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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]

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 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]

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]