Dihydroquercetin and biochaga reduce H2O2 induced DNA damage in peripheral blood mononuclear cells of obese women in vitro-a pilot study.

Systemic oxidative stress stemming from increased free radical production and reduced antioxidant capacity are common characteristics of obese individuals. Using hydrogen peroxide (H2O2) to induce DNA damage in vitro, in peripheral blood mononuclear cells (PBMCs) from obese subjects and controls, the DNA protective ability of dihidroqercetin (DHQ) and biochaga (B) alone or in combination, were evaluated. The effects of DHQ and B were estimated under two experimental conditions: pre-treatment, where cells were pre-incubated with the substances prior to H2O2 exposure; and post-treatment when cells were first exposed to H2 H2O2, and further treated with the compounds. DNA damage was evaluated using the comet assay. The results of pre- and post-treatment showed a significant decrease in DNA damage produced by H2O2 in the obese group. This decrease was not significant in control group probably due to a small number of subjects in this pilot study. More prominent attenuation was noted in the pre-treatment with DHQ (250 µg/mL). Analysis of antioxidant properties revealed that DHQ's remarkable reducing power, 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging activity, and potent ∙OH scavenging properties may contribute to strong attenuation of H2O2 induced DNA damage. Also, B showed strong reducing power, DPPH, and ∙OH scavenging ability, while reducing power and DPPH scavenger effects were increased in the presence of DHQ. Conclusively, DHQ and B may reduce H2O2-induced DNA damage in PBMCs from obese subjects when challenged in vitro, and could be valuable tools in future research against oxidative damage-related conditions.

New caffeoyl derivatives with potent DPPH radical scavenging activity from Elephantopus tomentosus.

Eight new caffeoyl derivatives, elephantomentosides A-H (1 - 8), together with ten known ones (9 - 18), were isolated from the whole plant of Elephantopos tomentosus L. Their structures were elucidated using detailed spectroscopic analysis. Structurally, compounds 1 - 8 are composed of ß-D-glucopyranose, and almost all of the substituent positions are at the C-1' and C-4' of glucopyranose. The anti-inflammatory and antioxidant activities of all isolated compounds were evaluated in vitro. Compounds 9-10, 13-15, and 17-18 exhibited significant DPPH scavenging capacity with IC50 values in the range of 10.01-25.07 µM, in comparison with Vc (IC50, 17.98 µM).

Fullerene C60 Conjugate with Folic Acid and Polyvinylpyrrolidone for Targeted Delivery to Tumor Cells.

The use of targeted drug delivery systems, including those based on selective absorption by certain receptors on the surface of the target cell, can lead to a decrease in the minimum effective dose and the accompanying toxicity of the drug, as well as an increase in therapeutic efficacy. A fullerene C60 conjugate (FA-PVP-C60) with polyvinylpyrrolidone (PVP) as a biocompatible spacer and folic acid (FA) as a targeting ligand for tumor cells with increased expression of folate receptors (FR) was obtained. Using 13C NMR spectroscopy, FT-IR, UV-Vis spectrometry, fluorometry and thermal analysis, the formation of the conjugate was confirmed and the nature of the binding of its components was established. The average particle sizes of the conjugate in aqueous solutions and cell culture medium were determined using dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA). The FA-PVP-C60 showed antiradical activity against •DPPH, •OH and O2•-, but at the same time, it was shown to generate 1O2. It was found that the conjugate in the studied concentration range (up to 200 µg/mL) is non-toxic in vitro and does not affect the cell cycle. To confirm the ability of the conjugate to selectively accumulate through folate-mediated endocytosis, its uptake into cells was analyzed by flow cytometry and confocal microscopy. It was shown that the conjugate is less absorbed by A549 cells with low FR expression than by HeLa, which has a high level of expression of this receptor.

Effects of Drying Methods on the Antioxidant Properties of Piper betle Leaves.

Piper betle leaf powder is increasingly utilised as a health supplement. In this study, P. betle leaves were subjected to four different drying methods: convective air-drying, oven-drying, sun-drying, and no drying, with fresh leaves as control. Their antioxidant properties were then evaluated using colourimetric assays and GC-MS. Results showed that the sun-dried leaves had the highest (p < 0.05) total antioxidant capacity (66.23 ± 0.10 mg AAE/g), total polyphenol content (133.93 ± 3.76 mg GAE/g), total flavonoid content (81.25 ± 3.26 mg CE/g) and DPPH radical scavenging activity (56.48 ± 0.11%), and the lowest alkaloid content (45.684 ± 0.265 mg/gm). GC-MS analysis revealed that major constituents of aqueous extracts of fresh and sun-dried P. betle leaves were hydrazine 1,2-dimethyl-; ethyl aminomethylformimidate; glycerin; propanoic acid, 2-hydroxy-, methyl ester, (+/-)-; and 1,2-Cyclopentanedione. In conclusion, sun-dried leaves exhibited overall better antioxidant properties, and their aqueous extracts contained biologically active phytoconstituents that have uses in various fields.

