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The trend towards alternative medicine and naturopathy increases the interest in the use of natural products. This requires larger quantities of qualitative raw material of medicinal plants, including the well-known genus Echinacea. The purpose of this study was to evaluate the quality of E. purpurea and pallida cultivated in Kazanlak, Bulgaria. We developed and validated a rapid, reliable, and inexpensive HPLC method for the quantitative determination of chicoric, caftaric, and caffeic acids, and of cynarin, echinacoside, quercetin, and apigenin. The amount of chicoric and caftaric acids was monitored in different phases of plant development in aerial parts and roots. Maximal concentrations of chicoric acid (3.4%) were reported in roots in the seed-formation phase, and a concentration of 2.8% was reported in aerial parts in the vegetative phase. Caftaric acid was 0.9% in aerial parts in the vegetative and flowering phases and 0.5% in roots in the vegetative and seeding phases. Their amounts significantly exceed the requirements of the European Pharmacopoeia 8.0. Therefore, Kazanlak-grown E. purpurea could be a reliable raw material for the formulation of phytopreparations. In addition, the proposed method was applied to the detection and determination of the above-described substances in phytopreparations containing Echinacea from commercial sources. The amounts of the tested substances were found to vary widely. [ABSTRACT FROM AUTHOR]

Simple Summary: Cognitive deficits, including spatial working and recognition memory impairment, are a common feature of Alzheimer's disease with current therapies offering limited efficacy. Marrubium vulgare, a member of the Lamiaceae family, has shown potential to alleviate spatial memory impairment in a model of experimental dementia in rats through its antioxidant and acetylcholinesterase inhibitory activities. The aim of this study was to examine the effect of M. vulgare on recognition memory in healthy and dementia-affected rats after 21 days of oral administration. Memory performance was evaluated by the novel object recognition test. Levels of neurotransmitters acetylcholine, noradrenaline (NA), and serotonin, as well as the protein expression of the brain-derived neurotrophic factor (BDNF) and the phosphorylation of the cAMP response element-binding protein (p-CREB), were measured. The expression levels of BDNF and CREB were evaluated via RT-PCR in the cortex and hippocampus. Our result revealed that M. vulgare ameliorated recognition memory impairment in dementia rats by preserving cholinergic function in the hippocampus, increasing NA levels in the brain, and restoring pCREB expression in the cortex following their reduction in the experimental model used. In healthy rats, the extract upregulated the expression of BDNF and pCREB in the cortex. These findings suggest that M. vulgare has potential as a therapeutic agent for cognitive impairments in various neurodegenerative diseases. The potential of Marrubium vulgare to alleviate scopolamine (Sco)-induced deficits in spatial working memory has drawn considerable scientific interest. This effect is partly attributed to its potent antioxidant and acetylcholinesterase inhibitory (AChEI) activities. This study examined the effects of M. vulgare extract, standardized to marrubiin content, on recognition memory in healthy and Sco-treated rats. Male Wistar rats (200–250 g) were divided into four groups. The extract was orally administered for 21 days and Sco (2 mg/kg) was intraperitoneally injected for 11 consecutive days. Memory performance was assessed using the novel object recognition test. Levels of acetylcholine (ACh), noradrenaline (NA), serotonin (Sero), and brain-derived neurotrophic factor (BDNF) and the phosphorylation of cAMP response element-binding protein (p-CREB) were evaluated in the cortex and hippocampus via ELISA. BDNF and CREB expression levels were assessed using RT-PCR. The results showed that M. vulgare significantly alleviated Sco-induced memory impairment, preserved cholinergic function in the hippocampus, increased NA levels in the brain, and restored pCREB expression in the cortex following Sco-induced reduction. In healthy rats, the extract upregulated BDNF, pCREB, and Bcl2 expression. Our findings indicate that the neuroprotective effects of M. vulgare may be linked to the modulation of cholinergic function, regulation of NA neurotransmission, and influence on key memory-related molecules. [ABSTRACT FROM AUTHOR]

Sambucus nigra L. (S. nigra, SN) or black elder is a traditional medicinal plant widely used worldwide for therapeutic and dietary purposes. The aim of the current study was to investigate the anti-inflammatory and antinociceptive activities of black elder fruit and flower extracts (SNFrE and SNFlE, respectively). The primary polyphenol constituents in the flower extract were flavonoids and phenolic acids, while anthocyanins were the main components in the fruit extract. SNFrE revealed pronounced and dose-dependent in vivo anti-inflammatory activity assessed by the cotton pellet-induced granuloma test. Doses of 10, 20, and 50 mg/kg BW of SNFrE reduced the weight of induced granuloma in rats by 20.3%, 20.5%, and 28.4%, respectively. At the highest dose (50 mg/kg BW), SNFrE had significant (p < 0.01) anti-inflammatory activity comparable to that of diclofenac, the reference compound used (10 mg/kg BW). In addition, the in vivo antinociceptive activity of the extracts in mice was estimated using the acetic-acid-induced writhing test. Both extracts at doses of 50 mg/kg BW inhibited the abdominal contractions induced by the acetic acid significantly comparing to the control group (p < 0.01). Our findings indicate that black elder extracts and particularly SNFrE possess anti-inflammatory and antinociceptive activities, providing experimental evidence for the use of S. nigra in traditional medicine. [ABSTRACT FROM AUTHOR]

