| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-576 | |
| Phytochemical name or plant extracts | Betulin | |
| PMID | 25885960 | |
| Literature evidence | H. syriacus extracts may provide important insight into the development of novel alternative therapies for breast cancer. | |
| IUPAC name | (1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(hydroxymethyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-icosahydro-1H-cyclopenta[a]chrysen-9-ol | |
| Phytochemicals’ class or type of plant extracts | Triterpenoid | |
| Source of phytochemicals or plant Extracts | Hibiscus Syriacus | |
| Geographical availability | China South-Central, China Southeast, Taiwan | |
| Plant parts | Root | |
| Other cancers | Breast cancer, Lung cancer, Liver cancer, Prostate cancer, Cervical cancer | |
| Target gene or protein | Bax, NOXA, PUMA, PERP, Bcl-x, TAp63, p21, Caspase 3, Bak, Caspase 7, Caspase 9, PARP | |
| Gene or Protein evidence | K02 (betulin) and K06 (betulinic acid) induced apoptotic protein expression, including BAX, NOXA, PUMA and PERP, and also increased caspase-3 cleavage as well reduced the anti-apoptotic gene Bcl-x in MDA-MB-231 and HBL100 cells, (3) K02 and K06 induced TAp63 in the p53- mutant MDA-MB-231 cell line, leading top53-related apoptosis, (4) betulin and its derivatives induced p21 activation and promoted cell cycle arrest. Importantly, Bax and Bak were rapidly translocated to the mitochondria 30 min after betulin treatment. The sequential activation of caspase-9 and caspase-3/-7 and the cleavage of poly(ADP-ribose) polymerase (PARP) were observed behind those mitochondrial events. Furthermore, specific downregulation of either caspase-9, Bax, or Bak by siRNA effectively reduced PARP cleavage and caspase-3 activation. | |
| Target pathways | Intrinsic apoptotic pathway | |
| IC50 | 13.6±1.7 μg/mL against MCF-7 | |
| Potency | The results showed that betulin significantly inhibited cell viability in cervix carcinoma HeLa cells, hepatoma HepG2 cells, lung adenocarcinoma A549 cells, and breast cancer MCF-7 cells with IC(50) values ranging from 10 to 15 microg/mL. | |
| Cell line/ mice model | HBL-100, MDA-MB-231, H184B5F5/M10, MCF-7, K562, HeLa, HepG2, A549, SK-HEP-1, PC-3, NCI-H460 | |
| Additional information | Betulin inhibited breast cancer cell viability and may have induced breast cancer cell apoptosis. | |
| PubChem ID | 72326 | |
| Additional PMIDs | 20564340 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:560890-1 | |
| Safety | NA |