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目的观察黄芩苷与γ-氨基丁酸(GABA)受体的关系及其所具有的抗焦虑作用。方法采用同位素标记GABA受体结合实验观察黄芩苷与GABA受体的关系;采用高台十字迷宫实验和四孔箱实验观察动物服用黄芩苷后行为的改变。结果 GABA受体竞争结合试验显示,黄芩苷可竞争性抑制50%GABA受体苯二氮类结合浓度(IC50)为(117.62±8.50)μmol·L-1,抑制结合常数(Ki)为(77.10±4.79)μmol·L-1。黄芩苷可增加实验动物进入十字迷宫开放侧次数,百分率和滞留时间,减少在四孔箱中探头和竖身的次数。这些变化与黄芩苷剂量有明显的关系,可被GABA受体阻断剂Ro 15-1788阻断。结论黄芩苷是GABA结合位点的配体,具有一定的抗焦虑作用。
Objective To observe the relationship between baicalin and γ-aminobutyric acid (GABA) receptor and its anti-anxiety effects. Methods The relationship between baicalin and GABA receptor was observed by isotope labeled GABA receptor binding assay. The behavior of baicalin after taking baicalin was observed by using the Gaucho maze test and the four-hole box experiment. Results The competition binding assay of GABA receptor showed that Baicalein could competitively inhibit the benzodiazepine binding concentration (IC50) of 50% GABA receptor to (117.62 ± 8.50) μmol·L-1 and the inhibitory binding constant (Ki) to (77.10 ± 4.79) μmol·L-1. Baicalin can increase the frequency, percentage and residence time of experimental animals entering the open maze and reduce the number of probes and erections in the four-hole box. These changes have a clear relationship with the dosage of baicalin and can be blocked by GABA receptor antagonist Ro 15-1788. Conclusion Baicalin is a ligand of GABA binding site and has some anti-anxiety effects.