Leclercq I, Desager J P, Horsmans Y
Gastroenterology Laboratory, Louvain Medical School, Brussels, Belgium.
Clin Pharmacol Ther. 1998 Aug;64(2):144-9. doi: 10.1016/S0009-9236(98)90147-3.
To investigate the effect of watercress on the metabolism of chlorzoxazone, an in vivo probe for CYP2E1, the oral pharmacokinetics of chlorzoxazone was studied in 10 healthy volunteers before and after a single ingestion of a watercress homogenate (50 gm). A third chlorzoxazone pharmacokinetic study was performed after a 1-week treatment with isoniazid (300 mg/day), a well-known CYP2E1 inhibitor. Ingestion of watercress or isoniazid did not affect the oral absorption of chlorzoxazone. The area under the chlorzoxazone plasma concentration-time curve was significantly increased by 56% (p < 0.05) after watercress ingestion and by 135% (p < 0.001) with isoniazid treatment. Similarly, chlorzoxazone elimination half-life was prolonged after watercress (53%; p < 0.05) and isoniazid (104%; p < 0.01) administration. These results show that a single ingestion of watercress inhibits the hydroxylation of chlorzoxazone, an in vivo probe for CYP2E1.
为研究水田芥对CYP2E1的体内探针氯唑沙宗代谢的影响，在10名健康志愿者单次摄入水田芥匀浆（50克）前后，对氯唑沙宗的口服药代动力学进行了研究。在用著名的CYP2E1抑制剂异烟肼（300毫克/天）进行为期1周的治疗后，进行了第三次氯唑沙宗药代动力学研究。摄入水田芥或异烟肼均不影响氯唑沙宗的口服吸收。摄入水田芥后，氯唑沙宗血浆浓度-时间曲线下面积显著增加56%（p<0.05），而异烟肼治疗后增加135%（p<0.001）。同样，服用水田芥（53%；p<0.05）和异烟肼（104%；p<0.01）后，氯唑沙宗的消除半衰期延长。这些结果表明，单次摄入水田芥可抑制CYP2E1的体内探针氯唑沙宗的羟基化。
