Structure-activity relationship studies of pyrogallol as a calcineurin/NFAT signaling suppressor.

Previously, we have shown that pyrogallol alleviated nasal symptoms and suppressed IL-9 gene up-regulation in allergy model rats by inhibiting calcineurin/NFAT signaling. As pyrogallol has antioxidative activity, it may be responsible for inhibiting calcineurin/NFAT signaling-mediated IL-9 gene expression. However, the relationship between antioxidative activity and suppression of IL-9 gene expression has not been elucidated yet. Here, we conducted the structure-activity relationship studies of pyrogallol and its structurally related compounds to understand the mechanism of IL-9 gene suppression by pyrogallol. 2, 2-Diphenyl-1-picrylhydrazyl radical scavenging assay showed that the antioxidative activity of catechol, resorcinol, phloroglucinol, and gallic acid is 60.1%, 10.4%, 18.8%, and 113.5% of pyrogallol, respectively. Catechol, resorcinol, and phloroglucinol did not suppress NFAT dephosphorylation. Gallic acid suppressed dephosphorylation of NFAT. Gallic acid also suppressed ionomycin-induced up-regulation of IL-9 gene expression with the IC50 value of 82.6 µM. However, catechol, resorcinol and phloroglucinol showed no suppressive activity. In addition, using gallic acid-immobilized beads, we isolated and identified Poly(U)-binding-splicing factor 60 (PUF60) as a pyrogallol binding protein. These results suggest that the antioxidative activity of pyrogallol is not likely to be the mechanism of IL-9 gene suppression. Data also suggest that PUF60 is one of its target molecules responsible for the suppression of calcineurin/NFAT signaling by pyrogallol.

New resveratrol analogs as improved biologically active structures: Design, synthesis and computational modeling.

New analogs of the well-known bioactive trihydroxy-stilbene resveratrol were synthesized to investigate their potential biological activity. The focus was on assessing their ability to inhibit cholinesterase enzymes (ChEs) and their antioxidative properties, which were thoroughly examined. New resveratrol analogs were synthesized through Wittig or McMurry reaction in moderate-to-good yields. In all synthetic pathways, mixtures of cis- and trans-isomers were obtained, then separated by chromatography, and trans-isomers were isolated as targeted structures. The stilbene derivatives underwent evaluation for antioxidant activity (AOA) using DPPH and CUPRAC assay, and their potential to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) was also measured. The biological tests have shown that the same compounds exhibited significant antioxidative and butyrylcholinesterase inhibitory potential, as evidenced by lower IC50 values compared to the established standards, trans-resveratrol, and galantamine, respectively. Additionally, molecular docking of the selected synthesized potential inhibitors to the enzyme's active site was performed, followed by assessing the complex stability using molecular dynamics simulation lasting 100 ns. Lastly, the new compounds underwent examination to determine their potential mutagenicity.

Improvement of Alginate Extraction from Brown Seaweed (Laminaria digitata L.) and Valorization of Its Remaining Ethanolic Fraction.

This study aimed to improve the conventional procedure of alginate isolation from the brown seaweed (Laminaria digitata L.) biomass and investigate the possibility of further valorization of the ethanolic fraction representing the byproduct after the degreasing and depigmentation of biomass. The acid treatment of biomass supported by ultrasound was modeled and optimized regarding the alginate yield using a response surface methodology based on the Box-Behnken design. A treatment time of 30 min, a liquid-to-solid ratio of 30 mL/g, and a treatment temperature of 47 °C were proposed as optimal conditions under which the alginate yield related to the mass of dry biomass was 30.9%. The use of ultrasonic radiation significantly reduced the time required for the acid treatment of biomass by about 4 to 24 times compared to other available conventional procedures. The isolated alginate had an M/G ratio of 1.08, which indicates a greater presence of M-blocks in its structure and the possibility of forming a soft and elastic hydrogel with its use. The chemical composition of the ethanolic fraction including total antioxidant content (293 mg gallic acid equivalent/g dry weight), total flavonoid content (14.9 mg rutin equivalent/g dry weight), contents of macroelements (the highest content of sodium, 106.59 mg/g dry weight), and microelement content (the highest content of boron, 198.84 mg/g dry weight) was determined, and the identification of bioactive compounds was carried out. The results of ultra high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry analysis confirmed the presence of 48 compounds, of which 41 compounds were identified as sugar alcohol, phenolic compounds, and lipids. According to the 2,2-diphenyl-1-picrylhydrazyl assay, the radical scavenging activity of the ethanolic fraction (the half-maximal inhibitory concentration of 42.84 ± 0.81 µg/mL) indicated its strong activity, which was almost the same as in the case of the positive control, synthetic antioxidant butylhydroxytoluene (the half-maximal inhibitory concentration of 36.61 ± 0.79 µg/mL). Gram-positive bacteria (Staphylococcus aureus, Enterococcus faecalis, and Bacillus cereus) were more sensitive to the ethanolic fraction compared to Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Shigella sonnei). The obtained results indicated the possibility of the further use of the ethanolic fraction as a fertilizer for plant growth in different species and antifouling agents, applicable in aquaculture.

