Roe A L, Snawder J E, Benson R W, Roberts D W, Casciano D A
Division of Genetic Toxicology, National Center for Toxicological Research, Jefferson, AR 72079.
Biochem Biophys Res Commun. 1993 Jan 15;190(1):15-9. doi: 10.1006/bbrc.1993.1003.
The human hepatoma cell line, HepG2, retains many cellular functions often lost by cells in culture. This research examined the constitutive bioactivation of acetaminophen and P450-dependent activity in microsomes from HepG2 cells and the effect of 0.1% acetone pretreatment on these activities. Low levels of acetaminophen bioactivation, P450 IIE1 activity, and P450 IA1-IA2 activity were demonstrated in non-induced HepG2 microsomes. Acetone increased acetaminophen bioactivation and IIE1-dependent metabolism but not P450 IA1-IA2-dependent activity. Thus, HepG2 cells may provide an in vitro model for assessing human xenobiotic metabolism of acetaminophen and other drugs.
人肝癌细胞系HepG2保留了许多在培养细胞中常常丧失的细胞功能。本研究检测了对乙酰氨基酚在HepG2细胞微粒体中的组成型生物活化及P450依赖性活性,以及0.1%丙酮预处理对这些活性的影响。在未诱导的HepG2微粒体中证实了低水平的对乙酰氨基酚生物活化、P450 IIE1活性和P450 IA1 - IA2活性。丙酮增加了对乙酰氨基酚的生物活化及IIE1依赖性代谢,但未增加P450 IA1 - IA2依赖性活性。因此,HepG2细胞可能为评估对乙酰氨基酚及其他药物的人体异生素代谢提供一个体外模型。