Abstract:
:Cytochrome P4501A1 is involved in the metabolism of carcinogenic polycyclic aromatic hydrocarbons; therefore, its inhibition interferes with the carcinogenesis process induced by these compounds in rats. The human and rat CYP1A1 differ by 21% in amino acid sequence, including the active site of the enzyme; this difference may be an important factor when results obtained using animal models are interpolated to humans. Based on its previously reported CYP inhibitory properties, we studied the effects of two molecules contained within grapefruit juice, naringenin and 6',7'-dihydroxybergamottin, on human and rat CYP1A1 activity. For this purpose, the kinetics of inhibition as well as computational simulations were used. Naringenin and 6',7'-dihydroxybergamottin were found to be competitive inhibitors of human and rat CYP1A1. Additionally, naringenin exerted a mixed type inhibition effect on rat CYP1A1. Computational docking showed that inhibitors might block the oxidation of 7-ethoxyresorufin by binding to the CYP1A1 active site. Our results demonstrate the differences in CYP inhibitory mechanisms for the same molecule when CYP from different species are considered.
journal_name
Toxicol Lettjournal_title
Toxicology lettersauthors
Santes-Palacios R,Romo-Mancillas A,Camacho-Carranza R,Espinosa-Aguirre JJdoi
10.1016/j.toxlet.2016.07.023subject
Has Abstractpub_date
2016-09-06 00:00:00pages
267-275eissn
0378-4274issn
1879-3169pii
S0378-4274(16)32299-8journal_volume
258pub_type
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