Band 77, Heft 1-2

Isolation and bioactive effects of the roots of Chaerophyllum bulbosum L. were firstly investigated herein. Enzyme (acetylcholinesterase, butyrylcholinesterase, urease, α-amylase, α-glucosidase, and tyrosinase) inhibitory effects of C. bulbosum root extracts were tested. Three known compounds, n -heptadecanyl eicosanoate ( 1 ), stigmasterol ( 2 ), and β -sitosterol-3- O - β - d -glucopyranoside ( 3 ) were isolated from C. bulbosum . Antioxidant and enzyme inhibitory effects of isolated compounds were investigated. The hexane extract (IC 50 : 349.58 ± 0.06 μg/mL) displayed a higher α-glucosidase inhibitory effect than the standard (IC 50 : 378.66 ± 0.14 μg/mL). The best inhibitory effect was found in compound 2 on AChE (46.40 ± 0.31%), BChE (56.41 ± 0.54%), and urease (92.47 ± 0.11%); compound 1 on α-amylase (22.27 ± 0.61%); and compound 3 on α-glucosidase (12.43 ± 0.25%) and tyrosinase (19.00 ± 0.16%). All isolated compounds showed moderate antioxidant effects in all assays. This study contributes to the therapeutic uses of Chaerophyllum roots and emphasizes the value of C. bulbosum species for the development of novel therapeutic agents.

The fungus, Mortierella polycephala is one of the most productive sources of anticancer bioactive compounds namely those of pigment nature. During our investigation of the produced bioactive metabolites by the terrestrial M. polycephala AM1 isolated from Egyptian poultry feather waste, two main azaphilonoid pigments, monascin ( 1 ) and monascinol ( 2 ) were obtained as major products; their structures were identified by 1D ( 1 H& 13 C) and 2D ( 1 H– 1 H COSY, HMBC) NMR and HRESI-MS spectroscopic data. Biologically, cytotoxic activities of these compounds were broadly studied compared with the fungal extract. To predict the biological target for the presumed antitumor activity, an in silico study was run toward three proteins, topoisomerase II α , topoisomerase II β , and VEGFR2 kinase. Monascinol ( 2 ) was expected to be moderately active against VEGFR2 kinase without any anticipated inhibition toward topo II isoforms. The in vitro study confirmed the docked investigation consistently and introduced monascinol ( 2 ) rather than its counterpart ( 1 ) as a potent inhibitor to the tested VEGFR2 kinase. Taxonomically, the fungus was identified using morphological and genetic assessments.

The importance of organometallic complexes in cancer biology has attracted attention in recent years. In this paper, we look for the in vitro cytotoxic capability of novel benzimidazole-based N-heterocyclic carbene (NHC) precursor ( 1 ) and its Ag(I)-NHC complex ( 2 ). For this purpose, these novel Ag(I)-NHC complex ( 2 ) was characterized by spectroscopic techniques ( 1 H, 13 C{ 1 H} nuclear magnetic resonance (NMR), and Fourier-transform infrared spectroscopy (FT-IR)). Then, in vitro cytotoxic activities of NHC precursor ( 1 ) and Ag(I)-NHC complex ( 2 ) were investigated against MCF-7, MDA-MB-231 human breast, DU-145 prostate cancer cells, and L-929 healthy cells using MTT assay for 24, 48, and 72 h incubation times. Ag(I)-NHC complex ( 2 ) showed promising in vitro cytotoxic activity against all cell lines for three incubation times, with IC 50 values lower than 5 µM. It was also determined that (NHC) precursor ( 1 ) were lower in vitro cytotoxic activity than Ag(I)-NHC complex ( 2 ) against all cell lines. Selectivity indexes (SI s ) of Ag(I)-NHC complex ( 2 ) against cancer cells were found higher than 2 for 24 and 48 h incubation time. Besides, the electronic structure and spectroscopic data of the newly synthesized precursor and its Ag-complex have been supported by density functional theory (DFT) calculations and molecular docking analysis. After, the anticancer activity of these compounds has been discussed considering the results of the frontier molecular orbital analysis. We hope that the obtained results from the experiments and computational tools will bring a new perspective to cancer research in terms of supported by quantum chemical calculations.

