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A detailed understanding of the stability of an active pharmaceutical ingredient and a pharmaceutical dosage form is essential for the drug-development process and for safe and effective use of medicines. Photostability testing as an inherent part of stability studies provides valuable knowledge on degradation pathways and structures of products generated under UV irradiation. Photostability is particularly important for topically administered drugs, as they are more exposed to UV radiation. Bexarotene is a more recent third-generation retinoid approved by the U.S. Food and Drug Administration and the European Medicines Agency as a topically applied anticancer agent. The present study aimed to assess bexarotene photostability, including the presence of UV filters, which have been permitted to be used in cosmetic products in Europe and the USA. The bexarotene photostability testing was performed in ethanol solutions and in formulations applied on PMMA plates. The UPLC-MS/MS technique was used to determine the tested substance. The presence of photocatalysts such as TiO2 or ZnO, as well as the organic UV filters avobenzone, benzophenone-3, meradimate, and homosalate, could contribute to degradation of bexarotene under UV irradiation. Four photocatalytic degradation products of bexarotene were identified for the first time. The antiproliferative properties of the degradation products of bexarotene were assessed by MTT assay on a panel of human adherent cancer cells, and concentration-dependent growth inhibition was evidenced on all tested cell lines. The cytotoxicity of the formed products after 4 h of UV irradiation was significantly higher than that of the parent compound (p &lt, 0.05). Furthermore non-cancerous murine fibroblasts exhibited marked concentration-dependent inhibition by bexarotene, while the degradation products elicited more pronounced antiproliferative action only at the highest applied concentration.

Objectives This study analyzed the content of substances with cosmetologic properties in the extracts obtained from the mycelial cultures of Ganoderma applanatum, Laetiporus sulphureus, and Trametes versicolor. The effect of these extracts on the inhibition of tyrosinase and hyaluronidase was determined, and their values of sun protection factor (SPF) were calculated. Results The total amount of phenolic acids in the extracts ranged from 2.69 (G. applanatum) to 10.30 mg/100 g dry weight (T. versicolor). The total amount of sterols was estimated at 48.40 (T. versicolor) to 201.04 mg/100 g dry weight (L. sulphureus), and that of indoles at 2.90 (G. applanatum) to 16.74 mg/100 dry weight (L. sulphureus). Kojic acid was determined in the extracts of L. sulphureus and G. applanatum. It was observed that L. sulphureus extract caused dose-dependent inhibition of hyaluronidase, while all the extracts inhibited tyrosinase. The extract of G. applanatum exhibited an SPF value of ~ 9. Conclusions The results showed that the mycelial cultures of the studied species may be used as an alternative source of substances used in cosmetology.

Cordyceps spp. mushrooms have a long tradition of use as a natural raw material in Asian ethnomedicine because of their adaptogenic, tonic effects and their ability to reduce fatigue and stimulate the immune system in humans. This review aims to present the chemical composition and medicinal properties of Cordyceps militaris fruiting bodies and mycelium, as well as mycelium from in vitro cultures. The analytical results of the composition of C. militaris grown in culture media show the bioactive components such as cordycepin, polysaccharides, γ-aminobutyric acid (GABA), ergothioneine and others described in the review. To summarize, based on the presence of several bioactive compounds that contribute to biological activity, C. militaris mushrooms definitely deserve to be considered as functional foods and also have great potential for medicinal use. Recent scientific reports indicate the potential of cordycepin in antiviral activity, particularly against COVID-19.

Effective disinfection is a basic procedure in medical facilities, including those conducting dental surgeries, where treatments for tissue discontinuity are also performed, as it is an important element of infection prevention. Disinfectants used in dentistry and dental and maxillofacial surgery include both inorganic (hydrogen peroxide, sodium chlorite-hypochlorite) and organic compounds (ethanol, isopropanol, peracetic acid, chlorhexidine, eugenol). Various mechanisms of action of disinfectants have been reported, which include destruction of the structure of bacterial and fungal cell membranes; damage of nucleic acids; denaturation of proteins, which in turn causes inhibition of enzyme activity; loss of cell membrane integrity; and decomposition of cell components. This article discusses the most important examples of substances used as disinfectants in dentistry and presents the mechanisms of their action with particular focus on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The search was conducted in ScienceDirect, PubMed, and Scopus databases. The interest of scientists in the use of disinfectants in dental practice is constantly growing, which results in the increasing number of publications on disinfection, sterilization, and asepsis. Many disinfectants often possess several of the abovementioned mechanisms of action. In addition, disinfectant preparations used in dental practice either contain one compound or are frequently a mixture of active compounds, which increases their range and effectiveness of antimicrobial action. Currently available information on disinfectants that can be used to prevent SARS-CoV-2 infection in dental practices was summarized.

There are about 3000 species of mushrooms, which have a high amount of substances that are beneficial to human health, such as antioxidants. It is well known that oxidative stress plays an important role in the etiopathogenesis of many diseases, including cancer, cardiovascular disorders, and diseases of the central nervous system. One way to prevent homeostasis disorders that occur as a result of excessive production of pro-oxidative substances is to include the ingredients having antioxidant properties in the diet. Several compounds, such as those with phenolic and indole derivatives as well as carotenoids and some vitamins, exhibit antioxidant activity. These substances are present in many foods, including mushrooms. In addition, they have certain unique compounds that are not found in other sources (e.g., norbadione A). The present work discusses selected ingredients exhibiting antioxidant activity, which are found in various species of mushrooms as wells as describes the content of these compounds in the extracts obtained from mushrooms using artificial digestive juice.

