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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

James S I, Ahokas J T

Key Centre for Applied and Nutritional Toxicology, RMIT University, Melbourne, Victoria, Australia.

Xenobiotica. 1992 Dec;22(12):1433-9. doi: 10.3109/00498259209056693.

Ethacrynic acid (EA), a phenoxyacetic acid diuretic, has similar effects to tienilic acid (TA) on rat liver glutathione S-transferase (GST) activity in vitro, using either 1-chloro-2,4-dinitrobenzene or sulphobromophthalein (BSP) as a substrate. EA inhibits the basic rat liver GST, with inhibition being greater with GST containing subunits 3 and 4 than with those containing subunits 1 and 2. 2. In vitro inhibitors of GST can inhibit biliary excretion of BSP in a perfused liver. 3. A single bolus dose of EA had no effect on BSP excretion from the isolated perfused rat liver, and this is most likely due to the rapid disappearance of EA from the perfusion media. Experiments using perfused rat liver indicated that a sustained high concentration of EA in the perfusion media has an inhibitory effect on the excretion of both unchanged and conjugated BSP. 4. A decrease in BSP excretion may not be an indicator of liver damage, but a consequence of GST inhibition.

依他尼酸（EA）是一种苯氧乙酸类利尿剂，在体外，以1-氯-2,4-二硝基苯或磺溴酞钠（BSP）为底物时，它对大鼠肝脏谷胱甘肽S-转移酶（GST）活性的影响与替尼酸（TA）相似。EA抑制大鼠肝脏的基础GST，含亚基3和4的GST受到的抑制作用比含亚基1和2的GST更大。2. GST的体外抑制剂可抑制灌注肝脏中BSP的胆汁排泄。3. 单次推注剂量的EA对离体灌注大鼠肝脏中BSP的排泄没有影响，这很可能是由于EA在灌注介质中迅速消失。使用灌注大鼠肝脏的实验表明，灌注介质中持续高浓度的EA对未结合和结合型BSP的排泄均有抑制作用。4. BSP排泄减少可能不是肝损伤的指标，而是GST抑制的结果。

James S I, Ahokas J T

Key Centre for Applied and Nutritional Toxicology, RMIT University, Melbourne, Victoria, Australia.

Xenobiotica. 1992 Dec;22(12):1433-9. doi: 10.3109/00498259209056693.

Ethacrynic acid (EA), a phenoxyacetic acid diuretic, has similar effects to tienilic acid (TA) on rat liver glutathione S-transferase (GST) activity in vitro, using either 1-chloro-2,4-dinitrobenzene or sulphobromophthalein (BSP) as a substrate. EA inhibits the basic rat liver GST, with inhibition being greater with GST containing subunits 3 and 4 than with those containing subunits 1 and 2. 2. In vitro inhibitors of GST can inhibit biliary excretion of BSP in a perfused liver. 3. A single bolus dose of EA had no effect on BSP excretion from the isolated perfused rat liver, and this is most likely due to the rapid disappearance of EA from the perfusion media. Experiments using perfused rat liver indicated that a sustained high concentration of EA in the perfusion media has an inhibitory effect on the excretion of both unchanged and conjugated BSP. 4. A decrease in BSP excretion may not be an indicator of liver damage, but a consequence of GST inhibition.

依他尼酸（EA）是一种苯氧乙酸类利尿剂，在体外，以1-氯-2,4-二硝基苯或磺溴酞钠（BSP）为底物时，它对大鼠肝脏谷胱甘肽S-转移酶（GST）活性的影响与替尼酸（TA）相似。EA抑制大鼠肝脏的基础GST，含亚基3和4的GST受到的抑制作用比含亚基1和2的GST更大。2. GST的体外抑制剂可抑制灌注肝脏中BSP的胆汁排泄。3. 单次推注剂量的EA对离体灌注大鼠肝脏中BSP的排泄没有影响，这很可能是由于EA在灌注介质中迅速消失。使用灌注大鼠肝脏的实验表明，灌注介质中持续高浓度的EA对未结合和结合型BSP的排泄均有抑制作用。4. BSP排泄减少可能不是肝损伤的指标，而是GST抑制的结果。