Bioactives of the essential oil from the leaves of Eugenia pyriformis Cambess (Myrtaceae) on the effects of tobacco.

Introduction: Lung cancer is the most commonly diagnosed and the main cause of cancer death, usually related to cigarette smoking. Furthermore, the microbiota of people exposed to cigarette smoke can be modified, making it difficult to eliminate opportunistic microorganisms. The leaves of Eugenia pyriformis are a by-product of fruit production and, to date, there have been no studies addressing the antiproliferative, anti-inflammatory, and antimicrobial activities. Objective: Investigate the antimicrobial, Nitric Oxide (NO)-production inhibition, and antiproliferative activities of the essential oil from E. pyriformis leaves and its possible effect on the treatment and prevention of damage caused by tobacco. Methods: The essential oil (EO) was obtained by hydrodistillation (3 h). Its chemical composition was investigated by GC-MS. It was proposed to investigate antiproliferative activity against human tumor cell lines, namely, breast adenocarcinoma (MCF-7), lung (NCI-H460), cervical (HeLa), and hepatocellular (HepG2) carcinomas. A non-tumor primary culture from pig liver (PLP2) was also tested. The EO capacity to inhibit nitric oxide (NO) production was evaluated by a lipopolysaccharide stimulated murine macrophage cell line. Antibacterial and antifungal activities against opportunistic pathogens were investigated against seven strains of bacteria and eight fungi. Results: The results indicated the presence of 23 compounds in the essential oil, the majority were spathulenol (45.63%) and ß-caryophyllene oxide (12.72%). Leaf EO provided 50% inhibition of nitric oxide production at a concentration of 92.04 µg mL-1. The EO also demonstrated antiproliferative activity against all human tumor cell lines studied, with GI50 values comprised between 270.86 and 337.25 µg mL-1. The essential oil showed antimicrobial potential against the bacteria Listeria monocytogenes (Murray et al.) Pirie (NCTC 7973) and Salmonella Typhimurium ATCC 13311 (MIC 1870 µg mL-1) and fungi Aspergillus versicolor ATCC 11730, Aspergillus ochraceus ATCC 12066, Penicillium ochrochloron ATCC 90288, Penicillium verrucosum var. cyclopium (Westling) Samson, Stolk & Hadlok (food isolate) (MIC 1870 µg mL-1) and Trichoderma viride Pers. IAM 5061 (1,400 µg mL-1). Conclusion: The demonstrated anti-inflammatory, antiproliferative, and antimicrobial activities in the leaves of E. pyriformis can add value to the production chain of this plant, being a possible option for preventing and combating cancer, including lung cancer.

New 1H-1,2,4-Triazolyl Derivatives as Antimicrobial Agents.

New 1H-1,2,4-triazolyl derivatives were synthesized, and six of them were selected based on docking prediction for the investigation of their antimicrobial activity against five bacterial and eight fungal strains. All compounds demonstrated antibacterial activity with MIC lower than that of the ampicillin and chloramphenicol. In general, the most sensitive bacteria appeared to be P. fluorescens, while the plant pathogen X. campestris was the most resistant. The antifungal activity of the compounds was much better than the antibacterial activity. All compounds were more potent (6 to 45 times) than reference drugs ketoconazole and bifonazole with the best activity achieved by compound 4 a. A. versicolor, A. ochraceus, A.niger, and T.viride showed the highest sensitivity to compound 4 b, while, T. viride, P. funiculosum, and P.ochrochloron showed good sensitivity to compound 4 a. Molecular docking studies suggest that the probable mechanism of antibacterial activity involves the inhibition of the MurB enzyme of E. coli, while CYP51 of C. albicans appears to be involved in the mechanism of antifungal activity. It is worth mentioning that none of the tested compounds violated Lipinski's rule of five.

Gut microbial dysbiosis occurring during pulmonary fungal infection in rats is linked to inflammation and depends on healthy microbiota composition.

