HEPG2 CELLS - AN INVITRO MODEL FOR P450-DEPENDENT METABOLISM OF ACETAMINOPHEN
HEPG2 CELLS - AN INVITRO MODEL FOR P450-DEPENDENT METABOLISM OF ACETAMINOPHEN
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DOI：
10.1006/bbrc.1993.1003
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发表时间：
1993-01-15
影响因子：
3.1
通讯作者：
CASCIANO, DA
中科院分区：
文献类型：
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作者：
ROE, AL;SNAWDER, JE;CASCIANO, DA
人类肝癌细胞系HepG2保留了许多细胞功能，但在培养过程中，细胞往往会失去这些功能。本研究检测了对乙酰氨基酚在HepG2细胞微粒体中的结构性生物激活和P450依赖活性，以及0.1%丙酮对这些活性的影响。在未诱导的HepG2微粒体中，显示出低水平的对乙酰氨基酚生物激活、P450 IIE1活性和P450 IA1-IA2活性。丙酮增加对乙酰氨基酚的生物活性和IIE1依赖的代谢，但不增加P450IA1-IA2依赖的活性。因此，HepG2细胞可能为评估扑热息痛等药物在人体内的异种代谢提供体外模型。
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 anin vitromodel for assessing human xenobiotic metabolism of acetaminophen and other drugs.