Inhibitory effect of caffeic acid and its derivatives on human liver cytochrome P450 3A4 activity

• Main Authors: Churdsak Jaikang, Kanokporn Niwatananun, Paitoon Narongchai, Siripun Narongchai, Chaiyavat Chaiyasut
• Format: Journal
• Published: 2018
• Subjects: Agricultural and Biological Sciences; Medicine; Pharmacology, Toxicology and Pharmaceutics
• Online Access: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84860417144&origin=inward; http://cmuir.cmu.ac.th/jspui/handle/6653943832/49579
• Institution: Chiang Mai University

Effects of caffeic acid (CAF) and its derivatives on human liver CYP3A4 activity were evaluated by using diazepam as a substrate. It was found that CAF inhibited CYP3A4 activity by uncompetitive inhibition with IC50 0.72 μM, whereas ester and amide analogues inhibited CYP3A4 by competitive inhibitio...