Mourelle M, Favari L
Departmento de Farmacologia y Toxicología, Centro de Investigación y de Estudios Avanzados del I.P.N., México, D.F.
Life Sci. 1988;43(3):201-7. doi: 10.1016/0024-3205(88)90309-8.
The profile of urinary salicylate metabolites was determined after an i.p. administration of acetylsalicylic acid (ASA) to CCl4-cirrhotic rats to rats which in addition to CCl4 received an oral dose of silymarin throughout the CCl4 treatment to produce cirrhosis and to control groups. ASA esterase activity was determined in serum and livers. The time course of plasma concentration of salicylates in similar groups was followed after the i.p. injection of ASA. The cirrhotic animals showed a lack of urinary glucuronides and an increase in urinary gentisic and salicylic acids. The activities of plasma and serum ASA esterase were significantly increased in cirrhosis and the plasma half-life of ASA was reduced. The simultaneous administration of silymarin (50 mg/kg of b.w.) along with CCl4, completely prevented all the alterations. The mechanism by which silymarin prevented those alterations is not completely known but our results establish the potential use of silymarin in cirrhotic patients to prevent disorders in drug metabolism and disposition frequently found in patients with liver diseases.
给四氯化碳诱导肝硬化的大鼠腹腔注射乙酰水杨酸(ASA),并给除四氯化碳外还在整个四氯化碳诱导肝硬化过程中口服水飞蓟宾的大鼠以及对照组大鼠,测定尿中水杨酸代谢物的情况。测定血清和肝脏中的ASA酯酶活性。腹腔注射ASA后,追踪相似组中水杨酸盐的血浆浓度随时间的变化过程。肝硬化动物的尿中葡萄糖醛酸苷缺乏,龙胆酸和水杨酸的尿排泄增加。肝硬化时血浆和血清ASA酯酶活性显著增加,ASA的血浆半衰期缩短。水飞蓟宾(50mg/kg体重)与四氯化碳同时给药,完全预防了所有这些改变。水飞蓟宾预防这些改变的机制尚不完全清楚,但我们的结果证实水飞蓟宾在肝硬化患者中具有潜在用途,可预防肝病患者中常见的药物代谢和处置紊乱。