Identification of sulphonamide-tethered N-((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease.

SARS-CoV-2 pandemic in the end of 2019 led to profound consequences on global health and economy. Till producing successful vaccination strategies, the healthcare sectors suffered from the lack of effective therapeutic agents that could control the spread of infection. Thus, academia and the pharmaceutical sector prioritise SARS-CoV-2 antiviral drug discovery. Here, we exploited previous reports highlighting the anti-SARS-CoV-2 activities of isatin-based molecules to develop novel triazolo-isatins for inhibiting main protease (Mpro) of the virus, a crucial enzyme for its replication in the host cells. Particularly, sulphonamide 6b showed promising inhibitory activity with an IC50= 0.249 µM. Additionally, 6b inhibited viral cell proliferation with an IC50 of 4.33 µg/ml, and was non-toxic to VERO-E6 cells (CC50 = 564.74 µg/ml) displaying a selectivity index of 130.4. In silico analysis of 6b disclosed its ability to interact with key residues in the enzyme active site, supporting the obtained in vitro findings.

Optimization of the production of roasted-nutty aroma by a newly isolated fungus Tolypocladium inflatum SRH81 and impact of encapsulation on its quality.

BACKGROUND: Pyrazines are used in food industry to impart the foods nutty-roasted flavor. However, their extraction from natural sources is difficult and expensive. At the same time, there is awareness against the chemical food additives. Microorganisms are approved as natural producers of flavors. The aim of the present study was to assess the ability of the newly isolated fungus Tolypocladium inflatum SRH81 to produce pyrazines and studying the effect of encapsulation in gum Arabic on the quality of the biogenerated volatiles. The parameters affecting the biogeneration of pyrazines were optimized. The headspace volatiles of each culture were isolated and identified by solid phase microextraction (HS-SPME) and gas chromatography coupled with mass spectrometry (GC-MS). The volatiles showed the highest pyrazines content and best nutty-roasty flavor was subjected to encapsulation. RESULTS: The selected fungus was identified as Tolypocladium inflatum SRH81. A high correlation was found between the consumed sugar and dry matter content of each culture. Incubation of the fungus culture enriched with 0.5 g amino acids/50 mL medium for 12 days at pH 8 showed the highest generation of pyrazines and best odor sensory quality. Nine pyrazines were identified among them 2-methylpyrazine was the major compound after incubation for 12 days. A positive correlation was found between the total pyrazines and intensity of roasty-nutty aroma. Encapsulation gave rise to a significant decrease in the total volatiles, while the odor intensity showed insignificant decrease. CONCLUSIONS: The results of the present study revealed the potential ability of Tolypocladium inflatum SRH81, that was isolated from Egyptian soil, to produce pyrazines having roasted- nutty aroma.

Productive Performance, Ovarian Follicular Development, Lipid Peroxidation, Antioxidative Status, and Egg Quality in Laying Hens Fed Diets Supplemented with Salvia officinalis and Origanum majorana Powder Levels.

This study aimed to assess the effect of dietary supplementation with different levels of Salvia officinalis and/or Origanum majorana on productive performance, ovarian follicular development, lipid peroxidation, antioxidative status, and egg quality in laying hens. Two hundred and ninety-four 45-week-old Bovans brown hens were allocated into seven groups, with seven replicates of six hens each. The first group was fed with the basal considered as a control (A); the second (B) and third (C) groups were provided with the same control diet further supplemented with 0.5 and 1 kg/ton Salvia officinalis, respectively; the fourth (D) and fifth (E) groups received the control diet further supplemented with 0.5 and 1 kg/ton Origanum majorana, respectively; while the sixth (F) and the seventh (G) groups were offered a diet supplemented with 0.5 kg/ton Salvia officinalis and 0.5 kg/ton Origanum majorana and 1 kg/ton Salvia officinalis and 1 kg/ton Origanum majorana, respectively. No significant effects were observed in the final body weight (BW) and feed intake (FI) of the laying hens. In the diets supplemented with Salvia officinalis and Origanum majorana, the egg weights for groups C, F, and G had significantly higher values only compared to group D. The supplementation of the diets with Salvia officinalis and/or Origanum majorana significantly (p < 0.05) increased the Follicle stimulating hormone (FSH), luteinizing hormone (LH), and estradiol estrogenic hormone concentration, except for Origanum majorana at both levels with regard to estradiol. The dietary utilization of Salvia officinalis and Origanum majorana did not significantly alter the plasma glutamic oxaloacetic transaminase (GOT) and glutamic pyruvic transaminase (GPT), total protein, albumin, globulin, and High density lipoprotein (HDL) parameters. Cholesterol, glucose, triglyceride, and Low density lipoprotein (LDL) were decreased (p < 0.05) in the birds fed with Salvia officinalis and/or Origanum majorana supplemented diets. Moreover, at both doses, the dietary supplementation with Salvia officinalis and Origanum majorana decreased (p < 0.05) the yolk cholesterol and liver Malondialdehyde (MDA) levels. In addition, the dietary enrichment with Salvia officinalis and/or Origanum majorana decreased (p < 0.05) the palmitoleic and stearic fatty acids' egg yolk concentration. In contrast, the yolk linoleic fatty acid concentration was significantly increased by Salvia officinalis and/or Origanum majorana. In conclusion, dietary supplementation with Salvia officinalis and/or Origanum positively affected productive performance, ovarian follicular development, antioxidant activity, hormonal status, and steroidogenesis in Bovans brown laying hens.

