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Proteinuria is a condition in which an excessive amount of protein is excreted in urine. It is, among others, an indicator of kidney disease or risk of cardiovascular disease. Rapid and reliable diagnosis and monitoring of proteinuria is of great importance for both patients and their physicians. For that reason, a paper-based sensor for proteinuria diagnosis was designed, optimized, and validated utilizing smartphone-assisted signal acquisition. In the first step, a few commonly employed protein assays were optimized and compared in terms of analytical performance on paper matrix. The tetrabromophenol blue method was selected as the one providing a sufficiently low limit of detection (39 mg·L−1) on the one hand and appropriate long-term stability (up to 3 months) on the other hand. The optimized assay was employed for protein-to-creatinine ratio (PCR) determination on a single paper-based sensor. For both analytes the linear ranges were within the clinically relevant range. The analytical usefulness of the developed sensors was demonstrated by a PCR recovery study in artificial urine. The obtained PCR recoveries were from ca. 80 to 150%.

For the preparation of activated carbon papers (APCs) as supercapacitor electrodes, impurity substances were removed from rice husks, before carbonization and various activation temperature treatments, to optimize electro chemical efficiency. The porosities and electrochemical performances of the ACPs depended strongly on activation temperature: The specific surface area increased from 202.92 (500 &deg, C) to 2158.48 m2 g&minus, 1 (1100 &deg, C). XRD and Raman analyses revealed that ACP graphitization also increased with the activation temperature. For activation at 1100 &deg, C, the maximum specific capacitance was 255 F g&minus, 1, and over 92% of its capacitance was retained after 2000 cycles.

The rapid dispersion of new psychoactive substances (NPS) presents challenges to customs services and analytical laboratories, which are involved in their detection and characterization. When the seized material is limited in quantity or of a complex nature, or when the target substance is present in very small amounts, the need to use advanced analytical techniques, efficient workflows and chemo-informatics tools is essential for the complete identification and elucidation of these substances. The current work describes the application of such a workflow in the analysis of a single blotter paper, seized by Swedish customs, that led to the identification of a lysergic acid diethylamide (LSD) derivative, 1-butyl-lysergic acid diethylamide (1B-LSD). Such blotter paper generally contains an amount in the range of 30&ndash, 100 ug. This substance, which is closely related to 1-propionyl-lysergic acid diethylamide (1P-LSD), seems to have only recently reached the drug street market. Its identification was made possible by comprehensively combining gas chromatography with mass spectrometry detection (GC&ndash, MS), liquid chromatography coupled with high-resolution tandem MS (LC&ndash, HR-MS/MS), Orbitrap-MS and both 1D and 2D nuclear-magnetic-resonance (NMR) spectroscopy. All the obtained data have been managed, assessed, processed and evaluated using a chemo-informatics platform to produce the effective chemical and structural identification of 1B-LSD in the seized material.

Myrciaria floribunda, also known as rumberry, is a tree native to the Brazilian Atlantic Forest, where its fruits have the potential for commercial use. This study evaluates the antioxidant potential, determines the phytochemical profile, and chemically characterizes the rumberry fruit. Accessions were sampled from the Rumberry Active Germplasm Bank of the Federal University of Alagoas, Brazil. Physical characteristics, chemical characteristics, and phenolic compound content were analyzed. Chemical profile characterization was carried out using PSMS. Accessions had an average weight of 0.86 g. Accession AC137 presented a higher pulp yield (1.12 g). AC132 and AC156 had larger fruits, AC137 showed greater firmness (5.93 N), and AC160 had a higher and total phenolic content ratio (279.01 ± 11.11). Orange-colored accessions scored higher in evaluated parameters, except for AC160 for phenolic content. Thirty-two compounds were identified on positive ionization mode and 42 compounds on negative ionization mode using PSMS. Flavonoids, followed by the derivatives of benzoic acid, sugars, and phenylpropanoids, were the most prominent. Myricitrin, quercitrin, and catechin stand out as flavonoids that have been reported in previous studies with antioxidant and antimicrobial properties, in addition to health and therapeutical benefits, demonstrating the potential of the rumberry fruit.

Molecules instituted some years ago a “Best Paper” award to recognize the most outstanding papers in the area of natural products, medicinal chemistry and molecular diversity published each year in Molecules. We are pleased to announce the third “Molecules Best Paper Award” for 2014. The winners were chosen by the Editor-in-Chief and selected editorial board members from among all the papers published in 2010. Reviews and research papers were evaluated separately. [...]

unsatisfactory and their proposed reassignments of GC peaks and component identities raised even more questions about the accuracy of claims published in [2]. Furthermore, during our investigation of this matter we also became aware of numerous papers concerning this same topic [6-10], that had not been cited by the authors. Almost six months have now elapsed since this was communicated to the authors, who have failed to respond to our numerous e-mails requesting some action on this matter, so in consideration of the doubts about the validity of the contents of [2] and in the absence of any data supporting the authors' claims, as Editor-in-Chief of