Cholinesterase Inhibition and Antioxidative Capacity of New Heteroaromatic Resveratrol Analogs: Synthesis and Physico-Chemical Properties.

The targeted compounds in this research, resveratrol analogs 1-14, were synthesized as mixtures of isomers by the Wittig reaction using heterocyclic triphenylphosphonium salts and various benzaldehydes. The planned compounds were those possessing the trans-configuration as the biologically active trans-resveratrol. The pure isomers were obtained by repeated column chromatography in various isolated yields depending on the heteroaromatic ring. It was found that butyrylcholinesterase (BChE) was more sensitive to the heteroaromatic resveratrol analogs than acetylcholinesterase (AChE), except for 6, the methylated thiophene derivative with chlorine, which showed equal inhibition toward both enzymes. Compounds 5 and 8 achieved the highest BChE inhibition with IC50 values of 22.9 and 24.8 µM, respectively. The same as with AChE and BChE, methylated thiophene subunits of resveratrol analogs showed better enzyme inhibition than unmethylated ones. Two antioxidant spectrophotometric methods, DPPH and CUPRAC, were applied to determine the antioxidant potential of new heteroaromatic resveratrol analogs. The molecular docking of these compounds was conducted to visualize the ligand-active site complexes' structure and identify the non-covalent interactions responsible for the complex's stability, which influence the inhibitory potential. As ADME properties are crucial in developing drug product formulations, they have also been addressed in this work. The potential genotoxicity is evaluated by in silico studies for all compounds synthesized.

Design, Synthesis and Biological Activity of Novel Methoxy- and Hydroxy-Substituted N-Benzimidazole-Derived Carboxamides.

This work presents the design, synthesis and biological activity of novel N-substituted benzimidazole carboxamides bearing either a variable number of methoxy and/or hydroxy groups. The targeted carboxamides were designed to investigate the influence of the number of methoxy and/or hydroxy groups, the type of substituent placed on the N atom of the benzimidazole core and the type of substituent placed on the benzimidazole core on biological activity. The most promising derivatives with pronounced antiproliferative activity proved to be N-methyl-substituted derivatives with hydroxyl and methoxy groups at the phenyl ring and cyano groups on the benzimidazole nuclei with selective activity against the MCF-7 cell line (IC50 = 3.1 µM). In addition, the cyano-substituted derivatives 10 and 11 showed strong antiproliferative activity against the tested cells (IC50 = 1.2-5.3 µM). Several tested compounds showed significantly improved antioxidative activity in all three methods compared to standard BHT. In addition, the antioxidative activity of 9, 10, 32 and 36 in the cells generally confirmed their antioxidant ability demonstrated in vitro. However, their antiproliferative activity was not related to their ability to inhibit oxidative stress nor to their ability to induce it. Compound 8 with two hydroxy and one methoxy group on the phenyl ring showed the strongest antibacterial activity against the Gram-positive strain E. faecalis (MIC = 8 µM).

Quality Evaluation of Lonicerae Flos Produced in Southwest China Based on HPLC Analysis and Antioxidant Activity.

