Inhibition of UGT1A1, 1A8, and 1A10 by (-)-Epicatechin Gallate (Ki determination) CSV JSON

In Vitro Enzyme Inhibition Experiment

Inhibition of UGT1A1, 1A8, and 1A10 by (-)-Epicatechin Gallate (Ki determination)

Inhibition was detected.  Cutoff used — Not provided

raloxifene 1513103

epicatechin gallate

raloxifene 6-glucuronide

  • UGT1A1 40782950
  • UGT1A10
  • UGT1A8

Cell fraction Pooled human intestinal microsomes -7999663

The precipitant used was (-)-epicatechin gallate. Information regarding enzymes involved in the formation of raloxifene metabolites was obtained from Gufford et al., 2015 (Drug Metab Dispos. 2015 Sep;43(9):1353-9).

Results

Using methods 1 and 2 provided by the authors, enterocyte concentrations for (-)-epicatechin gallate were estimated to be 8.5 and 0.29 µM, respectively, after administration of one bag of T21 green tea. With the Ki value of approximately 1 µM, the corresponding AUCi/AUC ratios were predicted to be 6.5 and 1.3, respectively.

Compound measured Measurement Value Study sequence Additional information N replicates

Experimental Conditions

0.05 mg/mL

Commercially available

1410074

4 min

UDPGA

Not available

Not available

0.25-10 µM

0.5-8 µM