While the effect of gut microbiota and/or inflammation on a distant body site, including the lungs (gut-lung axis), has been well characterized, data about the influence of lung microbiota and lung inflammation on gut homeostasis (lung-gut axis) are scarce. Using a well-characterized model of pulmonary infection with the fungus Aspergillus fumigatus, we investigated alterations in the lung and gut microbiota by next-generation sequencing of the V3-V4 regions of total bacterial DNA. Pulmonary inflammation due to the fungus A. fumigatus caused bacterial dysbiosis in both lungs and gut, but with different characteristics. While increased alpha diversity and unchanged bacterial composition were noted in the lungs, dysbiosis in the gut was characterized by decreased alpha diversity indices and modified bacterial composition. The altered homeostasis in the lungs allows the immigration of new bacterial species of which 41.8% were found in the feces, indicating that some degree of bacterial migration from the gut to the lungs occurs. On the contrary, the dysbiosis occurring in the gut during pulmonary infection was a consequence of the local activity of the immune system. In addition, the alteration of gut microbiota in response to pulmonary infection depends on the bacterial composition before infection, as no changes in gut bacterial microbiota were detected in a rat strain with diverse gut bacteria. The data presented support the existence of the lung-gut axis and provide additional insight into this mechanism. IMPORTANCE Data regarding the impact of lung inflammation and lung microbiota on GIT are scarce, and the mechanisms of this interaction are still unknown. Using a well-characterized model of pulmonary infection caused by the opportunistic fungus Aspergillus fumigatus, we observed bacterial dysbiosis in both the lungs and gut that supports the existence of the lung-gut axis.

Lung microbiota changes during pulmonary Aspergillus fumigatus infection in rats.

Since the realization that the lungs are not sterile but are normally inhabited by various bacterial species, studies have been conducted to define healthy lung microbiota and to investigate whether it changes during lung diseases, infections, and inflammation. Using next-generation sequencing, we investigated bacterial microbiota from whole lungs in two rat strains (previously shown to differ in gut microbiota composition) in a healthy state and during pulmonary infection caused by the opportunistic fungus Aspergillus fumigatus. No differences in alpha diversity indices and microbial composition between DA and AO rats before infection were noted. Fungal infection caused dysbiosis in both rat strains, characterized by increased alpha diversity indices and unchanged beta diversity. The relative abundance of genera and species was increased in DA but decreased in AO rats during infection. Changes in lung microbiota coincided with inflammation (in both rat strains) and oxidative stress (in DA rats). Disparate response of lung microbiota in DA and AO rats to pulmonary fungal infection might render these two rat strains differentially susceptible to a subsequent inflammatory insult.

Antimicrobial activity of Tetradenia riparialeaf essential oil / Actividad antimicrobiana del aceite esencial de hoja de Tetradenia riparia

Food spoilage is a widely neglected problem and the constant use of synthetic fungicides could develop resistant fungi. The objective of this study was to evaluate the chemical composition and antimicrobial activity of Tetradenia riparialeaf essential oil against foodborne disease microorganisms. Leaf essential oil was obtained by hydrodistillation and identified by gas chromatography coupled to mass spectrometry. The antimicrobial activity was studied by broth microdilution. The major compounds identified were oxygenated sesquiterpenes (43.6%): 14-hydroxy-9-epi-(E)-cariophylene (20.8%) and τ-cadinol (18.4%); followed by oxygenated diterpenes (24.6%): 6,7-dehydroroyleanone (12.6%) and 9ß, 13ß-epoxy-7-abiethene (10.6%); sesquiterpenic hydrocarbons (17.1%) and oxygenated monoterpenes (7.4%): fenchone (5.6%). The essential oil had broad antibacterial and antifungal activity, mainly against A. versicolor and P. ochrochloron with fungistatic and fungicidal activities and B. cereus, L. monocytogenes, and S. aureuswith bacteriostatic and bactericidal activities. T. riparialeaf essential oil is a potential alternative to control microorganisms-

