Publication date: Jul 03, 2025
Viral infections, including arboviruses such as chikungunya, zika, dengue, and mayaro fever, remain significant global health and economic challenges, fueled by the emergence and resurgence of mosquito-borne diseases. Natural products, especially plant-derived compounds, have been crucial in drug discovery and often serve as scaffolds for synthetic drug development. This study focused on modifying paulownin, an isolated lignan, through a Click reaction to incorporate 1,2,3-triazole and quinolinic ring frameworks. The resulting derivative 7 was evaluated for its in vitro antiviral activity against Alphavirus chikungunya (CHIKV). The paulownin derivative 7 did not exhibit cytotoxicity in Vero cells and demonstrated potent activity against CHIKV, with median effective concentration value of 9. 05 uM and a selectivity index exceeding 16. 8. Furthermore, compound 7 outperformed positive controls, being over 46 times more active against CHIKV. Cytopathic effect assays confirmed this anti-CHIKV activity. The virucidal assay indicated that the compound does not exert a direct effect on CHIKV particles before cell infection. RT-qPCR studies further demonstrated derivative 7 significantly reduces CHIKV replication. These findings highlight the paulownin derivative 7 as a promising and selective candidate for CHIKV treatment.
| Concepts | Keywords |
|---|---|
| Arboviruses | alphavirus |
| Chloroquinoline | click chemistry |
| Effective | drug discovery |
| Global | pharmaceuticals |
| Microbiol | viral replication inhibitor |
Semantics
| Type | Source | Name |
|---|---|---|
| pathway | KEGG | Viral replication |
| disease | IDO | replication |
| disease | MESH | infection |
| disease | IDO | cell |
| disease | IDO | assay |
| disease | MESH | mosquito-borne diseases |
| disease | MESH | dengue |
| disease | MESH | Viral infections |