Lonicera macranthoides, the main source of traditional Chinese medicine Lonicerae Flos, is extensively cultivated in Southwest China. However, the quality of L. macranthoides produced in this region significantly varies due to its wide distribution and various cultivation breeds. Herein, 50 Lonicerae Flos samples derived from different breeds of L. macranthoides cultivated in Southwest China were collected for quality evaluation. Six organic acids and three saponin compounds were quantitatively analyzed using HPLC. Furthermore, the antioxidant activity of a portion of samples was conducted with 2,2'-Azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) and 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging experiments. According to the quantitative results, all samples met the quality standards outlined in the Chinese Pharmacopoeia. The samples from Guizhou, whether derived from unopened or open wild-type breeds, exhibited high quality, while the wild-type samples showed relatively significant fluctuation in quality. The samples from Chongqing and Hunan demonstrated similar quality, whereas those from Sichuan exhibited relatively lower quality. These samples demonstrated significant abilities in clearing ABTS and DPPH radicals. The relationship between HPLC chromatograms and antioxidant activity, as elucidated by multivariate analysis, indicated that chlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, and isochlorogenic acid C are active components and can serve as Q-markers for quality evaluation.

High density lipoprotein heterogeneity & function among Indians with coronary artery disease.

Background & objectives: Impaired high density lipoprotein (HDL) functionality has been shown to be associated with cardiovascular disease risk. The study was aimed to identify the alterations in HDL function [antioxidative activity (AOA)] and subfraction distribution between acute coronary syndrome (ACS) and stable coronary artery disease (SCAD) individuals and analysing the accuracy of HDL parameters to discriminate between the groups. Methods: HDL subfraction distribution analysis was performed in 200 coronary artery disease patients (ACS and SCAD) and 60 control individuals using dextran sulphate, heparin and manganese chloride precipitation method. In terms of HDL function, AOA was evaluated by dihydrorhodamine-based fluorescent cell-free assay and paraoxonase (PON1) enzyme paraoxonase and arylesterase activity. Results: We found that higher AOA [odds ratio (95% confidence interval {CI})]: 0.09 (0.02-0.44), P<0.01 for SCAD; 0.008 (0.001-0.07), P<0.001 for ACS and higher PON1 activity [0.22 (0.8-0.59), P<0.01 for SCAD; 0.16 (0.06-0.4), P<0.001 for ACS] were associated with a lower odds of developing coronary artery disease (CAD). AOA of apoB-depleted serum was significantly correlated with HDL2-C/HDL3-C (HDL-cholesterol) ratio in controls (r=-0.31, P=0.01) and ACS (r=-0.18, P=0.04). It was observed that AOA and HDL subfraction distribution together could discriminate between the two groups of CAD with an accuracy of 72.8 per cent (P=0.004). Interpretation & conclusions: Impaired AOA and altered subfraction distribution of HDL may be responsible for its diminished anti-athero protective activity and can discriminate between the two groups of CAD individuals.

Fatty acid metabolism and antioxidant capacity in Gymnocypris przewalskii (Kessler, 1876) response to thermal stress.

The Qinghai-Tibet Plateau is undergoing a wet-warming transition, which could affect the survival of the native fish. However, the tolerance and physiological response to thermal stress is rarely studied in Gymnocypris przewalskii, a rare native fish in the Tibetan plateau. In this study, first, we detected the thermal tolerance of five groups of six-month G. przewalskii which acclimated at 8, 12, 16, 20, and 24 °C for two weeks, respectively, by critical thermal methodology. Then, through heat challenge, we detected the metabolites, key enzyme activities, and gene expressions involved in metabolism and antioxidant in the hepatopancreas when the temperatures increased from 16 °C to 18, 20, 22, 24, 26, and 28 °C for 12 h, respectively. The results showed that although the fish are sensitive to high temperatures, the quick acclimation at mild high temperatures could significantly improve the tolerance to acute high-temperature stress in juvenile G. przewalskii. During the heat challenge study, blood glucose significantly increased at heat stress (P < 0.05). At the same time, total cholesterol (TC), triglyceride (TG), and free fatty acid (FFA) significantly decreased when the temperature rose continuously to 20 °C. Metabolic enzyme activities of carnitine palmityl transferase I (CPT-Ⅰ), acetyl-CoA carboxylase (ACC), and fatty acid synthase (FAS) significantly decreased at 20 °C (P < 0.05). Superoxide dismutase (SOD) and antioxidant capacity (T-AOC) significantly increased at 20 °C (P < 0.05). The relative transcript levels of genes involved in antioxidant and glycolysis/gluconeogenesis were markedly higher than the control at 20-26 °C (P < 0.05). The genes involved in fatty acid biosynthesis or metabolism showed different expression patterns under heat stress. Heat shock protein 70 (Hsp70) and Hsp90 were significantly higher than the control at 18 °C and 26 °C, respectively. These results confirmed the prediction that G. przewalskii is sensitive to high temperatures, so conservation efforts should pay more attention to the warming damage.

