Red wine and component flavonoids inhibit UGT2B17 in vitro

Area of Science:

• Biochemistry
• Pharmacology
• Nutritional Science

Background:

• Testosterone metabolism and excretion involve glucuronidation by UGT enzymes, forming testosterone glucuronide for urinary elimination.
• Altered UGT enzyme activity can impact testosterone excretion rates and bioavailability.
• UGT2B17 is a key enzyme in steroid metabolism.

Purpose of the Study:

• To investigate the potential inhibitory effect of red wine on the UGT2B17 enzyme.
• To identify specific phenolic compounds in red wine responsible for enzyme inhibition.
• To assess the in vitro impact of these compounds on testosterone glucuronidation.

Main Methods:

• Assay of testosterone glucuronidation using human UGT2B17 supersomes.
• Quantification of unglucuronidated testosterone via HPLC with DAD detection.
• Analysis of red wine and its phenolic components for inhibitory effects on UGT2B17.

Main Results:

• Red wine inhibited testosterone glucuronidation by up to 70% in a concentration-dependent manner.
• Ethanol content of red wine did not significantly affect UGT2B17 activity.
• Quercetin, caffeic acid, and gallic acid showed varying degrees of inhibition, with quercetin being the most potent.

Conclusions:

• Phenolic compounds found in red wine can inhibit the UGT2B17 enzyme in vitro.
• Dietary intake of these phenolics may influence testosterone metabolism and circulating levels.
• Further in vivo and human studies are warranted to confirm these findings and explore health implications.