Inhibition of UGT1A1, 1A8, and 1A10 by (+)-catechin (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 UGT1A1, 1A8, and 1A10 by (+)-catechin (Screening)

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

Object compound

raloxifene 1513103

Precipitant

catechin 43012577

Object metabolite investigated

raloxifene 4'-glucuronide

Enzymes involved in metabolite pathway

UGT1A1 40782950
UGT1A10
UGT1A8

Test system used

Cell fraction Pooled human intestinal microsomes -7999663

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 (-)-gallocatechin did not signficiantly inhibit the formation of raloxifene 4'-glucuronide. Percent inhibition value was estimated from Fig. S2.

Sample	Compound measured	Value	Measurement	Study sequence	Additional information	N replicates

Experimental Conditions

Test system preparation

Commercially available

Test system lot number

1410074

Protein linearity

Not available

Time linearity

Not available

Precipitant concentrations tested

100 µM

Control Experiment

Inhibition of UGT1A1, 1A8, and 1A10 by Nicardipine (Positive Control; Screening)

NOTE