Exposure of a drug to UV irradiation could affect its physicochemical properties. Hence, photostability testing is essential for topically administered drugs. Tazarotene, a receptor-selective, third-generation retinoid, is commonly used to treat acne vulgaris and psoriasis. In the present study, an in-depth analysis of the photostability of tazarotene in ethanolic solution in the presence of zinc oxide and/or titanium dioxide as well as benzophenone-type UV filters was performed. Eleven presumed products were derived from the photocatalytic degradation of tazarotene using ultra-performance liquid chromatography&ndash, tandem mass spectrometry, and transformation pathways were proposed. The degradation process mainly affected the 4,4-dimethyl-3,4-dihydro-2H-thiopyran moiety. The fragments most susceptible to oxidation were the methyl groups and the sulfur atom. Moreover, in the presence of sulisobenzone, under UV irradiation, tazarotene was subjected to a degradation process, which resulted in two photodecomposition products. In silico studies performed by OSIRIS Property Explorer demonstrated that five of the degradation products could be harmful in terms of the reproductive effects, which are associated with 3,4-dihydro-6-methyl-2H-1-benzothiopyran 1,1-dioxide, while one of them demonstrated potential irritant activity. The cytotoxic properties of the degradation products of tazarotene were assessed by MTT assay on a panel of human adherent cancer cells. Time- and concentration-dependent growth inhibition was evidenced in ovary (A2780) and breast (MDA-MB-231) cancer cell lines. The potential implication of the outcomes of the present research requires further studies mainly concerning the photostability of tazarotene in the topical formulations.

Release of bioelements and phenolic compounds from edible mushrooms (Agaricus bisporus, Cantharellus cibarius, and Lentinula edodes) enriched with zinc, selenium, l -phenylalanine, alone and as a mixture was examined using a simulated human gastrointestinal digestion method. Due to the extensive amount of data obtained, in order to interpret them more precisely in the work, the methods of chemometric analysis (Cluster Analysis—CA and Principal Compenent Analysis—PCA) were additionally applied. The results showed mycelium of L. edodes has the best health-promoting properties and addition of mixture to the media increased significantly the synthesis of p-hydroxybenzoic and protocatechuic acid (267 and 16.3 mg/100 g d.w.). After extraction into artificial digestive juices, 97.4 mg/100 g d.w. p-hydroxybenzoic acid and 15.6 mg/100 g d.w. of protocatechuic acid were released. The greatest amounts of Se and Zn were extracted from enriched A. bisporus mycelium (32.3 and 342 mg/100 g d.w., respectively). This study confirmed that mycelium might prevent nutritional deficiencies in the diet through use of functional foods.

Chlorella vulgaris Beijerinck is a spherical, green alga belonging to the genus Chlorella and family Chlorellaceae. It has high nutritional value and shows multiple biological effects. Dietary supplements that contain extracts of C. vulgaris are sold in the form of tablets, capsules, powders, and aqueous solutions. To the best of our knowledge, this is the first study to determine the content of bioelements (zinc, iron, and magnesium), phenolic compounds, and lutein before and after incubation with artificial digestive juices from preparations containing C. vulgaris. In this study, we used commercial preparations in the form of powder and tablets. The samples were incubated in artificial gastric juice and then in artificial intestinal juice for 30 and 90 min. The contents of bioelements were determined by using the flame atomic absorption spectrometric method. Lutein and phenolic compounds were analyzed by high-pressure liquid chromatography. We also aimed to evaluate the quality of chlorella-containing formulations by using the methods described in the European Pharmacopoeia 8th edition. According to the results, the preparations containing C. vulgaris demonstrated the presence of phenolic compounds and lutein. Therefore, daily supplementation of preparations containing C. vulgaris substantiates its usefulness for humans. The qualitative composition of the examined organic substances and bioelements was found to be in accordance with the manufacturer’s declarations on the packaging containing C. vulgaris compared with the control samples; however, the contents of bioelements were found to be negligible after incubation with artificial digestive juices. This shows that the examined preparations containing C. vulgaris are not good sources of bioelements such as zinc, iron, or magnesium.

One of the most popular edible species of wild mushrooms in many countries is Imleria badia (Fr.) Vizzini. It is a species valued due to its taste, intense aroma after drying and dietary, medicinal properties. Significant amounts of carbohydrates, proteins, polyunsaturated fatty acids and β-tocopherol, but also γ-tocopherol were determined in I. badia fruiting bodies. The presence of low molecular weight organic acids: malic, citric, fumaric and oxalic acids, and phenolic compounds with antioxidant properties, such as p-hydroxybenzoic acid, cinnamic acid and protocatechuic acid, were also found. This species is high in another antioxidant compound – theanine. Recent reports indicated that I. badia fruiting bodies’ extracts showed favorable therapeutic and health-promoting benefits and showed their anti-inflammatory, anti-cancer and antioxidant potential, consisting mainly in an inhibition of lipid peroxidation. Biological properties were also determined and confirmed for mycelium obtained from in vitro cultures of I. badia.

International audience; Background: The sprouts of Brassica vegetables are known from their nutritional and chemopreventive values. Moreover, sprouts fortification with some trace elements, like selenium, may increase their importance in human diet. Thus, the aim of our study was to examine if selenium enrichment of kale and kohlrabi sprouts may influence their biochemical properties (phenolic acids and L-tryptophan content, antioxidant potential) or cytotoxic activity. Additional aim of the study was to evaluate the profile of selenium compounds and to describe the multidimensional interactions between the mentioned parameters. Methods: Selenium content in the sprouts was evaluated by double-channel atomic fluorescence spectrometer AFS-230 with the flow hydride-generation system. Separation of selenium species in water soluble fraction was performed by size-exclusion LC-ICP-MS. The identification and quantification of phenolic acids and L-tryptophan was performed by HPLC. For antioxidant activity DPPH and FRAP methods were used. Cytotoxic activity of the sprouts extracts on a panel of human metastatic carcinoma cells was evaluated by MTT test. Results: Selenium content in the fortified sprouts was several orders of magnitude higher than in the unfortified ones. Only small percentage of supplemented selenium (ca. 10 %) was incorporated into the sprouts as seleno-L-methionine, while the other detected selenium species remained unidentified. Selenium fortification differently stimulated the production of phenolic acids (sinapic, chlorogenic, isochlorogenic and caffeic acid) in the tested sprouts, depending on the particular species, selenium dose and the investigated compound. PCA analysis revealed strong correlation between antioxidant parameters and phenolic acids and L-tryptophan, while Se correlated only with caffeic acid. The sprouts extracts (≥1 mg/mL) showed cytotoxic potency to all the studied cancer cell lines (SW480, SW620, HepG2, SiHa), regardless the selenium supplementation. Conclusion: Se-fortified kale and kohlrabi sprouts are good candidates for functional food ingredients. Moreover, these results indicate that the sprouts enriched with sodium selenite show higher nutritional value, without significant changes in their cytotoxic activity.

