| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1976 | |
| Phytochemical name or plant extracts | Parthenolide | |
| PMID | 31080076 | |
| Literature evidence | Parthenolide, a natural product from the feverfew plant and member of the large family of sesquiterpene lactones, exerts multiple biological and therapeutic activities including anti-inflammatory and anti-cancer effects. | |
| IUPAC name | (1S,2R,4R,7E,11S)-4,8-dimethyl-12-methylidene-3,14-dioxatricyclo[9.3.0.02,4]tetradec-7-en-13-one | |
| Phytochemicals’ class or type of plant extracts | Sesquiterpene lactone | |
| Source of phytochemicals or plant Extracts | Tanacetum parthenium | |
| Geographical availability | Afghanistan, Albania, Bulgaria, East Aegean Is., Greece, Iran, Iraq, Krym, Pakistan, Transcaucasus, Turkey, Turkey-in-Europe, West Himalaya, Yugoslavia | |
| Plant parts | NA | |
| Other cancers | Breast cancer, Cervical cancer, Liver cancer | |
| Target gene or protein | AMPK, JNK, NF-κB, STAT-3, MAP kinase, FAK1 | |
| Gene or Protein evidence | Here, we showed that parthenolide increased reactive oxygen species (ROS), induced cell death, activated AMPK and autophagy, and led to M phase cell cycle arrest in breast cancer cells. In this report, we show that parthenolide activates c-Jun N-terminal kinase (JNK), which is independent of inhibition of NF-kappaB DNA binding and generation of reactive oxygen species. The antitumor activity of the sesquiterpene lactone parthenolide, an active ingredient of medicinal plants, is believed to be due to the inhibition of DNA binding of transcription factors NF-kappaB and STAT-3, reduction in MAP kinase activity and the generation of reactive oxygen. We find that parthenolide, as well as other related exocyclic methylene lactone-containing sesquiterpenes, covalently modify cysteine 427 of focal adhesion kinase 1 (FAK1), leading to impairment of FAK1-dependent signaling pathways and breast cancer cell proliferation, survival, and motility. | |
| Target pathways | NF-κB/IkappaB signaling pathway | |
| IC50 | 16.35 ± 0.27 μM against MDA-MB-231 | |
| Potency | EC50 = 2.8 microg/mL against MCF-7 | |
| Cell line/ mice model | Hs605T, MCF-7, SiHa, MCF-7/HER2, MDA-MB-231, BT-474 | |
| Additional information | The experimental results showed that MZ-6 and parthenolide suppressed, to a similar degree, migration of MCF-7, but not more aggressive MDA-MB-231 cells. These results identify a new antitumor activity of parthenolide, which can be exploited to reverse resistance of cancer cells to TRAIL, particularly those with elevated XIAP levels. Antitumor agent parthenolide reverses resistance of breast cancer cells to tumor necrosis factor-related apoptosis-inducing ligand through sustained activation of c-Jun N-terminal kinase. | |
| PubChem ID | 7251185 | |
| Additional PMIDs | 15286701 29519321 31080076 33810340 15015572 24619908 21992414 23065294 31012734 26089941 24405079 15743683 16579729 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:252460-1 | |
| Safety | NA |