In the present study, chromatic coordinates, phenolic acids, flavonoids and antioxidant capacity assessed by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonate (ABTS) and lipid peroxidation inhibition capacity (LPIC) essays and their relative IC50 were investigated in 25 fig cultivars growing in Morocco. The aims of this study were to determine (i) the variation in these compounds among light and dark-colored cultivars, (ii) their partitioning between fruit peel and pulp and (iii) to display network connections among these variables. Twelve phenolic compounds (PCs) were isolated in peel extract versus eight in pulp samples. Anthocyanins, mainly cyanidin-3,5-diglucoside and cyanidin-3-O-rutinoside, were the predominant compounds in peels, where the mean concentrations were 75.90 ± 18.76 and 77.97 ± 18.95 µg/g dw, respectively. On the other hand, (−)-epicatechin and cyanidin-3-O-rutinoside were the major compounds in the pulp extracts, where the mean values were 5.23 ± 4.03 and 9.01 ± 5.67 µg/g dw, respectively. A two-dimensional hierarchically clustered heatmap was applied to the dataset to explore correlations in the dataset and similarities between cultivars, without dimensionality reduction. Results showed that anthocyanins, particularly pelargonidin-3-O-rutinoside, cyanidin-3,5-diglucoside and cyanidin-3-O-rutinoside, were the main contributors to the peels’ free radical scavenging capacity. This capacity was particularly higher in the peel of dark-colored figs compared to the fruit pulp. The local cultivar “INRA 1301” showed the most promising phenolic profile due to its very high levels of almost all detected PCs, especially (−)-epicatechin, quercetin-3-O-rutinoside, quercetin-3-O-glucoside, cyanidine-3,5-diglucoside, cyanidine-3-O-rutinoside and pelargonidin-3-O-rutinoside (54.66, 141.08, 35.48, 494.08, 478.66, 12.56 µg/g dw, respectively). Having the darkest figs in the collection (L* = 25.72, c* = 22.09 and h° = 20.99), this cultivar has also combined promising IC50 values, which were of 19.85, 40.58 and 124.78 µg/mL for DPPH, ABTS and LPIC essays, respectively.

Norma Transitória DL57/2016 Presently, water quantity and quality problems persist both in developed and developing countries, and concerns have been raised about the presence of emerging pollutants (EPs) in water. The circular economy provides ways of achieving sustainable resource management that can be implemented in the water sector, such as the reuse of drinking water treatment sludges (WTSs). This study evaluated the potential of WTS containing a high concentration of activated carbon for the removal of two EPs: the steroid hormones 17β-estradiol (E2) and 17α-ethinylestradiol (EE2). To this end, WTSs from two Portuguese water treatment plants (WTPs) were characterised and tested for their hormone adsorbance potential. Both WTSs showed a promising adsorption potential for the two hormones studied due to their textural and chemical properties. For WTS1, the final concentration for both hormones was lower than the limit of quantification (LOQ). As for WTS2, the results for E2 removal were similar to WTS1, although for EE2, the removal efficiency was lower (around 50%). The overall results indicate that this method may lead to new ways of using this erstwhile residue as a possible adsorbent material for the removal of several EPs present in wastewaters or other matrixes, and as such contributing to the achievement of Sustainable Development Goals (SDG) targets. publishersversion published

Apple (Malus pumila Mill.) is a popular fruit with high economic values and various biological activities that are beneficial to human health. In this study, 35 apple cultivars were collected and were evaluated for their basic quality indexes, phenolic compositions, antioxidant activity, anti-tumour, and anti-diabetic activities. The compositions of phenolics were detected by using high-performance liquid chromatography (HPLC) and high-resolution mass spectroscopy (HRMS) assays. The antioxidant activities of peel and pulp extracts from 35 apple cultivars were evaluated by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging assay and ferric reducing antioxidant power (FRAP) assay. Results showed that the contents of phenolic acids and proanthocyanidins showed significant correlations with the antioxidant activities. Phenolic-rich extracts significantly inhibited HepG2 cell proliferation, with the inhibition activity varied significantly between cultivars. &lsquo, Gold Delicious&rsquo, pulp extract, &lsquo, Xiboliyabaidian&rsquo, peel and pulp extracts showed protective effects on H2O2-induced injury of human umbilical vein endothelial cells (HUVEC). &lsquo, Red Fuji&rsquo, peel extract, &lsquo, peel and pulp extracts, as well as &lsquo, peel extract, significantly increased glucose consumption of HepG2 cells, in a dose-dependent manner. This research may provide theoretical guidance for further nutritional investigation of the apple resources.

Sanitary landfill leachates usually have characteristics that depend on the region where they are generated and according to the age of the landfill, which is why a unique treatment for their sanitation has not been found. However, the adsorption preceded by the Fenton process has been proven to be highly efficient at removing contaminants. In this study, the adsorptive capacity of two types of activated carbon, granular and powdered, was analyzed to determine which was more efficient in the adsorption stage in the Fenton-adsorption process. Likewise, its behavior was analyzed using three isotherm models (Langmuir, Freundlich and Temkin), testing the raw leachate and the Fenton-treated one with both carbons. The adsorption that is carried out on the carbons is better adjusted to the Freundlich and Temkin models. It concludes that multilayers, through the physical adsorption, carry out the adsorption of pollutants on the surface of the carbons. The results show that, statistically, granular activated carbon is more efficient at removing chemical oxygen demand (COD), and powdered activated carbon removes color better. Finally, an adsorption column was designed for the Fenton-adsorption process that was able to remove 21.68 kgCOD/kg carbon. Removal efficiencies for color and COD were &gt, 99%.

The present work describes the volatile compounds profile and phytochemical content of Ceratonia siliqua L. Fifty different components have been identified. Among them, three constituents are shared i.e., 2-methlybutanoic acid, methyl hexanoate and limonene by different common carob preparations: pulp decoction (PD), seeds decoction (SD) and Rob, a sweet syrup extracted from the pulp of the carob pod. Each extract exhibits different volatile aromatic emission profiles. The antioxidant activity of the extracts was evaluated using three methods, DPPH, ABTS and FRAP, producing a dose-dependent response. The IC50, when determined by FRAP, gave the lowest values (0.66 &plusmn, 0.01, 0.73 &plusmn, 0.05 and 0.55 &plusmn, 0.00 mg/mL PD, SD and Rob, respectively). The nociception essay, after intraperitoneal injection of acetic acid in mice, demonstrated that Rob, pulp and seeds decoction extracts showed an efficient inhibition of writhes over time, with persistence over 30 min. The SD decoction revealed the highest efficacy in decreasing the writhing reflex (90.3 &plusmn, 1.2%, p &lt, 0.001). Furthermore, the proapoptotic activity of SD against three human cell line, THP-1, MCF-7 and LOVO, evaluated by flow cytometry, showed a significantly stronger proapoptotic activity on colon cancer (LOVO) than on the other cell lines, a phenomenon known as phenotypic selectivity.

