基于α-葡萄糖苷酶抑制作用的两种青藤属药用植物的活性物质发现与初步作用机制

Glycemic variability is an important factor causing vascular endothelial damage in diabetic patients and leading to numerous complications.Management on glycemic variability is an imperative means for preventing diabetic complications. Alpha-glucosidase inhibitors reduce the impact of dietary carbohydrates on blood sugar and is an important target for the treatment of diabetes mellitus. Our previous investigation suggested the 95% ethanol extracts of the roots of Illigera parviflora and I. celebica possessed noticeable α-glucosidase inhibit activity, a subsequent bioassay-guided phytochemical investigation showed the diterpenes might be the bioactive constituents. The structures of diterpenes from I.parviflora contained two special fragments: oxabicyclic [3.2.1] heptane and cinnamyl group, quite different from the aporphine alkaloids and the monoterpenoids previously isolated from the Illigera genus. No scholars had carried out the diterpenoids constituents and hypoglycemic activity on the the Illigera plants. A further investigation on the active constituents in the above mentioned medicinal plants and their alpha-glucosidase inhibiting mechanism is necessary, which could provide the research basis for the development of new antidiabetic drugs.

血糖波动是造成糖尿病患者血管内皮损伤从而导致众多并发症的重要因素，血糖控制对于治疗糖尿病意义重大。α-葡萄糖苷酶抑制剂能够有效降低餐后血糖水平，减少血糖波动，是治疗糖尿病的重要靶点。前期研究显示小花青藤、宽药青藤根具有显著的α-葡萄糖苷酶抑制作用，生物活性指导下的初步化学成分研究表明，二萜可能为其中的有效降糖成分。该类成分具有氧杂双环[3.2.1]庚烷片段，并与单萜单元缩合形成新颖的螺环结构，同时具有(二氢)肉桂酰基，或3,4-二羟基肉桂酰基取代。两种青藤属植物二萜成分及降糖作用迄今未见报道，开展上述两种药用植物α-葡萄糖苷酶抑制活性物质及作用机制研究，可为开发具有自主知识产权的降糖药物提供研究基础。

血糖波动是造成糖尿病患者血管内皮损伤从而导致众多并发症的重要因素，血糖控制对于治疗糖尿病意义重大。α-葡萄糖苷酶抑制剂能够有效降低餐后血糖水平，减少血糖波动，是治疗糖尿病的重要靶点。本项目系统开展青藤属植物小花青藤和宽药青藤两种药用植物的化学成分及其生物活性研究，从两种药用植物中共分离到六十五个化合物，新化合物十四个, 其中单萜或二萜单元多与(二氢)肉桂酰基，或3,4-二羟基肉桂酸成酯。对分离得到的化合物开展α-葡萄糖苷酶抑制活性评价，部分化合物已被发现显示出较好的降糖活性。在本项目资助下，目前共计发表论文4篇，其中SCI论文2篇；申请发明专利3项，其中授权1项。依托本项目，培养硕士研究生3名。研究成果丰富和扩充了我国青藤属植物化学成分的研究内容和结构类型，为该属植物萜类成分的药用开发提供新的线索和科学依据。