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•2-thiohydantoin derivatives were synthesized and enaminone function was discussed at position 5 using DMFDMA catalyst.•Elucidation of the target compound’s structure and ...configuration using 2D NMR.•Molecular docking studies were conducted to assess the inhibitory potential of the target compounds against the aromatase cytochrome P450 enzyme.
A set of novels 2-thiohydantoin derivatives were synthesized and enaminone function was discussed at position 5 using DMFDMA catalyst which result in formation of pyrazole, isoxazole, benzoxazepine by using reagents such as hydrazine, hydroxylamine and 2-aminothiophenol. These newly synthesized compounds were evaluated for their antioxidant and antiproliferative activity. In vitro studies on the effect of 2-thiohydantoin on scavenging 2,2-diphenyl-1-picrylhydrazyl radical (DPPH•) confirmed the free radical scavenging and antioxidant activity of 2-thiohydantoin. The synthesized compounds show significant antioxidant activity. The in vitro antitumor activity of 2-thiohydantoin on MCF7 (breast) and PC3 cells (prostate) was evaluated using MTT assay. Some of the synthesized compounds show significant to moderate antiproliferative properties compared to reference drug erlotinib. Among all, compound 4a exhibit potent antitumor properties against MCF7 and PC3 cancer cell lines with IC50 = 2.53 ± 0.09 /ml & with IC50 = 3.25 ± 0.12 µg/ml respectively and has potent antioxidant activity with IC50 = 10.04 ± 0.49 µg/ml.
•Antioxidant films based on chitosan or starch containing thyme extract were obtained.•Thyme extract changed the microstructural and physical properties of the films.•Crosslinking between polyphenols ...and chitosan enhanced filḿs mechanical response.•Antioxidant activity of thyme extract was better preserved when using chitosan films.
The aim of this study was to analyse the antioxidant activity of different polymeric matrices based on chitosan and starch, incorporating a thyme extract (TE) rich in polyphenols. TE provided the films with remarkable antioxidant activity. When mixed with chitosan, the polyphenols interacted with the polymer chains, acting as crosslinkers and enhancing the tensile behaviour of films. The opposite effect was observed when incorporated into the starch matrix. All the films became darker, more reddish and less transparent when TE was incorporated. These colour changes were more marked in starch matrices, which suggests that TE compounds were poorly encapsulated. The use of chitosan-based matrices carrying TE polyphenols is recommended as a means of obtaining antioxidant films, on the basis of their tensile response and greater antioxidant activity, which could be associated with the development of polyphenol-chitosan interactions, contributing to a better protection of the functionality of polyphenols during film formation and conditioning.
The mycofabricated metal nanoparticles (NPs) plays a significant role in cancer therapeutics and imparts a strategy in medicine. The current investigation focused to synthesize the Copper Oxide ...Nanoparticles (CuONPs) using an endophytic fungus isolated from Aegle marmelosa medicinal tree located in Western Ghats, India. The endophytic fungus FCBY1 explored the highest antagonistic and antioxidant activities among the 16 pigmented endophytic fungal strains which were isolated from the collected samples. The fungus FCBY1 was identified for its morphological and molecular characteristics where the (Internal Transcribed Spacer) ITS 1, 5.8 ribosomal gene and ITS 2 were sequenced; and the organism FCBY1 is Aspergillus terreus. The endophyte was put through for the synthesis of CuONPs and the size and structure of the synthesized particles were characterized by Scanning Electron Microscope (SEM). The confirmation of the CuONPs was characterized by FT-IR, EDAX and XRD analyses. The CuONPs exhibited the maximized antibacterial and antifungal activities against the human clinical pathogens; moreover the particles also explicated the free radicals/ROS scavenging at minimum concentration, which was assessed through DPPH, nitric oxide radical scavenging assays, and reductive power ability. The anti-cancer activity of CuONPs on colon cancer cell lines (HT-29) was evaluated by MTT (IC50: 22 μg/mL) and FACS analyses (32.11% cells gated in S phase of cell cycle). Angiogenesis inhibition in tumor cells was estimated through in vivo HET- CAM assessment and the highest concentration 60 μL tested inhibited the blood vessels at the percentage of 31.36% and 81.81%. The CuONPs explicated the anti-cancer activities in a concentration – dependent manner and the results of this investigation manifest the significant role of the CuONPs in cancer therapeutics.
