鱼胆草提取物及其活性成分獐牙菜苦苷的药理学初探

Preliminary pharmacological study of the extracts of Swertiae davidi Franch and swertiamarin as its active constituent

为了初步考察鱼胆草提取物及其活性成分獐牙菜苦苷(含量为61%)的体外抑菌效果和安全性,以及獐牙菜苦苷对α-葡萄糖苷酶活性的影响,试验采用小鼠急性毒性试验的方法测定其安全浓度、试管二倍稀释法测定其体外最小抑菌浓度和紫外分光光度法检测獐牙菜苦苷对α-葡萄糖苷酶活性的抑制率。结果表明:鱼胆草提取物及獐牙菜苦苷以5 g/kg灌胃时,小鼠均无死亡发生;醇沉前后的鱼胆草提取物和獐牙菜苦苷对大肠杆菌的最小抑菌浓度(MIC)均为125 mg/mL,对金黄色葡萄球菌的MIC均为31.25 mg/mL;当獐牙菜苦苷浓度为1 mg/mL时对α-葡萄糖苷酶活性的抑制率为30.19%,浓度为100 mg/mL时抑制率为84.92%。说明可尝试用鱼胆草提取物及獐牙菜苦苷防治由金黄色葡萄球菌等细菌感染引起的疾病,獐牙菜苦苷无毒副作用,有望被研发成一种新的降糖药物。

To preliminarily investigate the antibacterial effect in vitro and the safety of the extracts of Swertiae Davidi Franch and 61% of swer-tiamarin as its active constituent, as well as the effect of swertiamarin on the alpha - glucosidase activity. The method of acute toxicity test was used to detect the safe concentration in mice,while the in vitro minimum inhibitory concentrations （MICs） were determined by the tube double dilution method and the inhibitory rate of swertiamarin on the alpha -glucosidase activity was measured with ultraviolet （UV） spectrophotometry. The result showed that no death occurred in the mice when drenched with 5 g/kg of the extracts of Swertiae davidi Franch and swertiamarin, respectively. The MICs of the extracts of Swertiae davidi Franch and swertiamarin against Escherichia coli and Staphylococcus aureus were 125, and 31.25 mg/mL before and after alcohol precipitation,respectively. When the concentration of swertiamarin was 1 mg/mL,its inhibition rate on the alpha - glucesidase activity was 30.19% ; when the concentration of swertiamarin was 100 mg/mL,its inhibition rate on the alpha - glucesidase activity was 84.92%. The results indicate that the extracts of Swertiae dav/di Franch and swertiamarin can be tried to prevent and treat the diseases caused by bacterial infections, such as Staphylococcus aureus and so on; the swertiamarin has no toxic side effect, and is expected to be developed into a new antidiabetic drug.