Rong Weiwei, Ding Kewen, Guo Sirui, Yuan Ziyue, Li Qing, Bi Kaishun
National and Local Joint Engineering Laboratory for Key Technology of Chinese Material Medica Quality Control, School of Pharmacy, Shenyang Pharmaceutical University 103 Wenhua Road Shenyang 110016 China
RSC Adv. 2018 Apr 18;8(27):14732-14739. doi: 10.1039/c8ra01765d.
Bunge is a folk medicine in China. Recently, the triterpenoids in its husks have attracted more and more attention for potential prevention against Alzheimer's disease. However, current studies on its bioactive substances were still insufficient. To reveal more bioactive substances, an efficient and practical strategy based on high resolution mass spectra coupled with multiple data mining techniques was developed to characterize the barrigenol type triterpenoids in the husks and dosed rat plasma. A total of 50 barrigenol type triterpenoids were identified in the husks, and 6 of these were detected in the rat plasma, which were regarded as bioactive candidates. To find the real bioactive substances, the neuroprotective effect of the candidates was further tested by calculating the PC12 cell viability against amyloid-β-induced cytotoxicity. As a result, three out of the six candidates exhibited obvious neuroprotction against amyloid-β-induced cytotoxicity on PC12 cells, indicating their potential to be bioactive substances against Alzheimer's disease. This study will be a valuable reference of the bioactive substances in Bunge husks against Alzheimer's disease and the provided strategy can also be applied to the exploration of the effective constituents in other medicines.
地锦是中国的一种民间药物。近年来，其外壳中的三萜类化合物因其对阿尔茨海默病的潜在预防作用而受到越来越多的关注。然而，目前对其生物活性物质的研究仍然不足。为了揭示更多的生物活性物质，开发了一种基于高分辨率质谱结合多种数据挖掘技术的高效实用策略，用于表征地锦外壳和给药大鼠血浆中的羽扇豆醇型三萜类化合物。在地锦外壳中总共鉴定出50种羽扇豆醇型三萜类化合物，其中6种在大鼠血浆中被检测到，这些被视为生物活性候选物。为了找到真正的生物活性物质，通过计算PC12细胞对淀粉样蛋白β诱导的细胞毒性的活力，进一步测试了候选物的神经保护作用。结果，6种候选物中的3种对PC12细胞上淀粉样蛋白β诱导的细胞毒性表现出明显的神经保护作用，表明它们具有成为抗阿尔茨海默病生物活性物质的潜力。本研究将为地锦外壳中抗阿尔茨海默病的生物活性物质提供有价值的参考，所提供的策略也可应用于其他药物有效成分的探索。
