Zhu Guangwei, Ma Shengjun, Li Xiwen, Zhang Peng, Tang Lin, Cao Lijuan, Liu Aoxue, Sugita Toru, Tomoda Takehisa
Institute of Chinese Materia Medica, China Academy of Chinese Medicinal Sciences, Beijing 100700, China.
School of Food Sciences and Pharmacy, Xinjiang Agriculture University, Urumqi, 830052, China.
J Pharmacol Sci. 2018 Feb;136(2):57-65. doi: 10.1016/j.jphs.2017.11.008. Epub 2017 Dec 1.
To investigate the inhibitory effect of Glycyrrhiza uralensis (G. uralensis) and its monomeric compounds on Nav1.4 voltage-gated sodium channels (VGSCs) and analyze the relationship between the content of its marker compounds and the inhibitory rate. Based on this study, we found that 4 mg/ml ethanol extract of G. uralensis at 30%, 50%, 70% and 90% (v/v) exhibited 77.00 ± 0.03%, 34.75 ± 0.09%, 100.00 ± 0.01% and 2.00 ± 0.01% inhibitory rates on I1.4 respectively, and 8 mg/ml ethanol extract of G. uralensis at 30%, 50%, 70% and 90% (v/v) exhibited 99.00 ± 0.01%, 97.10 ± 0.02%, 100.00 ± 0.01% and 17.00 ± 0.04% inhibitory rates on I1.4 respectively. Isoliquiritigenin, echinatin, liquiritin and glycyrrhizic acid exhibited higher inhibitory rates of 39.98 ± 4.55%, 33.20 ± 1.61%, 22.62 ± 0.30% and 20.54 ± 4.82% respectively. However, liquiritigenin, formononetin, neoisoliquiritin and glycyrrhetinic acid exhibited lower inhibitory rates of less than 20%. Further, liquiritin apioside, isoliquiritin and neoliquiritin exhibited almost no effect on I1.4. These findings showed that glycyrrhizic acid reached a maximum concentration of 49.15 μg/ml, while echinatin had the lowest concentration. The ethanol extract of G. uralensis has significant inhibitory effects on Nav1.4 VGSCs. This may be an important mechanism in the treatment of gastrocnemius spasm and could guide further research regarding material basis and mechanism of the treatment of gastrocnemius spasm with peony and licorice decoction.
研究甘草及其单体化合物对Nav1.4电压门控钠通道（VGSCs）的抑制作用，并分析其标志性化合物含量与抑制率之间的关系。基于本研究，我们发现4mg/ml甘草乙醇提取物在30%、50%、70%和90%（v/v）时对I1.4的抑制率分别为77.00±0.03%、34.75±0.09%、100.00±0.01%和2.00±0.01%，8mg/ml甘草乙醇提取物在30%、50%、70%和90%（v/v）时对I1.4的抑制率分别为99.00±0.01%、97.10±0.02%、100.00±0.01%和17.00±0.04%。异甘草素、刺芒柄花素、甘草苷和甘草酸的抑制率较高，分别为39.98±4.55%、33.20±1.61%、22.62±0.30%和20.54±4.82%。然而，甘草素、芒柄花素、新甘草苷和甘草次酸的抑制率较低，均低于20%。此外，甘草苷元芹菜糖苷、异甘草苷和新甘草苷对I1.4几乎没有影响。这些结果表明，甘草酸达到最大浓度49.15μg/ml，而刺芒柄花素浓度最低。甘草乙醇提取物对Nav1.4 VGSCs有显著抑制作用。这可能是治疗腓肠肌痉挛的重要机制，可为进一步研究芍药甘草汤治疗腓肠肌痉挛的物质基础和作用机制提供指导。
