Lee Ki Yong, Yoon Jeong Seon, Kim Eun Sil, Kang So Young, Kim Young Choong
College of Pharmacy and Research Institute of Pharmaceutical Science, Seoul National University, Seoul, Korea.
Planta Med. 2005 Jan;71(1):7-11. doi: 10.1055/s-2005-837743.
We previously reported that seven pregnane glycosides including cynatroside B isolated from the roots of Cynanchum atratum significantly inhibited acetylcholinesterase (AChE) activity. In the present study, we have characterized the mode of AChE inhibition of cynatroside B, the most potent of these isolated pregnane glycoside inhibitors. We have also examined the anti-amnesic activity of cynatroside B. Cynatroside B inhibited AChE activity in a dose-dependent manner and its IC50 value was 3.6 microM. The mode of AChE inhibition by cynatroside B was reversible and non-competitive in nature. Moreover, cynatroside B (1.0 mg/kg body weight i.p.) significantly ameliorated memory impairments induced in mice by scopolamine (1.0 mg/kg body weight s.c.) as measured in the passive avoidance and the Morris water maze tests. We suggest, therefore, that cynatroside B has both anti-AChE and anti-amnesic activities that may ultimately hold significant therapeutic value in alleviating certain memory impairments observed in Alzheimer's disease.
我们之前报道过，从白薇根部分离出的七种孕烷糖苷，包括白薇苷B，能显著抑制乙酰胆碱酯酶（AChE）的活性。在本研究中，我们已对这些分离出的孕烷糖苷抑制剂中最有效的白薇苷B抑制AChE的作用方式进行了表征。我们还检测了白薇苷B的抗遗忘活性。白薇苷B以剂量依赖性方式抑制AChE活性，其IC50值为3.6微摩尔。白薇苷B对AChE的抑制方式本质上是可逆且非竞争性的。此外，在被动回避和莫里斯水迷宫试验中测定，白薇苷B（腹腔注射1.0毫克/千克体重）能显著改善东莨菪碱（皮下注射1.0毫克/千克体重）诱导的小鼠记忆损伤。因此，我们认为白薇苷B具有抗AChE和抗遗忘活性，这最终可能在缓解阿尔茨海默病中观察到的某些记忆损伤方面具有重要的治疗价值。
