| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-2112 | |
| Phytochemical name or plant extracts | Budlein A methylacrylate (BAM) | |
| PMID | 33022283 | |
| Literature evidence | New therapeutic agents with unique mechanisms of action are urgently needed; therefore, this study investigated the potential anti-TNBC effects of budlein A methylacrylate (BAM), a natural sesquiterpene lactone isolated from plants of the Helianthus genus. | |
| IUPAC name | NA | |
| Phytochemicals’ class or type of plant extracts | Sesquiterpene lactone | |
| Source of phytochemicals or plant Extracts | Helianthus genus | |
| Geographical availability | NA | |
| Plant parts | NA | |
| Other cancers | Breast cancer | |
| Target gene or protein | IκBα kinase, exportin-1 | |
| Gene or Protein evidence | Budlein A methylacrylate demonstrates potent activity against triple-negative breast cancer by targeting IκBα kinase and exportin-1 | |
| Target pathways | NA | |
| IC50 | 1.45–6.29 μM against MDA-MB-231, MDA-MB-453, MDA-MB-436 | |
| Potency | In conclusion, this study provides evidence that co-inhibition of IKKβ and XPO-1 by BAM was effective against TNBC, demonstrating it as a representative new generation inhibitor with potential for TNBC treatment. | |
| Cell line/ mice model | MDA-MB-231, MDA-MB-453, MDA-MB-435, MDA-MB-468, HCC1937, HCC2218, HCC1954, HCC202, HCC1500, MCF-7 | |
| Additional information | Mechanistically, BAM co-inhibited inhibitor of nuclear factor κBα (IκBα) kinase subunit β (IKKβ) and exportin-1 (XPO-1; chromosome region maintenance 1, CRM1), which are two dysregulated onco-related proteins in TNBC cells, by covalently modifying key functional cysteine residues (Cys179 of IKKβ, Cys528 of XPO-1). Dual inhibition led to the stabilization and nuclear retention of IκBα, impairment of NF-κB transcriptional activity, and consequent induction of TNBC cell apoptosis. | |
| PubChem ID | NA | |
| Additional PMIDs | NA | |
| Additional sources of information | NA | |
| Safety | NA |