- Natural product: Green tea (Camellia sinensis)
- Associated study: Identification of Intestinal UDP-Glucuronosyltransferase Inhibitors in Green Tea (Camellia sinensis) Using a Biochemometric Approach: Application to Raloxifene as a Test Drug via In Vitro to In Vivo Extrapolation
In Vitro Enzyme Inhibition Experiment
Inhibition of UGT1A1, 1A8, and 1A10 by (-)-Epicatechin Gallate (Screening)
Inhibition was detected. Cutoff used — 50% inhibition vs. control
- 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 | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Commercially available
1410074
Not available
Not available
100 µM