Properties | Information | |
---|---|---|
PhytoCAT-ID | PhytoCAT-2159 | |
Phytochemical name or plant extracts | Thaliblastine (TBL) | |
PMID | 7562498 | |
Literature evidence | Mechanistic studies showed that this striking resistance reversal was achieved without alteration of cellular levels of glutathione and without inhibition of glutathione S-transferase, glutathione peroxidase or P450 reductase by TBL, each of which is significantly altered in MCF/AdR cells, and each of which has been proposed to contribute to AdR resistance in this MDR line. | |
IUPAC name | (6aS)-9-[2-[[(1S)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]methyl]-4,5-dimethoxyphenoxy]-1,2,10-trimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline | |
Phytochemicals’ class or type of plant extracts | Alkaloid | |
Source of phytochemicals or plant Extracts | Thalictrum foliolosum | |
Geographical availability | Assam, China South-Central, East Himalaya, India, Myanmar, Nepal, Pakistan, Thailand, Tibet, Vietnam, West Himalaya | |
Plant parts | NA | |
Other cancers | Breast cancer | |
Target gene or protein | P-gp | |
Gene or Protein evidence | These results establish that MDR associated with P-gp overexpression can be fully reversed by the potent P-gp inhibitor TBL. | |
Target pathways | NA | |
IC50 | NA | |
Potency | Rather, resistance reversal by TBL can be entirely explained by this drug's capacity to restore the intracellular accumulation of AdR in the resistant cells. These results establish that MDR associated with P-gp overexpression can be fully reversed by the potent P-gp inhibitor TBL. They further indicate that although changes in multiple drug-metabolizing enzymes may accompany the development of MDR, these multiple biochemical alterations need not correspond to multiple functional determinants for drug resistance. | |
Cell line/ mice model | MCF/AdR | |
Additional information | Mechanistic studies showed that this striking resistance reversal was achieved without alteration of cellular levels of glutathione and without inhibition of glutathione S-transferase, glutathione peroxidase or P450 reductase by TBL, each of which is significantly altered in MCF/AdR cells, and each of which has been proposed to contribute to AdR resistance in this MDR line. | |
PubChem ID | 21470 | |
Additional PMIDs | NA | |
Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:714441-1 | |
Safety | NA |