An enhanced productivity of pink oyster mushroom with improved nutritional profile, characterization and attempt for commercial exploitation.

BACKGROUND: An attempt has been made to explore the nutritional profile of pink oyster mushrooms that have been grown in various agricultural residues, including sugarcane bagasse, rice straw, coconut coir and sawdust, along with other nutrient supplements such as defatted mustard and chickpea powder, for appropriate growth and fruiting body formation in a short span of time. The spawn production was experimented with five different grain varieties. The study became interesting when the observations differed slightly from the traditional practices, with the addition of defatted mustard supplements resulting in a positive correlation with respect to reducing the fruiting time, as well as improving yield and the nutritional profile of Pleurotus djamor. RESULTS: An elevated yield of 651.93 g kg-1 was recorded in the medium where the RS and DM were used in the ratio of 1:0.01 (rice straw +1% w/w defatted mustard) bag, whereas, in terms of protein content, a maximum yield of 32.57 ± 0.79 mg g-1 was observed when SB:DM was in the same ratio (sugarcane bagasse +1% w/w defatted mustard) bag. CONCLUSION: To confer the best outcomes from the screened substrates, a series of experiments were performed by varying the concentration of RS and SB, with 1% w/w DM. It is worth noting that the highest protein content of 32.76 ± 0.38 mg g-1 was obtained along with the total yield of 702.56 ± 2.9 g kg-1 of mushroom when the ratio of RS:SB was 0.7:0.3. © 2024 Society of Chemical Industry.

Development and evaluation of a vacuum impregnation system for enhancement of biochemical properties of food materials.

Vacuum impregnation is a novel methodology for adding various substances to porous foods. This study aimed to develop a cost effective automate system for vacuum impregnation of food materials to enhance their nutritional, functional and sensory properties depending on the functionality of the impregnation solution. The developed vacuum impregnation system includes a vacuum chamber, vacuum pump and an automation setup for creating and maintaining vacuum conditions, feeding impregnated solutions to the samples and releasing vacuum. Fresh-cut spinach leaves were impregnated with ascorbic acid (AsA) and calcium chloride (Cacl2) (10% concentration) in the setup in order to test the effect of the process on some biochemical properties. Statistical analysis revealed significant effect of vacuum impregnation on the biochemical properties (total soluble solids, total phenolic content, flavonoid content and free radical scavenging activity) and color of spinach leaves during storage up to 4 days. Impregnation process showed significant increase in the total phenolic and flavonoid content of the spinach leaves. Increment up to 78% in antioxidant activity was seen for the uncoated impregnated leaves as compared to 59% activity in untreated samples. Thus, products with desired parameters can be produced with this process with minimal impact on their properties at a lower cost and in a shorter time period.

3,4-Dihydroxybenzalacetone Inhibits the Propagation of Hydrogen Peroxide-Induced Oxidative Effect via Secretory Components from SH-SY5Y Cells.

The polyphenol derivative 3,4-dihydroxybenzalacetone (DBL) is the primary antioxidative component of the medicinal folk mushroom Chaga (Inonotus obliquus (persoon) Pilat). In this study, we investigated whether the antioxidative effect of DBL could propagate to recipient cells via secreted components, including extracellular vesicles (EVs), after pre-exposing SH-SY5Y human neuroblastoma cells to DBL. First, we prepared EV-enriched fractions via sucrose density gradient ultracentrifugation using conditioned medium from SH-SY5Y cells exposed to 100 µM hydrogen peroxide (H2O2) for 24 h, with and without 1 h of 5 µM DBL pre-treatment. CD63 immuno-dot blot analysis demonstrated that fractions with density of 1.06-1.09 g/cm3 had CD63-like immuno-reactivities. Furthermore, the 2,2-diphenyl-1-picrylhydrazyl assay revealed that the radical scavenging activity of fraction 11 (density of 1.06 g/cm3), prepared after 24-h H2O2 treatment, was significantly increased compared to that in the control group (no H2O2 treatment). Notably, 1 h of 5 µM DBL pre-treatment or 5 min of heat treatment (100 °C) diminished this effect, although concentrating the fraction by 100 kDa ultrafiltration enhanced it. Overall, the effect was not specific to the recipient cell types. In addition, the uptake of fluorescent Paul Karl Horan-labeled EVs in concentrated fraction 11 was detected in all treatment groups, particularly in the H2O2-treated group. The results suggest that cell-to-cell communication via bioactive substances, such as EVs, in conditioned SH-SY5Y cell medium, propagates the H2O2-induced radical scavenging effect, whereas pre-conditioning with DBL inhibits it.