Methanol Extracts from Cirsium japonicum DC. var. australe Kitam. and Their Active Components Reduce Intracellular Oxidative Stress in Caenorhabditis elegans.

Cirsium japonicum DC. var. australe Kitam. has been used as an herbal remedy and often involves using the whole plant or roots. However, the bioactivities of different parts of the plant have been far less explored. This study aimed to evaluate the antioxidative ability of methanol extracts from the flowers, leaves, stems, and roots of the Cirsium plant and their possible active components against juglone-induced oxidative stress in the nematode Caenorhabditis elegans. The results showed that the highest dry weight (12.3 g per plant) was observed in leaves, which was followed by stems (8.0 g). The methanol extract yields from the flowers, leaves, and roots were all similar (13.0-13.8%), while the yield from stems was the lowest (8.6%). The analysis of the silymarin contents in the extracts indicated that the flowers, leaves, stems, and roots contained silychristin and taxifolin; however, silydianin was only found in the leaves, stems, and roots. The flower, leaf, and stem extracts, at a concentration of 10 mg/L, significantly reduced juglone-induced oxidative stress in C. elegans, which was potentially due to the presence of silychristin and taxifolin. Overall, C. japonicum DC. var. australe Kitam. contains a significant amount of silymarin and exhibits in vivo antioxidative activity, suggesting that the prospects for the plant in terms of health supplements or as a source of silymarin are promising.

Antioxidant and Antiproliferative Activities of Kale (Brassica oleracea L. Var. acephala DC.) and Wild Cabbage (Brassica incana Ten.) Polyphenolic Extracts.

Brassicaceae are rich in healthy phytochemicals that have a positive impact on human health. The aim of this study was to analyze the phenolic compounds and antioxidant and anticancer potential of traditional Croatian kale (Brassica oleracea L. var. acephala DC.) and wild cabbage (Brassica incana Ten.) extracts. The phenolic groups and antioxidant activity were determined by spectrophotometry, selected phenolic compounds (ferulic acid, sinapic acid, salicylic acid, kaempferol, and quercetin) were analyzed by LC-MS/MS, and anticancer potential was evaluated in vitro using HeLa cells. The extracts of both plant species are rich in phenolic compounds and showed significant antioxidant activity at similar levels. LC-MS/MS detected sinapic acid as the most abundant phenolic acid, followed by ferulic acid, while salicylic acid was present at lower concentrations. A comparative analysis showed that wild cabbage contained significantly more sinapic acid, while kale contained more kaempferol and quercetin. Both Brassica extracts at a concentration of 50 µg mL-1 showed an antiproliferative effect on HeLa cells, while they did not affect the proliferation of normal human skin fibroblasts. Wild cabbage extract also showed an antiproliferative effect on HeLa cells at a lower applied concentration of 10 µg mL-1 of extracts. The clonogenic analysis also revealed the inhibitory effect of the extracts on HeLa colony growth.

Composition and Antioxidative and Antibacterial Activities of the Essential Oil from Farfugium japonicum.

The composition of volatile oils of the leaf and stem of Farfugium japonicum (L.) Kitamura were prepared by supercritical fluid extraction (SFE)-CO2. A total 47 and 40 compounds were identified by GC/MS analysis, respectively, and only 13 compounds coexisted. The main constituent types in the leaf oil included alcohols (34.1%), hydrocarbons (24.1%), terpenoids (16.2%), benzenes (7.5%), and fatty acids (4.9%). In the stem oil, the constituent types chiefly included benzenes (18.8%), ketones (13.9%), terpenoids (17.0%), fatty acids (8.8%), phenolics (8.7%), steroids (8.6%), hydrocarbons (8.0%), and esters (5.7%). The predominant volatile compounds in the stem were 2-(1-cyclopent-1-enyl-1-methylethyl) cyclopentanone (11.7%), 1,2,3,4,5,6,7,8-octahydro- 9,10-dimethyl-anthracene (8.4%), 5-heptylresorcinol (6.5%), and α-sitosterol (5.2%). Those in the leaf mainly included (E)-3-hexen-1-ol (13.7%) and (Z)-3-hexen-1-ol (14.0%). This demonstrated a significant difference in the composition of both oils. Further study showed that stem oils demonstrated the highest DPPH (1,1-diphenyl-2-pinylhydrazyl) and ·OH free radical scavenging capacities at IC50 values of 9.22 and 0.90 mg/mL, respectively. In addition, they demonstrated the strongest antibacterial capacity against the Gram-positive bacteria methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus (MRSA) at a minimum inhibitory concentration (MIC) of 0.16 mg/mL. This could be due to the SFE-CO2 extraction and the high accumulation of benzenes, terpenoids, and phenolics in the stem. In particular, the monoterpenes presented in terpenoids could play a special role in these findings.

