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Emergence of COVID-19 and thereafter intensive research on bioactive natural compounds against SARS-CoV-2, identified a large number of phytochemicals (i.e., plants-derived) and mycochemicals (i.e., fungi-derived) as potential inhibitors with proven antiviral properties against SARS-CoV-2, but there are no comparative study on the reported compounds. A comparative study among the previously identified/reported main protease (Mpro) inhibitors of SARS-CoV-2 can lead to the most potent compound that eventually helps to make an effective drug lead against SARS-CoV-2. Through manual literature curation, we selected 57 potential bioactive compounds and screened them against Mpro protein of SARS-CoV-2. A series of in silico screening such as binding affinity, drug-like properties, pharmacokinetic, physicochemical, and ADMET studies identified top ten compounds as potential Mpro inhibitors. Further, docking studies prioritized the top two compounds namely Norquinadoline A and Quinadoline B, based on their predicted affinity for the target protein. Binding free energy calculations further emphasized them as top candidates for effective Mpro inhibitors that hold promise for drug development against COVID-19. In-depth molecular dynamics studies and MM/PBSA analysis culminated in the recognition of Norquinadoline A as the most potent Mpro inhibitor of SARS-CoV-2. Thus, Norquinadoline A can be used as lead compound in further drug discovery process after in vitro and in vivo experimental studies.

Type-2 diabetes affects an increasing percentage of the world's population and its control through dietary management, involving the consumption of health-promoting foods or their derived supplements, is a common strategy. Several mushroom species have been demonstrated to be endowed with antidiabetic properties, resulting from their ability in improving insulin sensitivity and production, or inhibiting the carbohydrate-hydrolyzing enzymes α-amylase and α-glucosidase. This study aimed to investigate for the first time the hypoglycemic properties of the edible mushroom Leccinum scabrum (Bull.) Gray. Mushroom extracts were prepared through the microwave-assisted extraction (MAE) technique using green solvents with different polarity degrees. The inhibition activity of all the obtained extracts on both α-glucosidase and α-amylase was evaluated and the highest activity was observed for the EtOAc extract which showed an IC50 value about 60-fold lower than the reference compound 1-deoxynojirimycin (DNJ) on α-glucosidase (0.42 ± 0.02 and 25.4 ± 0.6 µg/mL, respectively). As expected on the basis of the literature data concerning both α-glucosidase and α-amylase inhibition, a milder inhibition activity on pancreatic α-amylase was observed. Preliminary in vivo tests on Drosophila melanogaster carried out on the most active obtained extract (EtOAc) confirmed the in vitro observed hypoglycemic activity. Finally, the EtOAc extract metabolic profile was determined through GC-MS and HRMS analyses. [ABSTRACT FROM AUTHOR]

Basidiomycetes found in forest ecosystems have been used traditionally as food and medicine for centuries, and various studies have validated many of their health benefits. In recent years, the focus in medicinal basidiomycetes has increased, and several notable trends in their application and research have been observed. In light of the emerging literatures, this review attempts to summarise and discuss evidences from the past decade on the importance of exploring basidiomycetes for their pharmacological properties. It also aims to serve as a critical reference for research works focused on the potentials of wild basidiomycetes in Malaysia, as well as from worldwide, to produce a diverse range of bioactive metabolites. Special attention is given to the low-molecular weight bioactive compounds produced in cultured mycelium and culture broth of these macrofungi. It further highlights the unique attributes of wild bioluminescent basidiomycetes species which hold great potential to be harnessed for mycopharmaceuticals with commercial applications in healthcare industries. [ABSTRACT FROM AUTHOR]

Since ancient times, mushrooms have been considered valuable allies of human well-being both from a dietary and medicinal point of view. Their essential role in several traditional medicines is explained today by the discovery of the plethora of biomolecules that have shown proven efficacy for treating various diseases, including cancer. Numerous studies have already been conducted to explore the antitumoural properties of mushroom extracts against cancer. Still, very few have reported the anticancer properties of mushroom polysaccharides and mycochemicals against the specific population of cancer stem cells (CSCs). In this context, β-glucans are relevant in modulating immunological surveillance against this subpopulation of cancer cells within tumours. Small molecules, less studied despite their spread and assortment, could exhibit the same importance. In this review, we discuss several pieces of evidence of the association between β-glucans and small mycochemicals in modulating biological mechanisms which are proven to be involved with CSCs development. Experimental evidence and an in silico approach are evaluated with the hope of contributing to future strategies aimed at the direct study of the action of these mycochemicals on this subpopulation of cancer cells. [ABSTRACT FROM AUTHOR]

