Studio of National Chinese Medical Science Master Shiyuan Jin, Bao'an Authentic TCM Therapy Hospital, Shenzhen 518101, China.
Key Laboratory of State Administration of Traditional Chinese Medicine, Dongguan HEC Cordyceps R&D Co., Ltd., Dongguan 523850, China.
Molecules. 2021 Oct 10;26(20):6111. doi: 10.3390/molecules26206111.
Polygoni Vivipari Rhizoma (PVR), the dried root of , has been used as herbal medicine in China for a long time. In the present study, a new method based on multi-step matrix solid-phase dispersion (MSPD), ultrafiltration and high performance liquid chromatography (HPLC) for screening alpha-glucosidase inhibitors (AGIs) from PVR was proposed. First, three different PVR extractions were prepared by multi-step MSPD with 15% methanol, 60% methanol and 100% methanol. Second, the alpha-glucosidase inhibition tests for the three extracts were carried out, and the 60% methanol extraction showed the best activity. Then, the AGIs screening experiment was performed with ultrafiltration and HPLC analysis using the 60% methanol extraction. Seven binding components (quercetin-3--vicianoside, quercetin 3--neohesperidoside, rutin, hyperoside, quercetin 3--glucuronide, luteolin-7--neohesperidoside, kaempferol 3-glucuronide) were found. These seven components were further validated as the AGIs by molecular docking analysis. The developed method was a rapid and efficient tool for screening AGIs from PVR, which provided scientific data for the bioactive components study of PVR.
何首乌的干燥根（首乌）在中国作为草药使用已有很长的历史。本研究提出了一种基于多步基质固相分散（MSPD）、超滤和高效液相色谱（HPLC）的新方法，用于从首乌中筛选α-葡萄糖苷酶抑制剂（AGIs）。首先，采用 15%甲醇、60%甲醇和 100%甲醇的多步 MSPD 法制备了三种不同的首乌提取物。其次，对三种提取物进行α-葡萄糖苷酶抑制试验，结果表明 60%甲醇提取物活性最好。然后，采用超滤和 HPLC 分析，用 60%甲醇提取物进行 AGIs 筛选实验。发现了 7 种结合成分（槲皮素-3-O-新橙皮苷、槲皮素 3-O-新橙皮苷、芦丁、圣草酚、槲皮素 3-O-葡萄糖醛酸苷、木樨草素-7-O-新橙皮苷、山奈酚 3-O-葡萄糖醛酸苷）。通过分子对接分析进一步验证了这七种成分是 AGIs。所开发的方法是一种从首乌中筛选 AGIs 的快速有效工具，为首乌的生物活性成分研究提供了科学数据。