Sideritis scardica Griseb. and Clinopodium vulgare L., belonging to the Lamiaceae family, are rich in terpenoids and phenolics and exhibit various pharmacological effects, including antioxidant, anti-inflammatory and anti-cancer activities. While the memory-enhancing impacts of S. scardica are well documented, the cognitive benefits of C. vulgare remain unexplored. This study assessed the potential effect of C. vulgare on learning and memory in healthy and scopolamine (Sco)-induced memory-impaired male Wistar rats, comparing it with the effects of S. scardica. Over a 21-day period, rats orally received extracts of cultivated S. scardica (200 mg/kg) and C. vulgare (100 mg/kg), either individually or in combination, with administration starting 10 days before and continuing 11 days simultaneously with Sco injection at a dose of 2 mg/kg intraperitoneally. The results showed that both extracts effectively mitigated Sco-induced memory impairment. Their combination significantly improved recognition memory and maintained monoaminergic function. S. scardica excelled in preserving spatial working memory, while C. vulgare exhibited comparable retention of recognition memory, robust antioxidant activity and acetylcholinesterase inhibitory activity. The extracts alleviated Sco-induced downregulation of p-CREB/BDNF signaling, suggesting neuroprotective mechanisms. The extract combination positively affected most of the Sco-induced impairments, underscoring the potential for further investigation of these extracts for therapeutic development. [ABSTRACT FROM AUTHOR]

Sideritis scardica Griseb. is a critically endangered Balkan endemic species, known for its antioxidant, neuroprotective and anti-inflammatory properties. The aim of the present study was to detail an efficient protocol for the micropropagation of S. scardica. In vitro cultures were initiated from the shoot tips of 40 days-old in vivo seedlings and the effects of different plant growth regulator treatments were examined. A Murashige and Skoog nutrient medium (MS) containing 1 mg/L zeatin and 0.1 mg/L indole-3-acetic acid (IAA) proved to be the most efficient for shoot multiplication as it produced quality, vigorous shoots with a mean number of six shoots per explant. For the first time, the antioxidant and antitumor activities of extracts from in vitro-obtained plants were evaluated. In vitro cultivated plants grown in the field revealed a higher total polyphenol content (3929.1 ± 112.2 mg GAE/100 g vs. 3563.5 ± 52.8 mg GAE/100 g) and higher ORAC antioxidant activity (1211.6 ± 27.3 µmol TE/g vs. 939.9 ± 52.4 µmol TE/g) than in situ cultivated plants. A comparison of the antitumor activities of extracts from in vitro propagated shoots, field-grown in vitro-obtained plants and in situ plants on HeLa (cervical adenocarcinoma), HT-29 (colorectal adenocarcinoma) and MCF-7 (breast cancer) human cancer cell lines showed that in vitro propagated shoots had a significant concentration-dependent cytotoxic effect on the cervical adenocarcinoma cell line HeLa, while the field-grown in vitro-obtained and in situ-collected samples induced the highest reduction in the viability of the mammary carcinoma cell line MCF-7. In both cases, the cells of the control non-tumor cell line, BALB/3T3, were significantly less affected. The results showed that the in vitro multiplication protocol ensured the obtainment of numerous plants with antioxidant and antitumor potential. [ABSTRACT FROM AUTHOR]

Sambucus nigra (SN) and Sambucus ebulus (SE) are widely used in folk medicine, primarily as antiviral agents for colds and influenza. In the current study, the antiviral activity of extracts of SN and SE fruits, flowers, and leaves were tested against herpes simplex virus type-2 (HSV-2). The HPLC analysis of the investigated extracts revealed the presence of phenolic acids, flavonoids, and anthocyanins. Rutin and chlorogenic acid were the main polyphenol constituents in flower and leaf extracts, whereas anthocyanins were predominant in fruit extracts. The flower extract of SN was characterized by the highest content of rutin and chlorogenic acid—14,232.1 mg/100 g dry weight (DW) and 7086.7 mg/100 g DW, respectively. SN fruit extract revealed the highest antioxidant activity measured using ORAC and HORAC methods—11,443.1 μmol TE/g and 8198.9 μmol GAE/g, respectively. To evaluate cytotoxicity, antiviral, and virucidal activities against HSV-2, the MTT assay and method of Reed and Muench were used. The least toxic extracts were PSNFrE and PSEFrE. The maximum tolerable concentration (MTC) of PSNFrE was 2000 μg/mL and the calculated CC50 value for that extract was 3570 μg/mL. The inhibitory activity against virus replication was established for three of the extracts—PSNFlE, PSNLE, and PSNFrE. PSEFrE showed neither activity against virus replication, nor virucidal activity. The data suggest a significant inactivation of more than 98% after 60 min of contact of HSV-2 virions with the PSNFrE applied in MTC. The current study provides evidence that Sambucus nigra reveals anti-HSV-2 activity; however, the most active parts of the species were fruits. Therefore, SN fruits and their extracts can be used as an attendant therapy for HSV-2 viral infections. [ABSTRACT FROM AUTHOR]

Plant-based milk alternatives are a fast-growing segment of food industry resulting in the generation of large amounts of by-products, often containing comparable and even higher amounts of valuable phytochemicals than the target products. Common buckwheat (Fagopyrum esculentum M.) Panda variety has been selected for this study, which aims to compare the antioxidant potential of beverages produced from buckwheat whole and dehulled grains, as well as cakes obtained as residues. After combining, evaporating and freeze-drying, extracts were subjected to RP-HPLC-DAD, total phenolics and in vitro antiradical and antioxidant assays (FRAP, ABTS, DPPH and lipid autoxidation). Flavonoids (3.09 mg/100 mL) exceeded the content of phenolic acids (2.35 mg/100 mL) in the beverages prepared from dehulled grains, but their content (1.69 mg/100 mL) in the beverages from whole grains was lower than that of phenolic acids (2.93 mg/100 mL). The antiradical capacity of beverages did not differ significantly, regardless of the method used. In case of by-products, a higher ferric-reducing capacity and scavenging activity towards DPPH• of cakes from whole grains compared to that from dehulled grains was established. The activity of cake extracts under lipid autoxidation conditions increased with the increase in their concentrations from 0.12 wt% to 0.16 wt% in the oxidizable substrate. [ABSTRACT FROM AUTHOR]

