详细描述实验推导出人工肝CYP1A1活动并使用微分表达式抑制ethoxyresorufin O-deethylation氟伏沙明。

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Sy SK,唐BK, Pastrakuljic,罗伯茨EA, Kalow W

详细描述实验推导出人工肝CYP1A1活动并使用微分表达式抑制ethoxyresorufin O-deethylation氟伏沙明。

欧元中国新药杂志。2001年8月,57 (5):377 - 86。doi: 10.1007 / s002280100330。

PubMed ID

11599655 (在PubMed

]

文摘

目的:描述的分布数学推导出人工肝CYP1A1活动使用微分抑制ethoxyresorufin O-deethylation氟伏沙明(EROD)。方法:定量CYP1A1和CYP1A2-mediated EROD活动测定42使用微分的EROD抑制氟伏沙明人类肝脏。CYP1A2-specific活动也是衡量非那西汀O-deethylation 3-demethylation和咖啡因。分布CYP1A1-mediated EROD CYP1-A2调查活动进行了分析使用累积分布(probit)情节和Kolgomorov-Smirnov测试。年龄影响CYP1A1和CYP1A2-mediated EROD活动是评估使用描述性统计和方差分析。结果:派生CYP1A1蛋白质浓度的0.58 + / - 1.04 pmol /毫克派生CYP1A2的仅为4%。自从CYP1A1本质上是在中介EROD远比CYP1A2活性,贡献的CYP1A1 EROD表示大约有25 - 40%的CYP1A2的贡献。三个42肝脏表现出没有CYP1A1-mediated EROD。大约8%的人表现出高CYP1A1活动基于累积分布曲线分析表型。肝CYP1A1活动比CYP1A2的变量。 The variance of CYP1A1-mediated EROD was significantly different from that of CYP1A2, using the Kolgomorov-Smirnov statistical test. Even though not statistically significant, an age-related pattern in CYP1A1-mediated activity was identified: activity was high in the pre-puberty group, then decreased in the young/mature adult group and, finally, a slight increase was observed in old age. CONCLUSIONS: Distribution pattern in CYP1A1-mediated EROD suggests that the low derived CYP1A1 expression is most likely induced rather than constitutive. CYP1A1 activity deviates from log-normal distribution; the variations in hepatic CYP1A1 activity may affect the conversion of procarcinogens to carcinogens. The age-related trend in CYP1A1-mediated EROD activity hints that CYP1A1 responsiveness to inducers may change with age as well as with exposure to environmental inducers. These findings prompt (1) future genotyping studies to determine whether increased CYP1A1 inducibility is a result of genetic factors and (2) studies to address whether CYP1A1 inducibility changes with age.

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药物酶

药物	酶	类	生物	药理作用	行动
氟伏沙明	细胞色素P450 1 a1	蛋白质	人类	未知的	抑制剂	细节