Wu Jinfu, Sun Hang, Zhao Yiyang, Lian Lian, Bian Hongsheng, Guo Yong, Li Dan, Huang Lili
College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, China.
Shineway Pharmaceutical Group Co., Ltd., Shijiazhuang, China.
Front Pharmacol. 2025 Jan 28;16:1538837. doi: 10.3389/fphar.2025.1538837. eCollection 2025.
This study aims to establish the fingerprint spectra of Kai-Xin-San (KXS) and investigate its spectrum-effect relationship in treating Alzheimer's disease (AD).
Initially, the fingerprints of 15 batches of KXS were established and analyzed using HPLC, with the method's precision, stability, and repeatability thoroughly evaluated. Subsequently, the effects of the 15 batches of KXS were assessed in an olfactory escape memory experiment, utilizing Aβ transgenic as a model. Finally, the spectrum-effect relationship between the KXS fingerprint and memory improvement was analyzed, with the active ingredients subjected to validation testing.
The results identified seventeen common peaks in the fingerprint, and eight active components were determined: polygalaxanthone III, 3-6-disinapoylsucrose, ginsenoside Rg1, ginsenoside Rb1, β-asarone, α-asarone, dehydrotumulosic acid, and dehydropachymic acid. Treatment with KXS (1%, for 4 days) significantly enhanced the performance index of Aβ flies in the olfactory experiment. Both spectrum-effect analysis and validation tests indicated that polygalaxanthone III, ginsenoside Rg1, ginsenoside Rb1, β-asarone, and α-asarone were positively correlated with the performance index and improved the performance index in the olfactory experiment. The HPLC fingerprint method for KXS demonstrated excellent precision, accuracy, and reproducibility, making it suitable for quality evaluation and control of KXS. Polygalaxanthone III, ginsenoside Rg1, ginsenoside Rb1, β-asarone, and α-asarone are identified as potential active ingredients of KXS for anti-AD effects.
These findings provide an experimental basis for developing new drugs based on KXS and its active ingredient combinations.
本研究旨在建立开心散（KXS）的指纹图谱，并探讨其治疗阿尔茨海默病（AD）的谱效关系。
首先，采用高效液相色谱法建立并分析15批次开心散的指纹图谱，对该方法的精密度、稳定性和重复性进行全面评估。随后，以Aβ转基因果蝇为模型，在嗅觉逃避记忆实验中评估15批次开心散的药效。最后，分析开心散指纹图谱与记忆改善之间的谱效关系，并对活性成分进行验证测试。
结果确定了指纹图谱中的17个共有峰，并鉴定出8种活性成分：远志山酮III、3,6-二芥子酰蔗糖、人参皂苷Rg1、人参皂苷Rb1、β-细辛醚、α-细辛醚、去氢土莫酸和去氢茯苓酸。开心散（1%，连续4天）处理显著提高了Aβ果蝇在嗅觉实验中的性能指标。谱效分析和验证测试均表明，远志山酮III、人参皂苷Rg1、人参皂苷Rb1、β-细辛醚和α-细辛醚与性能指标呈正相关，并在嗅觉实验中提高了性能指标。开心散的高效液相色谱指纹图谱方法具有良好的精密度、准确性和重现性，适用于开心散的质量评价和控制。远志山酮III、人参皂苷Rg1、人参皂苷Rb1、β-细辛醚和α-细辛醚被确定为开心散抗AD作用的潜在活性成分。
这些发现为基于开心散及其活性成分组合开发新药提供了实验依据。