Ultrasonic-Assisted Extraction of Astaxanthin from Shrimp By-Products Using Vegetable Oils.

BACKGROUND: The use of conventional astaxanthin extraction methods, typically involving organic solvents, leads to a heightened environmental impact. The aim of this study was to explore the potential use of environmentally friendly extraction solvents, such as vegetable oils, for recovering the shrimp by-product astaxanthin. METHODS: Ultrasound-assisted extraction (UAE) in vegetable oils, including olive oil (OO), sunflower oil (SO), and flaxseed oil (FO), was employed to extract astaxanthin. The astaxanthin antioxidant activity was evaluated using an ABTS assay, and a mixture of gum Arabic and soy lecithin was used to form coacervates to produce astaxanthin encapsulation. RESULTS: A by-product-vegetable oil ratio of 1:60, extraction time of 210 min, 60% amplitude of the extraction process, and the use of OO as the extracting medium resulted in an astaxanthin yield of 235 ± 4.07 µg astaxanthin/g by-products. The astaxanthin encapsulation efficiency on day 0 and astaxanthin recovery on day 1 were recorded at 66.6 ± 2.7% and 94.4 ± 4.6%, respectively. CONCLUSIONS: The utilization of OO as an extraction solvent for astaxanthin from shrimp by-products in UAE represents a novel and promising approach to reducing the environmental impact of shrimp by-products. The effective astaxanthin encapsulation efficiency highlights its potential application in food industries.

Phenolic Compounds from the Fruits of Prunus davidiana (Rosaceae) and Their Antioxidant Activities.

This research was supported by Cooperative Research Program for Agriculture Science & Technology Development (Project No. PJ014204032019) and the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (NRF-2020R1A6A3A01100042).

Chemometric study for the performances of deep eutectic solvents during the recovery of high-added-value substances from Moringa oleifera leaves: Principal component analysis.

INTRODUCTION: Moringa oleifera is a plant with high antioxidant content in its leaves, flowers and seeds. It attracts the attention of researchers with the effect of its nutritional and medical advantages. OBJECTIVE: The purpose of the current study is to propose a deep eutectic solvent (DES)-based ultrasound-assisted extraction of bioactive substances from M. oleifera leaves by the application of a chemometric study. METHODOLOGY: A total of 18 different choline chloride-based DESs were prepared by using several hydrogen bond donors (glucose, sucrose, glycerol, ethylene glycol, urea and dimethyl urea) with various molar ratios (1:1, 1:2 and 2:1) by addition of diluents (water and 50% methanol) or alone. In order to decide the best DES combination, principal component analysis (PCA) was applied. The response surface method (RSM) was used as statistical experimental design approach through the Box-Behnken design. RESULTS: The best phenolic (TPC), flavonoid (TFC) and antioxidant activity yields of M. oleifera leaf extract were found to be 19.102 mg-GAE, 10.47 mg-CE and 24.404 mg-TEAC per gram dried leaf under the optimal conditions (50% water content, 20% amplitude, 15 min time). The model fitting has been also found reliable depending on the statistical indicators such as p-value (<0.0001), coefficients of determination (R2 = 0.9827, 0.9916 and 0.9864) and root mean square error (RMSE = 1.0562, 2.4656 and 0.7713). CONCLUSIONS: A chemometric study through PCA was carried out to determine the similarities and differences between the solvent groups, and the ethylene glycol-based DES (1:2, molar ratio) with the addition of water showed the best performance.

Investigation on Antioxidant Activity and Different Metabolites of Mulberry (Morus spp.) Leaves Depending on the Harvest Months by UPLC-Q-TOF-MS with Multivariate Tools.