This research aimed to reveal the chemical composition of different fractions obtained by sequential extraction of purple coneflower (Echinacea purpurea) roots and to evaluate the antimicrobial activity of some of them. Hexane, chloroform, ethyl acetate, and water were used as solvents to obtain the corresponding extracts. A GC-MS analysis was employed to reveal the chemical composition of hexane, chloroform, and ethyl acetate fractions. Conventional and ultrasound-assisted water extraction was performed to isolate inulin-type polysaccharides. Eighteen microorganisms were used for testing the antimicrobial activity of the obtained organic extracts. From GC-MS analysis more than forty compounds were detected in the fractions, including fatty acids, organic acids, fatty alcohols, sterols, and terpenes. Only in ethyl acetate extract were found mannitol and fructose isomers, while in chloroform extract were detected α- and β-amyrin, and betulin. Ethyl acetate fraction demonstrated the highest antimicrobial activity against 11 microorganisms (Bacillus cereus, B. amyloliquefaciens, Staphylococcus aureus, Listeria monocytogenes, Salmonella enteritis, Escherichia coli, Enterococcus faecalis, Pseudomonas aeruginosa, Candida albicans, Saccharomices cerevisiae, and Peniclium sp.). The polysaccharide fractions were structurally characterized by FT-IR and NMR studies as linear inulin having β-(2→1)-linked Fru units and a T-Glc unit linked α-(1→2). Inulin from coneflower roots showed poor flowability, promising bulk and tapped density, swelling properties, and better oil-holding than water-holding capacity. This study demonstrated the potential of coneflower root fractions as a rich source of phytochemicals with antimicrobial activities and potential prebiotic activity due to inulin content (15% yield) and echinacea root as a useful biobased industrial crop/material. [ABSTRACT FROM AUTHOR]

Featured Application: The present study explores the possibility of the preparation of aromatized wine-type beverages with added byproducts of the essential rose oil industry. The study revealed the opportunity for the production of new wine-type beverages with distinctive and pleasant rose aromas, and enhanced amounts of polyphenols. The potential production of these types of beverages would contribute to both diversification of the wine market and the valorization of byproducts of the essential rose oil industry. While satisfying the customer demand for more versatile natural products, the process is in line with the concept of circular economy, where either zero or minimal waste is generated in human industrial life. The aroma bouquet of wine depends mainly on grape (variety, crop, climate, location, and so on), yeasts/microorganisms, and wine aging. Additionally, the wine flavor can be modulated by adding herbs, extracts, byproducts, and so on. The aim of the present study was to characterize aromatized wine-type beverages (AWTBs) prepared by supplementation with rose oil industry byproducts (ROIBs). Three approaches were employed: 1. dried ROIBs were added to the grape must, followed by fermentation with Saccharomyces cerevisiae (ARW_CoF); 2. dried ROIBs were added to preliminarily prepared rosé (ARW_M); 3. 70% (v/v) ethanolic extracts of ROIBs were added to preliminarily prepared rosé (ARW_E). The polyphenol content in the modified beverages increased significantly from 230.00 ± 5.21 (control) to 296.13 ± 3.57 (ARW_M_100), 295.50 ± 3.78 (ARW_CoF_100), and 293.73 ± 4.29 (ARW_E_400) µmol GAE/L. The addition of ROIBs did not alter the formation of higher alcohols, since their contents in the AWTBs and the control were below 65 mg/L. The amount of phenethyl alcohol increased significantly from 1.07 ± 0.15 mg/L to 4.08 ± 0.30, 4.96 ± 0.24, and 5.77 ± 0.28 mg/L in the ARW_E_400, ARW_M_100, and ARW_CoF_100, respectively. The sensory evaluation revealed a preference for AWTBs from the ARW_CoF series. The results suggested that rose byproducts could be successfully utilized for the preparation of new AWTBs enriched with phenolic antioxidants, while exhibiting a distinctive and pleasant rose aroma. [ABSTRACT FROM AUTHOR]

Common tansy (Tanacetum vulgare L.) is a plant with medicinal properties that has traditionally been used in folk medicine for its anthelmintic, antispasmodic, and choleretic effects, for the treatment of diarrhea and digestive problems, and externally, as an insecticide in veterinary practices. In the current study, we investigated, for the first time, the chemical profile and antioxidant activity of essential oil from a wild population of T. vulgare L. growing in Bulgaria. Common tansy essential oil (EO), which is rich in bicyclic monoterpenes, was obtained using hydrodistillation and characterized by using gas chromatography–mass spectrometry (GC-MS). Thirty-seven compounds were identified in Bulgarian tansy EO. Among the major constituents were oxygenated monoterpenes, including compounds such as camphor (25.24%), trans-chrysantenyl acetate (18.35%), cis-verbenol (10.58%), thujone (6.06%), eucaliptol (5.99%), and α-campholenal (5.98%). The analysis results identified the essential oil from T. vulgare L. grown in the western Rhodope Mountains of Bulgaria as the camphor chemotype. Furthermore, its antioxidant activity was analyzed using the oxygen radical absorbance capacity (ORAC) method and was found to be 605.4 ± 49.3 µmol TE/mL. The essential oil was also tested for single-dose acute toxicity on Wistar rats and was found to be non-toxic by oral administration. The mean lethal dose by intraperitoneal administration was LD50 i.p. = 14.9 g/kg body weight. The results of the conducted study can serve as a basis for the evaluation and subsequent exploration of other pharmacotherapeutic effects of the essential oil obtained from the inflorescences of the Bulgarian species T. vulgare L. [ABSTRACT FROM AUTHOR]

