| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1215 | |
| Phytochemical name or plant extracts | Indole-3-carbinol | |
| PMID | 22012859 | |
| Literature evidence | Expression of the wild type and Δ205 elastase in MDA-MB-231 human breast cancer cells demonstrated that the carboxyterminal domain of elastase is required for the I3C and 1-benzyl-I3C inhibition of enzymatic activity, accumulation of the unprocessed form of the CD40 elastase substrate (a tumor necrosis factor receptor family member), disruption of NFκB nuclear localization and transcriptional activity, and induction of a G1 cell cycle arrest. | |
| IUPAC name | 1H-indol-3-ylmethanol | |
| Phytochemicals’ class or type of plant extracts | 3-alkylindoles | |
| Source of phytochemicals or plant Extracts | Brassica oleracea | |
| Geographical availability | France, Great Britain, Spain | |
| Plant parts | NA | |
| Other cancers | Breast cancer, Prostate cancer, Cervical cancer | |
| Target gene or protein | BRCA1, EGFR , MUC1, BRCA1, BRCA2, p53, MDM2, GATA3, ERalpha | |
| Gene or Protein evidence | Suppression of breast cancer invasion and migration by indole-3-carbinol: associated with up-regulation of BRCA1 and E-cadherin/catenin complexes. EGFR and Src are involved in indole-3-carbinol-induced death and cell cycle arrest of human breast cancer cells. In this report, we demonstrate that the naturally occurring cancer preventative, indole-3-carbinol (I3C), inhibits the expression of MUC1 in breast cancer cells. BRCA1 and BRCA2 as molecular targets for phytochemicals indole-3-carbinol and genistein in breast and prostate cancer cells. I3C promotes the interaction of nucleostemin with MDM2 (Murine Double Mutant 2), an inhibitor of the p53 tumor suppressor, and disrupts the MDM2 interaction with p53. I3C also induced nucleostemin to sequester MDM2 in a nucleolus compartment, thereby freeing p53 to mediate its apoptotic activity. I3C inhibits endogenous binding of ERalpha with the 3'-enhancer region of GATA3 and disrupts endogenous GATA3 interactions with the ERalpha promoter, leading to a loss of GATA3 and ERalpha expression. | |
| Target pathways | We have identified a new target for the chemopreventive dietary agent indole-3-carbinol (13C) in the antiapoptotic signaling pathway involving phosphatidylinositol 3'-kinase and protein kinase B (PKB)/Akt. 13C inhibited phosphorylation and activation of PKB in the tumor-derived breast cell line MDA MB468, but not in the immortalized breast line HBL100. | |
| IC50 | 30 µM against MDA-MB-468 | |
| Potency | Indole-3-carbinol (I3C) is a promising phytochemical agent in chemoprevention of breast cancer. | |
| Cell line/ mice model | MDA-MB-231, T47D, MCF-7, MDA-MB-468, PC3, LNCaP, DU-145, 10AT-Her2, tumor xenograft | |
| Additional information | Indole 3 Carbinol is under investigation in clinical trial NCT00033345 (Indole-3-Carbinol in Preventing Breast Cancer in Nonsmoking Women Who Are at High Risk For Breast Cancer). Furthermore, expression of an I3C-resistant form of elastase, the only known target protein for I3C, prevented I3C anti-proliferative responses in cells and in tumor xenografts in vivo, as well as disrupt the I3C stimulated nucleostemin-MDM2 interactions. | |
| PubChem ID | 3712 | |
| Additional PMIDs | 34066056 11525599 16434996 16152627 18025290 18486294 19064917 20130088 33925607 9496644 15665315 12479697 11739883 19056653 21767081 21234288 1893517 7846734 9168187 10449193 12738179 16488130 19864400 28382865 10652612 8912651 12570340 11931841 11849035 12840220 15840385 16544949 18023427 17515958 20570586 22012859 25209720 30715794 10096555 12094623 10825461 10653634 15027113 9547584 30972283 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:279435-1 | |
| Safety | NA |