Fomitopsis officinalis is a medicinal mushroom used in traditional European eighteenth and nineteenth century folk medicine. Fruiting bodies of F. officinalis were collected from the natural environment of Świętokrzyskie Province with the consent of the General Director for Environmental Protection in Warsaw. Mycelial cultures were obtained from fragments of F. officinalis fruiting bodies. The taxonomic position of the mushroom mycelium was confirmed using the PCR method. The presence of organic compounds was determined by HPLC–DAD analysis. Bioelements were determined by AF-AAS. The biochemical composition of the tested mushroom material was confirmed with the FTIR method. Antioxidant properties were determined using the DPPH method, and the antiproliferative activity was assessed with the use of the MTT test. The presence of indole compounds (l-tryptophan, 6-methyl-d,l-tryptophan, melatonin, 5-hydroxy-l-tryptophan), phenolic compounds (p-hydroxybenzoic acid, gallic acid, catechin, phenylalanine), and sterols (ergosterol, ergosterol peroxide) as well as trace elements was confirmed in the mycelium and fruiting bodies of F. officinalis. Importantly, a high level of 5-hydroxy-l-tryptophan in in vitro mycelium cultures (517.99 mg/100 g d.w) was recorded for the first time. The tested mushroom extracts also showed antioxidant and antiproliferative effects on the A549 lung cancer cell line, the DU145 prostate cancer cell line, and the A375 melanoma cell line.

Edible mushrooms are classified as a functional food. The study aimed to initiate in vitro cultures of selected species of Pleurotus: P. citrinopileatus, P. djamor, P. eryngii, P. florida, P. ostreatus, and P. pulmonarius and to optimize the method of cultivation of these species to obtain raw materials characterized by pro-health properties. Another objective was to analyze the biologically active substances in the obtained mushroom materials. By determining the organic compounds and bioelements present in the species selected for the study, it was found that the fruiting bodies obtained by cultivation were characterized by a high content of phenolic and indole compounds. Similarly, the mycelia obtained from in vitro culture were found to contain significant amounts of organic compounds exhibiting biological effects such as lovastatin. The study revealed that the composition of biologically active substances varied between the mycelia obtained from in vitro cultures and the fruiting bodies obtained by cultivation.

Chronic unpredictable mild stress (CUMS) - a rodent model of depression mimics a variety of neurochemical and behavioral alterations similar to those seen in human depression. This study evaluated the antidepressant activity of hyperforin in the CUMS model using fluoxetine (FLX) as a reference drug. The antidepressant-like effects of hyperforin and FLX were evaluated in the tail suspension test (TST), forced swim test (FST), and splash test (SPT). CUMS induced an increase in immobility time in mice (pro-depressive effects) in the FST and TST. CUMS-induced changes were reversed by chronic treatment with hyperforin (2.5 and 5 mg/kg), as well as FLX (10 mg/kg). SPT results revealed a decrease in the frequency and duration of grooming in stressed mice. These effects were normalized by hyperforin (5 mg/kg) and FLX treatment. Hyperforin (2.5 mg/kg) only reversed the CUMS-induced deficits related to the frequency of grooming. CUMS also caused a decrease in zinc concentration in the frontal cortex (FC) and hippocampus (Hp) of mice; hyperforin (2.5 mg/kg) increased zinc concentration in the Hp of control rats. CUMS also induced a decrease in BDNF protein levels in the FC and Hp, while decreasing the pCREB/CREB ratio only in the Hp. Hyperforin (2.5 and 5 mg/kg) reversed the CUMS-induced reduction of BDNF only in the Hp. Our results demonstrate the antidepressant-like activity of hyperforin in the CUMS model in mice and the possible involvement of hippocampal BDNF/zinc alterations in this activity.

Kynurenic acid (KYNA) is a metabolite of tryptophan formed enzymatically along kynurenine pathway in bacteria, fungi, plants and animals. It was suggested that yeast may produce KYNA during the fermentation process. Since KYNA was found to interact with alcohol metabolism by inhibition of aldehyde dehydrogenase activity the aim of this study was to measure the content of KYNA in selected alcoholic beverages of various type, beer, wine, mead and spirits. Moreover, the absorption and elimination rate of KYNA administered as a beverage was investigated in humans. Twelve healthy volunteers (6 female and 6 male) were studied. Fifty six samples of alcoholic beverages were of commercial origin. KYNA was determined by means of high-performance liquid chromatography method with fluorometric detection. KYNA was identified in all studied beverages. The amounts of KYNA found in various types of beverages differed significantly: mead 9.4–38.1 µg/100 ml, wine 1.4–10.9 µg/100 ml, beer 0.1–5.2 µg/100 ml, spirits 0.01–0.1 µg/100 ml. In human, it was found that KYNA is rapidly absorbed from digestive tract reaching its maximal concentration in blood 30 min after administration. Thus, the potential interaction between KYNA and alcohol occurring in human body after ingestion of alcoholic beverages was proven.

The mycelium of Lentinula edodes produces enzymes which may degrade xenobiotics including steroid hormones. The aim of the study was to determine whether the mycelium from in vitro cultures of L. edodes are able to degrade endocrine disruptors such as testosterone and 17α-ethynylestradiol. To prove the possibility of xenobiotics degradation, cultures of L. edodes were cultivated in an Oddoux liquid medium with the addition of synthetic 17α-ethynylestradiol and synthetic testosterone. The endocrine disruptors were extracted from the mycelium and determined qualitatively by RP-HPLC. The degradation products of testosterone and 17α-ethynylestradiol were identified using a UPLC/MS/MS analysis. Undegraded testosterone was determined at the amount of 2.97 mg/g dry weight but only in one of the L. edodes extracts from in vitro cultures supplemented with 50 mg of this compound. In turn, 17α-ethynylestradiol was not determined in any samples. Additionally in all extracts, mushroom sterols (ergosterol peroxide and ergosterol) were determined. Their total amounts were significantly lower in samples containing the abovementioned steroids than in extracts from mycelium L. edodes without the addition of steroid hormones. The results demonstrated that the mycelium of L. edodes can be used in the biodegradation process of a water environment contaminated with endocrine disruptors. Electronic supplementary material The online version of this article (10.1007/s13205-018-1458-x) contains supplementary material, which is available to authorized users.

