Vinburnine exhibits a wide range of bioactivities encompassing antimalarial, anticancer, antiviral, and DNA replication-modulating properties. It demonstrates significant inhibition of the malarial parasite plastid, with potency values ranging from 2332.3 nM to 13115.4 nM, and it inhibits growth in various human tumor cell lines with GI50 values between 1309.18 nM and 100000.0 nM. The compound also induces DNA re-replication in normal breast cells and colon adenocarcinoma cells, and shows potency in inhibiting interactions related to Hepatitis C Virus, Vif-A3G interactions, GLP-1 Receptor, and ATXN expression.
In addition, Vinburnine inhibits human tyrosyl-DNA phosphodiesterase 1 (TDP1) in the presence and absence of CPT and exhibits synthetic lethality in tumor cells as well as inhibition of Vaccinia Orthopoxvirus. The compound blocks the entry of Ebola Virus in various assays. It also shows significant activity as an acetylcholinesterase (AChE) inhibitor but exhibits much lower activity against horse butyrylcholinesterase (BChE).
Cytotoxicity assays reveal that Vinburnine has potent cytotoxic effects on various human cell lines, including KMS-12-BM, U266, RPMI8226, LNCAP, and MDA-MB-231 cells, with an IC50 value of 41800.0 nM against MDA-MB-231 cells after 96 hours. It also demonstrates high inhibition of sodium fluorescein uptake in OATP1B1-transfected and OATP1B3-transfected CHO cells, suggesting potent inhibitory effects on these transporters.
Furthermore, Vinburnine shows antiviral activity against SARS-CoV-2, inhibiting cytotoxicity in Caco-2 and VERO-6 cells at 10 µM concentrations, with various degrees of efficacy. The compound also exhibits 9.522% inhibition of SARS-CoV-2 3CL-Pro protease at a concentration of 20 µM and moderate inhibition of human HDAC6 in enzymatic assays.
Overall, Vinburnine is a multifunctional compound with potential applications in treating malaria, cancer, and viral infections, including SARS-CoV-2..
Note: Summary generated by AI. Data source: ChEMBL 