Ensuring the microbiological safety of food products is a pressing global concern. With the increasing resistance of microorganisms to chemical agents and the declining effectiveness of synthetic preservatives, there is a growing need for alternative sources of natural, bioactive compounds with antimicrobial activity. The incorporation of probiotics and plant extracts into food formulations not only enriches foodstuffs with microorganisms and phytochemicals with biologically active compounds, but also provides a means for product preservation. The current review considers the importance of the process of biological preservation for providing safe foods with high biological value, natural origin and composition, and prolonged shelf life, thereby improving consumers' quality of life. To accomplish this goal, this review presents a series of examples showcasing natural preservatives, including beneficial bacteria, yeasts, and their metabolites, as well as phenolic compounds, terpenoids, and alkaloids from plant extracts. By summarizing numerous studies, identifying research challenges and regulatory barriers for their wider use, and outlining future directions for investigation, this article makes an original contribution to the field of biopreservation. [ABSTRACT FROM AUTHOR]

Echinacea purpurea is a perennial plant that belongs to the Asteraceae family. It has a wide range of applications mainly in the treatment and prevention of inflammations in the respiratory system. The current study aimed to perform a phytochemical characterization of purple coneflower (Echinacea purpurea) roots and their extracts (water, 40%, 50%, 60% ethanol, and 60% glycerol). Phytochemical characterization was carried out by gravimetric, spectrophotometric, and chromatographic methods. Echinacea roots were characterized by a low lipid (0.8%) content. In contrast, carbohydrates (45%) and proteins (20%) occupied a large part of the dry matter. Amongst the extracts, the highest yield was obtained using water as a solvent (53%). Water extract was rich in protein and carbohydrates as fructans (inulin) were the most abundant carbohydrate constituent. The most exhaustive recovery of the phenolic components was conducted by extraction with 40% ethanol and 60% glycerol. It was found that water is the most suitable extractant for obtaining a polysaccharide-containing complex (PSC) (8.87%). PSC was composed mainly of fructans (inulin) and proteins with different molecular weight distributions. The yield of PSC decreased with an increasing ethanol concentration (40% > 50% > 60%) but the lowest yield was obtained from 60% glycerol extract. The obtained results showed that Echinacea roots contained a large amount of biologically active substances—phenolic components and polysaccharides and that glycerol was equally efficient to ethanol in extracting caffeic acid derivatives from purple coneflower roots. The data can be used for the preparation of extracts having different compositions and thus easily be incorporated into commercial products. [ABSTRACT FROM AUTHOR]

Clinopodium vulgare L. is a valuable medicinal plant used for its anti-inflammatory, antibacterial and wound-healing properties. The present study describes an efficient protocol for the micropropagation of C. vulgare and compares, for the first time, the chemical content and composition and antitumor and antioxidant activities of extracts from in vitro cultivated and wild-growing plants. The best nutrient medium was found to be Murashige and Skoog (MS) supplemented with 1 mg/L BAP and 0.1 IBA mg/L, yielding on average 6.9 shoots per nodal segment. Flower aqueous extracts from in vitro plants had higher total polyphenol content (29,927.6 ± 592.1 mg/100 g vs. 27,292.8 ± 85.3 mg/100 g) and ORAC antioxidant activity (7281.3 ± 82.9 µmol TE/g vs. 7246.3 ± 62.4 µmol TE/g) compared to the flowers of wild plants. HPLC detected qualitative and quantitative differences in phenolic constituents between the in vitro cultivated and wild-growing plants' extracts. Rosmarinic acid was the major phenolic constituent, being accumulated mainly in leaves, while neochlorogenic acid was a major compound in the flowers of cultivated plants. Catechin was found only in cultivated plants, but not in wild plants or cultivated plants' stems. Aqueous extracts of both cultivated and wild plants showed significant in vitro antitumor activity against human HeLa (cervical adenocarcinoma), HT-29 (colorectal adenocarcinoma) and MCF-7 (breast cancer) cell lines. The best cytotoxic activity against most of the cancer cell lines, combined with the least detrimental effects on a non-tumor human keratinocyte cell line (HaCaT), was shown by the leaf (250 µg/mL) and flower (500 µg/mL) extracts of cultivated plants, making cultivated plants a valuable source of bioactive compounds and a suitable candidate for anticancer therapy. [ABSTRACT FROM AUTHOR]

Rosmarinic acid (RA), an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid, is a potent radical scavenger, a chelator of prooxidant ions, and an inhibitor of lipid peroxidation. RA-containing extracts are widely used natural antioxidants in food products, and many herbal preparations and food supplements, containing RA, are marketed with claims of beneficial health effects. The current study investigated the effectiveness of subcritical water extraction (SWE) for the recovery of RA from lemon balm (Melissa officinalis), as a "green" alternative to conventional hydro-alcoholic extraction. Different durations (10 min and 20 min) and extraction temperatures (100 °C and 150 °C) were applied. Subcritical water applied at a temperature of 100 °C was equally efficient as 50% ethanol in extracting RA. However, the further elevation of temperature to 150 °C decreased RA content by up to 20% due to thermal degradation. The content of RA in dried extracts was between 2.36% and 5.55% and the higher temperature of SWE increased extract yield by up to 41%. The higher extraction yield resulted from the degradation of plant material by subcritical water as evidenced by the increased extraction and degradation of proteins, pectin, and cellulose. These results reveal that SWE is an efficient technology for the extraction of RA and other antioxidants from lemon balm at reduced extraction time and without the use of toxic organic solvents. Furthermore, by modification of SWE conditions, dry extracts with different purity and content of RA are obtained. These extracts could be used in the food industry as food antioxidants, or in the development of food supplements and functional foods. [ABSTRACT FROM AUTHOR]