El deterioro de los alimentos es un problema ampliamente desatendido y el uso constante de fungicidas sintéticos podría desarrollar hongos resistentes. El objetivo de este estudio fue evaluar la composición química y la actividad antimicrobiana del aceite esencial de hoja de Tetradenia riparia contra microorganismos patógenos transmitidos por los alimentos. El aceite esencial de hoja se obtuvo por hidrodestilación y se identificó mediante cromatografía de gases acoplada a espectrometría de masas. La actividad antimicrobiana estudiada fue por microdilución en caldo. Los compuestos principales del aceite esencial se identificaron como sesquiterpenos oxigenados (43,6%): 14-hidroxi-9-epi-(E)-cariofileno (20,8%) y τ-cadinol (18,4%); seguido de diterpenos oxigenados (24,6%): 6-7-deshidroroileanona (12,6%) y 9ß, 13ß-epoxi-7-abieteno (10,6%); hidrocarburos sesquiterpénicos (17,1%) y monoterpenos oxigenados (7,4%): fenchona (5,6%). Tenía amplia actividad antibacteriana y antifúngica, principalmente contra A. versicolor y P. ochrochloron con actividades fungistáticas y fungicidas, y principalmente contra B. cereus, L. monocytogenes y S. aureus con actividades bacteriostáticas y bactericidas. El aceite esencial de hoja de T. riparia es una alternativa potencial para controlar microorganismos.

Antimicrobial Activity of Catechol-Containing Biopolymer Poly[3-(3,4-dihydroxyphenyl)glyceric Acid] from Different Medicinal Plants of Boraginaceae Family.

This study reports the antimicrobial activities of the biopolymers poly[3-(3,4-dihydoxyphenyl)glyceric acid] (PDHPGA) and poly[2-methoxycarbonyl-3-(3,4-dihydroxyphenyl)oxirane] (PMDHPO), extracted from the six plants of Boraginaceae family: Symphytum asperum (SA), S. caucasicum (SC), S. gr and iflorum (SG), Anchusa italica (AI), Cynoglosum officinale (CO), and Borago officinalis (BO) collected in various parts of Georgia. The study revealed that the antibacterial activities were moderate, and biopolymers from only three plants showed activities against all tested bacteria. Biopolymers from CO stems as well as SC and AI did not show any activity except low activity against a resistant P. aeruginosa strain, which was the most resistant among all three resistant strains. On the other hand, the antifungal activity was better compared to the antibacterial activity. Biopolymers from BO stems exhibited the best activities with MIC/MFC at 0.37-1.00 mg/mL and 0.75-1.5 mg/L, respectively, followed by those from SG stems. Biopolymers from SC and AI roots showed antifungal activities against all six fungi, in contrast to the antibacterial activity, while biopolymers from CO stems and SA roots had activities against four fungi and one fungus, respectively. The sugar-based catechol-containing biopolymers from BO stems demonstrated the best activities among all tested biopolymers against T. viride, P. funiculosum, P. cyclpoium var verucosum, and C. albicans (MIC 0.37 mg/mL). In addition, biopolymers from SG stems were half as active against A. fumigatus and T. viride as ketoconazole. Biopolymers from all plant materials except for CO stems showed higher potency than ketoconazole against T. viride. For the first time, it was shown that all plant materials exhibited better activity against C. albicans, one of the most dreadful fungal species.

Antimicrobial Activity of Some Steroidal Hydrazones.

Twelve steroid based hydrazones were in silico evaluated using computer program PASS as antimicrobial agents. The experimental evaluation revealed that all compounds have low to moderate antibacterial activity against all bacteria tested, except for B. cereus with MIC at a range of 0.37-3.00 mg/mL and MBC at 0.75-6.00 mg/mL. The most potent appeared to be compound 11 with MIC/MBC of 0.75/1.5 mg/mL, respectively. The evaluation of antibacterial activity against three resistant strains MRSA, E. coli and P. aeruginosa demonstrated superior activity of compounds against MRSA compared with ampicillin, which did not show bacteriostatic or bactericidal activities. All compounds exhibited good antifungal activity with MIC of 0.37-1.50 mg/mL and MFC of 1.50-3.00 mg/mL, but with different sensitivity against fungi tested. According to docking studies, 14-alpha demethylase inhibition may be responsible for antifungal activity. Two compounds were evaluated for their antibiofilm activity. Finally, drug-likeness and docking prediction were performed.

A Comparative Study of Lactarius Mushrooms: Chemical Characterization, Antibacterial, Antibiofilm, Antioxidant and Cytotoxic Activity.

