Inhibition of human P450 enzymes by natural extracts used in traditional medicine.
Different medicinal plants are widely used in Cuba and Mexico to treat several disorders. This paper reports in vitro inhibitory effects on the P450 system of herbal products commonly used by people in Cuba and Mexico in traditional medicine for decades. Experiments were conducted in human liver microsomes. The catalytic activities of CYP1A1/2, 2D6, and 3A4 were measured using specific probe substrates. The Heliopsis longipes extract exhibited a concentration-dependent inhibition of the three enzymes, and similar effects were produced by affinin (an alkamide isolated from the H. longipes extract) and two catalytically reduced alkamides. Mangifera indica L. and Thalassia testudinum extracts, two natural polyphenol-rich extracts, diminished CYP1A1/2 and 3A4 activities, but not the CYP2D6 activity. These results suggest that these herbs inhibit the major human P450 enzymes involved in drug metabolism and could induce potential herbal-drug interactions.
Rodeiro
Idania
I
Laboratorio de Farmacología, Centro de Química Farmacéutica, 200 y 21, Atabey, Playa, Ciudad de La Habana, Cuba.
Donato
María T
MT
Jimenez
Nuria
N
Garrido
Gabino
G
Molina-Torres
Jorge
J
Menendez
Roberto
R
Castell
José V
JV
Gómez-Lechón
María J
MJ
D019659:Asteraceae / Q000737:chemistry; D065607:Cytochrome P-450 Enzyme Inhibitors; D005260:Female; D005419:Flavonoids / Q000494:pharmacology; D041743:Herb-Drug Interactions; D006801:Humans; D031321:Hydrocharitaceae / Q000737:chemistry; D008297:Male; D031022:Mangifera / Q000737:chemistry; D008519:Medicine, Traditional; D008862:Microsomes, Liver / Q000187:drug effects* / Q000201:enzymology; D010636:Phenols / Q000494:pharmacology; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000378:metabolism; D059808:Polyphenols; D053284:Polyunsaturated Alkamides / Q000494:pharmacology
D065607:Cytochrome P-450 Enzyme Inhibitors; D005419:Flavonoids; C489347:N-isobutyl-2E-decenamide; D010636:Phenols; D010936:Plant Extracts; D059808:Polyphenols; D053284:Polyunsaturated Alkamides