International audience; Different methods were tested to evaluate the performance of a pretreatment before anaerobic digestion. Besides conventional biochemical parameters, such as the biochemical methane potential (BMP), the methane production rate, or the extent of solubilization of organic compounds, methods for physical characterization were also developed in the present work. Criteria, such as the particle size distribution, the water retention capacity, and the rheological properties, were thus measured. These methods were tested on samples taken in two full-scale digesters operating with cattle manure as a substrate and using hammer mills. The comparison of samples taken before and after the pretreatment unit showed no significant improvement in the methane potential. However, the methane production rate increased by 15% and 26% for the two hammer mills, respectively. A relevant improvement of the rheological properties was also observed. This feature is likely correlated with the average reduction in particle size during the pretreatment operation, but these results needs confirmation in a wider range of systems.

Electrochemical technologies have been broadly applied in wastewaters treatment, but few studies have focused on comparing the performance of the different electrochemical processes, especially when used to treat highly-polluted streams. The electrochemical treatment of a reverse osmosis concentrate of sanitary landfill leachate was performed by means of electrocoagulation (EC), anodic oxidation (AO) and electro-Fenton (EF) processes, and the use of different electrode materials and experimental conditions was assessed. All the studied processes and experimental conditions were effective in organic load removal. The results obtained showed that EC, with stainless steel electrodes, is the cheapest process, although it presents the disadvantage of sludge formation with high iron content. At high applied current intensity, AO presents the best treatment time/energy consumption ratio, especially if the samples&rsquo, initial pH is corrected to 3. However, pH correction from natural to 3 deeply decreases nitrogen-containing compounds&rsquo, removal. For longer treatment time, the EF process with a carbon-felt cathode and a BDD anode, performed at natural iron content and low applied current intensity, is the most favorable solution.

This study focused on the reduction of the treatment cost of mature landfill leachate (LL) by enhancing the coagulation pre-treatment before a UVA-LED photo-Fenton process. A more efficient advanced coagulation pretreatment was designed by combining conventional coagulation (CC) and electro-coagulation (EC). Regardless of the order in which the two coagulations were applied, the combination achieved more than 73% color removal, 80% COD removal, and 27% SUVA removal. However, the coagulation order had a great influence on both final pH and total dissolved iron, which were key parameters for the UVA-LED photo-Fenton post-treatment. CC (pH = 5, 2 g L−1 of FeCl36H2O) followed by EC (pH = 5, 10 mA cm−2) resulted in a pH of 6.4 and 100 mg L−1 of dissolved iron, whereas EC (pH = 4, 10 mA cm−2) followed by CC (pH = 6, 1 g L−1 FeCl36H2O) led to a final pH of 3.4 and 210 mg L−1 dissolved iron. This last combination was therefore considered better for the posterior photo-Fenton treatment. Results at the best cost-efficient [H2O2]:COD ratio of 1.063 showed a high treatment efficiency, namely the removal of 99% of the color, 89% of the COD, and 60% of the SUVA. Conductivity was reduced by 17%, and biodegradability increased to BOD5:COD = 0.40. With this proposed treatment, a final COD of only 453 mg O2 L−1 was obtained at a treatment cost of EUR 3.42 kg COD−1.

Studies on polyphenols and flavonoids in natural products reveal benefits in the prevention of multiple diseases. Proper extraction, treatment of extracts, and quantification of polyphenols and flavonoids demand attention from the scientific community in order to report more specific biological action. Total polyphenol content (TPC) and total flavonoid content (TFC) (measured at three different times) of ethanol, methanol and acetone extracts of Mauritia flexuosa (aguaje) and Theobroma grandiflorum (copoazú) fresh pulp, from the Colombian Amazon region, were evaluated with the purpose of focusing in the polyphenol/flavonoid proportion and its effective antioxidant activity. This objective could help to explain specific flavonoid biological action based on higher flavonoid proportion rather than higher total polyphenol content. Differences in extracting solvents resulted in statistically significant different yields; the highest TPC was observed with acetone 70% in Mauritia flexuosa and ethanol 80% for T. grandiflorum. The best flavonoid/polyphenol ratio in M. flexuosa was about 1:2.4 and 1:12.8 in T. grandiflorum and the antioxidant efficacy was proportionally higher for flavonoids extracted from T. grandiflorum. HPLC analysis revealed 54 µg/g of the flavonoid kaempferol in M. Flexuosa and 29 µg/g in T. grandiflorum. Further studies evaluating this proportionality, in seeds or peel of fruits, as well as, other specific biological activities, could help to understand the detailed flavonoid action without focusing on the high total polyphenol content.

The prebiotic potential of longan juice obtained by a commercial Viscozyme L for conversion of constituent sucrose to fructo-oligosaccharide was investigated. The physicochemical properties and carbohydrate composition of the longan juice was evaluated before and after enzymatic treatment. The stimulation effects of the treated longan juice on probiotic bacteria growth were also studied in vitro. The results showed that total soluble solids, yield and clarity of longan juice were all significantly improved after enzyme treatment. The water-soluble polysaccharide content, including pectin, was significantly increased. Compared with the natural longan pulp, the enzyme treated juice showed a significant decrease in sucrose content. Substantial fructo-oligosaccharides including 1-kestose and nystose were synthesized after enzyme treatment. The molecular weight distribution and the monosaccharide composition of the water-soluble polysaccharide were significantly changed by enzyme treatment. The treated longan juice and its ethanol-soluble sugar fraction promoted the growth of Streptococus thermophiles, Lactobacillus acidophilus and Lactobacillus delbrueckii, showing a good potential of the treated longan juice for producing functional foods and nutraceuticals.

