| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1246 | |
| Phytochemical name or plant extracts | Xanthohumol | |
| PMID | 25044854 | |
| Literature evidence | METHODS AND RESULTS: ABCG2-inhibitory activity of xanthohumol (XN), isoxanthohumol (IX), 6-prenylnaringenin (6-PN), 8-prenylnaringenin (8-PN), and 6,8-diprenylnarigenin (6,8-diPN) was evaluated using mitoxantrone accumulation and vesicular transport assays. | |
| IUPAC name | (E)-1-[2,4-dihydroxy-6-methoxy-3-(3-methylbut-2-enyl)phenyl]-3-(4-hydroxyphenyl)prop-2-en-1-one | |
| Phytochemicals’ class or type of plant extracts | Flavonoid | |
| Source of phytochemicals or plant Extracts | Humulus lupulus | |
| Geographical availability | Much of Europe, including Britain, to W. Asia | |
| Plant parts | NA | |
| Other cancers | Breast cancer, Colon cancer, Ovarian cancer | |
| Target gene or protein | EGFR, STAT-3, PHB2, NIS | |
| Gene or Protein evidence | Multi-drug resistance 1 (MDR1), epidermal growth factor receptor (EGFR) and signal transducer and activator of transcription 3 (STAT3) expression levels in MCF-7/ADR cells were suppressed by xanthohumol treatment. XN treatment effectively prevented the BIG3-PHB2 interaction, thereby releasing PHB2 to directly bind to both nuclear- and cytoplasmic ERα. This event led to the complete suppression of the E2-signalling pathways and ERα-positive breast cancer cell growth both in vitro and in vivo, but did not suppress the growth of normal mammary epithelial cells. Our findings suggest that XN may be a promising natural compound to suppress the growth of luminal-type breast cancer. Northern blot analysis showed no difference in NIS mRNA transcript levels between control cells and those treated with different concentrations of XN. | |
| Target pathways | NA | |
| IC50 | 6.7 µM against MDA-MB-231 | |
| Potency | Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone. | |
| Cell line/ mice model | MDA-MB-231, SKBR-3, MCF-7, HT-29, A-2780 | |
| Additional information | Xanthohumol is under investigation in clinical trial NCT01367431 (Xanthohumol and Metabolic Syndrome). | |
| PubChem ID | 639665 | |
| Additional PMIDs | 23562496 23246576 16092068 25483453 | |
| Additional sources of information | https://www.drugbank.ca/drugs/DB15359 | |
| Safety | NA |