Oxyphenonium bromide exhibits diverse bioactivities across various biological assays. It demonstrates significant potency in multiple quantitative high-throughput screening (qHTS) assays, including 730.8 nM for lipid storage modulators in Drosophila S3 cells, 1122.0 nM for inhibitors of cell surface uPA generation, 281.8 nM for TGF-b inhibitors, and 1258.9 nM for DNA re-replication in SW480 colon adenocarcinoma cells. Additionally, it shows varied potencies in primary qHTS assays for delayed death inhibitors of the malarial parasite plastid (11689.1 nM and 13115.4 nM), Nrf2 inhibitors (ranging from 7307.8 nM to 18356.4 nM), HP1-beta chromodomain interactions inhibitors (112201.8 nM), and inhibitors of Pin1 (44668.4 nM).
Moreover, Oxyphenonium bromide displays antiviral activities, including inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 cells (1.46% inhibition at 10 µM) and VERO-6 cells (0.37% inhibition at 10 µM). It also acts as a SARS-CoV-2 3CL-Pro protease inhibitor with a 9.003% inhibition at 20 µM, as determined by a FRET assay. Furthermore, it exhibits an AC50 of 7.943 µM for blocking Ebola Virus entry.
In terms of antibacterial and antifungal activities, Oxyphenonium bromide inhibits various strains including Escherichia coli (3.27% inhibition), Klebsiella pneumoniae (20.0% inhibition), Pseudomonas aeruginosa (14.05% inhibition), Acinetobacter baumannii (27.96% inhibition), and Staphylococcus aureus MRSA (12.65% inhibition). It also demonstrates antifungal activity against Candida albicans with 2.42% inhibition, while showing negative inhibition against Cryptococcus neoformans (-6.44%), indicating lack of activity or possible stimulation.
Overall, Oxyphenonium bromide's bioactivities encompass inhibiting lipid storage, various enzymes, viral entry, and exhibiting antibacterial and antifungal effects, highlighting its broad-spectrum potential..
Note: Summary generated by AI. Data source: ChEMBL 