Polyphenolic profile and in vitro biological activity of Serbian orange (skin fermented white) wines.

Orange wines are made from white grapes, but with prolonged skin contact during fermentation. Available data on their composition and potential health benefits are limited, so polyphenolic profile (HPLC analysis) and in vitro biological activities (enzyme inhibition, antioxidant, and anti-inflammatory) of 24 Serbian orange wines were analyzed, including the correlation between determined composition and bioactivities. The wines displayed distinct polyphenolic profiles, enabling partial differentiation based on overall polyphenol content, including dominant components (catechin, gallic and caffeic acids), along with occasional occurrences of anthocyanins. However, no discernible distinctions were noted based on grape varieties, vintage, or producer. All twenty-four orange wines showed a reasonable inhibition of digestive enzymes and lipid peroxidation, twenty-one samples reduced ROS generation in the cell-based assay, but only two suppressed both PGE2 and TXA2 production in U937 cells, implicating possible functional food properties. No significant correlation between polyphenolic profile and determined biological activities was noticed.

Elemental Profile and Health Risk of Fruska Gora Wines.

The elemental composition of wine is influenced by endogenous sources and interventions from winemakers. The ICP-MS analysis of Fruska Gora wines (113) from vintages spanning across a decade (2011-2020), produced by 30 wineries and representing 18 autochthonous and international wine varieties, allowed a comprehensive insight into their elemental composition. Based on the mean concentrations of 23 investigated elements, B, Fe, and Mn, which were determined in mg per L of wine regardless of its colour or origin, were the most abundant. Red and white wines showed significant concentration differences in the case of B, Mn, and Sr (higher in red) as well as Be, Al, V, As, Mo, and Pb (higher in white). The elements of the highest toxicological concern were found in all (Pb and As) or almost all of the samples (Cd and Hg). Pb levels (maximum 47.1, 61.6, and 73.2 µg/L in red, rose, and white, respectively) were well below the legal limit. The applied risk assessment approaches (hazard quotient and index, margin of exposure) revealed no health concerns associated with consumption of Fruska Gora wines, except for a slightly increased lifetime cancer risk in the case of high wine consumption, and thus supported the promotion of Fruska Gora wines in the highly competitive international market.

Could elderberry fruits processed by modern and conventional drying and extraction technology be considered a valuable source of health-promoting compounds?

The influence of drying and extraction processes on the phytochemical composition and biopotential of elderberry is challenging for the food industry. For this reason in this research two drying techniques (lyophilization and natural convection) and three extraction techniques (ultrasound (UAE), microwave (MAE), and conventional (maceration (MAC)) was applied using two"green" solvents (water and 50 % ethanol). Results of the research showed that lyophilization was a better way of drying than natural convection, while MAE extraction was the most efficient technique for the isolation of secondary metabolites. The most abundant phenolic compounds established by LC-MS/MS analysis, were chlorogenic acid and rutin, identified in extracts of lyophilized elderberries. Elderberry extracts achieved great antioxidant (CUPRAC: 2.30-5.13 mg TE/mL) and enzyme inhibitor potential (α-amylase: 0.51-8.34 mg ACAE/mL). The results suggest that elderberry is a rich natural source of bioactive compounds and could be used for the future development of dietary supplements and functional foods.

Plantain (Plantago L.) species as modulators of prostaglandin E2 and thromboxane A2 production in inflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: Worldwide distributed plantains (genus Plantago L.) are extensively used in the traditional, but some of them are also accepted in the modern medicine. Wide range of usages is mainly connected to the inflammation processes. AIM OF THE STUDY: To support usage of renowned P. lanceolata L. and P. major L., underinvestigated P. altissima L., P. argentea Chaix, P. holosteum Scop. and P. media L. methanol extracts, and their typical constituents (aucubin, apigenin, apigenin-7-O-glucoside, luteolin, luteolin-7-O-glucoside, chlorogenic and ursolic acid) in treatment of inflammation disorders, we conducted study on plantain potential to inhibit production of inflammatory mediators, prostaglandin E2 (PGE2) and thromboxane A2 (TXA2). MATERIALS AND METHODS: LPS-stimulated monocytes (U937 cell line) were used as a model-system to examine anti-inflammatory potential of plantains and their constituents. Produced PGE2 and TXA2 were quantified by LC-MS/MS; qPCR was applied to examine related gene (PLA2, COX-1, COX-2, mPGES-1, mPGES-2, cPGES, TXAS) expression; LC-MS/MS and LC-UV/VIS techniques to analyze extracts composition. RESULTS: In general, examined plantain extracts showed comparable inhibition activity of PGE2 and TXA2 production as aspirin at low-dose concentration. Underinvestigated P. altissima can be pointed out, since it exerted the strongest effect on both PGE2 production and related gene expression. Notable suppression of TXA2 production by P. lanceolata and P. major was observed. But, PCA analysis showed no obvious grouping, implicating that different mechanisms of action are responsible for each sample activity. In most cases, positive correlation was found between content of apigenin and ursolic acid and extracts suppression of PGE2 and TXA2 production and related genes expression. CONCLUSIONS: P. altissima can be regarded as promising anti-inflammatory agent, while novel aspect of P. lanceolata and P. major application (anti-aggregation) can be suggested. P. argentea and P. media could be considered as a good source of ursolic acid.

Elderberry (Sambucus nigra L.) juice as a novel functional product rich in health-promoting compounds.