Biodegradation of dairy wastewater using bacterial and fungal local isolates.

Dairy wastewater contains high levels of organics and other pollutants. The present study was carried out to investigate the biodegradation process of dairy effluents using some locally isolated bacteria and fungi. Four different dairy effluent samples were collected from Obour and 6th October industrial cities, Egypt. Five bacterial species (Pseudomonas aeruginosa, Bacillus subtilis, Lactobacillus delbrueckii, Staphylococcus aureus and Enterococcus hirae) and three fungal strains (Alternaria sp., Fusarium sp. and Aspergillus sp.) were isolated from dairy wastewater samples, identified and used for biodegradation process. Bacterial and fungal consortia were prepared separately in the laboratory. Two-stages (aeration and filtration) laboratory scale model was designed. Rice straw and activated carbon layers were used as filtration media. Results indicated the great ability of both studied bacteria and fungi for removal of organics (biological oxygen demand removal percent were 78.7% and 74.7% for bacteria and fungi, respectively) and the improvement of the physicochemical quality (total suspended solids removal percent were 99.3% and 99.0% for bacteria and fungi, respectively) of the dairy effluent. The addition of rice straw and activated carbon increased removal efficiencies. Biodegradation of dairy wastewater depending on local microorganisms is an effective, cheap and eco-friendly technology.

Kojic Acid production from agro-industrial by-products using fungi.

A total of 278 different isolates of filamentous fungi were screened using synthetic medium for respective ability to produce kojic acid. Nineteen, six, and five isolates proved to be low, moderate, and high kojic acid producers, respectively. Levels of kojic acid produced were generally increased when shaking cultivation was used rather than those obtained using static cultivation. A trial for the utilization of 15 agro-industrial wastes or by-products for kojic acid production by the five selected higher kojic acid producer isolates was made. The best by-product medium recorded was molasses for kojic acid. A. flavus numbers 7 and 24 were able to grow and produce kojic acid on only 12 out of 15 wastes or by-products media. The best medium used for kojic acid production by A. flavus number 7 was rice fragments followed by molasses, while the best medium used for kojic acid production by A. flavus number 24 was the molasses followed by orange, pea, and rice fragments. An attempt for production of kojic acid using a 1.5 L laboratory fermentor has been made. Aspergillus flavus number 7 was used and grown on molasses medium; maximum level (53.5 g/L) of kojic acid was obtained after eight days of incubation.

Bacterial Biodegradation of Crude Oil Using Local Isolates.

An experimental study was undertaken to assess the efficiency of Pseudomonas aeruginosa, Bacillus subtilis, and Acinetobacter lwoffi isolated from petroleum contaminated water and soil samples to degrade crude oil, separately and in a mixed bacterial consortium. Capillary gas chromatography was used for testing the effect of those bacterial species on the biodegradation of crude oil. Individual bacterial cultures showed less growth and degradation than did the mixed bacterial consortium. At temperature 22°C, the mixed bacterial consortium degraded a maximum of 88.5% of Egyptian crude oil after 28 days of incubation. This was followed by 77.8% by Pseudomonas aeruginosa, 76.7% by Bacillus subtilis, and 74.3% by Acinetobacter lwoffi. The results demonstrated that the selected bacterial isolates could be effective in biodegradation of oil spills individually and showed better biodegradation abilities when they are used together in mixed consortium.