All food scientists must utilize plants for their application as functional foods to reduce hypercholesterolemia incidence through diet. Canarium odontophyllum (dabai) is a novel source for new healthy oil and functional foods. In this work, we evaluate the hepatoprotective effects of supercritical carbon dioxide (SC-CO2) extracted dabai pulp oil (DPO) and defatted dabai pulp (DDP) against hypercholesterolemia elicited by a high-cholesterol diet in rats. Our results show that DPO and DDP supplementation exerted beneficial hypocholesterolemic effects against the high-cholesterol diet-fed rat. Nevertheless, supplementation with DDP revealed superior total cholesterol, low-density lipoprotein, and HMG-CoA reductase lowering efficacy (p < 0.05). Supplementation of either DPO or DDP did not significantly affect AST and ALT levels than normal rats (p > 0.05). Therefore, DDP and DPO are considered as having no toxicological significance. The histological section of rats treated with DPO and DDP showed improved steatosis in hepatocytes. HPLC analysis revealed that DPO and DDP contained syringic acid, which plays an important role in the beneficial effect. In conclusion, our results support the hypocholesterolemic and hepatoprotective effects of DPO and DDP in the hypercholesterolemic rats model.

Forsythiae Fructus, as a traditional Chinese medicine, has been widely used both as a single herb and in compound prescriptions in Asia, mainly due to its heat-clearing and detoxifying effects. Modern pharmacology has proved Forsythiae Fructus possesses various therapeutic effects, both in vitro and in vivo, such as anti-inflammatory, antibacterial and antiviral activities. Up to now, three hundred and twenty-one compounds have been identified and sensitive analytical methods have been established for its quality control. Recently, the pharmacokinetics of Forsythiae Fructus and its bioactive compounds have been reported, providing valuable information for its clinical application. Therefore, this systematic review focused on the newest scientific reports on Forsythiae Fructus and extensively summarizes its phytochemistry, pharmacology, pharmacokinetics and standardization procedures, especially the difference between the two applied types—unripe Forsythiae Fructus and ripe Forsythiae Fructus—in the hope of providing a helpful reference and guide for its clinical applications and further studies.

China is one of the most important centers of diversity for Eriobotrya japonica Lindl. in the world. In this study, seven loquat cultivars grown in China were evaluated for their phenolic compounds and antioxidant activity. Eleven phenolic compounds, i.e., 3-p-coumaroylquinincacid (3-p-CoQA), 5-caffeoylquinic acid (5-CQA), 4-caffeoylquinic acid (4-CQA), 3-caffeoylquinic acid (3-CQA), 5-feruloylquinic acid (5-FQA), quercetin-3-O-galactoside (Q-3-Gal), quercetin-3-O-glucoside (Q-3-Glu), quercetin-3-O-rhamnoside (Q-3-Rha), kaempferol-3-O-galactoside (K-3-Gal), kaempferol-3-O-rhamnoside (K-3-Rha), and kaempferol-3-O-glucoside (K-3-Glu) were identified and quantified in the peel and pulp of the cultivars tested. 3-CQA and 5-CQA were the predominant components in both fruit parts. 2,2-Diphenyl-1-picrylhydrazyl radicals (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonate (ABTS), and ferric reducing antioxidant power (FRAP) assays were used for the antioxidant evaluation. Results showed that peel extracts had higher antioxidant activities than their pulp counterparts in all the cultivars tested, which was correlated with their higher total phenolic contents. The antioxidant potency composite (APC) index showed obvious variations ranging from 64.15 to 100 in the peel and from 59.49 to 97.95 in the pulp of different cultivars, where “Dahongpao” (DHP) and “Luoyangqing” (LYQ) had the highest APC index in the peel and pulp, respectively. Overall, loquat cultivars rich in hydroxycinnamic acids (HCAs) such as 3-p-CoQA, 5-CQA, 4-CQA, 3-CQA and 5-FQA showed relatively higher antioxidant activities, and may be excellent sources of phytochemicals and natural antioxidants.

This paper describes an improved procedure for the efficient and facile synthesis of 4-aryl substituted 3, 4-dihydropyrimidinones under mild reaction conditions with excellent yields using inexpensive silica chloride under solvent free conditions.

Phenolic compounds are known to have antioxidant capacity; however, there is little information about molecular interactions between particular phenolics found in fruits at different developmental stages. Therefore, the total antioxidant capacity of the phenolic compounds of a fruit may not correspond to the sum of individual antioxidant capacity given by antioxidants from that tissue. In this study, individual antioxidant capacity and the interactions of four major phenolic compounds (chlorogenic, gallic, protocatechuic and vanillic acid) found in ‘Ataulfo’ mango pulp were tested using the DPPH assay. Significant synergism was found in the majority of the all combinations, as well as the combination of the four phenolics. However, antagonism was also observed between some molecules. This work demonstrated particular interactions that may occur in a complex environment within the complex framework of a natural food. The present results may also assist in the future design of functional foods or ingredients based on their antioxidant activity and their synergistic or antagonist interactions.

Variations of phenolics, antioxidant activity, and mineral contents in peel and pulp of five apple (Malus domestica Borkh.) cultivars from Pakistan, namely Red Delicious, Golden Delicious, Kashmiri Amri, Kala Kulu and Sky Spur were appraised. The mean extract yield of antioxidant components obtained with 80:20 methanol-water (v/v), was found to be 22.1 g/100 g for peel and 14.2 g/100 g for pulp on a dry weight basis. The amounts of total phenolics and total flavonoids in peel and pulp of different cultivars of apple ranged from 1,907.5–2,587.9 mg gallic acid equivalent/100 g DW and 1,214.3–1,816.4 mg catechin equivalent/100 g DW and 1,185.2–1,475.5 mg GAE/100 g DW and 711.8–999.3 mg CE/100 g DW, respectively. The inhibition of linoleic acid peroxidation and DPPH scavenging activity of the extracts varied from 71.7–84.9 and 66.6–80.8% in peel, and 43.9–52.8 and 42.9–51.1% in pulp, respectively. Reducing power of the tested fruit part extracts at concentration 12.5 mg/mL ranged from 2.54–2.89 and 1.37–1.73, respectively. With regard to minerals analysis, both fruit parts showed the amount of K to be the highest, followed by Mg, Ca, Fe, Na and Zn. The results revealed that peel of the tested apple cultivars in this study had superior antioxidant capacity and mineral concentration than the pulp, indicating significant variations between the parts tested. Thus, consumption of apple fruits along with peel might be recommended to gaining better nutritive benefits.