The present study aims to explore the dietary nutrient levels of the edible mushroom, A. bisporus by biochemical analysis and evaluated their medicinal value in treating the human pathogenic microorganisms and free radical scavenging effects. A. bisporus mushroom exhibits a high amount of carbohydrates (41.6 ± 0.66 %) and crude proteins (39.84 ± 0.66 %). The crude fibre (8.6 ± 0.42 %), ash (8.23 ± 0.44 %), nitrogen (protein) contents (9.1 ± 0.44 %) were available at a significant level and also possessed a lesser amount of fat (1.73 ± 0.33 %). The quantitative determination of mycochemicals in A. bisporus reveals the presence of flavonoids (0.783 ± 0.03 g/100 g), phenolic content (0.441 ± 0.01 g/100 g), free amino acids (0.128 ± 0.12 g/100 g), saponin (0.121 ± 0.01 g/100 g), alkaloids (0.034 ± 0.01 g/100 g), tannins (0.027 ± 0.03 g/100 g) and vitamin C (12.8 ± 0.33 mg/g). Flame photometer and Inductivity Coupled Plasma Optical Emission Spectrometry (ICP-OES) study reveals the presence of minerals viz., potassium (2925.14 ± 0.67 mg/100 g), phosphorus (1230 ± 0.67 mg/100 g), magnesium (115.05 ± 0.24 mg/100 g) and calcium (107.21 ± 0.34 mg/100 g) in A. bisporus mushroom. Moreover, the Fourier transform infrared (FTIR) spectrum established the presence of possible biomolecules in A. bisporus mushroom. A greater antimicrobial effect against Staphylococcus aureus (14.3 ± 0.24 mm) and Candida albicans (14.2 ± 0.12 mm) was observed compared to Streptococcus pyogenes (10.8 ± 0.12 mm), Shigella flexneri (10.8 ± 0.21 mm), Klebsiella pneumoniae (11.1 ± 0.33 mm) and Aspergillus fumigatus (11.2 ± 0.33 mm). The mushroom extract of A. bisporus have an excellent radical scavenging activity with an IC 50 of 12.5 µg/mL against 1,1-diphenyl-2-picrylhydrazyl (DPPH). This investigation revealed that A. bisporus mushroom has great potential to be used as food supplement to fight against pathogens in the near future. [Display omitted] • Biochemical evaluation of dietary nutrients in A. bisporus were determined. • Functional mycochemicals in A. bisporus were confirmed by FTIR spectra. • bisporus showed antimicrobial effects against clinically important pathogens. • bisporus showed DPPH radical scavenging activity. [ABSTRACT FROM AUTHOR]

Pluteus cervinus is a mushroom species that demands a systematic study of its medicinal values. This study aims to explore the mycochemical contents of Pluteus cervinus extract, and evaluate their anti-diabetic and antioxidant potency. Twelve organic compounds were identified using Gas Chromatogram-Mass Spectroscopy(GC-MS) analysis of the methanolic extract. All the mycochemicals identified were evaluated for their drug-likeness, pharmacokinetics and bioactivity using admetSAR and molinspiration webservers. The extract was evaluated for the inhibitory effect of α-amylase and DPPH free radical scavenging ability. To further support the anti-diabetic and antioxidant characteristic, in silico molecular docking analysis was done for all the identified mycochemicals. It was found that, 2-(3,4-dimethoxyphenyl)-N-[4-(4-methoxyphenyl)-tetrahydropyran-4-ylmethyl]-acetamide, one of the compounds in the extract shares structural similarity and comparable docking binding energy with natural α-amylase inhibitor. Further, the 2-(3,4-dimethoxyphenyl)-N-[4-(4-methoxyphenyl)-tetrahydropyran-4-ylmethyl]-acetamide also showed high binding energy with Human peroxiredoxin 5 and has a structural relationship with natural antioxidants containing tetrahydropyran derivatives. [ABSTRACT FROM AUTHOR]