The changes in active components in mulberry leaves harvested in different months and their antioxidant activities were investigated. Ultra-high-performance liquid chromatography-tandem quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) with multivariate statistical tools was used to investigate the chemical constituents in the extracts of mulberry leaves. The results indicated that mulberry leaves were rich in phenolic acids, flavonoids, organic acids, and fatty acid derivatives. In addition, 25 different compounds were identified in the different batches of mulberry leaves. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity was measured to evaluate the in vitro antioxidant activities of mulberry leaves. Among the four batches, batch A, harvested in December, exhibited the strongest DPPH radical-scavenging activity, while batch B, harvested in March, showed the weakest activity. This was related to the total phenolic content in the mulberry leaves of each batch. The optimal harvest time of mulberry leaves greatly influences the bioactivity and bioavailability of the plant.

Phenolic Compound Profile and Antioxidant Capacity of Flax (Linum usitatissimum L.) Harvested at Different Growth Stages.

The profile of phenolic compounds changes during the growth of a plant and this change affects its antioxidant potential. The aim of this research has been to find the growth stage of flax with the highest antioxidant capacity, and to determine the phenolic compounds responsible for such a capacity. Flax was harvested in six growth stages: from stem extension to mature seeds. The phenolic compounds were identified using LC-TOF-MS and quantified in an extract and in the fresh matter (FM) of each growth stage. The radical scavenging activity against ABTS•+ and DPPH•, the ferric-reducing antioxidant power (FRAP), and the antioxidant activity in the ß-carotene-linoleic acid emulsion system were determined. Mono- and di-C-glycosyl flavones were found to be the most abundant phenolics of the aerial parts of flax, which also showed the highest content of isoorientin (210-538 µg/g FM). Coniferin, its derivative, and hydroxycinnamic acid derivatives were also detected. The plant was richer in flavone C-glycosides from stem extension to seed ripening (1105-1413 µg/g FM) than at the mature seed stage (557 µg/g FM). Most of the individual flavone C-glycoside contents in the extracts decreased when increasingly older plants were considered; however, the isoorientin content did not change significantly from the steam extension to the seed ripening stages. The antiradical activity against ABTS•+ and FRAP was higher for the aerial parts of the flax harvested at the flowering, brown capsule, and seed ripening stages, mainly due to the presence of flavone C-glycosides. The oxidation of ß-carotene-linoleic acid emulsion was instead inhibited more effectively by the extracts from plants at the brown capsule and mature seed stages. Coniferin and its derivative were significantly involved in this activity. The extracts from the aerial parts of the flax harvested from flowering to seed ripening could be a valuable source of flavone C-glycosides for use as nutraceuticals and components of functional foods.

Fabrication and characterization of nanoemulsions for encapsulation and delivery of vitexin: antioxidant activity, storage stability and in vitro digestibility.

BACKGROUND: Nanoemulsions were prepared as an encapsulation and delivery system for vitexin, a poorly water-soluble antioxidant. This study evaluated how the type and concentration of the dispersed oil phase and vitexin loading impacted droplet characteristics and nanoemulsion stability. The influences of storage temperature on antioxidant activity and in vitro gastrointestinal digestion on nanoemulsion stability were also investigated. RESULTS: Nanoemulsions prepared at different dispersed oil concentrations showed diverse characteristics and stability. Highest stability against droplet aggregation and phase separation with small oil droplets (< 150 nm) was observed for nanoemulsions prepared using 300 g kg-1 medium-chain triglyceride oil. These nanoemulsions are able to entrap and deliver vitexin with high encapsulation efficiency (88-90%) with no significant effect on emulsion stability. Vitexin-loaded nanoemulsions were stable during storage when refrigerated (4 °C) and at room temperature (25 °C) for up to 45 days with no effect on their antioxidant activity. Significantly delayed lipolysis rate and decreased extent of lipid digestion were observed in vitexin-loaded nanoemulsions. CONCLUSIONS: Stable vitexin-loaded nanoemulsions were successfully produced by high-pressure homogenization using a mixture of Tween 80 and lecithin as emulsifiers. Vitexin-loaded nanoemulsions stabilized with a mixture of these two emulsifiers were effective in retaining antioxidant activity during storage and protecting vitexin from changes during gastrointestinal digestion. Our results suggested that nanoemulsions were effective vitexin delivery systems for food applications. © 2022 Society of Chemical Industry.

The dose-response relationships of the direct scavenging activity of amide-based local anesthetics against multiple free radicals.

