- 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 (Ki determination)
Inhibition was detected. Cutoff used — Not provided
- 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.
| Sample | Compound measured | Value | Measurement | 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