Gamma irradiation has been applied as an efficient and inexpensive method for the sterilization of nuts for years. However, along with the benefits of such treatment, negative effects are possible because of the formation of reactive oxygen species with a toxic effect on important biologically active substances. Because of the scarce and contradictory information in the literature about gamma-irradiated almonds, the aim of our work was the examination of the lipid changes, antioxidant activity, and oxidative stability of almonds treated by 10 and 25 kGy gamma rays, as well as changes in intensity of the EPR spectra as an indicator for the stability of radiation-induced free radicals. The results revealed no significant differences in the EPR spectra of almonds treated at 10 and 25 kGy doses, neither in their intensity nor in kinetic behaviour. The EPR signals decayed exponentially over 250 days, with a decreasing of central line by 90%, with satellite lines by about 73%. No significant changes in the fat content, fatty acids composition, and acid value of irradiated almonds were observed. However, the amount of (alpha)tocopherols decreased from 292 to 175 mg/kg, whereas the conjugated dienes and trienes increased, K232 from 1.3 to 3 and K268 from 0.04 to 0.15, respectively, with the increasing of irradiation dose. The same was observed for total polyphenols in defatted almonds (1374 to 1520 mg/100 g), where in vitro antioxidant activity determined by ORAC and HORAC methods increased from 100 to 156 µmol TE/g and from 61 to 86 µmol GAE/g, respectively. The oxidative stability of oil decreased from 6 to 4 h at 120 °C and from 24.6 to 18.6 h at 100 °C (measured by Rancimat equipment). The kinetic parameters characterizing the oxidative stability of oil from 10 kGy irradiated almonds were studied before and after addition of different concentrations of ascorbyl palmitate as a synergist of tocopherols. Its effectiveness was concentration-dependent, and 0.75 mM ensured the same induction period as that of non-irradiated nut oil. Further enrichment with alpha-tocopherol in equimolar ratio with palmitate did not improve the oil stability. In conclusion, gamma irradiation is an appropriate method for the treatment of almonds without significant changes in fat content and fatty acids composition. The decreasing of oxidative stability after higher irradiation could be prevented by the addition of ascorbyl palmitate. [ABSTRACT FROM AUTHOR]

1H-benzimidazol-2-yl hydrazones with varying hydroxy and methoxy phenyl moieties were designed. Their effect on tubulin polymerization was evaluated in vitro on porcine tubulin. The compounds elongated the nucleation phase and slowed down the tubulin polymerization comparably to nocodazole. The possible binding modes of the hydrazones with tubulin were explored by molecular docking at the colchicine binding site. The anticancer activity was evaluated against human malignant cell lines MCF-7 and AR-230, as well as against normal fibroblast cells 3T3 and CCL-1. The compounds demonstrated a marked antineoplastic activity in low micromolar concentrations in both screened in vitro tumor models. The most active were the trimethoxy substituted derivative 1i and the positional isomers 1j and 1k, containing hydroxy and methoxy substituents: they showed IC50 similar to the reference podophyllotoxin in both tumor cell lines, accompanied with high selectivity towards the malignantly transformed cells. The compounds exerted moderate to high ability to scavenge peroxyl radicals and certain derivatives—1l containing metha-hydroxy and para-methoxy group, and 1b-e with di/trihydroxy phenyl moiety, revealed HORAC values high or comparable to those of well-known phenolic antioxidants. Thus the 1H-benisimidazol-2-yl hydrazones with hydroxy/methoxy phenyl fragments were recognized as new agents exhibiting promising combined antioxidant and antineoplastic action. [ABSTRACT FROM AUTHOR]

Gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system of mammals and plays an important role in the suppression of neurons' excitability. GABA is formed from the decarboxylation of glutamic acid (Glu), and both GABA and Glu could be considered as important biologically active food components. In the current study, we validated a HPLC method for concomitant detection of GABA and Glu in plant samples after derivatization with dansyl chloride. The validated method had high precision and a high recovery rate and was successfully used for GABA and Glu quantification in 55 plant foods (fruits, vegetables, legumes, cereals, pseudocereals, and nuts) and 19 medicinal plants. Vegetables were the most important dietary source of these amino acids, with the highest quantity of GABA found in potatoes—44.86 mg/100 g fresh weight (FW) and yellow cherry tomatoes—36.82 mg/100 g FW. The highest amount of Glu (53.58 mg/100 g FW) was found in red cherry tomatoes. Analyzed fruits were relatively poor in GABA and Glu, and European gooseberry was the richest fruit with 13.18 mg/100 g FW GABA and 10.95 mg/100 g FW Glu. Cereals, pseudocereals, nuts, and legumes contain much higher amounts of Glu than GABA. The obtained results enrich the available information on the content of gamma-aminobutyric and glutamic acids in plant foods and could be used for the development of GABA-enriched functional foods. [ABSTRACT FROM AUTHOR]

