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The tyrosinase inhibitory activity and inhibition mechanism of pyrimidine-2-thiol (PT) and pyrimidine-2,4-dithiol (PDT) were investigated. In the anti-tyrosinase activity evaluation assay, PT exhibited 2-fold stronger activity than kojic acid in the presence of L-Tyrosine and L-Dopa, and PDT showed 13 times higher activity than kojic acid, respectively. Kinetic analysis revealed PT and PDT acted as mixed inhibitors. Copper ions chelation, fluorescence quenching, H NMR titration, and molecular docking assays manifested PT and PDT could participate in chelation with copper ions in the tyrosinase. Furthermore, UV and CD assay results suggested that PT or PDT could induce conformational changes in tyrosinase. Critically, both compounds delayed fresh-cut apple browning and did not exhibit appreciable toxicity on normal cells. These findings demonstrate that PT and PDT are highly potent, safe, and promising tyrosinase inhibitors, with significant potential as novel anti-browning agents for extending the shelf life of fresh-cut fruits in the food industry.
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http://dx.doi.org/10.1016/j.foodchem.2025.146057 | DOI Listing |
ACS Omega
September 2025
Centre of Artificial Intelligence Driven Drug Discovery, Faculty of Applied Science, Macao Polytechnic University, Macao SAR 999078, China.
Tyrosinase, a copper-dependent oxidase, plays a critical role in melanin biosynthesis and is a target in skin-whitening cosmetics. Conventional inhibitors like arbutin and kojic acid are widely used but suffer from cytotoxicity, instability, and inconsistent efficacy, highlighting the need for safer, more effective alternatives. In this study, two ligand-based machine learning models were developed: one to predict the biological activity of compounds and the other to estimate specific pIC values.
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August 2025
Engineering Laboratory of Peptides of Chinese Academy of Sciences, Key Laboratory of Bioactive Peptides of Yunnan Province, KIZ-CUHK Joint Laboratory of Bioresources and Molecular Research in Common Diseases, National Resource Center for Non-Human Primates, National Research Facility for Phenotypic
Background: Fairmaire is a medicinal insect that has been used for a long time by minority ethnic groups in Yunnan, China, due to its immunomodulatory function. However, its potential applications in cosmetics have not been reported.
Methods: experiments were used to verify whether the extracts of Fairmaire (EBR) have the effect of inhibiting TYR activity and eliminating melanin deposition.
Food Sci Nutr
September 2025
Physiology and Biochemistry Laboratory, Department of Biology, Science Faculty Selcuk University Konya Turkey.
The current investigation was designed to explore the chemical composition, antioxidant capacity, enzyme inhibitory activity, and cytotoxic potential of four different extracts (Ethyl Acetate, Ethanol, Ethanol/Water (70%) and Water) derived from the aerial parts of . In vitro, assessments were performed utilizing diverse antioxidant assays, along with evaluations of neuroprotective enzyme inhibition targeting acetylcholine and butyl choline enzymes, as well as antidiabetic activities against α-amylase and α-glucosidase and a potential candidate for a tyrosinase inhibitor. LC-ESI-QTOF-MS identification provided a total of 70 compounds in the extracted samples of , including kaempferol 3-(deoxyhexosyl-hexoside)-7-hexoside, rutin, quercetin dideoxyhexoside, caffeic acid hexoside, quinoline alkaloids, morphine derivatives, and scoulerine.
View Article and Find Full Text PDFChem Biodivers
August 2025
Chemical, Pharmacological and Gallenic Development Laboratory, Faculty of Pharmacy, University of Monastir, Monastir, Tunisia.
Collagenase and tyrosinase are key enzymes involved in skin aging and melanin synthesis, making the search for effective natural inhibitors increasingly important in cosmetic and pharmaceutical fields. In this context, the present study explores the chemotaxonomy, antioxidant capacity, and enzyme inhibitory potential of essential oils (EOs) from three Tunisian varieties of Cupressus sempervirens: var. horizontalis, var.
View Article and Find Full Text PDFPlants (Basel)
August 2025
Department of Biomedical Sciences, Chung Shan Medical University, Taichung City 402, Taiwan.
Carnivorous plants have garnered attention as sources of pharmacologically active compounds, yet their floral tissues remain largely underexplored. In this study, we investigated the bioactive properties of flower extracts prepared using water, methanol, ethanol, and acetone. Among these, the ethanol extract exhibited the highest total phenolic content (18.
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