Mushrooms are valued worldwide for their nutritional, organoleptic and chemical properties. The aim of this study was to determine the chemical composition (free sugars, organic acids, fatty acids, tocopherols and phenolic compounds) and bioactivity of three wild mushrooms (Lactarius piperatus, Lactarius quietus and Lactarius vellereus) from Serbia. Chemical analysis was performed with HPLC-RI and UFLC-PDA (for hydrophilic compounds) and with GC-FID and HPLC-FP (for lipophilic compounds). The analysis of phenolic compounds was performed by UFLC-DAD. Biological activities were evaluated using three different assays (microdilution, TBARS and SRB assays). The results showed that the fruiting bodies were rich in mannitol and trehalose. The main organic acids were oxalic acid and citric acid. As for lipophilic components, stearic, oleic and linoleic acids and ß-tocopherol dominated in all the species studied. In addition, the methanolic and ethanolic extracts obtained showed antibacterial, antibiofilm and antioxidant properties. As for cytotoxicity, the extracts were not toxic or only moderately toxic toward different tumor cell lines. According to the results, the selected Serbian mushrooms are a rich source of bioactive compounds, and due to their good biological potential, they can be further exploited as functional ingredients beneficial to human health (antimicrobial agents, antioxidants).

Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents.

In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound 2j was found to be the most potent (MIC/MBC at 0.23-0.94 mg/mL and 0.47-1.88 mg/mL) On the other hand, compounds showed good antifungal activity (MIC/MFC at 0.06-0.47 and 0.11-0.94 mg/mL respectively) with 2d being the most active one. The docking studies revealed that inhibition of E. coli MurB and 14-lanosterol demethylase probably represent the mechanism of antibacterial and antifungal activities.

Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies.

Herein, we report the design, synthesis, and evaluation of the antimicrobial activity of new heteroaryl (aryl) thiazole derivatives. The design was based on a molecular hybridization approach. The in vitro evaluation revealed that these compounds demonstrated moderate antibacterial activity. The best activity was achieved for compound 3, with MIC and MBC in the range of 0.23-0.7 and 0.47-0.94 mg/mL, respectively. Three compounds (2, 3, and 4) were tested against three resistant strains, namely methicillin resistant Staphylococcus aureus, P. aeruginosa, and E. coli, which showed higher potential than the reference drug ampicillin. Antifungal activity of the compounds was better with MIC and MFC in the range of 0.06-0.47 and 0.11-0.94 mg/mL, respectively. The best activity was observed for compound 9, with MIC at 0.06-0.23 mg/mL and MFC at 0.11-0.47 mg/mL. According to docking studies, the predicted inhibition of the E. coli MurB enzyme is a putative mechanism of the antibacterial activity of the compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.

The Synthesis of Triazolium Salts as Antifungal Agents: A Biological and In Silico Evaluation.

The control of fungal pathogens is increasingly difficult due to the limited number of effective drugs available for antifungal therapy. In addition, both humans and fungi are eukaryotic organisms; antifungal drugs may have significant toxicity due to the inhibition of related human targets. Furthermore, another problem is increased incidents of fungal resistance to azoles, such as fluconazole, ketoconazole, voriconazole, etc. Thus, the interest in developing new azoles with an extended spectrum of activity still attracts the interest of the scientific community. Herein, we report the synthesis of a series of triazolium salts, an evaluation of their antifungal activity, and docking studies. Ketoconazole and bifonazole were used as reference drugs. All compounds showed good antifungal activity with MIC/MFC in the range of 0.0003 to 0.2/0.0006-0.4 mg/mL. Compound 19 exhibited the best activity among all tested with MIC/MFC in the range of 0.009 to 0.037 mg/mL and 0.0125-0.05 mg/mL, respectively. All compounds appeared to be more potent than both reference drugs. The docking studies are in accordance with experimental results.

Basidiocarp structures of Lentinus crinitus: an antimicrobial source against foodborne pathogens and food spoilage microorganisms.

