Title : Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: role of phenolic hydroxyl groups in the resorcinol moiety.

Pub. Date : 2011 Apr 11

PMID : 21356216






5 Functional Relationships(s)
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1 CBD competitively inhibited the activity of CYP3A4, CYP3A5, and HLMs (K(i)=1.00, 0.195, and 6.14 muM, respectively). Cannabidiol cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 The lesser inhibitory effects of monomethyl and dimethyl ethers of CBD indicated that the ability of CYP3A inhibition by the cannabinoid attenuated with the number of methylation on the phenolic hydroxyl groups in the resorcinol moiety. Cannabidiol cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 SIGNIFICANCE: This study indicated that CBD most potently inhibited catalytic activity of human CYP3A enzymes, especially CYP3A4 and CYP3A5. Cannabidiol cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 SIGNIFICANCE: This study indicated that CBD most potently inhibited catalytic activity of human CYP3A enzymes, especially CYP3A4 and CYP3A5. Cannabidiol cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 These results suggest that two phenolic hydroxyl groups in the resorcinol moiety of CBD may play an important role in the CYP3A inhibition. Cannabidiol cytochrome P450 family 3 subfamily A member 4 Homo sapiens