Songklod Sarapusit. Inhibition effect of cytochrome P4502A6 enzyme mutant alleles 7 (CYP2A6*7) activity by luteolin. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2024.
Inhibition effect of cytochrome P4502A6 enzyme mutant alleles 7 (CYP2A6*7) activity by luteolin
Abstract:
Nicotine, one of the major substances in cigarette smoke, has been previously reported as a key
compound responsible for smoking addiction. Inhaled nicotine passes to the brain and stimulates dopamine
secretion, resulting in pleasure feeling. Nicotine is metabolized by liver-specific cytochrome P4502A6
(CYP2A6) enzyme. This nicotine clearance mechanism, however, could lead to cigarette craving and smoking
more frequently in order to maintain nicotine levels in the bloodstream. Thus, maintaining blood-nicotine
level by inhibiting the CYP2A6 activity is an alternative approach to decrease cigarette smoking. Luteolin has
been previously reported as one of flavonoid compounds that could effectively inhibit the wild-type CYP2A6
(wt-CYP2A6) mediated coumarin 7-hydroxylation activity in vitro. This study aims to determine the
inhibitory effect of Luteolin against the polymorphic cytochrome P450 2A6 mutant 7 (CYP2A6*7) that has
been report in Thai population. 7-hydroxy coumarin hydroxylation was measured. The results indicated that
Luteolin could inhibit wt-CYP2A6 and CYP2A6*7 with IC50 values of 1.93 ± 0.08 μM and 4.81 ± 0.43 μM,
respectively. The molecular docking experiment indicated that wt-CYP2A6 and CYP2A6*7 were bound to
Luteolin with different non-covalent interactions
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2024
Modified:
2024-12-04
Issued:
2024-12-04
บทความ/Article
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BibliograpyCitation :
In Kasetsart University. Faculty of Science. The Pure and Applied Chemistry International Conference 2024 (PACCON 2024) (pp.835-839). Bangkok : Kasetsart University, 2024