Lentinus crinitus basidiocarps are an alternative to antimicrobials, but the stipe (24% basidiocarp) is discarded even with potential antimicrobial activity. This study evaluated the antimicrobial activity of L. crinitus basidiocarp pileus and stipe extracts against foodborne pathogens and food spoilage microorganisms. Basidiocarps of L. crinitus were grown in sugarcane bagasse and rice husks and the pileus and stipe methanolic extract was analyzed by broth microdilution method for antimicrobial activity against eight bacteria and eight fungi. The minimum bactericidal concentration values for pileus and stipe ranged from 0.40 to 0.50 mg mL- 1, for streptomycin from 0.10 to 0.50 mg mL- 1, and for ampicillin from 0.40 to 1.20 mg mL- 1. The minimum fungicidal concentration values for pileus and stipe ranged from 0.06 to 0.60 mg mL- 1, for bifonazole from 0.20 to 0.25 mg mL- 1, and for ketoconazole from 0.30 to 3.50 mg mL- 1. Extracts had bacteriostatic, bactericidal, fungistatic and fungicidal activity against all microorganisms, but with greater efficiency and specificity for some microorganisms. Both pileus and stipe are promising and sustainable alternatives for use in food, agricultural, and pharmaceutical industries.

Antimicrobial activity of Annona muricata leaf oleoresin.

Bioactive compounds extracted from plants such as antimicrobials have attracted the attention of consumers and the food industry. This study aimed to determine the antimicrobial activity and chemical composition of Annona muricata leaf oleoresin obtained by supercritical CO2 extraction. The oleoresin was obtained by supercritical CO2 extraction and the chemical identification by gas chromatography coupled to mass spectrometry. Antimicrobial activity was evaluated by broth microdilution method against 14 foodborne fungi and bacteria. The oleoresin major chemical class was phytosterols (22.7%) and the major compounds were γ-sitosterol (15.7%), α-tocopherol (13.7%), phytol (13.1%), and hexadecanoic acid (11.5%). Minimum inhibitory concentration against bacteria ranged from 0.0025 to 0.010 mg mL-1. The oleoresin had high bactericidal activity against all bacteria, mainly Enterobacter cloacae and Pseudomonas aeruginosa with 0.005 mg mL-1 minimum bactericidal concentration. However, it had low fungicidal activity. The leaf oleoresin of A. muricata has promising applications in food, cosmetic, and pharmaceutical industries.

4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation.

This manuscript deals with the synthesis and computational and experimental evaluation of the antimicrobial activity of twenty-nine 4-(indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole acylamines. An evaluation of antibacterial activity against Gram (+) and Gram (-) bacteria revealed that the MIC of indole derivatives is in the range of 0.06-1.88 mg/mL, while among fourteen methylindole derivatives, only six were active, with an MIC in the range of of 0.47-1.88 mg/mL. S. aureus appeared to be the most resistant strain, while S. Typhimurium was the most sensitive. Compound 5x was the most promising, with an MIC in the range of 0.06-0.12 mg/mL, followed by 5d and 5m. An evaluation of these three compounds against resistant strains, namely MRSA P. aeruginosa and E. coli, revealed that they were more potent against MRSA than ampicillin. Furthermore, compounds 5m and 5x were superior inhibitors of biofilm formation, compared to ampicillin and streptomycin, in terms Compounds 5d, 5m, and 5x interact with streptomycin in additive manner. The antifungal activity of some compounds exceeded or was equipotent to those of the reference antifungal agents bifonazole and ketoconazole. The most potent antifungal agent was found to be compound 5g. Drug likeness scores of compounds was in a range of -0.63 to 0.29, which is moderate to good. According to docking studies, E. coli MurB inhibition is probably responsible for the antibacterial activity of compounds, whereas CYP51 inhibition was implicated in antifungal activity. Compounds appeared to be non-toxic, according to the cytotoxicity assessment in MRC-5 cells.

Unravelling Anti-Melanogenic Potency of Edible Mushrooms Laetiporus sulphureus and Agaricus silvaticus In Vivo Using the Zebrafish Model.