The mushrooms have contributed to the development of active ingredients of fundamental importance in the field of pharmaceutical chemistry as well as of important tools in human and animal health, nutrition, and functional food. This review considers studies on the beneficial effects of medicinal mushrooms on the nutrition and health of humans and farm animals. An overview of the chemical structure and composition of mycochemicals is presented in this review with particular reference to phenolic compounds, triterpenoids and sterols, fatty acids and lipids, polysaccharides, proteins, peptides, and lectins. The nutritional value and chemical composition of wild and cultivated mushrooms in Italy is also the subject of this review which also deals with mushrooms as nutraceuticals and the use of mushrooms in functional foods. The nutraceutical benefits of UV irradiation of cultivated species of basidiomycetes to generate high amounts of vitamin D2 is also highlighted and the ability of the muhsrooms to inhibit glycation is analyzed. Finally, attention is paid to studies on bioactivities of some Italian wild and cultivated mushrooms with particular reference to species belonging to the genus Pleurotus. The review highlights the potential of medicinal mushrooms in the production of mycochemicals that represent a source of drugs, nutraceutical, and functional food. [ABSTRACT FROM AUTHOR]

Hericium erinaceus (Bull.) Persoon, a popular medicinal edible mushroom, owns a long history of usage in traditional Chinese medicine and also in other oriental countries. Along with this, its several bioactive compounds have been evolved into food supplements. Meanwhile, this present investigation aimed at extracting bioactive components from fruiting bodies of H. erinaceus using two different solvents and evaluating its in vitro antioxidant, antimicrobial, and antiproliferative efficacy. Chemical analysis showed extracts were rich in phenol, flavonoids, and ascorbic acids while lesser amount of carotenoids were also detected in these extracts. Both extracts were able to scavenge 1,1‐diphenyl‐2‐picrylhydrazyl (~76%) and 2,2′‐azinobis‐(3‐ethylbenzthiazoline‐6‐sulphonate) radicals (~81%) and also showed chelating activity (~73.05%). The ethanolic extract exhibited the highest antioxidant activity (total antioxidant capacity 2.17 µg ascorbic acid equivalent/mg of extract) whereas methanolic extract showed moderate capacity (total antioxidant capacity 1.42 µg ascorbic acid equivalent/mg of extract). All extracts displayed antibacterial activity against both Gram‐positive and Gram‐negative bacteria as well (minimum inhibition concentration 1,575–2,750 µg/ml) although methanolic extract showed some selectivity towards bacterial strains. Apart from these, ethanolic fraction has found to exhibit potent cytotoxicity (IC50 403.12 µg/ml) towards lung adenocarcinoma cells. These studies thus provide the reference data that could support this mushroom as an easily accessible source of natural bioactive components. Practical applications: Mushroom extracts have long been traditionally used as miracle medicine to treat an extensive range of ailments. These findings indicate the potential benefits of the Hericium erinaceus (Bull.) Persoon extracts for the development of multi‐target therapeutics as well as extraction with appropriate solvents also provide leads for the isolation of various principle compounds. The extracts thus could be used to treat oxidative stress‐related disorders as they are found to contain antioxidant compounds like phenols and others and also they possessed good antimicrobial and anticancer activity. [ABSTRACT FROM AUTHOR]

The present study aimed at the evaluation of chemical composition and bioactive potential of methanolic extract obtained from Lepista sordida in terms of antioxidative and antimicrobial efficacy. The macrofungus is recognized for its high nutritional value and medicinal properties. However, to the best of our knowledge bioactivity of its methanolic extract is yet to be explored. In this investigation, quantitative analysis of mycochemicals revealed the extract contained significant amount of phenolic compounds such as phenols and flavonoids. Ascorbic acid was found in higher amount than β carotene and lycopene which were present in vestigial amounts. A phenolic profile was also determined using high performance liquid chromatography that further confirmed the presence of 10 phenolic constituents in the extract. Furthermore, the extract was subjected for determining antioxidant potential in different in-vitro assays. The findings showed remarkable 2, 2-Diphenyl-1-picrylhydrazyl and ABTS radical scavenging ability which was evident by low EC50 values, 330 µg/mL and 30 µg/mL respectively. The extract also demonstrated good chelating and reducing ability, an important marker of antioxidant compounds. Antimicrobial screening displayed positive results against Staphylococcus aureus and Escherichia coli. Altogether, the observations recommend therapeutic application of this mycotaxon on a commercial basis.