This study provides new data on the various carotenoids found in bambangan (Mangifera pajang Kosterm.) peel and pulp extracts, such as all-trans-α- and β-carotene, cis-β-carotene, 9-cis-β-carotene, and cryptoxanthin. Chemical and biological antioxidant assays were determined to evaluate the antioxidant capacity of bambangan peel and pulp extracts. Bambangan pulp had higher α- and β-carotene contents (7.96 ± 1.53 and 20.04 ± 1.01 mg/100 g) than its peel (4.2 ± 0.14 and 13.09 ± 0.28 mg/100 g), the cryptoxanthin contents of bambangan peel and pulp were 0.60 and 1.18 mg/100 g, respectively. The antioxidant activity results determined by chemical assay using the 2,2-diphenyl-2-picrylhydrazyl (DPPH) method showed that bambangan peel extract had higher DPPH radical scavenging activity than its pulp. In the biological assays bambangan peel and pulp had protective effects against hemoglobin and LDL oxidation at an extract concentration of 1 ppm. Bambangan peel is a therefore a potential source of natural antioxidants and could be utilized as a functional ingredient.

Natural antioxidants such as polysaccharides with strong antioxidant activities are used to protect against oxidative damage, yet little is known so far about the antioxidant effects of litchi fruit polysaccharides. In the present study, four different polysaccharide-enriched fractions were isolated from litchi pulp tissue and partially purified by a stepwise method of ethyl alcohol (EtOH) precipitation. Their chemical and physical characteristics were determined by chemical methods, gas chromatography and IR spectrophotometry. Antioxidant activities of these fractions were investigated using various in vitro assay systems. These four polysaccharide-enriched fractions exhibited a dose-dependent free radical scavenging activity as shown by their DPPH radical, superoxide anion and hydroxyl radical inhibition, chelating ability and reducing power. Among the different fractions, LFP-III showed the strongest scavenging activity against DPPH radical, superoxide and hydroxyl radicals and chelating ability. These findings suggest litchi polysaccharides from pulp tissue have potential as functional foods with enhanced antioxidant activity.

Hydnophytum formicarum Jack. (Rubiaceae) is a medicinal plant whose tubers possesses cardiovascular, anti-inflammatory and antiparasitic effects and have been used for the treatment of hepatitis, rheumatism and diarrhea. Herein we report the isolation of its active constituents and the testing of their antimicrobial activity against 27 strains of microorganisms using an agar dilution method and of their antioxidative activity using the DPPH and SOD assays. The results show that the crude hexane, dichloromethane, ethylacetate and methanol extracts exert such activities. Particularly, the crude ethyl acetate extract exhibits antigrowth activity against many Gram-positive and Gram-negative bacteria with MIC 256 microg/mL. Shewanella putrefaciens ATCC 8671 is completely inhibited at a lower MIC (128 microg/mL). Interestingly, Corynebacterium diphtheriae NCTC10356 is inhibited by all the tested extracts. Significantly, the ethyl acetate extract is also the most potent antioxidant, showing 83.31% radical scavenging activity with IC50 8.40 microg/mL in the DPPH assay. The other extracts display weak to moderate antioxidative activities, ranging from 28.60-56.80% radical scavenging. The SOD assay shows that methanol extract exhibits the highest activity (74.19% inhibition of superoxide radical). The dichloromethane and ethyl acetate extracts display comparable SOD activity. The promising bioactivities of the crude ethyl acetate extract guided the first isolation of bioactive flavonoid and phenolic compounds: isoliquiritigenin (2), protocatechualdehyde(3), butin (4) and butein (5) from this species. Their structures have been fully established by 1D and 2D NMR. In addition, stigmasterol was isolated from the crude hexane and dichloromethane extracts. The antimicrobial and cytotoxic activities of compounds 3-5 were evaluated. The tested compounds were inactive against HuCCA-1 and KB cell lines,showing ED50> 10 microg/mL. Protocatechualdehyde (3) completely inhibits the growth of Plesiomonas shigelloides with MIC

We report the synthesis, antioxidant and antiproliferative activity and a QSAR analysis of synthetic diphenylpropionamide derivatives. Synthesis of these compounds was achieved by direct condensation of 2,2- and 3,3-diphenylpropionic acid and appropriate amines using 1-propylphoshonic acid cyclic anhydride (PPAA) as catalyst. Compound structures were elucidated by NMR analysis and their melting points were measured. The in vitro antioxidant activity of these compounds was tested by evaluating the amount of scavenged ABTS radical and estimating ROS and NO production in LPS stimulated J774.A1 macrophages. All compounds were tested for their effect on viability of cells and results demonstrated that they are not toxic towards the cell lines used. The cytotoxic activity of all compounds was evaluated by a Brine Shrimp Test.