Agaricus bisporus and Imleria in vitro cultures were cultivated on modified Oddoux medium, and Oddoux medium was enriched with serine or anthranilic acid. Serine or anthranilic acid was used at the concentrations of 0.1, 0.25, 0.5, and 0.75 g/L of medium. Determination of indole compounds in the obtained biomass was carried out using thin-layer chromatography (TLC) with densitometric detection. In every analyzed sample, presence of serine or anthranilic acid was studied. Comparison of the results obtained for the treatment and control samples allowed us to determine the optimum concentration of serine or anthranilic acid in the medium in order to obtain biomass with increased content of indole compounds. A. bisporus with addition of anthranilic acid or serine to the medium at the concentration of 0.5 g/L was the most beneficial. In the case of Imleria badia, anthranilic acid at the concentration of 0.5 g/L was the most optimal. This is the first report demonstrating the content of indole derivatives in bi...

Agaricus bisporus (white button mushroom) is one of the most popular culinary-medicinal mushrooms worldwide. This species has for decades been the subject of numerous scientific studies. The aim of this study was to examine the pro- or anti-inflammatory properties of A. bisporus and biomass extracts from in vitro cultures growing in Oddoux medium enriched with α-linolenic acid in colon epithelial Caco-2 cells activated with lipopolysaccharide (LPS) and tumor necrosis factor (TNF)-α. Incubation of Caco-2 cells with A. bisporus extracts resulted in decreased expression of cyclooxygenase-2 and prostaglandin F2α receptor compared with the LPS- and/or TNF-α-activated cells, whereas the expression of nuclear factor (erythroid-derived 2)-like 2 increased after incubation. Interleukin-6 level decreased significantly in Caco-2 cells after supplementation with mushroom extracts. The amounts of monoun-saturated and polyunsaturated fatty acids differed significantly in Caco-2 cell membranes after supplementation with A. bisporus extracts. Our findings suggest the presence of anti-inflammatory and antioxidant properties of A. bisporus biomass extracts from in vitro cultures.

Rutabaga and kohlrabi provide valuable and beneficial constituents of human diet. Compounds such as tryptamine, melatonin, indole and methyltryptamine were determined in kohlrabi bulbs in the respective amounts of 1.38 ± 0.31, 0.78 ± 0.09, 0.32 ± 0.03 and 0.67 ± 0.09 μg/100 g fw. Rutabaga roots contained l -tryptophan, tryptamine, melatonin, serotonin and methyltryptamine in the amounts of 3.04 ± 0.95, 1.80 ± 0.20, 0.56 ± 0.09, 0.16 ± 0.06 and 0.98 ± 0.04 μg/100 g fw, respectively. In their seeds three compounds (μg/100 g fw) were found, namely serotonin (0.36 ± 0.05) and l -tryptophan (21.97 ± 1.07) in rutabaga seeds, whereas in kohlrabi seeds serotonin (4.00 ± 0.07) and indole (0.31 ± 0.01). Evaluated sprouts contained more indole derivates than seeds. Serotonin was observed solely in rutabaga sprouts, in rather small amounts 0.10 ± 0.00–0.38 ± 0.06 μg/100 g fw. Melatonin concentrations in 8 days sprouts of rutabaga and kohlrabi were at the level of 0.51 ± 0.11 and 0.70 ± 0.02 μg/100 g fw, respectively. As relatively high concentrations of indole derivates were detected in rutabaga and kohlrabi, both in ripe plants and their sprouts, these vegetables provide an important source of such compounds.

Summary Thin-layer chromatography (TLC) methods coupled with densitometric detection were employed in analyses for the presence of nonhallucinogenic indole compounds in methanol extracts from the garlic (Allium sativum L.) bulbs originating from China, Georgia, Spain, Mexico, and Poland, and from granulated garlic in the form of seasoning (commercial product). Four indole compounds for which the garlic bulbs were analyzed, were detected: 5-methyltryptamine, L-tryptophan, 5-hydroxy-L-tryptophan, and melatonin, the amounts of which ranged from 4.2 to 199.6 mg kg−1 dry weight. In contrast, only 3 indole compounds were found in the garlic bulbs from Spain: 5-methyltryptamine, L-tryptophan and melatonin (85.7, 120.1, and 9.6 mg kg−1 dry weight, respectively). The total amount of indole compounds in the extracts from the garlic bulbs from China was the highest (415.4 mg kg −1 dry weight), while the amounts in the others (from Georgia, Spain, Mexico, Poland) were similar and ranged from 215.4 to 283 mg kg −1 dry weight. The granular, freeze-dried garlic contained the lowest content of indole compounds, and their total amount was only 207 mg kg−1 dry weight.

The aim of the study was chemical analysis of polysaccharide fractions from sporocarps of Sarcodon imbricatus collected in natural sites and from the mycelium of in vitro cultures. Three polysaccharide fractions (FOI, FOII, FOIII) were isolated from sporocarps and two (FKI, FKII) from in vitro cultures. Qualitative analysis by HPLC method showed that they are composed of galactose and fucose (FOI, FKI) or glucose and fucose (FOII, FKII). FOIII fraction of the sporocarps consisted of glucose only. Molecular weights of isolated fractions ranged from 3.8 to 16.3 kDa for fractions from the sporocarps and from 5.8 to 14.7 kDa for that ones isolated from in vitro culture. The total percentage of sugar content for all fractions ranged from 97.8% to 99.1%. The percentage of uronic acids contents in acidic fractions was 2.6% and 2.7% for the FOI and FKI respectively. The work included also an assessment of cytotoxic activity of polysaccharide fractions in relation to tumor cell lines of human breast cancer MCV-7. FOI polysaccharide fraction of the sporocarps inhibited the growth of cancer cells in 50% compared to the control at a concentration of 0.0125%, while the polysaccharide fraction FKI from in vitro cultures inhibited cell growth in a concentration of 0.016%.