The Health-Promoting and Sensory Properties of Tropical Fruit Sorbets with Inulin.

Inulin is a popular prebiotic that is often used in the production of ice cream, mainly to improve its consistency. It also reduces the hardness of ice cream, as well as improving the ice cream's organoleptic characteristics. Inulin can also improve the texture of sorbets, which are gaining popularity as an alternative to milk-based ice cream. Sorbets can be an excellent source of natural vitamins and antioxidants. The aim of this study was to evaluate the effect of the addition of inulin on the sensory characteristics and health-promoting value of avocado, kiwi, honey melon, yellow melon and mango sorbets. Three types of sorbets were made­two with inulin (2% and 5% wt.) and the other without­using fresh fruit with the addition of water, sucrose and lemon juice. Both the type of fruit and the addition of inulin influenced the sorbet mixture viscosity, the content of polyphenols, vitamin C, acidity, ability to scavenge free radicals using DPPH reagent, melting resistance, overrun and sensory evaluation of the tested sorbets (all p < 0.05). The addition of inulin had no impact on the color of the tested sorbets, only the type of fruit influenced this feature. In the sensory evaluation, the mango sorbets were rated the best and the avocado sorbets were rated the worst. Sorbets can be a good source of antioxidant compounds. The tested fruits sorbets had different levels of polyphenol content and the ability to scavenge free radicals. Kiwi sorbet had the highest antioxidant potential among the tested fruits. The obtained ability to catch free radicals and the content of polyphenols proved the beneficial effect of sorbets, particularly as a valuable source of antioxidants. The addition of inulin improved the meltability, which may indicate the effect of inulin on the consistency. Further research should focus on making sorbets only from natural ingredients and comparing their health-promoting quality with the ready-made sorbets that are available on the market, which are made from ready-made ice cream mixes.

Beyond Traditional Use of Alchemilla vulgaris: Genoprotective and Antitumor Activity In Vitro.

Alchemilla vulgaris L. (lady's mantle) was used for centuries in Europe and Balkan countries for treatments of numerous conditions and diseases of the reproductive system, yet some of the biological activities of lady's mantle have been poorly studied and neglected. The present study aimed to estimate the potential of A. vulgaris ethanolic extract from Southeast Serbia to prevent and suppress tumor development in vitro, validated by antioxidant, genoprotective, and cytotoxic properties. A total of 45 compounds were detected by UHPLC-HRMS analysis in A. vulgaris ethanolic extract. Measurement of antioxidant activity revealed the significant potential of the tested extract to scavenge free radicals. In addition, the analysis of micronuclei showed an in vitro protective effect on chromosome aberrations in peripheral human lymphocytes. A. vulgaris extract strongly suppressed the growth of human cell lines derived from different types of tumors (MCF-7, A375, A549, and HCT116). The observed antitumor effect is realized through the blockade of cell division, caspase-dependent apoptosis, and autophagic cell death. Our study has shown that Alchemilla vulgaris L. is a valuable source of bioactive compounds able to protect the subcellular structure from damage, thus preventing tumorigenesis as well as suppressing tumor cell growth.

Antioxidant and Antimicrobial Activities of Thai Edible Plant Extracts Prepared Using Different Extraction Techniques.

This study investigated the antioxidant and antimicrobial activities of six Thai edible plant leaf extracts, including Cashew (CN), Chamuang (CM), Monpu (MP), Thurianthet (TT), Kradon (KD) and Pakliang (PL), extracted using ethanol extraction (EE), microwave-assisted extraction (MAE), and ultrasonic-assisted extraction (UAE). The leaf extracts were characterized for percentage yield, total phenolic content (TPC), total flavonoid content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) and-ferric reducing antioxidant power (FRAP) activity, and antimicrobial activity against spoilage. MAE produced the highest percentage yields, among which MAE-extracted MP exhibited the highest yield. Furthermore, the highest TPC and TFC were obtained for MAE, with MAE-extracted KD and CN showing the highest TPC and TFC, respectively, among the samples. The highest DPPH and FRAP values were seen in MAE-processed CN, KD, and MP extracts. The inhibition zone of pathogenic bacteria, minimum inhibitory concentration, and minimum bacterial concentration were determined in all samples except TT. These findings indicate that, compared to EE and UAE, MAE improved the antioxidant and antimicrobial efficacy of the leaf extracts. The aforementioned extracts could be employed as natural food additives to prevent chemical and microbial spoilage of foods.

