摘要
基于小分子荧光探针的中药活性成分筛选研究方兴未艾。该研究应用具有聚集诱导发光现象（AIE）的新型小分子荧光探针,对中成药消渴安中二肽基肽酶-4（DPP-4）抑制剂进行筛选。采用系统分离法,从消渴安中分离和制备了43个化学组分;以抑二肽素A为阳性对照药,对消渴安的43个组分进行筛选,发现13个化学组分对DPP-4的活性具有抑制作用;采用LC-MS技术对这13个组分进行定性分析,鉴定推断出16个化合物。进一步对其中14个化合物进行验证,发现5个化合物对DPP-4具有较高的抑制作用,其中丹酚酸C、人参皂苷Rg5、知母皂苷AI在5~50μmol·L-1呈良好的量效抑制关系。该研究为运用小分子荧光探针技术筛选发现中药药效物质提供了成功实例。
Fluorescent bio-probes have attracted increasing attentions in studies for screening bioactive compounds from traditional Chinese medicines. In this study,a new-type fluorescent probe with the function of aggregation-induced emission（ AIE） was used to screen dipeptidyl peptidase-4（ DPP-4） inhibitor from Xiaokean formula,which has been clinically used for the treatment of type 2 diabetes mellitus. Potential DPP-4 inhibitors were screened by the fluorescent probe,with diprotin A as the positive control; totally 43 components were isolated from Xiaokean formula by systematic separation. The results showed that 13 components can exert inhibitory effects on DPP-4 activity; 16 compounds were further identified by liquid chromatography-mass spectrometry（ LC-MS） from those active components. The inhibitory effects of 14 compounds were further verified,while five of them showed significant inhibition against DPP-4. Salvianolicacid C,ginsenoside Rg5 and timosaponin AI inhibited DPP-4 activity at the concentration of 5-50 μmol·L- 1in a dose-dependent manner. Thus,our study provided a successful example for screening bioactive compounds from traditional Chinese medicines by using a novelfluorescent probe.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2016年第7期1241-1245,共5页
China Journal of Chinese Materia Medica
关键词
DPP-4抑制剂
消渴安
2型糖尿病
聚集诱导发光现象
荧光探针
DPP-4inhibitor
Xiaokean formula
type 2 diabetes mellitus
aggregation-induced emission
fluorescent probe
