| Properties | Information | |
|---|---|---|
| PhytoCAT-ID | PhytoCAT-1953 | |
| Phytochemical name or plant extracts | Theaflavin-3-gallate | |
| PMID | 34958756 | |
| Literature evidence | Theaflavin-3-gallate, a natural antagonist for Hsp90: In-silico and in-vitro approach. | |
| IUPAC name | [(2R,3R)-2-[1,2-dihydroxy-9-oxo-4-[(2R,3R)-3,5,7-trihydroxy-3,4-dihydro-2H-chromen-2-yl]-5,6,7,8-tetrahydrobenzo[7]annulen-6-yl]-5,7-dihydroxy-3,4-dihydro-2H-chromen-3-yl] 3,4,5-trihydroxybenzoate | |
| Phytochemicals’ class or type of plant extracts | Flavonoid | |
| Source of phytochemicals or plant Extracts | Camellia sinensis | |
| Geographical availability | Assam, China South-Central, China Southeast, East Himalaya, Hainan, Laos, Myanmar, Thailand, Vietnam | |
| Plant parts | NA | |
| Other cancers | Breast cancer | |
| Target gene or protein | HSP90, MMP9, VEGFA, SPP1 | |
| Gene or Protein evidence | Furthermore, theaflavin-3-gallate significantly downregulated the mRNA expression patterns of the HSP90, MMP9, VEGFA, and SPP1 genes. | |
| Target pathways | NA | |
| IC50 | NA | |
| Potency | Collectively, our results demonstrated theaflavin-3-gallate as a potential natural Hsp90 inhibitor that can be used to enhance the therapeutic efficacy of existing breast cancer therapies and improve overall survival of breast cancer patients. | |
| Cell line/ mice model | MCF-7, Caco-2 | |
| Additional information | Prior to the transport of theaflavin (TF), theaflavin-3-gallate (TF3G), theaflavin-3'-gallate (TF3'G), and theaflavin-3, 3'-digallate (TFDG), we found the cytotoxicity of theaflavins was in the order of TF3'G > TFDG > TF3G > TF, suggesting the galloyl moiety enhances the cytotoxicity of theaflavins. Moreover, theaflavins increased the expression of P-gp, MRP1, MPR3, and BCRP while decreased the expression of MRP2 at the transcription and translation levels. Additionally, the gallated theaflavins were degraded into simple theaflavins and gallic acids when transported through Caco-2 monolayers. Overall, the structural instability, efflux transporters, and cell metabolism were all responsible for the low bioavailability of four theaflavins in Caco-2 monolayers. | |
| PubChem ID | 71307578 | |
| Additional PMIDs | 34463173 | |
| Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:828548-1 | |
| Safety | Further in-vitro validation of the cytotoxic effect of theaflavin-3-gallate in human breast carcinoma cell line MCF7 and normal cell line MCF10A revealed that theaflavin-3-gallate significantly inhibited the cell proliferation of MCF7 cells whereas no cytotoxic effect was observed on MCF10A cells. |