Properties | Information | |
---|---|---|
PhytoCAT-ID | PhytoCAT-1810 | |
Phytochemical name or plant extracts | Falcarindiol 3-acetate | |
PMID | 24269959 | |
Literature evidence | They display interesting bioactivities and hold potential as health-promoting and therapeutic agents. | |
IUPAC name | [(3R,8S,9Z)-8-hydroxyheptadeca-1,9-dien-4,6-diyn-3-yl] acetate | |
Phytochemicals’ class or type of plant extracts | Polyacetylene | |
Source of phytochemicals or plant Extracts | Daucus carota | |
Geographical availability | Afghanistan, Albania, Algeria, Austria, Azores, Baleares, Baltic States, Belarus, Belgium, Bulgaria, Canary Is., Cape Verde, Central European Rus, China South-Central, China Southeast, Corse, Cyprus, Czechoslovakia, Denmark, East Aegean Is., East European Russia, Eritrea, Ethiopia, France, Germany, Great Britain, Greece, Hungary, Iran, Iraq, Ireland, Italy, Kazakhstan, Kirgizstan, Kriti, Krym, Lebanon-Syria, Libya, Madeira, Morocco, Nepal, Netherlands, North Caucasus, Northwest European R, Norway, Pakistan, Palestine, Poland, Portugal, Romania, Sardegna, Sicilia, South European Russi, Spain, Sweden, Switzerland, Tadzhikistan, Transcaucasus, Tunisia, Turkey, Turkey-in-Europe, Turkmenistan, Ukraine, Uzbekistan, West Himalaya, Yugoslavia | |
Plant parts | NA | |
Other cancers | Breast cancer | |
Target gene or protein | NA | |
Gene or Protein evidence | NA | |
Target pathways | NA | |
IC50 | NA | |
Potency | In this study, falcarinol, falcarindiol, falcarindiol 3-acetate and falcarindiol 3,8-diacetate were examined for their modulation on breast cancer resistance protein (BCRP/ABCG2), an efflux transporter important for xenobiotic absorption and disposition, and multidrug resistance in cancer. | |
Cell line/ mice model | HEK293 | |
Additional information | The polyacetylenes inhibited mitoxantrone (an ABCG2 substrate) efflux in ABCG2-overexpressing HEK293 cells. The inhibitory effect was confirmed in the vesicular transport assay, in which concentration-dependent inhibition of methotrexate (an ABCG2 substrate) uptake into ABCG2-overexpressing Sf9 membrane vesicles was observed (IC50=19.7-41.7µM). The polyacetylenes also inhibited baseline and sulfasalazine-stimulated vanadate-sensitive ATPase activities in ABCG2-overexpressing Sf9 membrane vesicles (IC50=19.3-79.3µM). This is the first report of an inhibitory effect of polyacetylenes on ABCG2. These results indicate a prospective use of polyacetylenes as multidrug resistance reversal agents, a possible role of ABCG2 in the absorption and disposition of polyacetylenes, and potential food-drug interactions between polyacetylene-rich foods and ABCG2 substrate drugs. | |
PubChem ID | 101256943 | |
Additional PMIDs | NA | |
Additional sources of information | https://powo.science.kew.org/taxon/urn:lsid:ipni.org:names:841063-1 | |
Safety | NA |