Severe drawbacks associated with the topical use of depigmenting agents in treatments of skin hyperigmentations impose a great demand for novel, effective, and safe melanogenesis inhibitors. Edible and medicinal mushrooms, known for numerous health-promoting properties, represent a rich reservoir of anti-melanogenic compounds, with the potential to be applied in preventing excessive skin pigmentation. Herein, using zebrafish (Danio rerio) as a preclinical animal model, we have demonstrated that ethanol extract of Laetiporus sulphureus (LSE) and Agaricus silvaticus (ASE) are not toxic at high doses up to 400-500 µg/mL while effectively inhibit melanogenesis in a dose-dependent manner. At depigmenting doses, the explored extracts showed no adverse effects on zebrafish embryos melanocytes. Even more, they did not provoke inflammation or neutropenia when applied at the highest dose ensuring almost complete the cells depigmentation. Since LSE and ASE have demonstrated significantly higher the therapeutic potential than kojic acid and hydroquinone, two well-known depigmenting agents, overall results of this study strongly suggest that the explored mushrooms extracts could be used as efficient and safe topical agents in treatments of skin hyperpigmentation disorders.

LC-MS Based Analysis and Biological Properties of Pseudocedrela kotschyi (Schweinf.) Harms Extracts: A Valuable Source of Antioxidant, Antifungal, and Antibacterial Compounds.

The impact of two extraction solvents on the phenolic composition, antioxidant, and enzymes inhibitory and antimicrobial activities of two parts (leaves and stem bark) of P. kotschyi was studied. Two different LC-DAD-MSn approaches were used to identify and quantify the bioactive compounds in the different extracts. A total of thirty-two compounds were quantified, being the procyanidin the most abundant in stem bark while catechin and flavonoids are most abundant in leaves. Overall, the stem bark extraction using methanol showed higher amounts of total phenolic (131.83 ± 1.81 mg GAE/g) and flavanol (14.14 ± 0.11 mg CE/g) while the leaves extraction using water exhibited stronger levels of total flavonoid (44.95 ± 0.38 mg RE/g) and phenolic acid (63.58 ± 2.00 mg CAE/g). As regards the antioxidant assays, methanol stem bark extracts were characterized by the highest antioxidant activities (DPPH: 1.94 ± 0.01 mmol TE/g, ABTS: 3.31 ± 0.01 mmol TE/g, FRAP: 2.86 ± 0.02 mmol TE/g, CUPRAC: 5.09 ± 0.08 mmol TE/g, phosphomolybdenum: 5.16 ± 0.23 mmol TE/g and metal chelating: 17.12 ± 0.46 mg EDTAE/g). In addition, the methanolic extracts of stem bark had highest impact on acetylcholinesterase (2.54 mg GALAE/g), butyrylcholinesterase (5.48 mg GALAE/g). In contrast, the methanolic extracts of leaves was potent against tyrosinase (77.39 ± 0.21 mg KAE/g) and α-glucosidase (0.97 ± 0.01 mmol ACAE/g), while a higher anti-α-amylase (0.97 ± 0.01 mmol ACAE/g) was observed for water extracts of the same part. All of the tested extracts showed inhibitory effects on elastase, except methanolic leaves extracts. Additionally, the extracts exhibited appreciable antifungal toward A. ochraceus, A. fumigatus, P. ochrochloron, T. viride, and P. funiculosum and promising antibacterial activity against M. flavus, S. aureus, L. monocytogenes, E. coli, P. aeruginosa, E. cloacae, and S. typhimurium. Taken together, the outcomes demonstrated P. kotschyi as a novel source of bioactive molecules of interest with an evident therapeutic value.

Chromenol Derivatives as Novel Antifungal Agents: Synthesis, In Silico and In Vitro Evaluation.

Herein we report the synthesis of some new 1H-1,2,4-triazole functionalized chromenols (3a-3n) via tandem reactions of 1-(alkyl/aryl)-2-(1H-1,2,4-triazole-1-yl) with salicylic aldehydes and the evaluation of their antifungal activity. In silico prediction of biological activity with computer program PASS indicate that the compounds have a high novelty compared to the known antifungal agents. We did not find any close analog among the over 580,000 pharmaceutical agents in the Cortellis Drug Discovery Intelligence database at the similarity cutoff of 70%. The evaluation of antifungal activity in vitro revealed that the highest activity was exhibited by compound 3k, followed by 3n. Their MIC values for different fungi were 22.1-184.2 and 71.3-199.8 µM, respectively. Twelve from fourteen tested compounds were more active than the reference drugs ketoconazole and bifonazole. The most sensitive fungus appeared to be Trichoderma viride, while Aspergillus fumigatus was the most resistant one. It was found that the presence of the 2-(tert-butyl)-2H-chromen-2-ol substituent on the 4th position of the triazole ring is very beneficial for antifungal activity. Molecular docking studies on C. albicans sterol 14α-demethylase (CYP51) and DNA topoisomerase IV were used to predict the mechanism of antifungal activities. According to the docking results, the inhibition of CYP51 is a putative mechanism of antifungal activity of the novel chromenol derivatives. We also showed that most active compounds have a low cytotoxicity, which allows us to consider them promising antifungal agents for the subsequent testing activity in in vivo assays.