This study aimed to illustrate the dose-response relationships of the direct scavenging activity of amide-based local anesthetics against multiple free radicals in vitro. We have demonstrated that amide-type local anesthetics selectively and directly scavenge some free radicals. Three kinds of free radicals were eliminated by all the four local anesthetics examined. Mepivacaine, lidocaine, bupivacaine, and dibucaine scavenged hydroxyl radicals in dose-dependent manners. Ascorbyl free radicals were also scavenged in dose-dependent manners, and lastly singlet oxygen was scavenged in dose-dependent manners. Three other free radicals were not scavenged by all of the four local anesthetics; tert-butoxyl radical was scavenged by all the anesthetics examined but dibucaine, nitric oxide by mepivacaine but not by the other three, and tyrosyl radical by mepivacaine and lidocaine but not by the other two. Some free radicals (superoxide anion, tert-butyl peroxyl radical, DPPH) were not scavenged by any of the four local anesthetics. The local anesthetics were also shown to inhibit lipid peroxidation by TBARS assay. These results suggest that local anesthetics have antioxidant properties through their free radical scavenging activities.

Retardation of oxidative rancidity in ghee adding orange peel powder at different storage temperature.

This study is aimed to determine and compare the antioxidant activity of Orange Peel Powder (OPP) in ghee at different temperatures (4 °C, 25 °C and 60 °C) for divergent storage periods (0, 7, 14 and 21 days). To compare the antioxidant potentiality, synthetic antioxidant BHA (Butylated Hydroxy Anisole) is used. Twelve ghee samples were prepared where one was control, another one was BHA treated and the rest ten were admixing OPP in ghee at different ratios. After sensory evaluation three highest scored ghee samples (0.5%. 1.0% and 1.5%) were selected. Samples were analyzed for peroxide (PV), thiobarbituric acid (TBA), free fatty acids (FFA) value and radical scavenging activity. Though storage temperature and storage period were increased OPP treated ghee samples peroxide, TBA and FFA values were lowered significantly compared to control samples. Moreover, 1.0% and 1.5% OPP treated ghee samples such values were lowered than BHA treated ghee samples and all these are on the favor of ghee quality. OPP treated ghee samples' DPPH quench potentiality is also stronger than BHA treated ghee samples. Therefore, OPP is a great source of antioxidants and this can be used in ghee as a natural source of antioxidants.

Screening of secondary metabolites and antioxidant potential of endophytic fungus Penicillium citrinum and host Digitaria bicornis by spectrophotometric and electrochemical methods.

Perennial grasses are hosts to an extremely diverse assemblage of endophytic fungi, but their significance is still underexplored. In the present study, an endophytic fungus was isolated from the aerial regions of Digitaria bicornis (Lam.) Roem. & Schult. and was characterized by morphological and molecular methods (ITS rDNA region), as Penicillium citrinum Thom. The crude extracts of endophytic fungus and host were recovered and evaluated for their antioxidant potential by spectrophotometric and electrochemical methods. The present study was also an attempt to compare the anti-radical power of extracts by spectrophotometric (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), hydrogen peroxide and nitric oxide radical scavenging assay) and electrochemical (cyclic voltammetry) methods and suggested that cyclic voltammetry could be used routinely instead of assaying by more number of spectrophotometric methods. The results indicated that the ethyl acetate extract of P. citrinum and methanolic extract of D. bicornis has potential compounds with antioxidant and other pharmaceutical activities. Nine and 17 antioxidant biomolecules, respectively, in P. citrinum and D. bicornis extracts were detected by OHR-LC-MS and the presence of function group of the bioactive compounds was confirmed by FTIR spectroscopy. Finally, the study also reported that the extracts of P. citrinum and D. bicornis have several bioactive compounds with application in commercial pharmaceutical industries.

Influence of Oxidation and Dialysis of Phlorotannins on Bioactivity and Composition of Ultrasound-Assisted Extracts from Ascophyllum nodosum.