The purpose of this study was to analyze the indolic, phenolic, and fatty acid content and antioxidant activity of garlic sprouts growing in the dark and in the daylight. The pro- or anti-inflammatory properties of the garlic sprout extract were investigated by evaluating the cyclooxygenase-2 (COX-2), prostaglandin E synthase (cPGES), glutathione S transferase (GSTM1), nuclear factor NF-κB, peroxisome proliferator-activated receptors (PPARs), and aryl hydrocarbon receptor (AhR) protein levels in the RAW 264.7 cells activated with lipopolysaccharide (LPS). The highest amount of total indolic (73.56 mg/100 g f.w.) and phenolic compounds (36.23 mg/100 g f.w.) was detected in garlic sprouts grown in the daylight. Studies on antioxidant activity (the FRAP and DPPH method) of garlic sprouts showed that this activity is significantly higher for sprouts grown in full access to light when compared to those grown in the dark. In garlic sprout extracts, α-linolenic acid (ALA) was found to be in greater amount. COX-2 and cPGES level was lower when compared to LPS alone activated cells. After garlic extract treatment, higher level of GSTM1, PPARΥ, cytosolic p50 and p65 protein, as well as a lower NF-ĸB p50/p65 activity was noted in the RAW 264.7 cells which suggested PPARs and AhR transrepression mechanism of NF-ĸB signalling. The obtained results indicate Allium sativum sprouts are a rich source of n-3 fatty acids, indolic and phenolic compounds characterized by anti-inflammatory and antioxidative activity, which may support their high therapeutic and dietary potential.

The content of two groups of compounds with biological activity (non-hallucinogenic indole compounds and free phenolic acids) were analyzed in extracts of fruiting bodies of four species of Phellinus: P. igniarius, P. pini, P. pomaceus and P. robustus. The presence of indole compounds in methanolic extracts was analyzed by high-performance liquid chromatography and thin-layer chromatography coupled with densitometric detection. Three metabolites (serotonin, tryptamine, and L-tryptophan) were identified. The contents of individual indole compounds ranged from 1.70 (tryptamine in P. robustus) to 8.32 mg x 100 g1 dry weight (L-tryptophan in P. robustus). Four free phenolic acids were detected in methanolic extracts by the HPLC method. The total content ranged from 9.9 mg x 100 g1 DW (P. igniarius) to 32.5 mg x 100 g1 DW (P. robustus).

The effect of carbon and nitrogen sources and initial pH and temperature of the medium on the mycelial growth of Sarcodon imbricatus (L.) P. Karst. in axenic liquid culture was investigated. The optimal composition of the medium was found to be: 5% fructose, 1% hydrolysate of casein, 1% yeast extract, and 0.3% KH2PO4 at pH = 6 and incubation temperature of 20°C. In this condition the maximum biomass growth was observed, yielding 10.2 g L−1 of dry weight after 3-week of growth. The medium regarded as optimal for growth of S. imbricatus mycelium was used for the production of the biomass and further chemical analysis. The quantitative and qualitative composition of phenolic acids, fatty acids, and sterols were determined using chromatographic methods. The total content of phenolic acids was 1.86 mg × 100 g−1 DW, with the largest amount of protocatechuic acid (1.27 mg × 100 g−1 DW). Nineteen fatty acids were estimated, including five unsaturated fatty acids, e.g., oleic and α-linolenic acid. The analysis of sterols composition revealed the presence of ergosterol and ergosterol peroxide (197.7 and 200.47 mg × 100 g−1 DW, respectively). These compounds were isolated and confirmed by 1H-NMR. Presented study constitutes the first report on the accumulation of substances (phenolic acids, fatty acids, and sterols) with multidirectional biological activity in the mycelial axenic culture of Sarcodon imbricatus.

Phenolic acids are plant metabolites important in phytotherapy and also in cosmetology. In this study, proliferating shoot and callus cultures of Aronia melanocarpa were established and maintained on Linsmaier and Skoog (L-S) medium containing different levels of α-naphthaleneacetic acid (NAA) and 6-benzyladenine (BA), ranging from 0.1 to 3.0 mg l−1. Methanolic extracts from the biomass of these cultures and from the fruits of soil-grown plants were used to determine the amounts of free phenolic acids and cinnamic acid using the high-performance liquid chromatography (HPLC) method. Out of a total of twelve analyzed compounds, all of the extracts contained four of them: caffeic acid, p-hydroxybenzoic acid, syringic acid, and vanillic acid. Moreover, shoot extracts also contained salicylic acid (o-hydroxybenzoic acid), while callus extracts contained p-coumaric acid. On the other hand, fruit extracts also contained both salicylic acid and p-coumaric acid. The total amount of the analyzed compounds in extracts from both shoot and callus cultures depended on the L-S medium used, and varied between 103.05 and 150.95 mg 100 g−1 dry weight (DW), and between 50.23 and 81.56 mg 100 g−1 DW, respectively. Both types of culture contained higher levels of phenolic acids than the fruit extracts (32.43 mg 100 g−1 DW). In shoot cultures, p-hydroxybenzoic acid and salicylic acid were the predominant metabolites (reaching 55.14 and 78.25 mg 100 g−1 DW, respectively), while in callus cultures, p-hydroxybenzoic acid (25.60 mg 100 g−1 DW) and syringic acid (41.20 mg 100 g−1 DW) were the main compounds. In fruit extracts, salicylic acid (15.60 mg 100 g−1 DW) and p-hydroxybenzoic acid (5.29 mg 100 g−1 DW) were predominant.

Methanolic extracts of processed fruiting bodies of six edible mushroom species (Basidiomycota) – Armillaria mellea, Boletus badius, Boletus edulis, Cantharellus cibarius, Lactarius deliciosus collected from natural habitats and Pleurotus ostreatus of commercial origin – were analysed for the presence of non-hallucinogenic indole compounds. Thermal processing was designed in such a way that it mimicked conditions used for cooking of mushroom dishes, since only a narrow group of mushrooms can be eaten raw, while indole compounds are thermolabile. All processed extracts were shown to contain l -tryptophan (up to 8.92 mg/100 g dw). The contents of the remaining compounds, 5-methyltryptophan, tryptamine, melatonin, indoleacetonitrile and indole, varied in different species (from 0.71 to 6.55 mg/100 g dw). Extract of processed C. cibarius fruiting bodies contained l -tryptophan, 5-methyltryptophan, tryptamine, melatonin, indoleacetonitrile and indole (1.96–4.94 mg/100 g dw) whereas l -tryptophan (2.78 mg/100 g dw) and tryptamine (2.77 mg/100 g dw) were the only indole compounds identified in the processed fruiting bodies of A. mellea.