The medicinal herbs of the Balkan Peninsula are highly represented in traditional medicine. The connection between traditional and modern life and health is reflected in the creation of new food products with added value. In this study, the plant species Sambucus nigra L. was used to obtain freshly pressed juice, whose chemical composition and various biological activities were evaluated. The most abundant compounds were phenolic acids: protocatechuic and chlorogenic acid, as well as flavonoids: quercetin-3-O-hexoside, quercetin, and rutin. The analyzed juice was very rich in total phenolic compounds (1945 mg GAE per mL juice), and a significant anthocyanin concentration was observed (30.85 mg Cy-3-GE per mL juice). Bioactivity testing revealed that elderberry juice was an extremely potent agent in the process of neutralizing NO free radicals (53.06 g TE per L juice), while in reducing over-enzyme activity, the best result was achieved in the inhibition of tyrosinase enzyme (54.70 mg KAE per g of juice).

The Effects of Trifluoromethylated Derivatives on Prostaglandin E2 and Thromboxane A2 Production in Human Leukemic U937 Macrophages.

BACKGROUND: A convenient approach to modulation of the inflammation has an influence on the production of inflammatory mediators - icosanoids, generated in arachidonic acid (AA) metabolism. The common therapeutic activity of non-steroidal anti-inflammatory drugs (NSAID), such as aspirin, includes inhibition of two crucial enzymes of AA metabolism - cyclooxygenase- 1 and -2 (COX-1/2), with certain risk for gastrointestinal and renal intolerance. Ever since the enrolment of COX-2, particularly overabundance of its main products prostaglandin E2 (PGE2) and thromboxane A2 (TXA2) in numerous pathological processes was recognized, it became a significant therapeutic target. OBJECTIVE: The aim of this study was to examine the effects of synthesized organo-fluorine compounds on PGE2 and TXA2 production in the inflammation process. METHODS: Trifluoromethyl compounds were synthesized from N-benzyl trifluoromethyl aldimine, commercially available 2-methyl or 2-phenyl α-bromo esters (ß-lactams trans-1 and trans-2 and trifluoromethyl ß-amino ester, respectively) and methyl 2-isocyanoacetate (2-imidazoline trans-4). The reactions proceeded with high geometric selectivity, furnishing the desired products in good yields. The influence of newly synthesized compounds on PGE2 and TXA2 production in human leukemic U937 macrophages on both enzyme activity and gene expression levels was observed. RESULTS: Among the tested trifluoromethyl compounds, methyl trans-1-benzyl-5-(trifluoromethyl)- 4,5-dihydro-1H-imidazole-4-carboxylate (trans-4) can be distinguished as the most powerful antiinflammatory agent, probably due to its trifluoromethyl-imidazoline moiety. CONCLUSION: Some further structural modifications in tested compounds and particularly in the synthesis of different trifluoromethyl imidazolines could contribute to the development of new COX-2 inhibitors and potent anti-inflammatory agents.

Activity profiling of Serbian and some other European Merlot wines in inflammation and oxidation processes.

Merlot are worldwide recognized red wines. Several studies show that red wines have health benefits, mainly due to their phenolic constituents. This study evaluates twelve Serbian and other five European (French, Italian, Macedonian, Slovenian, Spanish) Merlot wines in respect of their phenolic composition and biological activity. The latter was evaluated through a set of in vitro experiments related to common benefits of moderate red wine consumption in the prevention of cardiovascular diseases. Among the examined phenolics, the most abundant acid in all samples was the gallic acid (14.3-58.3 mg/L), catechin (9.1-49.3 mg/L) was the dominant flavonoid, malvidin-3-O-glucoside (2.63-66.5 mg/L) leading anthocyanin, whereas resveratrol was found in a usual concentration (0.18-4.67 mg/L). Differences determined in phenolic profiles, mainly in content of quercetin, rutin and p-coumaric acid, leaded to separation of Serbian from foreing Merlot wines. Results of standard antioxidant assays (DPPH•, ABTS•+ and •NO scavenger capacity reducing power (FRAP), lipid peroxidation) revealed French Merlot as the most potent, but also pointed out some Serbian samples. The correlation between the content of dominant phenolics and antioxidant activity was sporadic, but samples with the highest overall phenolic content, generally had higher antioxidant potential. Concentration of wines and number of cells in ant-inflammatory assay were chosen to mimic in vivo conditions. So, the potency of examined wines to decrease the production of macrophage-derived PGE2 and TXA2 (up to 65.5 and 47.9%, respectively), could be considered as in vitro evidence of positve health effect. Regarding the phenolic content and anti-inflammatory contribution of the most abundant compounds, no correlation was witnessed. In general, this study showed interesting potential of Serbian Merlot wines, comparable to health-promoting effects of renewed Eurepean ones.

Phytochemical composition and in vitro functional properties of three wild rose hips and their traditional preserves.

The aim of the present study was investigation of the phenolic profile, ascorbic acid content, antioxidant, anti-acetylcholinesterase, anti-inflammatory and cytotoxic activity of rose hips and the preserves (purée and jam) of three insufficiently examined Rosa species: Rosa dumalis Bechst., R. dumetorum Thuill. and R. sempervirens L. The liquid chromatography-tandem mass spectrometry analysis resulted in quantification of 14 of the 45 phenolic compounds examined, with ellagic acid as the most dominant. Notable antioxidant activity of all three species was confirmed through several assays. Moderate inhibition of acetylcholinesterase by extracts of all investigated Rosa species was observed. Several extracts of examined Rosa species demonstrated inhibition potency towards production of some monitored eicosanoids in cyclooxygenase-1 and 12-lipoxygenase pathways. Two R. sempervirens extracts exerted cytotoxic activity against HeLa and HT-29 cell lines, but were inactive towards MRC-5 and MCF7. The results support the potential of these rose hips as food with health-promoting properties.