Experiment 784137

Compounds isolated

Details

PropertyValue
Pharmacology
OrganismEmpty organism
CitationGUTMANN,H: BRUGGISSER,R: SCHAFFNER,W: BOGMAN,K: BOTOMINO,A: DREWE,J:. (2002). TRANSPORT OF AMENTOFLAVONE ACROSS THE BLOOD-BRAIN BARRIER IN VITRO.. (68)
Amount utilized
Compound isolated
DiseaseTHE PENETRATION OF [3H]-AMENTOFLAVONE THROUGH BBB WAS STUDIED IN AN IN VITRO MODEL CONSISTING OF PRIMARY CELL CULTURES OF PORCINE BRAIN CAPILLARY ENDOTHELIAL CELLS (BCEC). CONCENTRATION-DEPENDENT UPTAKE (37-200 NM) WAS NEITHER SATURABLE NOR TEMPERATURE-SENSITIVE INDICATING PASSIVE DIFFUSION AS THE MAJOR UPTAKE MECHANISM. THIS FINDING WAS CONFIRMED BY TRANSPORT EXPERIMENTS THROUGH BCEC MONOLAYERS (>2% OF APPLIED DOSE WAS TRANSPORTED AFTER 30 MIN). CO-ADMINISTRATION OF HYPERICUM EXTRACT INCREASED AMENTOFLAVONE TRANSPORT SIGNIFICANTLY INDICATING THAT HYPERICUM CONSTITUENTS ENHANCE AMENTOFLAVONE TRANSPORT POSSIBLY BY MODULATING PARA-CELLULAR PERMEABILITY. EXPERIMENTS WITH THE P-GLYCOPROTEIN (P-GP) OVEREXPRESSING CELL LINE P388-MDR SHOWED THAT AMENTOFLAVONE UPTAKE WAS SIGNIFICANLTY ENHANCED BY ADDITION OF THE P-GP INHIBITORS VERAPAMIL, SUGGESTING A P-GP MEDIATED BACK-TRANSPORT OUT OF THE CELLS. IN CONCLUSION. OUR FINDINGS SHOW, THAT AMENTOFLAVONE IS ABLE TO PASS THE BLOOD-BRAIN BARRIER IN VITRO BY PASSIVE DIFFUSION.
Dose amountVAR
Number1
Qualitative resultACTIVE
AnimalCELL CULTURE
Dose expressionDOSE