Present study deals with the plectological and molecular analysis as well as use of economically important wild Russuloid mushrooms against food pathogenic fungus Aspergillus niger. Three different species of mushrooms viz., Russla laeta, R. nobilis, and R. nigricans were collected and identified from Himalayan range of Pakistan and are found as new records for this country. Major objective of this study was to highlight the importance of these wild creatures as antifungal agents against A. niger. For this purpose methanolic extract of selected mushrooms of different concentration levels viz., 1, 1.5, 2 and 3% were used. This activity is also first time reported from Pakistan by using this group of mushrooms. Results showed that all tested mushrooms exhibit growth inhibition of A. niger and can be used as biocontrol agents. R. nigricans showed maximum inhibition of fungus growth that is 62% at 3% concentrations while minimum inhibition was observed in R. nobilis at same concentration that is 43.6%. [ABSTRACT FROM AUTHOR]

The present study was carried out to find out mycochemical profile of culture filtrates of Alternaria japonica through GC-MS analysis. The fungus was incubated for 21 days using malt extract broth as growth medium. Culture filtrate was filtered and concentrated by evaporating water at 45 °C. Filtrates were partitioned using n-hexane followed by chloroform. Both the organic solvent fractions were analyzed through GC-MS. In n-hexane and chloroform fractions, 14 and 10 compounds were identified, respectively. Major compounds in n-hexane fraction were o-xylene (36.9%); ethyl benzene (19.3%), hexane, 2-4-dimethyl- (16.8%), 1-2 dimethylbenzene (7.56%), cyclohexane, 1-ethyl-1-methyl (3.36%), heptane, 2,5-dimethyl- (3.36%) and octane, 4-methyl- (2.52%). Likewise, predominant compounds in chloroform fraction were octane-4 methyl (24.62%), carbonic dihydrazine (16.41%), octane, 2,4,6-trimethyl (12.56%), hydrazine, (1,1-dimethylethyl) (8.75%), 16-hexadecanoyl hydrazide (7.66%) and stearic acid hydrazide (7.08%). Literature surveyed showed that many compounds identified in both the fractions possess antimicrobial, pharmacological, antioxidant, antidepressant, anticancer and anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

Mycochemical composition, calorific value, the antioxidant activity of Pleurotus tuber- regium was analyzed and impact of P. tuber- regium extract on rat model especially glycemic, vitamins and blood parameters were explored to validate its medicinal importance. Mycochemical screening showed the presence of biochemicals such as phenols, flavonoids, proteins, carbohydrates etc. The extract showed good antioxidant activity (33.62% total antioxidant activity equivalent to 21.30 µg ascorbic acid). The extract showed dose -dependent hypoglycaemic activity by significant decreased average blood glucose level at high dose (100.62 ± 1.04mg/dL) compare to control (124.40 ± 1.45 mg/dL), haematinic activity by elevation of hemoglobin (14.75 ± 0.24 g/dL) at a high dose of extract compared to control (11.66 ± 0.21 g/dL). P. tuber-regium extract elevated vitamin B12 of rats at high dose of extract (449.60 ± 3.12 pg/mL) compared to control (420.00 ± 2.86pg/mL). P. tuber-regium extract showed a positive response to hypoglycemic, haematinic, and vitamin level of the body and posses high calorific value. Hence P. tuber-regium can be used as good fodder, medicinal and nutritional supplement. [ABSTRACT FROM AUTHOR]

Biomass of Aspergillus awamori was investigated for mycochemicals, total phenolic compounds (TPC), condensed tannin content (CTC), free-radical scavenging potential (FRSP), and DNA damage protection activity. FRSP was determined using DPPH, ABTS, FRAP (Ferric reducing antioxidant power), metal chelating activity, and cupric reducing antioxidant capacity) assays. Water (Aq), aqueous ethanol 50% (AqE), and methanol were used as extraction phase at 44.5 °C for 23.8 min. AqE shows the presence of maximum mycochemicals (coumarins, glucose, saponins, flavonoids, and tannin). Further quantitative analysis shows maximum TPC (23.17 mg GAE/g dwb) in AqE and CTC (.89 mg CE/g dwb) in ME. Qualitative and quantitative analysis for identification of specific bioactive compound in AqE was carried out using HPLC. HPLC analysis confirmed the presence of bioactive compounds: p′-Coumaric acid (5.96 mg/g dwb), cinnamic acid (4.31 mg/g dwb), gallic acid (2.27 mg/g dwb), and ascorbic acid (.98 mg/g dwb). All the extracts show significant DNA damage protection activity; however, AqE showed the maximum activity. Pearson correlations were also calculated to find the relationships between bioactive compounds and antioxidant potential. [ABSTRACT FROM AUTHOR]

