In Vitro Enzyme Inhibition Experiment

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

Inhibition was detected.  Cutoff used — 50% inhibition vs. control

raloxifene 1513103

epicatechin gallate

raloxifene 4'-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

At 10 µM (-)-epicatechin gallate inhibited the formation of raloxifene 4'-glucuronide by about 65%. Percent inhibition values were estimated from Fig. S2.

Sample Compound measured Measurement Value Study sequence Additional information N replicates

Experimental Conditions

Commercially available

1410074

Not available

Not available

100 µM

Control Experiment