The experiments on Bacopa monnieri from Scrophulariaceae family were performed in in vitro shoot cultures conditions in media enriched with Mg ions and serine or anthranilic acid (L1 vitamin). As there is limited literature data available on the content of elements in shoots from B. monnieri in vitro cultures, analyses of magnesium, zinc, potassium, calcium, copper, sodium and iron in plant shoots constituted the aim of the present study. The next aim of the work, for the first time, consists of evaluation of the content and concentration of magnesium and other metals in in vitro shoot cultures of B. monnieri and their influence on bacoside levels, as well as establishment of interactions between the listed analytes. The highest accumulation of magnesium was determined in the plant tissues cultured in media doped with 0.1 g/L serine and 0.5 g/L Mg (2104 µg/g dry weight), and 0.5 mg/g of anthranilic acid and 1.0 g/L Mg (2163 µg/g). The highest concentration of bacosides in the obtained in vitro shoot cultures of B. monnieri (37.3 mg/g dry weight) was found in cultures of the following media composition: MS1 with addition of 0.25 g/L serine and 0.1 g/L Mg, and MS1 with addition of 0.5 g/L serine and 0.5 g/L magnesium. Considering the observed shortage of plant reserves in the natural environment and its curative properties, it seems to be of utmost importance to obtain, as a result of the presented experiment, in vitro shoot cultures of B. monnieri characterized by optimal and reproducible composition of the physiologically active elements and metabolites.

Bacopa monnieri L. Pennell (Scrophulariaceae) is one of the most important plants in the system of Indian medicine (Ayurveda).This paper studies the optimal growth of B. monnieri for effective accumulation of metabolites. Biomass growth of this plant could be accomplished in liquid cultures on MurashigeSkoog medium.Powdered shoots of in vitro cultures of B. monnieri were extracted by methanol for indole compounds, phenolic compounds and bacosides for RP-HPLC analysis. Fatty acid analysis was performed via gas chromatography. Anti-inflammatory effect of B. monnieri extracts was evaluated in the A549 cells. COX-2 and cPGES expression was analyzed using Western blots.l-Tryptophan and serotonin were found in biomass from in vitro cultures of B. monnieri on MS medium and in biomass from the MS mediums enriched with the different additions such as of 0.1 g/L magnesium sulphate, 0.1 g/L zinc hydroaspartate, 0.1 g/L l-tryptophan, 0.25 g/L serine, 0.5 g/L serine and 0.5 mg/L anthranilic acid. The content of l-tryptophan and serotonin compounds was significant in biomass from medium with the addition of 0.1 g/L zinc hydroaspartate (0.72 mg/g dry weight and 1.19, respectively). Phenolic compounds identified in biomass from the same variants of MS medium were chlorogenic acid (ranging from 0.20 to 0.70 mg/g dry weight), neochlorogenic acid (ranging from 0.11 to 0.40 mg/g dry weight) and caffeic acid (ranging from 0.01 to 0.04 mg/g dry weight). The main group of fatty acids in biomass was saturated fatty acids (53.4%). The predominant fatty acid was palmitic acid. A significant decrease of COX-2 and cPGES expression was observed in the A549 cells activated with LPS and treated with B. monnieri extracts.As far as we know, this is the first analysis of indole compounds and phenolic acids in this plant. The multi-therapeutic effect of B. monnieri is expressed by the activity of bacosides. Information about the presence of indole and phenolic compounds, and fatty acids in this plant is limited, but the content of these compounds might participate in the physiological activity of B. monnieri.

The analysis demonstrated that biomass of Agaricus bisporus, Boletus badius, and Cantharellus cibarius contains non-hallucinogenic indole compounds. Addition of l-tryptophan to the in vitro cultures raised the total content of indole compounds. l-Tryptophan became metabolized, causing an increase of the concentration of some indole compounds. The compounds found in the tested biomass from in vitro culture on Oddoux medium without and with addition of l-tryptophan were l-tryptophan, 5-hydroxy-l-tryptophan, serotonin, melatonin, tryptamine, and 5-methyltryptamine (ranged from 4.28 to 132.51 mg/100 g dry weight). l-Tryptophan is an amino acid exogenous to the human body, and therefore, it must be supplied to the body with food. The highest amount of 5-hydroxy-l-tryptophan was found in the extracts from biomass of B. badius cultured on medium with addition of l-tryptophan (132.51 mg/100 g dry weight). Also, in this case, the highest total content of examined indole compounds (168.00 mg/100 g dry weight) was d...

Metal responsive transcription factor 1 (MTF-1) is a zinc dependent transcription factor which is involved in the regulation of intracellular signaling pathways. MTF-1 regulates the expression of two streams of genes functioning in metal homeostasis and anti-oxidative response. MTF-1 acts in the process of binding of toxic metal ions in the cell, due to the activation of the expression of metallothioneins (MTs). Additionally, MTF-1 regulates transcription of genes involved in the sequestration of zinc and its intracellular transport. Disruption of zinc and MT homeostasis has an indispensable influence on the development of several pathological states. Moreover, by increasing MT activity, MTF-1 can effectively protect cells from oxidative and hypoxic stresses. The mechanism of MTF-1 action in cells includes the regulation of the proper immune response through activation/repression of anti- and pro-inflammatory cytokines. MTF-1 function in immune response is related to nuclear factor-κB (NF-κB) activity. Synthesis of insulin is also related to the activity of this transcription factor and zinc balance. Insulin transport also depends on zinc. In pancreatic β-cells, several types of the zinc transporters are found. Zinc transporters coordinated action is crucial for the synthesis and secretion of insulin. Disturbances in the regulation of signaling pathways connected with MTF-1 function can entail further alterations in zinc intracellular status and this growing imbalance can promote the pathophysiology of degenerative disorders.

