School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine , Tianjin , China and.
Drug Metab Rev. 2015 May;47(2):229-38. doi: 10.3109/03602532.2015.1029634. Epub 2015 Mar 31.
Glycyrrhizin (GZ), the main active component of licorice, is a widely used therapeutic in the clinic. Depending on the disease, the treatment may involve a long course of high dose GZ. Another component of licorice, glycyrrhetinic acid (GA), is the main active metabolite of GZ and is thought to be responsible for the majority of the pharmacological properties of GZ. Therefore, GZ and GA are both used for therapeutic purposes. In addition, GZ and GA are also widely used to sweeten and flavor foods. Due to this widespread, multifaceted use of these substances, potential drug interactions with GZ and GA have recently gained attention. Along these lines, this review covers the known effects of GZ and GA on drug-metabolizing enzymes and efflux transporters. We conclude that both GZ and GA may have an effect on the activity of CYPs. For example, GZ may induce CYP3A activity through activation of PXR. Also, GZ and GA may affect glucuronidation in rats and humans. Furthermore, 18β-GA is a potent inhibitor of P-gp, while GZ and GA are inhibitors of MRP1, MRP2 and BCRP. The pharmacokinetics and pharmacodynamics of many medications may be altered when used concurrently with GZ or GA, which is also covered in this review. Overall, GZ, GA or related products should be taken with caution when taken with additional medications due to the possible drug interactions.
甘草酸（GZ）是甘草的主要活性成分，是临床上广泛应用的治疗药物。根据疾病的不同，治疗可能需要长期大剂量使用 GZ。甘草中的另一种成分，甘草次酸（GA），是 GZ 的主要活性代谢物，被认为是 GZ 大多数药理学特性的主要原因。因此，GZ 和 GA 都被用于治疗目的。此外，GZ 和 GA 也被广泛用于食品的增甜和调味。由于这些物质的广泛、多方面的用途，GZ 和 GA 与药物的相互作用最近引起了关注。基于此，这篇综述涵盖了 GZ 和 GA 对药物代谢酶和外排转运蛋白的已知影响。我们得出结论，GZ 和 GA 都可能对 CYP 的活性产生影响。例如，GZ 可能通过激活 PXR 诱导 CYP3A 活性。此外，GZ 和 GA 可能会影响大鼠和人类的葡萄糖醛酸化。此外，18β-GA 是 P-gp 的强效抑制剂，而 GZ 和 GA 是 MRP1、MRP2 和 BCRP 的抑制剂。当与 GZ 或 GA 同时使用时，许多药物的药代动力学和药效学可能会发生改变，这也在本综述中讨论。总的来说，由于可能存在药物相互作用，当与其他药物同时使用 GZ、GA 或相关产品时应谨慎使用。