We report here the characterisation of eight newly synthesized thioureides of 2-(4-chlorophenoxymethyl)-benzoic acid and the evaluation of the in vitro antimicrobial activity of the new compounds against Gram-positive [Listeria monocytogenes,Staphylococcus aureus, Bacillus subtilis], Gram-negative [Psedomonas aeruginosa,Escherichia coli, Salmonella enteritidis], as well as Candida spp., using both reference and clinical multidrug resistant strains to establish the minimal inhibitory concentration (MIC)values. Our results showed that the tested compounds exhibited specific antimicrobial activities, both concerning the spectrum of antimicrobial activity and the corresponding MIC values, which ranged widely between 1024 and 32 mug/mL, depending on the nature and position of the substituents on the benzene ring. The most active compounds were N-[2-(4-chlorophenoxymethyl)-benzoyl]-N'-(2,6-dichlorophenyl)-thiourea (5 g) and N-[2-(4-chlorophenoxymethyl)-benzoyl]-N'-(4-bromophenyl)-thiourea (5h), which showed a broad spectrum of antimicrobial activity against enterobacterial strains (E. coli and S. enteritidis),P. aeruginosa, S. aureus and Candida spp. All the tested compounds except 5f were highly active against S. aureus (MIC=32 mug/mL), suggesting their possible use in the treatment of MRSA infections. Four of compounds also exhibited antifungal activity (MIC =256-32 microg/mL) against C. albicans, but L. monocytogenes as well as B. subtilis were resistant to all tested compounds. Our studies thus demonstrated that among other biological activities,the thioureides of 2-(4-chlorophenoxymethyl)-benzoic acid also exhibit selective and effective antimicrobial properties that could lead to the selection and use of these compounds as efficient antimicrobial agents, especially for the treatment of multidrug resistant infections.

The article describes a two-step synthesis of diastereomeric 3-hydroxy-2-methyl-3-(4-biphenylyl)butanoic acids. In the first step an intermediate alpha-bromo propanoic acid 1-ethoxyethyl ester was synthesized. The second step is a new modified Reformatsky reaction in presence of Zn in tetrahydrofuran (THF) at -5 to 10 degrees C between the previously synthesized intermediate and 4-acetylbiphenyl. Synthesis of the other studied beta-hydroxy-beta-arylpropanoic acids has already been reported. These beta-hydroxy-beta-arylpropanoic acids belong to the arylpropanoic acid class of compounds, structurally similar to the NSAIDs such as ibuprofen. The anti-inflammatory activity and gastric tolerability of the synthesized compounds were evaluated. Molecular docking experiments were carried out to identify potential COX-2 inhibitors among the beta-hydroxy-beta-aryl-alkanoic acids class. The results indicate that all compounds possess significant anti-inflammatory activity after oral administration and that the compounds 2-(9-(9-hydroxy-fluorenyl))-2-methylpropanoic acid (5) and 3-hydroxy-3,3-diphenyl-propanoic acid (3) possess the strongest anti-inflammatory activity, comparable to that of ibuprofen, a standard NSAID,and that none of tested substances or ibuprofen produced any significant gastric lesions.

3-Alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones 2a-g reacted with 4-diethylaminobenzaldehyde to afford the corresponding 3-alkyl(aryl)-4-(4-diethyl-aminobenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones 3a-g. The acetylation reactions of compounds 3a-e were investigated and compounds 4a-e were thus obtained. The new compounds were characterized using IR, (1)H-NMR, (13)C-NMR, UV and MS spectral data. In addition, the newly synthesized compounds 3a-g were titrated potentiometrically with tetrabutylammonium hydroxide in four non-aqueous solvents such as isopropyl alcohol, tert-butyl alcohol, acetone and N,N-dimethylformamide (DMF), and the half-neutralization potential values and the corresponding pKa values were determined for all cases. Moreover, 3 and 4 type compounds were also screened for their antioxidant activities.

Some novel Schiff bases have been prepared by reacting 6-azido-5-formyl-2-pyridone 1 with a series of aromatic amines 2a-f . 5-Arylaminomethylene-6-( E )-aryl-iminopyridones 3a-e were obtained by reaction of 1 with 2a-e at room temperature, whereas with , the 6-azido-5-naphthalen-2-yl 2f -iminomethylpyridone derivative 4 was formed. On the other hand, heating 1 with 2a-d at 140-150°C yielded two sets of isomeric products, ( E )- 3a-d and ( Z )- 5a-d . Refluxing compounds ( Z )- 3a,c with hydroxyl-amine in methanol gave the corresponding hydroxyliminopyridones 8a,c . Heating of ( E )- 3a-d with excess POCl 3 at reflux did not give the expected tricyclic compound 9 , but rather the isomeric products ( Z )- 5a-d were obtained. The structures of all these products have been characterized using IR and 1 H- and 13 C-NMR spectroscopy. Keywords: 6-Azido-5-formyl-2-pyridones, arylamines, Schiff bases, NMR spectroscopy. Introduction The importance of Schiff bases in organic synthesis has increased over the past few decades because they are among the most versatile organic synthetic intermediates [1] and they also present a broad range of biological activities such as herbicidal [2], antifungal [3], antimicrobial [4-7] and antitumor properties [8,9]. Moreover, Schiff bases have also attracted much attention because of their

An improved synthetic method affording 4-chlorocoumarin-3-sulfonyl chloride (4) in very good yield (ca. 85 %) is reported. This compound was reacted with various bidentate nucleophiles such as 2-aminopyridines and 2-aminothiazoles in order to obtain substituted pyrido- and thiazino-1,2,4-thiadiazino-benzopyranone dioxides (potential anticancer and anti-HIV agents). These reactions occurred rapidly at room temperature giving yellowish precipitates, which are insoluble in common organic solvents, making the purification process challenging. Further investigation has shown that these fused heterocycles are not stable and decompose with opening of the 1,2,4-thiadiazine ring. © 2007 by MDPI. DAAD

(-)-Epicatechin-3-gallate (ECG) is a polyphenolic compound similar to (-)-epigallocatechin-3-gallate (EGCG) which is abundant in green tea. Numerous workers have proposed that EGCG protects epidermal cells against UVB-induced damage. However, little has been known about whether ECG protects keratinocytes against UVB-induced damage. We decided to investigate the protective effects and underlying mechanisms of ECG on UVB-induced damage. Cell viability was determined by the MTT assay. Activation of ERK1/2, p38 and JNK was analyzed by Western blotting. Intracellular H2O2 production and DNA content was analyzed by flow cytometry. Lipid peroxidation was assayed by colorimetry. In our study, we found that ECG dose-dependently attenuated UVB-induced keratinocyte death. Moreover, ECG markedly inhibited UVB-induced cell membrane lipid peroxidation and H2O2 generation in keratinocytes, suggesting that ECG can act as a free radical scavenger when keratinocytes were photodamaged. In parallel, H2O2-induced the activation of ERK1/2, p38 and JNK in keratinocytes could be inhibited by ECG. UVB-induced pre-G1 arrest leading to apoptotic changes of keratinocytes were blocked by ECG. Taken together, we provide here evidence that ECG protects keratinocytes from UVB-induced photodamage and H2O2-induced oxidative stress, possibly through inhibition of the activation of ERK1/2, p38 and JNK and/or scavenging of free radicals.