A New 1,3-Benzodioxole Compound from Hypecoum erectum and Its Antioxidant Activity.

The purpose of this study was to identify the chemical components in aerial parts of Hypecoum erectum. A new 1,3-benzodioxole derivative, identified as Hypecoumic acid (1), was isolated, together with the three known compounds: protopine (2), coptisine (3), and cryptopine (4). Their structures were identified based on extensive spectroscopic experiments, including nuclear magnetic resonance (NMR) and high-resolution electrospray ionization mass spectra (HR-ESI-MS), as well as comparison with those reported in the literature. Meanwhile, the in vitro antioxidative activity of all compounds was determined using a DPPH-scavenging assay, and compound 1 (IC50 = 86.3 ± 0.2 µM) was shown to have moderate antioxidative activity.

Effect-Directed Profiling of Strawberry Varieties and Breeding Materials via Planar Chromatography and Chemometrics.

Strawberries are an important fruit in the European diet because of their unique taste and high content of essential nutrients and bioactive compounds. The anthocyanins are known to be colorful phenolics in strawberries. In 17 samples of six strawberry cultivars produced in Serbia, i.e., the common varieties Alba, Asia, and Clery as well as promising breeding materials (11.29.11, 11.34.6, and 11.39.3), the anthocyanin profile as well as antimicrobial and antioxidative activity profiles were determined. All investigated extracts showed antioxidative and antibacterial activities against Gram-negative Aliivibrio fischeri. The responses were quite similar in number and intensity. The HPTLC-DPPH• scavenging assay and HPTLC-Aliivibrio fischeri bioassay coupled with high-resolution mass spectrometry identified pelargonidin-3-O-glucoside (Pg-3-glc) as the main anthocyanin and prominent antioxidative and antimicrobial compound in strawberries. The density functional theory calculations at the M06-2X/6-31+G(d,p) level showed that Pg-3-glc quenches free radicals via sequential proton loss electron transfer mechanism in water and in pentyl ethanoate, where the 5-OH group is the most reactive site for proton and hydrogen atom transfer. The results were confirmed via spectrophotometry. The highest total phenolic content was found in Clery and 11.39.3, while statistically significant differences between the genotypes regarding the antioxidant activity were not confirmed. Although very similar in the anthocyanin, antioxidative, and antimicrobial profile patterns, the strawberry genotypes were successfully classified using principal component analysis.

Beneficial Effects of Laurel (Laurus nobilis L.) and Myrtle (Myrtus communis L.) Extract on Rat Health.

Polyphenols of Laurel and Myrtle exhibit structural diversity, which affects bioavailability, metabolism, and bioactivity. The gut microbiota plays a key role in modulating the production, bioavailability and, thus the biological activities of phenolic metabolites, particularly after the intake of food containing high-molecular-weight polyphenols. The aim of this study was to investigate whether the polyphenolic components of Laurel and Myrtle aqueous extract have beneficial effects on rat health. The growth of lactic acid bacteria (LAB), ß-glucuronidase, ß-glucosidase, ß-galactosidase activity, pH value, body weight change and food efficacy ratio after intragastric treatment of rats with Laurel and Myrtle extract at doses of 50 and 100 mg/kg for two weeks were investigated. The endogenous populations of colonic probiotic bacteria (Lactobacilli and Bifidobacteria) were counted on selective media. According to the obtained data, Laurel extract in the applied dose of 50 and 100 and Myrtle extract (100 mg/kg) positively affects the rats health by increasing the number of colonies of Lactobacilli and Bifidobacteria compared to the control group, causes changes in glycolytic enzymatic activity and minor change in antioxidative tissue activity. In addition, high doses of Laurel increase food efficiency ratio, while Myrtle has the same effect at a lower dose.

Antioxidative capacity of fresh kombucha cheese fortified with sage herbal dust and its preparations.

