School of Natural Product Studies, Jadavpur University, Kolkata, Kolkata, India.
Phytother Res. 2011 Oct;25(10):1429-34. doi: 10.1002/ptr.3426. Epub 2011 Feb 24.
The rhizome of Glycyrrhiza glabra L. (licorice) is used very widely in Indian and Chinese traditional medicine, and it is a popular flavor ingredient of drinks, sweets and candies. Its medicinal uses include treating bronchitis, dry cough, respiratory infections, liver disorders and diabetes. Glycyrrhizin is normally considered to be its biologically active marker, so a rapid RP-HPLC method was developed for the quantitative estimation of glycyrrhizin in the extract. The effect of the standardized extract and its marker on drug metabolizing enzymes was evaluated through CYP3A4 and CYP2D6 inhibition assays to evaluate the safety through its drug interaction potential. The inhibition of CYP3A4 and CYP2D6 isozymes was analysed by the fluorescent product formation method. In the CYP450-CO assay, the interaction potential of the standardized extract and pooled microsomes (percentage inhibition 23.23 ± 1.84%), was found to be less than the standard inhibitor. In the fluorimetric assay, G. glabra extracts showed higher IC(50) values than their positive inhibitors, ketoconazole and quinidine for CYP3A4 and CYP2D6, respectively. Furthermore, the interaction potential of the plant extract was greater than the pure compound. The results demonstrate that G. glabra and its principle bioactive compound, glycyrrhizin, when co-administered with conventional medicines showed only a weak interaction potential with drug metabolizing enzymes.
甘草的根茎在印度和中国传统医学中被广泛使用，它是饮料、糖果和甜食中常用的香料成分。其药用用途包括治疗支气管炎、干咳、呼吸道感染、肝脏疾病和糖尿病。甘草酸通常被认为是其具有生物活性的标志物，因此开发了一种快速反相高效液相色谱法（RP-HPLC）用于定量测定提取物中的甘草酸。通过 CYP3A4 和 CYP2D6 抑制试验评估标准化提取物及其标志物对药物代谢酶的影响，以通过其药物相互作用潜力评估安全性。通过荧光产物形成法分析 CYP3A4 和 CYP2D6 同工酶的抑制作用。在 CYP450-CO 测定中，标准化提取物与混合微粒体（抑制率为 23.23±1.84%）的相互作用潜力小于标准抑制剂。在荧光测定中，甘草提取物对 CYP3A4 和 CYP2D6 的 IC50 值均高于其阳性抑制剂酮康唑和奎尼丁。此外，植物提取物的相互作用潜力大于纯化合物。结果表明，甘草及其主要生物活性化合物甘草酸与常规药物同时使用时，与药物代谢酶的相互作用潜力较弱。