The new methyl orthoformate of the powerful antioxidant hydroxytyrosol (or 2-(3,4-dihydroxyphenyl)ethanol) has been synthesized by a two-step high yielding procedure. The protection stabilizes hydroxytyrosol against fast oxidation and allows both easy chromatographic purification and long term storage. The protective group is hydrolyzed over pH = 10 and below pH = 5, thus allowing the release of the active principle under physiological conditions. The use of the methyl orthoformate-protected hydroxytyrosol allows the preparation of protected hydroxytyrosyl esters, like the acetate herein reported, by selective esterification of the alcoholic function. The subsequent quantitative deprotection under non-aqueous and mild conditions affords the hydroxytyrosyl acetate in high yields.

The antioxidant activity of flavonoids is believed to increase when they are coordinated with transition metal ions. However, the literature on this subject is contradictory and the outcome seems to largely depend on the experimental conditions. In order to understand the contribution of the metal coordination and the type of interaction between a flavonoid and the metal ion, in this study a new metal complex of Cu (II) with naringin was synthesized and characterized by FT-IR, UV-VIS, mass spectrometry (ESI-MS/MS), elemental analysis and 1H-NMR. The results of these analyses indicate that the complex has a Cu (II) ion coordinated via positions 4 and 5 of the flavonoid. The antioxidant, anti-inflammatory and antimicrobial activities of this complex were studied and compared with the activity of free naringin. The Naringin–Cu (II) complex 1 showed higher antioxidant, anti-inflammatory and tumor cell cytoxicity activities than free naringin without reducing cell viability.

A simple synthesis of sulfonamides 4–22 as novel histone deacetylase (HDAC) inhibitors is described. The key synthetic strategies involve N–sulfonylation of L–proline benzyl ester hydrochloride (2) and coupling reaction of N–sulfonyl chloride 3 with amines in high yields. It was found that several compounds showed good cellular potency with the most potent compound 20 exhibiting an IC50 = 2.8 μM in vitro.

Three kinds of molecular complexes based on tetrathiafulvalene (TTF) and dialkylviologens were prepared and their crystal structures elucidated. While TTF-dimethylviologen complex forms a mixed stack arrangement of donors and acceptors in its crystal structure, TTF donors aggregate with long alkyl groups by CH/π and/or van der Waals interactions in a couple of TTF-heptylviologen complexes. Keywords: Molecular complex; CT complex; TTF; viologen; crystal structure Introduction Considerable attention has recently been paid in the field of supramolecular and materials chemistry to the incorporation of electroactive components into supramolecular assemblies. Among them, the supramolecular and macrocyclic assemblies derived from redox-controllable TTF 1 and dialkyl-4,4’-bipyridinium dications (dialkylviologens) such as 2 , have evoked attention, not only as catenanes and rotaxanes, but also as molecular switche s and potential molecular el ectronics devices [1]. The assembly of such kinds of molecular complexes relies strongly upon non-covalent charge-transfer (CT) interactions between donors and acceptors [2]. Since a dialkylviolgen

Phenolics were extracted from litchi fruit pericarp (LFP) tissues, purified and their antioxidant properties analyzed. LFP phenolics strongly inhibited linoleic acid oxidation and exhibited a dose-dependent free-radical scavenging activity against α,α-diphenyl-β-picrylhydrazyl (DPPH·) and hydroxyl radicals and superoxide anions. The degradation of deoxyribose by hydroxyl radicals was inhibited by phenolics acting mainly as iron ion chelators, rather than by directly scavenging the radicals. Phenolics from litchi fruit pericarp were found to display similar reducing power activity as ascorbic acid. The effect of phenolic compound treatment on pericarp browning and electrolyte leakage of litchi fruit was also evaluated and it was observed that application of exogenous litchi phenolics to harvested litchi fruit significantly prevented pericarp browning and delayed increases in electrolyte leakage. These results suggest that litchi pericarp tissue phenolics could be beneficial in scavenging free radicals, maintaining membrane integrity and, thereby inhibiting pericarp browning of litchi fruit.

During the course of studies directed towards the discovery of novel aldose reductase inhibitors for the treatment of diabetic complications, we synthesized a series of new (Z)-3-phenyl-2-benzoylpropenoic acid derivatives and tested their in vitro inhibitory activities on rat lens aldose reductase. Of these compounds, (Z)-3-(3,4-dihydroxyphenyl)-2-(4-methylbenzoyl)propenoicacid (3k) was identified as the most potent inhibitor, with an IC50 of 0.49 microM. The theoretical binding mode of 3k was obtained by simulation of its docking into the active site of the human aldose reductase crystal structure.

Chinese water chestnut (CWC) is one of the most popular foods among Asian people due to its special taste and medical function. Experiments were conducted to test the antioxidant activity and then determine the major phenolic compound components present in CWC. CWC phenolic extract strongly inhibited linoleic acid oxidation and exhibited a dose-dependent free-radical scavenging activity against α,α-diphenyl-β-picrylhydrazyl (DPPH) radicals, superoxide anions and hydroxyl radicals, which was superior to ascorbic acid and butylated hydroxytoluene (BHT), two commercial used antioxidants. Furthermore, the CWC extract was found to have a relatively higher reducing power, compared with BHT. The major phenolic compounds present in CWC tissues were extracted, purified and identified by high-performance liquid chromatograph (HPLC) as (–)-gallocatechin gallate, (–)-epicatechin gallate and (+)-catechin gallate. This study suggests that CWC tissues exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.