Antimicrobial activity, chemical composition and cytotoxicity of Lentinus crinitus basidiocarp.

Lentinus crinitus (L.) Fr. (Basidiomycota: Polyporales) is a wild mushroom with several biotechnological applications; however, there are few studies on its chemical composition and antimicrobial activity. Therefore, this study aims to evaluate the chemical composition, cytotoxicity, and antimicrobial activity of L. crinitus basidiocarp. For that, its nutritional value (AOAC procedures) and its composition in some hydrophilic and lipophilic compounds (chromatographic techniques) were assessed. Moreover, the potential hepatotoxic effects were evaluated using a primary cell culture obtained from porcine liver, and its growth inhibitory capacity was also evaluated against four human tumour cell lines (spectrophotometric assays). The antimicrobial activity was evaluated by microdilution against eight bacteria and fungi. The basidiocarp has a high content of carbohydrates and, therefore, a relatively high energetic value. It is also rich in soluble sugars, ß-tocopherol, phenolic acids, mainly p-hydroxybenzoic acid, and organic acids, mainly malic acid. L. crinitus did not show cytotoxicity in non-tumour cells, but it did not inhibit the growth of human tumour cell lines either. The basidiocarp has a wide antimicrobial activity, inhibiting the growth of different species of bacteria and fungi. It showed minimum bactericidal and fungicidal concentration values similar to or lower than those verified by commercial antibiotics or food additives used as preservatives. The antimicrobial activity was more evident against Listeria monocytogenes, Salmonella enterica, and Penicillium ochrochloron, followed by Aspergillus ochraceus and Trichoderma viride, when compared to the controls. The results obtained in this study showed that L. crinitus basidiocarp has great potential to be used by the industry without toxicity risks.

Ethnomycological Investigation in Serbia: Astonishing Realm of Mycomedicines and Mycofood.

This study aims to fill the gaps in ethnomycological knowledge in Serbia by identifying various fungal species that have been used due to their medicinal or nutritional properties. Ethnomycological information was gathered using semi-structured interviews with participants from different mycological associations in Serbia. A total of 62 participants were involved in this study. Eighty-five species belonging to 28 families were identified. All of the reported fungal species were pointed out as edible, and only 15 of them were declared as medicinal. The family Boletaceae was represented by the highest number of species, followed by Russulaceae, Agaricaceae and Polyporaceae. We also performed detailed analysis of the literature in order to provide scientific evidence for the recorded medicinal use of fungi in Serbia. The male participants reported a higher level of ethnomycological knowledge compared to women, whereas the highest number of used fungi species was mentioned by participants within the age group of 61-80 years. In addition to preserving ethnomycological knowledge in Serbia, this study can present a good starting point for further pharmacological investigations of fungi.

Chemical characterization of carob seeds (Ceratonia siliqua L.) and use of different extraction techniques to promote its bioactivity.

Nowadays, the use of carob (Ceratonia siliqua L.) is reduced to its seeds. In fact, the food additive E410, locust bean gum, is obtained from its endosperm. However, the available information regarding the bioactive potential of carob seeds is limited and, often, with poorly established terminologies, not allowing the reader to know if the studied samples included seedless or seeded samples. So, the present study intended to carry out a chemical characterization of carob seeds focused on their bioactive compounds and test their bioactive properties. Carob seeds proved to be a source of tocopherols and organic acids, including phenolic compounds. Its antioxidant potential was demonstrated in vitro, as well as its antimicrobial capacity. This work proves that carob seeds have other functions in addition to those associated with E410. Thus, another potential can be given to the locust bean seed, namely the function of food preservative.