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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。
Screening of Active Constituents from Traditional Chinese Medicine Based on Small Molecule Fluorescent Probes. In this study, a new small molecule fluorescent probe with aggregation-induced luminescence (AIE) was used to screen the Chinese traditional medicine Diabetes Dipeptidyl peptidase-4 (DPP-4) inhibitor. A total of 43 chemical constituents were isolated and prepared from Xiaoke’an by systematic separation method. The 43 constituents of Xiaokean were screened out by using pepstatin A as a positive control. The results of 13 chemical pairs DPP-4 activity was inhibited; qualitative analysis of these 13 components using LC-MS technology identified 16 compounds were inferred. Further verification of 14 of these compounds showed that 5 compounds had a higher inhibitory effect on DPP-4, of which, salvianolic acid C, ginsenoside Rg5 and timosaponin AI showed a good amount of 5 ~ 50μmol·L-1 Inhibit the relationship. This study provides a successful example of using small molecule fluorescent probe technology to screen and find Chinese medicine efficacy substances.