| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-82 | |
| Phytochemical name or plant extracts | Triptolide | |
| PMID | 1819894 | |
| Literature evidence | The results suggest that Tri might have a potential therapeutic effect on some types of solid tumors, e.g., breast and stomach cancers. | |
| IUPAC name | (1S,2S,4S,5S,7R,8R,9S,11S,13S)-8-hydroxy-1-methyl-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-17-one | |
| Phytochemicals’ class or type of plant extracts | Diterpenoid | |
| Source of phytochemicals or plant Extracts | Tripterygium wilfordii | |
| Geographical availability | China South-Central, China Southeast, Myanmar, Taiwan, Tibet, Vietnam | |
| Plant parts | NA | |
| Other cancers | Breast cancer, Stomach cancer, Leukemia | |
| Target gene or protein | ADAM10, ATM, PARP-1, XRC1, RAD51, miR-146a, Bcl-2 family, RhoA, Rac1, PD-L1, CD206, Arginase 1, CD204, NF-κB, AP-1, MMP9, Notch-1, HES-1, HEY-1, DCLK1, ALDH1, CD133 | |
| Gene or Protein evidence | Triptolide treatment of MCF-7 breast cancer cells expressing ectopic ADAM10 or dominant negative ADAM10 (DN ADAM10) resulted in a decreased expression of ADAM10 with a concomitant increase in ADAM10 cleaved products. Triptolide reportedly inhibits RNA polymerase II-mediated transcription and ATM activities to interfere with DNA repair. Western blot analysis shows triptolide down-regulated the levels of PARP1 and XRCC1, and slightly decreases the levels of RAD51. miRNAome variation in MDA-MB-231 cells with or without triptolide treatment demonstrated that miR-146a was upregulated following treatment with triptolide. Tritpolide-induced ERK activation modulated the expression of the Bcl-2 protein family member Bax but was not involved in the downregulation of Bcl-xL expression. In addition, following treatment with triptolide, the expression of RhoA and Rac1 was found to be decreased. Triptolide, a natural compound purified from the Chinese herb Tripterygium wilfordii, has been reported to inhibit PD-L1 otherwise known as the B7 homolog 1 (B7-H1) expression in breast cancer. Furthermore, triptolide inhibited the expression of M2 markers, such as CD206, Arginase 1, and CD204, and inhibited the secretion of anti-inflammatory cytokines. The results demonstrated that triptolide decreased the expression of MMP-9 through inhibition of the TPA-induced phosphorylation of extracellular signal-regulated kinase (ERK) and the downregulation of nuclear factor-κB (NF-κB) and activator protein-1 (AP-1) activity. Both celastrol or triptolide reduced Notch -1 activation and expression of its downstream target proteins HES-1 and HEY-1. Furthermore, the compound suppressed expression of cancer stem cell marker proteins DCLK1, ALDH1, and CD133. | |
| Target pathways | NF-κB and AP-1 signaling Wnt/β-catenin signaling pathway ERα-mediated signaling pathway p53 pathway PD-1/PD-L1 pathway | |
| IC50 | 0.504-1.22 μg/L | |
| Potency | Triptolide (5-200 nmol/L) dose-dependently inhibited the viability of both MCF-7 and MDA-MB-231 cells, with a more potent inhibition on MCF-7 cells. Triptolide, an extract of Tripterygium wilfordii, has been shown to have a potent anticancer activity. In vitro, TPL inhibited the proliferation and colony formation of tumor cells at extremely low concentrations (2-10 ng/ml) and was more potent than Taxol. Since its isolation from Tripterygium wilfordii in 1972, triptolide has been shown to possess potent anticancer activity against a variety of cancers, and has entered phase I clinical trial. | |
| Cell line/ mice model | MCF-7, BT-20,MKN-45, MKN-7, KATO-III, HL-60 , MDA-MB-231, BT-474 | |
| Additional information | In addition, Triptolide could also induce interleukin-2 secretion and overcome interleukin-10 inhibition caused by glioma cells under IFN-γ treated condition. In addition, TPL inhibited experimental metastasis of B16F10 cells to the lungs and spleens of mice. In addition, a Transwell assay revealed that triptolide reduced the ability of MCF-7 cells to invade Matrigel. | |
| PubChem ID | 107985 | |
| Additional PMIDs | 25009609 25864647 30563138 1842005 21486687 24043955 31289559 31072418 27609747 18572307 30551406 33924995 31663424 19783906 23467622 25047443 1819894 34093777 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:162908-1 | |
| Safety | Acute toxic in pubmed database. |