•Copper oxide nanoparticles were synthesized using Aspergillus terreus FCBY1.•Synthesized nanoparticles were characterized using FTIR, XRD and SEM.•Nanoparticles displayed antibacterial, antifungal and radical scavenging activities.•Anti-cancer properties of nanoparticles evaluated on HT-29 cell lines.•The inhibition of angiogenesis was assessed via in vivo HET- CAM assessment.
Food-derived antioxidant peptides have become the focus of research due to their high safety and low cost. However, the discovery is suffering from a low efficient and empirical approach, involving ...multi-step off-line separation and identification. In this work, an on-line stop-flow RPLC × SEC-MS/DPPH radical scavenging activity analysis system was developed. For optimization, the conditions: 10 m reaction loop, 200 μM DPPH radical concentration, 40℃ temperature and 0.06 % formic acid were recommended. The system was fully validated by its application in glutathione analysis. The system was further applied in analysis of complex mixed standards, and the dipeptides GC (Gly-Cys) and CW (Cys-Trp) with relatively strong DPPH radical scavenging activity were validated. Maize protein hydrolysates were used for tests and the peptide AC (Ala-Cys) of high probability with strong DPPH radical scavenging activity was identified, demonstrating a high potential of the system. This would help to facilitate the discovery of antioxidative peptides in the future.
•The aroma characteristics of chaya leaves were investigated for the first time.•3-Methylbutanal, with a malt-like aroma, is the key volatile in dried chaya leaves.•Oven drying (120 °C) enhances ...5′-ribonucleotide content 3-fold in dried chaya leaves.•Umami taste was most pronounced in oven-dried (120 °C) and pan-roasted samples.•Freeze-dried chaya leaves exhibited the highest antioxidant activity levels.
Chaya (Cnidoscolus chayamansa) leaves are known for their strong umami taste and widespread use as a dried seasoning. This study aimed to assess the impact of different drying methods freeze drying (FD), vacuum drying, oven drying at 50 °C and 120 °C (OD120) and pan roasting (PR) on the metabolome using mass spectrometry, umami intensity, and antioxidant properties of chaya leaves. The predominant volatile compound among all samples, 3-methylbutanal, exhibited the highest relative odor activity value (rOAV), imparting a malt-like odor, while hexanal (green grass-like odor) and 2-methylbutanal (coffee-like odor) are the second highest rOAV in the FD and PR samples, respectively. OD120 and PR samples possessed the highest levels of umami-tasting amino acids and 5′-ribonucleotides as well as the most intense umami taste, whereas FD samples exhibited the highest antioxidant capacity. These findings enhance our understanding of the aroma characteristics, umami taste, and antioxidant potential of processed chaya leaves.
Bovine colostrum is the initial milk produced after birth that contains high levels of immunoglobulins and antimicrobial peptides. This study examined the production of bovine colostrum powder using ...two methods including spray- and freeze-drying. Spray-drying involves quickly drying a liquid or slurry with hot gas, while freeze-drying is a low-temperature dehydration process that preserves the product by freezing it and at reduced pressure. The aim was to compare the effectiveness of spray-drying versus freeze-drying in producing colostrum powder, focusing on protein and defensive protein content. The freeze-drying sample contained higher levels of protein and defensive proteins (IgG and IgA) compared to spray-drying. The DPPH value was high in freeze-dried samples, while higher values of FRAP, TPC, and ABTS were found in spray-dried samples. Microbiological analysis indicated freeze drying generally yielding lower counts. Sensory evaluation suggested that spray-dried colostrum scored higher for flavor and aroma, while freeze-dried samples were preferred in appearance. Overall, the study underscored the distinction between spray=drying and freeze-drying in producing bovine colostrum powder, with implications for nutritional content and sensory attributes.
