对乙酰氨基酚肝毒性的抑制作用及其与大鼠肝脏微粒体蛋白的不可逆结合。
Inhibition of the hepatotoxicity of paracetamol and its irreversible binding to rat liver microsomal protein.
作者信息
Younes M, Siegers C P
出版信息
Arch Toxicol. 1980 May;45(1):61-5. doi: 10.1007/BF00303296.
PMID:6249238
Abstract
Dithiocarb and (+)-cyanidanol-3-prevented paracetamol-induced liver injury in rats in vivo. Both, as well as two other antihepatotoxic agents, deanol and DMSO, inhibited covalent binding of [3H]-paracetamol to rat liver microsomal proteins in vitro. Dithiocarb and (+)-cyanidanol-3 were the most effective inhibitors. The concentrations of the antidotes yielding 50% inhibition (I50) valued 1 . 8 x 10(-5) M for dithiocarb and 2 . 1 x 10(-5) M for (+)-cyanidanol-3.
摘要
二硫代氨基甲酸盐和（+）-氰定醇-3可预防对乙酰氨基酚在大鼠体内诱导的肝损伤。这两种物质以及另外两种抗肝毒素药物——二甲氨基乙醇和二甲基亚砜，在体外均能抑制[3H]-对乙酰氨基酚与大鼠肝微粒体蛋白的共价结合。二硫代氨基甲酸盐和（+）-氰定醇-3是最有效的抑制剂。产生50%抑制作用（I50）的解毒剂浓度，二硫代氨基甲酸盐为1.8×10⁻⁵M，（+）-氰定醇-3为2.1×10⁻⁵M。
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