Inhibition of UGT by (-)-Epicatechin (Screening) CSV JSON

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 UGT by (-)-Epicatechin (Screening)

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

Object compound

4-methylumbelliferone

Precipitant

(-)-epicatechin

Object metabolite investigated

4-methylumbelliferone glucuronide

Enzymes involved in metabolite pathway

Test system used

Cell fraction Pooled human intestinal microsomes -7999663

Results

(-)-Epicatechin did not significantly inhibit UGT enzymes--observed UGT activity was 110% of control.

Sample	Compound measured	Value	Measurement	Study sequence	Additional information	N replicates

Experimental Conditions

Purified green tea catechins 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 protien linearity were obtain therein.
Bovine serum albumin (0.05%) was added into the incubation system.

Protein concentration

0.2 mg/mL

Test system preparation

Commercially available

Test system lot number

1410074

Incubation volume

150 µL

Incubation time

20 min

Co-substrate

UDPGA

Protein linearity

Available

Time linearity

Not available

Object concentrations tested

100 µM

Precipitant concentrations tested