The inflammasome as a multiprotein complex has a role in activating ASC and caspase-1 resulting in activating IL-1β in various infections and diseases like corona virus infection in various tissues. It was shown that these tissues are affected by COVID-19 patients. According to the current evidence, melatonin is not veridical while possessing a high safety profile, however, it possesses indirect anti-viral actions owing to its anti-oxidation, anti-inflammation, and immune improving properties. This study aims to assess the impacts of melatonin as the complementary treatments on oxidative stress agents and inflammasome activation in patients with COVID-19. Melatonin supplement (9 mg daily, orally) was provided for the patients hospitalized with a COVID-19 analysis for 14 days. For measuring IL-10, IL-1β, and TNF-α cytokines and malondialdehyde (MDA), nitric oxide (NO), and superoxide dismutase (SOD) level and the expression of CASP1 and ASC genes, blood samples were gathered from the individuals at the start and termination of the therapy. Our findings indicated that melatonin is used as a complementary treatment to reduce the levels of TNF-α and IL-1β cytokines, MDA, and NO levels in COVID-19 patients and significantly increase SOD level, however, the levels of IL-10 cytokine possesses no considerable changes. The findings revealed that genes of CASP1 and ASC were dysregulated by melatonin regulating the inflammasome complex. Based on the findings of the current study, it is found that melatonin can be effective as a medicinal supplement in decreasing the inflammasome multiprotein complex and oxidative stress along with beneficial impacts on lung cytokine storm of COVID-19 patients.

Poly-N-acetyl- d -glucosamine (CH; chitin) is the main component of the insect skeleton, fungal cell wall, and many crustaceans, including crab and shrimp. CH is the most abundant in nature after cellulose, and it has a complex and hardly soluble structure. Poly- d -glucosamine (CHO; chitosan) is a soluble derivative of CH produced by deacetylation used in many fields, including human health. This study carried out the cytotoxic, genotoxic, and oxidative effects of CHO on human whole blood (hWB) and lymphocytes (LYMs) in dose ranges 6.25–2000 μg/mL, in vitro . Total antioxidant capacity (TAC) and total oxidant status (TOS) analyzes were performed on plasma to appreciate oxidative stress. 3-(4,5-Dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays were applied to understand the cytotoxicity. Chromosomal aberration (CA) and micronucleus (MN) methods were practiced to evaluate genotoxicity. 6.25–150 μg/mL doses increased TAC and decreased TOS. A decreasing and increasing curve from 200 to 2000 μg/mL on TAC and TOS values were determined, respectively. 0–250 μg/mL doses did not provide any cytotoxic data. However, 500–2000 μg/mL doses showed increasing cytotoxicity and genotoxicity. The study results showed that CHO does not pose a toxic risk to human health at low doses but may pose a threat at high doses.

The emergence of antibacterial resistance has significantly increased. Pseudomonas aeruginosa is associated with nosocomial infection and difficult to control. Artocarpin, a flavonoid from Artocarpus heterophyllus Lam. exhibits several pharmacological properties including antibacterial. The study was performed to evaluate interaction between artocarpin and antibiotics including tetracycline against P. aeruginosa . Its mechanism of action on membrane permeability was also investigated. Broth microdilution was conducted for the susceptibility assay. The interaction of artocarpin and antibiotics was evaluated using checkerboard method, the effect on alteration of membrane cell was investigated using bacteriolysis and the released of 260 nm materials. Artocarpin showed moderate to weak activity against the Gram-negative bacteria including P. aeruginosa with MIC values in the range of 31.25–250 μg/mL. A synergistic effect against P. aeruginosa was produced by the combination of artocarpin (31.25 μg/mL) and tetracycline (1.95 μg/mL) with FICI of 0.37. The time-killing assay showed that artocarpin enhance the antibacterial activity of tetracycline against  P. aeruginosa by completely inhibiting the bacterial growth. Additionally, the mixture of artocarpin (31.25 μg/mL) and tetracycline (1.95 μg/mL) disrupted membrane permeability and lead to cell death. These results proposed that the combination of artocarpin and tetracycline may be used to overcome P. aeruginosa infection.

After wreaking havoc on a global level with a total of 5,488,825 confirmed cases and 349,095 deaths as of May 2020, severe acute respiratory syndrome coronavirus 2 is truly living up to the expectations of a 21st-century pandemic. Since the major cause of mortality is a respiratory failure from acute respiratory distress syndrome, the only present-day management option is supportive as the transmission relies solely on human-to-human contact. Patients suffering from coronavirus disease 2019 (COVID-19) should be tested for hyper inflammation to screen those for whom immunosuppression can increases chances of survival. As more and more clinical data surfaces, it suggests patients with mild or severe cytokine storms are at greater risk of failing fatally and hence these cytokine storms should be targets for treatment in salvaging COVID-19 patients.

Probiotics are living organisms that have beneficial effects on host by regulating the microbial balance of the intestinal system. While probiotics are naturally found in yogurt and other fermented foods, they can also be added to many products. Although mostly in dairy products, it is possible to see examples of food products supplemented by probiotics in bakeries, chocolates and confectioneries. Nowadays, the COVID-19 pandemic that the world suffers increased the demand for such functional food products including probiotics. Due to probiotics having potential effects on strengthening the immune system, confectioneries supplemented by probiotics were comprehensively discussed in this review together with the suggestion of a novel gelly composition. The suggested formulation of the product is a gel-like snack contains natural ingredients such as carrot, lemon juice and sugar provided from apples. This research review article provided a guide together with the recommendations for potential probiotic research in candy and confectionery industry.