CAS Key Laboratory of Separation Science for Analytical Chemistry, National Chromatographic R. & A. Center, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, 116023, China.
CAS Key Laboratory of Separation Science for Analytical Chemistry, National Chromatographic R. & A. Center, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, 116023, China.
J Ethnopharmacol. 2022 Nov 15;298:115641. doi: 10.1016/j.jep.2022.115641. Epub 2022 Aug 13.
Tianzhi granule (TZG) is a traditional Chinese formula that is widely used for the treatment of vascular dementia (VaD).
To discover the herbs in TZG possessing acetylcholinesterase (AChE) inhibitory activity and to screen the anti-acetylcholinesterase ingredients from active herbs.
In vitro AChE inhibitory activity assay of eleven herbal extracts was conducted. An ultrafiltration combined with ultra-performance liquid chromatography-mass spectrometry method was established to screen and identify the anti-acetylcholinesterase ingredients from active extracts. In addition, in vitro AChE inhibitory activity assay and molecular docking were adopted for further investigation. Moreover, ultra-performance liquid chromatography-mass spectrometry was performed for the content determination of active compounds in TZG.
Three herbs in TZG showed significant AChE inhibitory activity. A total of thirteen active ingredients were screened out and identified, and all of these compounds were present in TZG. Five available commercial standards presented moderate AChE inhibitory activity, and all of which have a relatively high content in TZG.
A number of herbs and compounds with acetylcholinesterase inhibitory activity were found in TZG, which provided a scientific basis for the material basis and quality control research of TZG.
天智颗粒（TZG）是一种广泛用于治疗血管性痴呆（VaD）的中药配方。
发现 TZG 中具有乙酰胆碱酯酶（AChE）抑制活性的草药，并从活性草药中筛选出抗乙酰胆碱酯酶成分。
对 11 种草药提取物进行体外乙酰胆碱酯酶抑制活性测定。建立超滤结合超高效液相色谱-质谱法筛选和鉴定来自活性提取物的抗乙酰胆碱酯酶成分。此外，采用体外乙酰胆碱酯酶抑制活性测定和分子对接进行进一步研究。此外，还进行了超高效液相色谱-质谱法测定 TZG 中活性化合物的含量。
TZG 中的三种草药表现出显著的乙酰胆碱酯酶抑制活性。共筛选出并鉴定了 13 种活性成分，且这些化合物均存在于 TZG 中。五种可用的商业标准品表现出中等的乙酰胆碱酯酶抑制活性，且均在 TZG 中具有相对较高的含量。
TZG 中发现了一些具有乙酰胆碱酯酶抑制活性的草药和化合物，为 TZG 的物质基础和质量控制研究提供了科学依据。
