Müller D
Friedrich Schiller University, Institute of Pharmacology and Toxicology, Jena, GDR.
Exp Pathol. 1990;39(3-4):187-94. doi: 10.1016/s0232-1513(11)80183-0.
Biotransformation of drugs and other xenobiotics in the liver plays an important role intoxication and detoxication processes, i.e. changes in biotransformation activity have significant biological consequences. For that reason the determination of biotransformation activity is useful. The rate of some biotransformation reactions can be markedly changed by very small doses of xenobiotics. These changes may be used for the sensitive detection of the exposure to xenobiotics. Among biotransformation reactions cytochrome P-450-dependent monooxygenation is very important. It can be induced and inhibited by xenobiotics. Induction of P-450 forms can be detected by various methods, e.g. by using model reactions. Ethoxycoumarin O-deethylation, ethoxyresorufin O-deethylation, pentoxyresorufin O-depentylation and ethylmorphine N-demethylation are catalyzed at different P-450 forms, and their determination is described in detail.
药物及其他外源性物质在肝脏中的生物转化在中毒和解毒过程中起着重要作用,也就是说,生物转化活性的改变具有重大的生物学意义。因此,生物转化活性的测定是有用的。极少量的外源性物质就能显著改变某些生物转化反应的速率。这些变化可用于灵敏检测外源性物质的暴露情况。在生物转化反应中,细胞色素P-450依赖的单加氧作用非常重要。它可被外源性物质诱导和抑制。P-450形式的诱导可通过多种方法检测,例如使用模型反应。乙氧香豆素O-脱乙基化、乙氧试卤灵O-脱乙基化、戊氧试卤灵O-脱戊基化和N-脱甲基乙基吗啡分别由不同的P-450形式催化,其测定方法将详细描述。