibit any significant cytotoxicity to cells.
The effects of the geographical region and the botanical origin of olive oils on the profile of fatty acids isolated from monovarietal virgin olive oils from Cyprus were investigated, in order to ...establish, for the first time, promising models for authentication and classification of monovarietal virgin olive oils produced on the island. The two dominant Cypriot olive cultivars, Cypriot (ladoelia), and Koroneiki (lianolia), were analyzed for fatty acid composition by GC/FID after preparation of Fatty Acid Methyl Esters from olive oil, using a cold esterification method. The data obtained were analyzed statistically using multivariate and univariate ANOVA, principal components analysis (PCA) and hierarchical cluster analysis. Results showed that the olive oils can be separated into two distinct groups using the FAME data bank obtained from 225 samples. Significant differences in the proportion of some variables such as polyunsaturated linoleic acid, and the ratio C18:1/C18:2 from oils of different varieties and geographical regions were detected. The ratios C18:1/C18:2 and MUFA/PUFA, as well SFA, ω-9 and PUFA showed the higher discriminant power based on the cultivar.
Discrimination of virgin olive oils of the two dominant Cypriot olive cultivars, Cypriot (ladoelia) and Koroneiki (lianolia) and the influence of the microclimate and altitude elevation by means of multivariate and univariate ANOVA, PCA and Hierarchical Cluster analysis. Display omitted
•Fatty acids composition of virgin olive oils (VOOs) from Cypriot and Koroneiki cultivars grown in Cyprus•Chemometrics of VOOs based on cultivar, and geographical origin (altitude and district area)•Discrimination of VOOs based on cultivar by C18:1/C18:2, MUFA/PUFA, and PUFA•Investigation of separation of VOOs of Cyprus by cultivar by PCA•Sufficient classification of VOOs into Cypriot and Koroneiki by Hierarchical Cluster Analysis
Lavandula angustifolia (Mill.) is a medicinal plant of great importance with a variety of applications in perfume and pharmaceutical industries or landscaping, but only limited information is ...available about its response to potassium supplementation. This experiment was conducted in order to determine the effects of potassium (K: 275-300-325-350-375 mg L-1) levels on the morphological and biochemical characteristics of lavender grown hydroponically. Results showed that K levels affected plant growth, mainly the root development while no differences were found for leaf chlorophyll content and stomatal conductance. Essential oil yield increased in the 300 mg L-1 in comparison to 275 or 325-375 mg L-1 of K application. The middle ranged K levels (300-325-350 mg L-1) enhanced leaf content in total phenols, flavonoids and antioxidant activity (DPPH, FRAP). Lipid peroxidation content (MDA) employed as damage index, was lower in the 325 mg L-1 of K treatment. No differences were observed in antioxidant enzymes (SOD, CAT, APX) activity and H2O2 content among K applications. The main constituents of leaves essential oil (1,8-cineole, borneol, camphor, α-terpineol, myrtenal) and mineral accumulation were affected by K treatments. Lavender grown in 300 mg L-1 of K was appropriate for the essential oil uses/production while the 325 mg L-1 of K were more appropriate for lavender cultivation for fresh and dry matter uses.
A preliminary study has been performed for the valorization of citrus peel waste (CPW) through the biorefinery platform aiming to produce succinic acid. Following extraction of essential oils and ...pectin, different conditions of dilute acid hydrolysis were evaluated based on estimation of the sugars liberated and subsequent fermentation of hydrolyzates for production of succinic acid by Actinobacillus succinogenes. The most suitable pretreatment conditions involved 116 °C for 10 min using 5% (w/v) of dry raw material (drm). Thus, a total sugar (ts) yield of 0.21 gts gdrm−1 and a succinic acid (sa) yield via microbial fermentations of 0.77 gsa gtsc−1 was achieved, while the use of lower solid contents resulted in higher sugar yields. The residues from dilute acid hydrolysis were applied for subsequent enzyme hydrolysis using commercial enzymes and the most suitable combination of enzyme units included 30 IU cellulases and 25 BGL β-glucosidases achieving a yield of 0.58 gts gdrm−1. Moreover, elemental analysis in hydrolyzates obtained from dilute acid hydrolysis and a combination of acid and enzyme hydrolysis indicated that during the combined treatment, high concentrations of Mg2+ and Ca2+ ions are liberated as compared to dilute acid hydrolysis, while the concentration of hydroxymethylfurfural was 0.038 g L−1 demonstrating low formation of inhibitors. The hydrolyzate generated through the combined pretreatment proposed was applied as feedstock for the production of succinic acid achieving a yield of 0.70 gsa gtsc−1. However, although the combined hydrolysis approach could approximately double the sugars released in the hydrolyzate, the economic analysis performed confirmed that the use of the enzymatic treatment could not be competitive. The developed bioprocess constitutes a valuable alternative to the application of energy intensive chemical technologies for succinic acid production.
•The yields via acid hydrolysis reached 0.21 gts gdrm−1 and 0.77 gsa gtsc−1.•The most suitable enzyme units in enzyme hydrolysis were 30 IU and 25 BGL.•The yields via combined pretreatment reached 0.58 gts gdrm−1 and 0.70 gsa gtsc−1.•High contents of Mg2+ and Ca2+ ions were formed via acid and enzyme hydrolysis.•Low concentrations of hydroxymethylfurfural were formed in citrus hydrolyzates.
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