Effective cytochrome P450 (CYP) inhibitors isolated from tarragon (Artemisia dracunculus).
Two effective cytochrome P450 (CYP) inhibitors were isolated from tarragon, Artemisia dracunculus. Their structures were spectroscopically identified as 2E,4E-undeca-2,4-diene-8,10-diynoic acid isobutylamide (1) and 2E,4E-undeca-2,4-diene-8,10-diynoic acid piperidide (2). Both compounds had dose-dependent inhibitory effects on CYP3A4 activity with IC50 values of 10.0 ± 1.3 µM for compound 1 and 3.3 ± 0.2 µM for compound 2, and exhibited mechanism-based inhibition. This is the first reported isolation of effective CYP inhibitors from tarragon (Artemisia dracunculus) purchased from a Japanese market.
Department of Nutritional Science, Faculty of Applied Bio-Science, Tokyo University of Agriculture, Japan.
Zeineb
Z
Brahmi
Tatsuya
T
Katho
Rie
R
Hatsumata
Asako
A
Hiroi
Nami
N
Miyakawa
Emi
E
Yakou
Kouichi
K
Sugaya
Jun-ichi
J
Onose
Naoki
N
Abe
D019306:Artemisia / Q000737:chemistry*; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D005231:Fatty Acids, Unsaturated / Q000737:chemistry* / Q000302:isolation & purification; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000737:chemistry; D007700:Kinetics; D009249:NADP / Q000737:chemistry; D010880:Piperidines / Q000737:chemistry* / Q000302:isolation & purification; D010936:Plant Extracts / Q000737:chemistry*; D012996:Solutions
C575818:2,4-undeca-2,4-diene-8,10-diynoic acid isobutylamide; C575819:2,4-undeca-2,4-diene-8,10-diynoic acid piperidide; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D005231:Fatty Acids, Unsaturated; D007527:Isoenzymes; D010880:Piperidines; D010936:Plant Extracts; D012996:Solutions; D009249:NADP; D003577:Cytochrome P-450 Enzyme System