Wort can be used as a basis for functional beverages production because of its content of fibres, antioxidants and vitamins. The biological value of wort depends on the malt used and the mashing regime. Therefore, we investigated the main brewing characteristics (extract, pH, and colour), phenolic compounds content, and antioxidant activity (measured by DPPH, FRAP, CUPRAC, ABTS, and ORAC) of wort, produced by Vienna, Melanoidin, Caramel pils and Special X malt or mixture of them. The results obtained were used for the modelling and optimisation of malt mixture that can be used for the production of functional beverages. Optimisation was made on the basis of wort extract, total phenolic compounds (measured by Folin–Ciocalteu method), and antioxidant activity, measured by DPPH, FRAP, and ORAC methods. Although optimised variants with high content of Special X malt showed highest antioxidant activity, they had an unpleasant taste and slow mash filtration rate. Therefore, the variant with 24.2% Vienna, 51.8% Melanoidin, 20% Caramel pils, and 4% Special X malts was chosen for the production of functional wort-based beverages. [ABSTRACT FROM AUTHOR]

Macrolepiota procera (MP) is an edible mushroom used in the treatment of diabetes, hypertension and inflammation. However, the structure and biological effects of its polysaccharides (PSs) are unclear. This study investigates the structural features of a PS complex from MP (MP-PSC), its immunomodulatory activities and effects on probiotic and pathogenic bacteria. MP-PSC was obtained by boiling water, and PSs were characterized by 2D NMR spectroscopy. The immunomodulatory effects on blood and derived neutrophils, other leukocytes, and murine macrophages were studied by flow cytometry, chemiluminescence, spectrophotometry, and ELISA. The total carbohydrate content of MP-PSC was 74.2%, with glycogen occupying 36.7%, followed by β-D-glucan, α-L-fuco-2-(1,6)-D-galactan, and β-D-glucomannan. MP-PSC (200 μg/mL) increased the number of CD14+ monocyte cells in the blood, after ex vivo incubation for 24 h. It dose-dependently (50–200 μg/mL) activated the spontaneous oxidative burst of whole blood phagocytes, NO, and interleukin 6 productions in RAW264.7 cells. MP-PSC exhibited a low antioxidant activity and failed to suppress the oxidative burst and NO generation, induced by inflammatory agents. It (2.0%, w/v) stimulated probiotic co-cultures and hindered the growth and biofilm development of Escherichia coli, Streptococcus mutans and Salmonella enterica. MP PSs can be included in synbiotics to test their immunostimulating effects on compromised immune systems and gut health. [ABSTRACT FROM AUTHOR]

The current study aimed to determine the major and minor nutritional constituents of Sorbus domestica L. fruits. It was revealed that palmitic acid was the most commonly occurring saturated fatty acid, while linoleic acid represented the major polyunsaturated fatty acid. The sterol fraction consisted mainly of β-sitosterol. Small amounts of lipophilic pigments were quantified. Potassium, iron, and boron were the most abundant macro-, micro-, and ultra-trace elements. The amino acid composition analysis suggested that the non-essential amino acids predominated over the essential ones. Soluble sugars (fructose and glucose) represented a large part of the total carbohydrate content, but pectin formed the major part of polysaccharides. Malic acid was the most abundant organic acid whereas quercetin-3-β-glucoside, neochlorogenic, and 3,4-dihydroxybenzoic acids were the major phenolic constituents. Fruits exhibited free-radical scavenging and protecting ability against peroxyl and hydroxyl radicals. Service tree fruits provided valuable bioactive constituents having a high nutritional value and potential health benefits. [ABSTRACT FROM AUTHOR]

The aim of the study is to evaluate the effect of Aronia melanocarpa fruit juice (AMJ) supplementation on age-related coronary arteries remodeled in aged rat hearts. Male Wistar rats (n = 24) were divided into three groups: (1) young controls (CY), aged 2 months, without AMJ supplementation; (2) old controls (CO), aged 27 months, without AMJ supplementation; and (3) the AMJ group (A), which used 27-month old animals, supplemented orally with AMJ for 105 days. AMJ supplementation did not influence the wall-to-diameter parameter (Kernohan index) of the coronary arteries of test animals. Aged rats supplemented with AMJ showed a significant decrease in the amount of collagen fibers in their coronary tunica media, as compared with the old controls. The intensity of the immunoreaction for alpha smooth muscle actin (αSMA) in the coronary tunica media was significantly lower in the supplemented group than in the old controls. The intensity of the angiotensin-converting enzyme 2 (ACE2) immunoreaction in the coronary tunica media of the supplemented group was significantly higher than the one observed in the old controls. These results indicate the positive effects of AMJ supplementation on the age-dependent remodeling of coronary arteries and support for the preventive potential of antioxidant-rich functional food supplementation in age-related diseases. [ABSTRACT FROM AUTHOR]

Gamma irradiation is efficiently applied to many foods, but nevertheless there is a distinct lack of information about the changes of macro- and micronutrients (e.g., carbohydrates, lipids, organic acids, and phenolics) in dried rose hip (RH) fruits. Therefore, in this study, for the first time, the effect of gamma irradiation (10 and 25 kGy) on RH constituents is investigated. Different analytical techniques (GC-FID, HPLC-UV, HPSEC-RID, IR-FT, and SEM) are employed to examine this effect. The irradiation treatment (10 kGy) increased the glucose content by 30% and released cellobiose from RH fruits, thus revealing cellulose destruction. The extractability of total uronic acids increased from 51% (control) to 70.5% (25 kGy-irradiated), resulting in a higher pectin yield (10.8% < 12.8% < 13.4%) and molecular heterogeneity. Moreover, de-esterification was not a major effect of the irradiation-induced degradation of pectin. The sample exposure to the highest dose did not change the content of total carotenoids, β-carotene, and (un)saturated fatty acids, but it affected the tocopherols levels. Gamma rays had a negligible effect on the phenolic constituents and did not affect ORAC and HORAC antioxidant activity. In conclusion, it can be compromised that the exposition of dried RH is safe and can be successfully applied to decontaminate fruits without affecting their nutritional value and biological activity. [ABSTRACT FROM AUTHOR]

