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兔和大鼠离体肝细胞中的磺胺乙酰化作用

Sulfonamide acetylation in isolated rabbit and rat liver cells.

作者信息

Olsen H, Mørland J, Rothschild M A

出版信息

Acta Pharmacol Toxicol (Copenh). 1981 Nov;49(5):438-46. doi: 10.1111/j.1600-0773.1981.tb00929.x.

DOI:10.1111/j.1600-0773.1981.tb00929.x
PMID:7345886
Abstract

Suspensions of isolated liver cells were prepared from rabbit livers perfused with Ca++-free buffer and 0.05% collagenase. Primary cell suspensions (containing both parenchymal and non-parenchymal liver cells) metabolized sulfadimidine and sulfanilamide at first-order kinetics for at least 2-3 hrs. Suspensions of purified rabbit liver parenchymal cells had an equal metabolic capacity, and it could be demonstrated that the metabolic rate of both sufadimidine and sulfanilamide was correlated to the amount of viable parenchymal cells in suspension. Suspensions of non-parenchymal cells were lacking the ability to metabolize both drugs. By means of homogenates of purified rabbit and rat liver cells, it could be demonstrated that the enzyme N-acetyltransferase was located in the cytosolic fraction of the parenchymal cells. It was concluded that the cytosolic fraction of the liver parenchymal cells is the main site of sulfonamide acetylation in both rabbit and rat.

摘要

从用无钙缓冲液和0.05%胶原酶灌注的兔肝脏中制备分离的肝细胞悬液。原代细胞悬液(包含实质肝细胞和非实质肝细胞)以一级动力学代谢磺胺二甲嘧啶和磺胺至少2 - 3小时。纯化的兔肝脏实质肝细胞悬液具有同等的代谢能力,并且可以证明磺胺二甲嘧啶和磺胺的代谢速率与悬液中活的实质肝细胞数量相关。非实质肝细胞悬液缺乏代谢这两种药物的能力。通过纯化的兔和大鼠肝细胞匀浆可以证明,N - 乙酰转移酶位于实质肝细胞的胞质部分。得出的结论是,兔和大鼠肝脏实质肝细胞的胞质部分是磺胺乙酰化的主要部位。

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