The isolation and chemical characterization of phlorotannins has gained special attention in recent years due to their specific health-promoting benefits. Flow-cell ultrasound-assisted extraction (90 W/cm2 of sonication power, 2 min of retention time and 20 g solvent/g algae of liquid-solid ratio) was carried out by using double-distilled water (WE) and acetone:water mixture (AWE) as extraction solvents. The AWE showed a higher total polyphenols content (TPC), carbohydrates (CHOs) and antioxidant activities than WE. However, when the WE was purified by using Amberlite XAD16 column, the purified WE (PWE) showed similar a TPC, decreased CHOs and increased antioxidant activity compared to WE. The oxidation of the PWE extract was evaluated under natural, forced and severe oxidation condition for 120 h. Only severe oxidation conditions were able to significantly reduce TPC and antioxidant activities. PWE was dialyzed (20, 10, 3.5 and 2 kDa). The main bioactive fraction of phlorotannins was obtained from 10 to 20 kDa. CHOs were distributed in fractions below 20 kDa. MALDI-TOF analysis was performed for PWE, PD20 and PD2 extracts to analyze the degree of polymerization of phlorotannins, which ranged from 4 to 17 phloroglucinol units/molecule. Fragmentation patterns allowed the proximate identification of several phlorotannins in Ascophyllum nodosum extracts.

Phenolics, Flavonoids Content and Antioxidant Activities of Tuber indicum at Different Maturity Stages.

The Chinese black truffle Tuber indicum (Ascomycota, Pezizales) is an ectomycorrhizal fungus forming hypogeous edible ascocarps. As a famous wild edible mushroom in the world, this species also attracted an increasing interest in their chemical composition and pharmacological activity. In this study, the total phenolic content, total flavonoid content and antioxidant activities of Tuber indicum collected from July to November at different maturity stages in China were analyzed. Our results showed that T. indicum collected in July (immature stage) possessed the highest amount of flavonoids (3.89 mg/g dw) and the highest ABTS.+ scavenging activity (EC50 =3.73 mg/ml). In addition, those samples collected in August (moderate mature stage) contained the highest phenolics content (4.78 mg/g dw), the highest DPPH⋅ radical scavenging activity (EC50 =3.73 mg/ml) and ferric reducing activity power (243.63 µmol FeSO4 /g). The study reveals T. indicum in the early maturity stage yield significantly higher content of phenolics and flavonoids and possessed stronger antioxidant activity than those collected in other months. This study provided important data for understanding the relationship between maturity stages and truffle formation and evaluating the quality of Chinese black truffle at different maturity.

Bioactive Metabolites of Microalgae from Canary Islands for Functional Food and Feed Uses.

Three freshwater microalgae (Spirogyra sp., Cosmarium sp., and Cosmarium blytii) collected from several locations in Gran Canaria have been studied to explore their potential as a novel source of bioactive compounds for biotechnological applications. Soluble carbohydrates were quantified after extraction with 3 M HCl at 100 °C, ranging from 35.8 to 43.3 %, and with water at room temperature, ranging from 19 to 22.8 %. Amino acids glutamic acid, proline and aspartic acid were quantified by RP-HPLC. Glutamic acid was the most abundant, ranging from 12.2 to 3.63 mg g-1 of dry biomass. Cosmarium blytii was the richest sample in amino acids (24.02 mg g-1 of dry weight). In addition, Cosmarium blytii and Spyrogira sp. exhibited higher radical scavenging activity (RSA) against 1,1-diphenyl-2-picrylhydrazyl (DPPH) than that of the synthetic antioxidant butylhydroxytoluene (BHT), commonly used as food additive. These results show a great potential of these microalgae for exploitation in the food, feed and pharmaceutical industries.

Тhio-containing pteridines: Synthesis, modification, and biological activity.

The present article is devoted to searching for biologically active agents among novel thio-containing pteridines. Synthetic protocols based on the condensation of 5,6-diamino-2-thioxo-2,3-dihydropyrimidin-4(1H)-ones with dicarbonyl compounds were elaborated and used for the synthesis of target products. The directions for further modification of the obtained thio-containing pteridines were substantiated and realized. The spectral properties of the obtained compounds were studied and described. The results of the in silico study revealed that the predicted affinity of the obtained compounds to the dihydrofolate reductase (DHFR) active site is comparable with the affinity of methotrexate, despite the differences in the nature of the ligand-enzyme interactions. The in vitro study of DHFR-inhibiting activity revealed that the most active compounds 3.9 and 4.2 have lg IC50 values of -5.889 and -5.233, respectively, significantly inferior to methotrexate (lg IC50 = -7.605). Additionally, the synthesized compounds were studied for their antiradical activity as a possible mechanism of pharmacological effects. Among the obtained pteridines, compounds 5.1 (lg EC50 = -4.82) and 5.3 (lg EC50 = -4.92) have antiradical activity higher than the reference compound ascorbic acid (lg EC50 = -4.81). The conducted structure-activity relationship analysis provided valuable data for the further search for biologically active agents among thio-containing pteridines and related compounds.