In this study, for the first time, the potential of rose flowers and lavender straw waste biomass was studied as feeding lignocellulose substrates for the cultivation of newly isolated in Bulgaria Ganoderma resinaceum GA1M with the objective of obtaining mycelium-based bio-composites. The chemical characterization and Fourier Transform Infrared (FTIR) spectroscopy established that the proximate composition of steam distilled lavender straw (SDLS) and hexane extracted rose flowers (HERF) was a serious prerequisite supporting the self-growth of mycelium bio-materials with improved antibacterial and aromatic properties. The basic physico-mechanical properties of the developed bio-composites were determined. The apparent density of the mycelium HERF-based bio-composites (462 kg/m³ ) was higher than that of the SDLS-based bio-composite (347 kg/m³ ) and both were much denser than expanded polystyren (EPS), lighter than medium-density fiber board (MDF) and oriented strand board (OSB) and similar to hempcrete. The preliminary testing of their compressive behavior revealed that the compressive resistance of SDLS-based bio-composite was 718 kPa, while for HERF-based bio-composite it was 1029 kPa and both values are similar to the compressive strength of hempcrete with similar apparent density. Water absorbance analysis showed, that both mycelium HERF- and SDLS-based bio-composites were hydrophilic and further investigations are needed to limit the hydrophilicity of the lignocellulose fibers, to tune the density and to improve compressive resistance. [ABSTRACT FROM AUTHOR]

The present study investigates the effect of the addition of medicinal plants, such as lady's mantle, lavender, rosehip, and meadowsweet, on the chemical composition, antioxidant activity, and color intensity of ready-to-drink aronia nectar during pasteurization and long-term storage. Pasteurization caused a significant decrease in anthocyanin content of aronia nectar, which reduced to 20% of the initial value after four months of storage. Herbs provided different protection to aronia anthocyanins that degraded more slowly during the four-month storage compared to pasteurized control without herbs. The addition of medicinal plants enriched aronia nectar with phenolic compounds and increased its antioxidant activity by up to 52% in meadowsweet-aronia nectar. Moreover, it was accompanied by a color intensity magnification due to co-pigmentation of aronia anthocyanins and herbal phenolics. In contrast to anthocyanins, which constantly degraded during the whole period, color intensity began to stabilize after 30 days, demonstrating that co-pigmentation was progressively established during the time and rosehip provided the best stabilization of aronia nectar color. Current research demonstrates for the first time that medicinal plants such as lady's mantle, rosehip, and especially meadowsweet can be used to increase antioxidant activity, color, and anthocyanin stability of black chokeberry functional beverages. [ABSTRACT FROM AUTHOR]

Plant-based foods rich in phenolic phytochemicals are among the promising strategies to counteract age-related changes in lipid profile. Aronia melanocarpa (AM) fruits are a rich source of phenolic compounds possessing lipid-modulating effects. The present study investigated the effect of 3-month supplementation of AM-based functional beverages on the lipid profile of healthy aging rats. Male Wistar rats (n = 40) were separated into five groups: (YC) young controls (2-month-old); (AC) adult controls (13-month-old); (A) adult animals supplemented with pure AM extract; (A + P) adult animals supplemented with pectin-enriched (1%) AM extract; (A + H) adult animals supplemented with AM extract enriched with a herbal mixture. Total cholesterol (TC), triglycerides (TG), HDL-cholesterol (HDL-C), LDL-cholesterol (LDL-C) and atherogenic indices were investigated at the end of the study. Adult controls demonstrated age-related dyslipidemia resulting in decreased HDL-C, and increased TG and TC/HDL index. The supplemented groups showed a significant increase in HDL-C levels: A + P (1.49 mmol/L) and A + H (1.61 mmol/L), respectively, vs. AC (1.09 mmol/L), p < 0.05. The TC/HDL-C and LDL-C/HDL-C indices were decreased in the A + P and A + H groups in comparison to the AC group (p < 0.05). These results indicate that supplementation with polyphenol-rich AM beverages can successfully alter HDL-C levels and this effect is further potentiated by pectin and herbs. [ABSTRACT FROM AUTHOR]

Malt is the main raw material for beer production, which determines not only its taste and aroma profile, but to a large extent its biological value, as well. The aim of the present research was to determine the antioxidant profile of different malt types as a basis for the development of new types of beer with increased antioxidant activity. In the present study the main brewing characteristics, the phenolic profile and the antioxidant potential of 20 malt types used in craft breweries in Bulgaria have been examined. The main brewing characteristics have been determined by the standardized methods of the European Brewing Convention. Malt phenolic content was determined by two methods, and antioxidant potential by five different methods. Based on a statistical factor analysis performed by the principal component analysis, it was confirmed that there was a relationship between malt color and phenolic compounds content. The principal component analysis confirmed that there was a link between the content of the Maillard reaction products and malt biological activity. Malts with the highest degree of heat treatment were characterized by the highest antioxidant activity, which was due to the content of Maillard reaction products with antioxidant capacity. [ABSTRACT FROM AUTHOR]