A series of benzothiazol-2-yl-dithiocarbamates 3a-d along with their copper complexes 4a-c were synthesized via the reaction of suitable alkyl, aralkyl or heteroaryl halides with the sodium salt of benzothiazol-2-yl-dithiocarbamic acid, followed by complexation with copper sulphate. N-(4-Acetyl-5-aryl-4,5-dihydro-1,3,4-thiadiazol-2-yl)-N-benzothiazol-2-yl-acetamides 7a-c were synthesized by cyclization of the appropriate thiosemicarbazones 6a-c in acetic anhydride. Selected compounds were screened for in vitro schistosomicidal activity against Schistosoma mansoni at three different dosage levels (10, 50 and 100 μg/ mL). Three of these products, 4a-c, showed schistosomicidal activity similar to praziquantel, with 100% worm mortality at 10 μg/mL. These compounds would constitute a new class of potent schistosomicidal agents.

We have synthesized a novel chiral NADH model compound, N-methyl-(R)-3-(tert-butyl)-sulphinyl-1,4-dihydropyridine with high enantioselectivity and used it in the reduction of methyl benzoylformate, producing (S)-methyl mandelate in 95% ee. The absolute structure of its precursor, 3-(tert-butyl)sulfinyl pyridine, was determined by X-ray analysis.

The isolation of four novel acylated flavonoid glycosides from the roots of Saussurea lappa and their identification using a combination of 1D and 2D NMR and mass spectrometry is described. The in vitro antifungal and antibacterial activities of the isolated compounds and their mixture were tested on nine fungal and four bacterial strains, using the microdilution method. The compounds and mixture showed moderate to high antifungal activity against most of the fungi tested, compared to a miconazole standard, while only one compound and the mixture showed antibacterial activity against all strains tested.

The complete characterization of two compounds obtained from the acetone extract of Populus tremula knotwood has been was achieved using LC-DAD-MS, MS/MS, IR and NMR. The new compounds were unequivocally identified as a mixture of the ester isomers of the (E) and (Z) p-coumarate of 1-O-rutinose. The isomers showed the capacity to inhibit lipid peroxidation induced by tert-butylhydroperoxide and to trap peroxyl radicals, as determined by a chemiluminescence method. These new phenyl disaccharides also showed a significant ORAC (oxygen radical absorbance capacity) value, i.e. 11.7 microM TE (Trolox Equivalents).

The antibacterial activity against Staphylococcus aureus of long-chain fatty alcohols was investigated, with a focus on normal alcohols. The antibacterial activity varied with the length of the aliphatic carbon chain and not with the water/octanol partition coefficient. 1-Nonanol, 1-decanol and 1-undecanol had bactericidal activity and membrane-damaging activity. 1-Dodecanol and 1-tridecanol had the highest antibacterial activity among the long-chain fatty alcohols tested, but had no membrane-damaging activity. Consequently, it appears that not only the antibacterial activity but also the mode of action of long-chain fatty alcohols might be determined by the length of the aliphatic carbon chain.

Based on the molecular modeling analysis against Y181C HIV-1 RT, dipyridodiazepinone derivatives containing an unsubstituted lactam nitrogen and 2-chloro-8-arylthiomethyl were synthesized via an efficient route. Some of them were evaluated for their antiviral activity against HIV-1 RT subtype E and were found to exhibit virustatic activity comparable to some clinically used therapeutic agents.

Two new oxindole alkaloids isatinone A (1) and B (2) have been isolated from Isatis costata, along with the known trisindoline. Their structures have been assigned on the basis of spectroscopic techniques and chemical studies. Both new compounds showed significant antifungal activity.

A series of eight new azomethine derivatives were synthesized by reacting 2-formylphenoxyacetic acid with aromatic amines. The chemical structures of these compounds were confirmed by means of 1H-NMR, 13C-NMR, MS and elemental analysis. The compounds were assayed by the disc diffusion method for antibacterial against Staphylococcus aureus and Escherichia coli. Among the compounds tested, 2a, 2b, 2e, 2g and 2h exhibited good antibacterial activity, almost equal to that of Ciprofloxacin used as standard.

Baicalein (1), 6-hydroxyapigenin (6), 6-hydroxygalangin (13) and 6-hydroxy-kaempferol (14), which are naturally occurring flavonoids from a set of 14 hydroxy-flavones tested, exhibited high inhibitory effects on tyrosinase with respect to l-DOPA, while each of the 5,6,7-trihydroxyflavones 1, 6, 13 or 14 acted as a cofactor to monophenolase. Moreover, 6-hydroxykaempferol (14) showed the highest activity and was a competitive inhibitor of tyrosinase compared to l-DOPA. 5,6,7-Trihydroxyflavones 1, 6, 13 or 14 showed also high antioxidant activities. Hence, we conclude that the 5,6,7-trihydroxy-flavones are useful as good depigmentation agents with inhibitory effects in addition to their antioxidant properties.

The synthesis of Cu(II) complexes derived from Schiff base ligands obtained by the condensation of 2-hydroxybenzaldehyde or terephtalic aldehyde with 4-amino-antipyrine (4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one) is presented. The newly prepared compounds were characterized by( 1)H-NMR, UV-VIS, IR and ESR spectroscopy. The determination of the antimicrobial activity of the ligands and of the complexes was carried out on samples of Escherichia coli, Klebsiella pneumoniae, Acinetobacter boumanii, Pseudomonas aeruginosa, Staphylococcus aureus and Candida sp. The qualitative and quantitative antimicrobial activity test results proved that all the prepared complexes are very active, especially against samples of Ps. aeruginosa, A. Boumanii, E. coli and S. aureus.