马醉木二萜成分及其乙酰胆碱酯酶抑制活性研究

Diterpenoids with acetylcholinesterase inhibitory activity from Pieris japonica

关键词:  杜鹃花科, 马醉木, 二萜, pierisformoside F, 乙酰胆碱酯酶抑制活性

Key words:  Ericaceae, Pieris japonica, diterpenoids, pierisformoside F, acetylcholinesterase inhibitory activities

摘要:

为研究马醉木叶中的二萜成分及其乙酰胆碱酯酶抑制活性,该研究根据薄层色谱显色特征,使用硅胶、MCI和半制备高效液相等色谱技术对其进行分离与纯化,并通过波谱数据(NMR和MS)分析且结合文献报道数据进行对比,鉴定了所得化合物的结构,同时采用Ellman法首次对其乙酰胆碱酯酶抑制活性进行评价。结果表明:从马醉木叶中分离并鉴定了8个二萜化合物,分别是pierisformoside F(1)、3-epi-grayanotoxin XVIII(2)、3-epi-grayanotoxin B(3)、asebotoxin-X(4)、pierisformosin B(5)、asebotoxin Ⅲ(6)、rhodojaponin Ⅲ(7)和pierisformosin C(8)。其中,化合物1为首次从该植物中分离得到,化合物8表现出乙酰胆碱酯酶抑制活性。综上表明,马醉木中含有丰富的二萜成分和活性成分。该研究结果丰富了马醉木的化学成分多样性,为其后续综合开发和利用提供了一定的理论依据,也为寻求更多的活性成分提供了借鉴。

Abstract:

In order to investigate the diterpenoid components from the leaves of Pieris japonica and their acetylcholinesterase(ACHE)inhibitory activities, with the aid of thin-layer chromatography color characteristics, silica gel, MCI and semi-preparative high-performance liquid chromatography technology, the target constituents were isolated and purified. The structures of the obtained compounds were identified by analyses of their spectral data(NMR and MS)and comparison of their data with those of reported in the literature. Meanwhile, AChE inhibitory effects of obtained diterpenoids were evaluated for the first time by a ellman method. The results showed that eight diterpenoid compounds were isolated and identified from the leaves of P. japonica, namely pieriformoside F(1), 3-epi-grayanotoxin XVIII(2), 3-epi-grayanotoxin B(3), asebotoxin-X(4), pieriformosin B(5), asebotoxin Ⅲ(6), rhodojaponin Ⅲ(7), and pieriformosin C(8). Among them, Compound 1 was isolated from this plant for the first time, and Compound 8 showed AChE inhibitory activity. In conclusion, the results enriches the diterpenoids and bioactive components of P. japonica, which provides a certain theoretical basis for its further development and utilization.