Pleurotus is a genus of edible mushrooms widely cultivated throughout the world in a variety of substrates and conditions which have an impact on the content of macronutrients and mycochemicals. It is an excellent source of crude fiber and β-glucans (10.3% and 25.9%, respectively). Particularly for P. ostreatus , the Amino Acid Score (AAS) meets the nutritional requirements of all essential amino acids for adults. The use of substrates containing bioactive compounds or supplemented with minerals, as well as postharvest treatments are some strategies to increase the nutraceutical value of Pleurotus species. P. ostreatus contains high quality protein and fiber (mainly β-glucans) that may be used as a functional food ingredient. Polysaccharides bioactivity and functionality depend on the degree of polymerization, branching and esterification with sulfates and other substituents groups. Pleurotus genus possess a unique mycochemical profile with proven antimicrobial, antiviral, anticancer, antioxidant, hypolipidemic, hypocholesterolemic, antihyperglycemic and immunomodulatory effects. It has been demonstrated that Pleurotus flour can be incorporated into baked goods and dairy products without significantly affecting their functional properties or sensorial attributes. The elaboration of processed foods supplemented with Pleurotus flour is a promising area of study to enhance their nutritional and nutraceutical values. [ABSTRACT FROM AUTHOR]

Fungal strain Aspergillus oryzae (MTCC 3107) was screened for antioxidant, anti-cancer, and debittering applications. Three different extraction solvents (water, aqueous ethanol 50%, and methanol 100%) were used to extract bioactive compounds from fungal biomass. Further mycelial mass was recovered, dried, and evaluated for mycochemicals and antioxidant properties. Naringinase production by A. oryzae was observed as 19.28 IU/mL. Treatment of Kinnow juice with crude fungal enzyme results a decrease in naringin and limonin content by 59.6% and 41.2% respectively. Bioactive metabolites (phenolics and condensed tannins) in fungal extracts were ranged from 13.73 to 20.08 mg GAE (gallic acid equivalent)/g and 0.62–1.81 mg CE (catechin equivalent)/g, respectively. Mycochemicals observed in fungal extracts were flavonoids, steroids, tannins, and saponins. Fungal extract showed the presence of gallic acid (1.18–2.43 μg/g), catechol (1.60 μg/g), ascorbic acid (2.9–4.09 μg/g), p -Coumaric acid (0.56–0.83 μg/g), benzoic acid (0.33–0.91 μg/g), and cinnamic acid (0.17 μg/g). An aqueous-alcohol (ethanol 50%) extract prepared from dried fungal biomass (45 °C, 30 min) showed significant antitumor potential against model MCF-7 breast cancer cell line by about 44% inhibition. After toxicological analysis, A. oryzae extracts could be used in the preparation of health benefiting food and pharmaceutical formulations. [Display omitted] • A. oryzae was studied for antioxidant properties and debittering potential. • Effect of different extraction phase on bioactive profile was studied. • HPLC was performed to identify bioactive metabolites and bitter compounds. • Limonin and naringin content of Kinnow juice was reduced by 41.2% and 59.6%. [ABSTRACT FROM AUTHOR]

• This is the first study of lipophilic mycochemicals in H. novae-zealandiae. • Two compounds unique to Hericium Chen et al., 2019a , 2019b , hericenone C and hericene B were identified. • Three compounds were isolated as hericene B, ergosterol and ergosterol peroxide. • An HPLC-DAD method was developed to quantify hericene B for the first time. • The content of hericene B was 28.53 mg/g DW (nearly 3%) of H. novae-zealandiae. Hericium novae-zealandiae is a native mushroom consumed by indigenous Māori people in New Zealand. The lipophilic mycochemicals of the mushroom were isolated using a normal column chromatography combined with a preparative HPLC. Structural characterisation based on spectroscopic methods, namely UV, MS, NMR and single crystal XRD have identified three lipophilic compounds as hericene B (a compound unique to Hericium), ergosterol and ergosterol peroxide. Following this, an HPLC-DAD method was developed and validated to quantify the hericene B and ergosterol. The method showed excellent selectivity, linearity, precision, accuracy and robustness. The content of hericene B was determined as 28.53 mg/g by dry weight of H. novae-zealandiae (approximately 3%). This discovery indicates the potential utilisation of H. novae-zealandiae as a natural source of hericene B. Current research revealed for the first time, the lipophilic constituents of H. novae-zealandiae and the method development for quantification of hericene B in the above species. [ABSTRACT FROM AUTHOR]