For thousands of years, the fruiting bodies of higher fungi have been used as a source of food. Edible mushrooms are increasingly being investigated because of their production of biologically active secondary metabolites. Qualitative and quantitative analyses of indole compounds in methanolic extracts from unprocessed and thermally processed fruiting bodies of selected edible mushroom species, belonging to the Basidiomycota taxon were performed. The methanol extracts from the unprocessed and processed mushrooms, after concentration in an evaporator, were purified by TLC preparative chromatography and then analyzed for indole compounds by the HPLC method. In all the extracts from mushrooms before and after thermal processing, several indole compounds with physiological activity were identified and quantified. On the basis of the analyses, the following indole compounds were found: l -tryptophan, 5-hydroxytryptophan, 5-methyltryptophan, tryptamine, 5-methyltryptamine, serotonin, indole, indoleacetic acid, indoleacetonitrile, melatonin, and kynurenine sulfate. The amounts ranged from 0.01 to 29.61 mg/100 g dry weight for raw mushrooms, and from 0.01 to 17.71 for heat-treated mushrooms.

The contents of nonhallucinogenic indole compounds were determined in methanol extracts from fruiting bodies of four common edible European species of higher fungi representing the most popular taxon Basidiomycota : Agaricus bisporus (J.E. Lange), Cantharellus cibarius Fr., Lactarius deliciosus (L. Fr.) S.F. Gray and Leccinum rufum (Schaef.) Kreisel. Amongst eleven compounds under analysis, 6–7 metabolites, distinct in different species, were identified in the extracts of fruiting bodies. Serotonin and melatonin were the only common compounds to all species. The contents of the analyzed compounds were diverse, ranging from 0.01 to almost 40 mg/100 g d.w. The contents of tryptophan, 5-hydroxytryptophan, tryptamine and melatonin were low (below 1.40 mg/100 g d.w.). Noteworthy, the serotonin contents were very high in all species under study and amounted to 5.21, 29.61, 18.42 and 31.71 mg/100 g d.w., respectively. Moreover, the fruiting bodies of these species contained indoleacetic acid (max. 2.04 mg/100 g d.w.) and tryptophan degradation products: kynureine sulfate (max. 39.20 mg/100 g d.w.) and kynurenic acid (6.21 mg/100 g d.w.).

For a long time fungi belonging to Basidiomycota phylum have been in the center of attention because of the presence in their fruiting bodies of compounds with known therapeutic activity. Mycelial cultures of two aphyllophorales species occurring in Poland, Hydnum repandum L., and Sparassis crispa (Wulf.) Fr., were analyzed in our study. The main aim of the study was qualitative and quantitative analysis of extracts obtained from the mycelial cultures for the presence of known biologically active compounds, including phenolic acids, non-hallucinogenic indole compounds and sterols. For analyses a reversed-phase chromatography (RP-HPLC) method was used. The presence of eight phenolic acids including gallic, gentisic, p-hydroxybenzoic, caffeic, p-coumaric protocatechuic, syringic, vanillic and cinnamic acids was confirmed in the extracts obtained from the biomass. The quantitatively predominant metabolites in biomass from in vitro cultures of H. repandum and S. crispa were protocatechuic acid (6.23 μg/g DW) and p-hydroxybenzoic acid (4.52 μg/g DW). Derivatives of indole such as indole, serotonin, tryptamine and tryptophan were measured quantitatively. Their total content was estimated as 1.28 μg/g DW and 3.07 μg/g DW in H. repandum and S. crispa extracts, respectively. The major metabolite found was tryptophan. In addition, ergosterol, one of the sterols present in the biomass of in vitro cultures of S. crispa was analyzed (700.87 μg/g DW). The obtained results confirm the hypothesis that mycelial cultures of domestic species of aphyllophorales are able to accumulate biologically active metabolites.

Bacopa monnieri is one of the most interesting plants from the Ayurveda system. The aims of present research were, basing on in vitro shoot culture of B. monnieri, to determine content and to evaluate the influence of physiologically important metabolites on the selected bioelements accumulation in biomass. The most significant increase in biomass production was observed in the culture medium enriched with 0.5 mg/L of anthranilic acid. In this medium also, the highest accumulation of Mg was noted. The highest concentration of iron was determined in B. monnieri in vitro culture enriched with 0.25 g/L of serine. The addition of l-tryptophan, magnesium sulfate, and zinc hydroaspartate caused only a small increase in the accumulation of copper in B. monnieri. Increase in Zn accumulation was obtained in biomass from in vitro culture of B. monnieri with the addition of magnesium sulfate and zinc hydroaspartate. In the case of Na, the maximum level of this element was in biomass from medium enriched with zinc hydroaspartate. Twofold increase in K concentration was obtained in biomass from cultures on medium with addition of serine and magnesium sulfate. The concentrations of Ca in biomass of all studied media were at the similar level.

Amounts of non-hallucinogenic indole compounds were determined in methanolic extracts from the fruiting bodies and biomass of Sarcodon imbricatus cultured in vitro. In both extracts there were non-hallucinogenic indole compounds present, l -tryptophan, tryptamine and serotonin. Additionally, melatonin was found also in the fruiting bodies. The total amount of indole compounds was 89.38 mg/100 g d.w. in the fruiting bodies and 8.45 mg/100 g d.w. in the cultured mycelia. The leading compound in the fruiting bodies and the mycelium was serotonin (52.02 mg/100 g d.w. and 3.03 mg/100 g d.w., respectively). This main indole compound was isolated and identified using spectral methods.

Background Species of phylum Basidiomycota are of great interest in many studies as a source of valuable biological compounds. Aims To estimate the levels of antioxidant compounds (phenolic acids, indole compounds and sterols) in edible species of Aphyllophorales (sensu lato): Hydnum repandum L. and Sparassis crispa (Wulf.) Fr. Methods A reversed-phase high performance liquid chromatography (RP-HPLC) method was used for the quantitative and qualitative analyses of antioxidant components (phenolic acids, indole compounds, and sterols). Results Analysis of phenolic acids revealed that 8 out of the 10 analyzed compounds were present. The quantitatively predominant in Hydnum repandum was protocatechuic acid (75.23 mg/100 g DW), and in Sparassis crispa it was p-hydroxybenzoic acid (43.92 mg/100 g DW). In turn, analysis of indole compounds identified 5 out of the 12 analyzed compounds: indole, melatonin, serotonin, tryptamine, and l -tryptophan. Moreover, ergosterol was also identified and quantitatively determined (150.37 mg/100 g DW) in Sparassis crispa extracts. Conclusions The data presented in this paper confirm the significant potential of chemical components with recognized antioxidant activity. The species can be considered as an alternative source of phenolic acids and ergosterol.

