Shanghai University of Traditional Chinese Medicine, The MOE Key Laboratory for Standardization of Chinese Medicines, Shanghai R&D Centre for Standardization of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai, China.
Department of Pharmacy, Fudan University Shanghai Cancer Center, Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, China.
Biomed Chromatogr. 2021 Jun;35(6):e5077. doi: 10.1002/bmc.5077. Epub 2021 Feb 2.
Stem-leaf saponins (SLSs), the total saponins from aerial part of P. notoginseng, are by-products of notoginseng, a famous traditional Chinese medicine. SLSs have been used as a health functional food in China, but its mild effects limited clinical applications in diseases. Inspired by steaming of notoginseng to enhance its pharmacological activity, a steaming protocol was developed to treat SLSs. SLSs were steamed at 100, 120, and 140°C for 1, 2, 3, and 4 h, respectively. The ultra-performance liquid chromatography coupled with quadrupole time-of-flight MS and ultra-performance liquid chromatography-tandem triple quadrupole mass spectrometry were applied to analyze the dynamic changes in chemical compositions. The anti-acetylcholinesterase activity of steamed SLS were assessed in vitro by directly determining the metabolic product of acetylcholine/choline. The components of SLSs were significantly changed by steaming. A total of 117 saponins and aglycones were characterized, and 35 of them were newly generated. The anti-acetylcholinesterase activity of steamed SLSs gradually increased with the extension of steamed time and the increase of steamed temperature and reached the maximum after 140°C for 3 h. Furthermore, ginsenosides Rk1 and Rg5, the main components of steamed SLSs, showed dose-dependent anti-acetylcholinesterase activities with half maximal inhibitory concentration (IC ) values of 26.88 ± 0.53 μm and 22.41 ± 1.31 μm that were only 1.8- and 1.5-fold higher than that of donepezil with IC values of 14.93 ± 4.17 μM, respectively.
茎叶总皂苷（SLSs）是三七地上部分的总皂苷，是三七的副产品。SLSs 已在中国被用作一种具有保健功能的食品，但由于其温和的效果，限制了其在疾病中的临床应用。受三七蒸制以提高其药理活性的启发，开发了一种蒸制方案来处理 SLSs。将 SLSs 在 100、120 和 140°C 下分别蒸制 1、2、3 和 4 h。采用超高效液相色谱-四极杆飞行时间质谱联用和超高效液相色谱-串联三重四极杆质谱联用分析化学成分的动态变化。通过直接测定乙酰胆碱/胆碱的代谢产物，体外评估了蒸制 SLSs 的抗乙酰胆碱酯酶活性。蒸制显著改变了 SLSs 的成分。共鉴定出 117 种皂苷和苷元，其中 35 种为新生成的。蒸制 SLSs 的抗乙酰胆碱酯酶活性随蒸制时间的延长、蒸制温度的升高而逐渐增加，在 140°C 下蒸制 3 h 后达到最大值。此外，蒸制 SLSs 的主要成分人参皂苷 Rk1 和 Rg5 表现出剂量依赖性的抗乙酰胆碱酯酶活性，半数最大抑制浓度（IC ）值分别为 26.88 ± 0.53 μM 和 22.41 ± 1.31 μM，仅分别比 IC 值为 14.93 ± 4.17 μM 的多奈哌齐高 1.8 倍和 1.5 倍。
