Modulatory actions of o -coumaric acid on carcinogen-activating cytochrome P450 isozymes and the potential for drug interactions in human hepatocarcinoma cells ∗

Autor: Şen, Alaattin, Terzioglu, Gülsüm, Atmaca, Pelin, Çelik, Gurbet, Özgün, Özden, Arslan, Şevki
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Conference Paper
Western blotting
Substrate Specificity
Activation
Metabolic

Carcinogen activation
Cytochrome P-450 Enzyme System
dose response
protein cleavage
cytochrome P450 (CYP)
genetics
Drug Interactions
HepG2 cells
antineoplastic agent
cytochrome P450 3A4
cytochrome P450 2C9
messenger RNA
Liver Neoplasms
Hep G2 Cells
xenobiotic metabolism
carcinogen
EC50
Isoenzymes
EC10
cytotoxicity
metabolic activation
coumaric acid
cytochrome P450 1A2
isoenzyme
Carcinoma
Hepatocellular

Coumaric Acids
cytochrome P450
enzymology
effective concentration
Antineoplastic Agents
densitometry
reverse transcription polymerase chain reaction
EC25
Humans
controlled study
human
RNA
Messenger

enzyme specificity
protein expression
cell viability
HepG2 cell line
drug interaction
Dose-Response Relationship
Drug

human cell
eye diseases
Carcinogens
cytochrome P450 2E1
pathology
metabolism
Popis: Context: Although humans are exposed to o-coumaric acid (OCA) in their diet, there is no available literature related to drug interaction and the carcinogen-activating potential of OCA in the HepG2 cell line. Objective: This study was undertaken to determine the effects of OCA on the cytochrome P450 (CYP) 1A2, CYP2E1, CYP2C9, and CYP3A4 enzymes, which are primarily involved in carcinogen and drug metabolism. Materials and methods: The cytotoxicity of OCA in HepG2 cells was investigated by measuring the cleavage of WST-1. The protein and mRNA levels of CYPs were determined by western blotting and RT-PCR, respectively. Results: The EC10, EC25, and EC50 values of OCA were calculated to be 1.84, 3.91 and 7.39mM, respectively. A sublethal dose of 5mM was used throughout this study. The CYP1A2 protein and mRNA levels were increased by 52 and 40% (p
Databáze: OpenAIRE