The current study investigates the content of sugars, organic acids, phenolic acids and flavonoids, as well as antioxidant and antimicrobial activity of Balkan-endemic Micromeria frivaldszkyana. Glucose was the most abundant sugar in the plant (2.77%), followed by fructose (1.18%) and galactose (0.82%). Eight organic acids were detected with quinic acid being in the highest content—556.3 mg/100 g DW. From the individual phenolic acids, rosmarinic acid was found in the most significant amounts (2040.1 ± 1.97 mg/100 g) and hesperidin was the major representative of flavonoids with content 131.2 ± 5.6 mg/100 g DW. The antioxidant activity of the plant was studied by six methods: 2,2′-diphenylpicrylhydrazyl (DPPH)—286.4 ± 10.43 mM TE/g, 2,2′azinobis (3)-ethylbenzthiazoline-6-sulfonic acid (ABTS)—358.4 ± 10.4 mM TE/g, ferric reducing antioxidant power (FRAP)—388.0 ± 32.4 mM TE/g, cupric reducing antioxidant capacity (CUPRAC)—905.6 ± 19.2 mM TE/g, Oxygen Radical Absorbance Capacity (ORAC)—3250.5 ± 208.1 µmol TE/g and Hydroxyl Radical Averting Capacity (HORAC)—306.1 ± 23.5 µmol GAE/g. In vitro antimicrobial activity against nine microorganism was evaluated but the extract displayed antimicrobial activity only against Listeria monocytogenes ATCC 19111 with inhibition zone diameter 9 mm and minimal inhibitory concentration (MIC) 10 mg/mL. [ABSTRACT FROM AUTHOR]

Until now, the interest to plants from genus Scutellaria in Bulgaria has been focused mainly on the terpenes in them. The purpose of this study is to enrich the information on the composition of the Bulgarian Scutellaria species in terms of both polyphenolic content as well as primary metabolites such as mono-, oligosaccharides and organic acids. An aerial part of three Scutellaria species growing in four low mountain regions of Southern Bulgaria was used. The flavonoids scutellarin, baicalin, baicalein, wogonin, wogonoside, luteolin, chrysin and a caffeoyl phenylethanoid glycoside-verbascoside have been identified via HPLC in different extracts from Scutellaria altissima, Scutellaria albida and Scutellaria galericulata. The antioxidant activity of the extracts has been evaluated. The Scutellaria altissima from Mezek and Scutellaria galericulata from Parvenets we studied, which are the richest in flavonoids (represented mainly by baicalin, scutellarin and wogonoside), show the highest Oxygen Radical Absorption Capacity. Hydroxyl Radical Averting Capacity of Scutellaria albida from Mezek and Scutellaria altissima from Bachkovo is the most pronounced, probably due to the content of scutellarin and luteolin and chrysin, respectively. Antioxidant activity of aqueous, methanolic and 70% and 96% ethanol extracts were also determined by the electrochemical method. [ABSTRACT FROM AUTHOR]

1H-benzimidazol-2-yl hydrazones with varying hydroxy and methoxy phenyl moieties were designed. Their effect on tubulin polymerization was evaluated in vitro on porcine tubulin. The compounds elongated the nucleation phase and slowed down the tubulin polymerization comparably to nocodazole. The possible binding modes of the hydrazones with tubulin were explored by molecular docking at the colchicine binding site. The anticancer activity was evaluated against human malignant cell lines MCF-7 and AR-230, as well as against normal fibroblast cells 3T3 and CCL-1. The compounds demonstrated a marked antineoplastic activity in low micromolar concentrations in both screened in vitro tumor models. The most active were the trimethoxy substituted derivative 1i and the positional isomers 1j and 1k , containing hydroxy and methoxy substituents: they showed IC 50 similar to the reference podophyllotoxin in both tumor cell lines, accompanied with high selectivity towards the malignantly transformed cells. The compounds exerted moderate to high ability to scavenge peroxyl radicals and certain derivatives- 1l containing metha -hydroxy and para -methoxy group, and 1b-e with di/trihydroxy phenyl moiety, revealed HORAC values high or comparable to those of well-known phenolic antioxidants. Thus the 1H-benisimidazol-2-yl hydrazones with hydroxy/methoxy phenyl fragments were recognized as new agents exhibiting promising combined antioxidant and antineoplastic action.

Gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the central nervous system of mammals and plays an important role in the suppression of neurons' excitability. GABA is formed from the decarboxylation of glutamic acid (Glu), and both GABA and Glu could be considered as important biologically active food components. In the current study, we validated a HPLC method for concomitant detection of GABA and Glu in plant samples after derivatization with dansyl chloride. The validated method had high precision and a high recovery rate and was successfully used for GABA and Glu quantification in 55 plant foods (fruits, vegetables, legumes, cereals, pseudocereals, and nuts) and 19 medicinal plants. Vegetables were the most important dietary source of these amino acids, with the highest quantity of GABA found in potatoes-44.86 mg/100 g fresh weight (FW) and yellow cherry tomatoes-36.82 mg/100 g FW. The highest amount of Glu (53.58 mg/100 g FW) was found in red cherry tomatoes. Analyzed fruits were relatively poor in GABA and Glu, and European gooseberry was the richest fruit with 13.18 mg/100 g FW GABA and 10.95 mg/100 g FW Glu. Cereals, pseudocereals, nuts, and legumes contain much higher amounts of Glu than GABA. The obtained results enrich the available information on the content of gamma-aminobutyric and glutamic acids in plant foods and could be used for the development of GABA-enriched functional foods.