Methanolic extracts obtained from the fruiting bodies of Cantharellus cibarius (the Chanterelle) and from the mycelium of this species cultured in vitro were analyzed for the qualitative and quantitative composition of non-hallucinogenic indole compounds. The extracts were found to contain eight indole compounds: L-tryptophan, 5-hydroxytryptophan, serotonin, melatonin, indole, kynurenine sulfate, 5-methyltryptophan, and indoleacetonitrile. The extract from the fruiting bodies also contained tryptamine. The amounts of individual compounds varied widely, ranging from 0.01 to 17.61 mg/100 g DW in the fruiting bodies, and from 0.01 to 35.34 mg/100 g DW in the biomass from in vitro cultures. The quantitatively dominating compounds included: serotonin (17.61 and 20.49 mg/100 g DW, respectively) and kynurenine sulfate (3.62 and 35.34 mg/100 g DW). In addition, the material from in vitro cultures contained a considerable amount of 5-hydroxytryptophan (12.52 mg/100 g DW). The levels of the remaining indole compounds under analysis: L-tryptophan, melatonin, indole, 5-methyltryptophan, and indoleacetonitrile in the material under study were low, below 1 mg/100 g DW.

Methanolic extracts of two species collected from natural habitats in Poland, Boletus edulis and Suillus luteus, and one species from a commercial source, Pleurotus ostreatus, were analyzed for the presence of non-hallucinogenic indole compounds. The contents of indole compounds in these species were both qualitatively and quantitatively diverse, ranging from 0.01 to 34.11 mg/100 g d.w. Two of 11 tested indole compounds, 5-hydroxytryptophan (0.18, 2.08, 1.63 mg/100 g d.w.) and serotonin (6.52, 10.14, 34.11 mg/100 g d.w.), were present in all three species under study. B. edulis and S. luteus were found to contain L-tryptophan (0.39 and 2.61 mg/100g d.w.) and melatonin (0.68 and 0.71 mg/100 g d.w.). Tryptamine was present in two species, i.e., B. edulis (1.17 mg/100 g d.w.) and in P. ostreatus (0.91 mg/100 g d.w.), in which slight amounts of indole acetonitrile (0.04 and 0.01 mg/100 g d.w., respectively) were also identified. Indoleacetic acid was a common metabolite for P. ostreatus and S. luteus and its contents amounted to 0.21 and 0.04 mg/100 g d.w., respectively. Indole compounds degradation products kynurenic acid (2.63 mg/100 g d.w.) and kynurenine sulfate were (19.57 mg/100 g d.w.) were observed only in S. luteus.

Recently, studies have been conducted on the chemical composition of fruiting bodies of the culinary-medicinal Honey mushroom, Armillaria mellea (Vahl.) P. Kumm. (higher Basidiomycetes). It is considered in Europe and Asia as edible and medicinal, when appropriately prepared, and has demonstrated the presence of different groups of organic compounds, including carbohydrates, sterols, sphingolipids, fatty acids, sesquiterpenes, non-hallucinogenic indole compounds, peptides, enzymes, adenosine derivatives, and many other components. Most of these metabolite groups possess potential therapeutic and dietary values. The results of quantitative analyses of indole compounds and heavy metals signal potential health hazards for humans. Some of the studies reviewed herein describe in detail the mechanism of symbiosis between A. mellea and the orchid species Gastrodia elata. This orchid is native to Asia, Australia, and New Zealand, and is used in therapeutics in official Chinese medicine.

Five indole compounds (5-hydroxy-L-tryptophan, L-tryptophan, indole-3-acetic acid, melatonin, serotonin) and hypericin were identified and quantified in methanolic extracts of shoot cultures of three Hypericum perforatum cultivars (Helos, Elixir, Topas) growing on two variants of Murashige -Skoog medium differing in concentrations of growth regulators (naphthalene-1-acetic acid and 6-benzylaminopurine). Extracts of the aboveground parts of field-grown plants ( Hyperici herba) were also analyzed by HPLC and TLC analysis coupled with densitometric detection. Determination of four compounds was based on our assay described earlier. The methods of determination of 5-hydroxy-L-tryptophan and hypericin were developed and validated in this study. The composition and contents of the metabolites under study differed between the cultivars cultured in vitro and between medium variants containing diverse contents of growth regulators. The contents of individual indole compounds in the biomass from in vitro cultures ranged from 39.6 to 343.2 mg/100 g dry mass. 5-Hydroxy-L-tryptophan was the dominating metabolite (from 78.2 to 343.2 mg/100 g dry mass). Extracts from shoots of the cultivar Helos also contained high contents of serotonin (319.9 and 197.4 mg/100 g dry mass). The contents of indole compounds in Hyperici herba were also diverse (from 7.1 to 55.3 mg/100 g dry mass). 5-Hydroxy-L-tryptophan was the dominating metabolite as well. Hypericin content of Hyperici herba, equaling 12.2 mg/100 g dry mass was from 3.3 to 10 times higher than in extracts from shoots cultured in vitro. The present report is the first analysis of endogenous accumulation of indole compounds in Hyperici herba which involves, apart from melatonin, four other compounds.

Bacopa monnieri (L.) Pennell (water hyssop) from the Scrophulariaceae family represents one of the best known plants of the Ayurveda system, with reported procognitive, antioxidant, anti-inflammatory, neuroprotective, and anticonvulsant activity. It is considered to be a central nervous system modulating agent. However, recent studies have indicated its potential use in cancer prevention and treatment. Here we report the findings from a study of the effects of B. monnieri extracts derived from artificial digestive juices on physiological traits of prostate cancer cells (DU 145), such as viability and migratory activity. The safety profile and chemopreventive potential of B. monnieri extracts were investigated in Vibrio harveyi mutagenicity assays. Additionally, in this study for the first time the content of phenolic compounds and bacosides released from B. monnieri biomass to artificial digestive juices was determined. The investigated extracts were cytotoxic to DU 145; however, in non-cytotoxic concentrations, they significantly reduced cancer cell motility, thereby demonstrated anti-invasive activity. All extracts under study exhibited very strong antimutagenic activity against nitroquinoline- N-oxide. Bacoside A and phenolic acids were determined, but qualitative and quantitative differences between extracts were found.