Recent studies have intensively investigated the possibility of kombucha application as non-conventional starter culture in manufacture of various fermented dairy products. Furthermore, natural extracts from medicinal and aromatic plants contain different biologically active components which often have antioxidant properties. Based on the stated above, the aim of this research was to investigate the possibility of kombucha inoculum application as a new starter culture in fresh cheese technology, as well as to investigate effects of sage (Salvia officinalis) herbal dust (by-product from filter tea factory), its essential oil and supercritical fluid extract on antioxidative activity and sensory characteristics of produced fresh kombucha cheese during 10 days of storage. In all samples, higher ABTS than DPPH radical scavenging activity was determined. Freshly prepared and 10 days stored kombucha cheeses fortified with different types of sage preparations had significantly higher FRAP values than the control sample. All analysed samples had satisfied sensory characteristics and same scores of sensory evaluation after the production. Kombucha fresh cheese with addition of different types of sage preparations can be an innovative and valuable dairy product.

The Changes in Antioxidant Activity of Selected Flavonoids and Caffeine Depending on the Dosage and Form of Thiamine.

Phenolic compounds and thiamine may serve as therapies against oxidative stress-related neurodegenerative diseases. However, it is important to note that these components show high instability under changing conditions. The study's aim was to determine the impact of the thiamine concentration (hydrochloride-TH and pyrophosphate-TP; in the range 0.02 to 20 mg/100 g on the indices of the chelating properties and reducing power, and free radicals scavenging indices of EGCG, EGC, ECG and caffeine added from 0.04 to 6.0 mg/100 g. Our research confirmed that higher concentrations of TH and TP can exhibit significant activity against the test antioxidant indices of all components. When above 5.0 mg/100 g of thiamine was used, the radical scavenging abilities of the compound decreased in the following order: EGCG > ECG > EGC > caffeine. The highest correlation was found for the concentration of thiamine pyrophosphate to 20.0 mg/100 g and EGCG. Knowledge of the impact of factors associated with the concentration of both EGCG, EGC, ECG or caffeine and thiamine on their activity could carry weight in regulating the quality supplemented foods, especially of nutrition support for people of all ages were oral, enteral tube feeding and parenteral nutrition).

Akt Phosphorylates NQO1 and Triggers its Degradation, Abolishing Its Antioxidative Activities in Parkinson's Disease.

The oxidative metabolism of dopamine and consequent oxidative stress are implicated in dopaminergic neuronal loss, mediating the pathogenesis of Parkinson's disease (PD). The inducible detoxifying antioxidative enzyme Quinone oxidoreductase (NQO1) (NAD(P)H: quinone oxidoreductase 1), neuroprotective to counteract reactive oxidative species, is most prominent in the active stage of the disease and virtually absent at the end stage of the disease. However, the molecular mechanism dictating NQO1 expression oscillation remains unclear. Here we show that Akt phosphorylates NQO1 at T128 residues and triggers its polyubiquitination and proteasomal degradation, abrogating its antioxidative effects in PD. Akt binds NQO1 in a phosphorylation-dependent manner. Interestingly, Akt, but not PINK1, provokes NQO1 phosphorylation and polyubiquitination with Parkin as an E3 ligase. Unphosphorylatable NQO1 mutant displays more robust neuroprotective activity than WT NQO1 in suppressing reactive oxidative species and against MPTP-induced dopaminergic cell death, rescuing the motor disorders in both α-synuclein transgenic transgenic male and female mice elicited by the neurotoxin. Thus, our findings demonstrate that blockade of Akt-mediated NQO1 degradation may ameliorate PD pathogenesis.SIGNIFICANCE STATEMENT Dopaminergic neurodegeneration in Parkinson's disease (PD) is associated with the imbalance of oxidative metabolism of dopamine. Quinone oxidoreductase (NQO1), a potent antioxidant system, its expression levels are prominently increased in the early and intermediate stages of PD and disappeared in the end-stage PD. The molecular modification behavior of NQO1 after it is upregulated by oxidative stress in the early stage of PD, however, remains unclear. This study shows that Akt binds and phosphorylates NQO1 at T128 residue and promotes its ubiquitination and degradation, and Parkin acts as an E3 ligase in this process, which affects the antioxidant capacity of NQO1. This finding provides a novel molecular mechanism for NQO1 oscillation in PD pathogenesis.