- 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 was detected. Cutoff used — 50% inhibition vs. control
- UGT
Cell fraction Pooled human intestinal microsomes -7999663
Methanol extracts and (sub)fractions (five fractions obtained using a 4 g silica gel column and a hexane-chloroform-methanol mobile phase at 18 mL/min; normal phase chromatography) from four widely-avaliable commercial teas were used.
Results
Extracts, fractions, and subfractions from the four green teas inhibited intestinal UGT activity in a concentration-dependent manner (by 30-100% relative to vehicle control, estimated from Fig. 3). The UGT inhibitory constituents tended to reside in the more hydrophilic subfractions of the fraction prepared from the representative extract. (−)-Epigallocatechin gallate (EGCG) and (−)-epicatechin gallate (ECG), two abundant catechins contained in green tea, were identified as major UGT inhibitors in these subfractions.
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
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Experimental Conditions
Green tea extracts, fractions, and subfractions were tested as inhibitors of UGT enzymes as described in Gufford et al., 2014 (Drug Metab Dispos. 2014 Oct;42(10):1675-83); information regarding incubation volume, time, and protein linearity were obtain therein.
Bovine serum albumin (0.05%) was added into the incubation system.
0.2 mg/mL
Commercially available
1410074
150 µL
20 min
UDPGA
Available
Not available
100 µM
20, 60, and 180 µg/mL