| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1083 | |
| Phytochemical name or plant extracts | Osthole | |
| PMID | 28350076 | |
| Literature evidence | Osthole, an active constituent isolated from the fruit of Cnidium monnieri (L.) Cusson, has been shown to induce various beneficial biochemical effects such as anti-inflammatory and antitumor. | |
| IUPAC name | 7-methoxy-8-(3-methylbut-2-enyl)chromen-2-one | |
| Phytochemicals’ class or type of plant extracts | Coumarin | |
| Source of phytochemicals or plant Extracts | Cnidium monnieri | |
| Geographical availability | Amur, Assam, Bangladesh, Buryatiya, China North-Central, China South-Central, China Southeast, Chita, India, Inner Mongolia, Irkutsk, Japan, Khabarovsk, Korea, Krasnoyarsk, Laos, Manchuria, Mongolia, Primorye, Qinghai, Taiwan, Tibet, Vietnam, Yakutskiya | |
| Plant parts | Fruits | |
| Other cancers | Breast cancer, Kidney cancer, Glioma | |
| Target gene or protein | GPX1, SOD2, GCL-c, G6pdh, NOX2, ACOX, FASN, c-met, c-FLIP, Bax, Akt, mTOR, p53, p21, Cdk2, cyclin D1 Caspase 3, Caspase 9 | |
| Gene or Protein evidence | Consistently, osthole significantly enhanced the expressions of antioxidant genes (GPX1, SOD2, GCL-c, and G6pdh), but suppressed those of pro-oxidant genes (NOX2 and ACOX). The use of Akt-overexpression revealed that the modulation of Akt and mTOR was required for osthole-induced FASN suppression. Interestingly, osthole blocked HGF-induced c-Met phosphorylation and repressed the expression of total c-Met protein in MCF-7 cells. Osthole induced downregulation of cellular FLICE-like inhibitory protein (c-FLIP) expression, and overexpression of c-FLIP markedly blocked apoptosis induced by the combined treatment with osthole and TRAIL. Moreover, osthole induced apoptosis by activating the pro-apoptotic protein, Bax, in both cell lines. We demonstrated that osthole is effective in inhibiting the proliferation of MDA-MB 435 cells, The mitochondrion-mediated apoptotic pathway was involved in apoptosis induced by osthole, as indicated by activation of caspase-9 and caspase-3 followed by PARP degradation. The mechanism underlying its effect on the induction of G1 phase arrest was due to the up-regulation of p53 and p21 and down-regulation of Cdk2 and cyclin D1 expression. | |
| Target pathways | c-Met/Akt/mTOR pathway Akt/mTOR pathway | |
| IC50 | NA | |
| Potency | These results suggested that osthole has the potential to advance as chemopreventive or chemotherapeutic agent for cancers that overexpress HER2. | |
| Cell line/ mice model | MDA-MB-231, MDA-MB-435, Caki, U251MG, | |
| Additional information | Osthole preferentially inhibited proliferation and induced apoptosis in HER2-overexpressing cancer cells. Moreover, osthole inhibited the phosphorylation of Akt and mTOR. | |
| PubChem ID | 10228 | |
| Additional PMIDs | 30315252 33727922 20622464 28938572 21806057 31731635 20218616 25859268 28350076 22017625 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:840463-1 | |
| Safety | NA |