Selective Inhibition of Bakuchicin Isolated from Psoralea corylifolia on CYP1A in Human Liver Microsomes. (9th February 2016)

• Record Type: Journal Article
• Authors: Kim, Sun Joo; Oh, Heung Chan; Kim, Youn-Chul; Jeong, Gil-Saeng; Lee, Sangkyu
• Other Names: Yang Ling Academic Editor.
• Is Part Of: Evidence-based complementary and alternative medicine. Volume 2016(2016)
• Publication Date: 2016-02-09
• Subjects: Alternative medicine -- Periodicals; 615.505
• DOI: 10.1155/2016/5198743
• Languages: English
• ISSNs: 1741-427X

Abstract

Abstract : Bakuchicin is a furanocoumarin isolated from Psoralea corylifolia and shows several biological activities. Although there have been studies on the biological effects of bakuchicin, its modulation potency of CYP activities has not been previously investigated. Here, we investigated the inhibitory effects of bakuchicin on the activities of CYP isoforms by using a cocktail of probe substrates in pooled human liver microsomes (HLMs) and human recombinant cDNA-expressed CYP. Bakuchicin strongly inhibited CYP1A-mediated phenacetin O -deethylation with an IC50 value of 0.43 μ M in HLMs. It was confirmed by human recombinant cDNA-expressed CYP1A1 and CYP1A2 with aK i value of 0.11 μ M and 0.32 μ M, respectively. A Lineweaver-Burk plot indicated that the inhibition mechanism of bakuchicin was competitive inhibition. Overall, this is the first study to investigate the potential CYP1A1 and CYP1A2 inhibition associated with bakuchicin and to report its competitive inhibitory effects on HLMs.