Liu J, Zhang H Y, Wang L M, Tang X C
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhongguo Yao Li Xue Bao. 1999 Feb;20(2):141-5.
To determine the anticholinesterase properties of huperzine B (Hup B) and compare with tacrine in vitro and in vivo.
Spectrophotometry was used to determine ChE activity.
Hup B showed much more selective inhibition to acetylcholinesterase (AChE) than tacrine. The IC50 ratios of Hup B and tacrine for butyrylcholinesterase (BuChE): AChE were 65.8 and 0.54, respectively. Hup B ig exhibited higher efficacy on the inhibition of brain AChE than that of tacrine. Tacrine was more effective in the inhibition of serum BuChE in mice with severe concomitant peripheral adverse effects than Hup B. A single ig dose of Hup B produced steady state of AChE inhibition in 4 h.
Hup B exhibits higher selectivity and efficacy in the inhibition of AChE, and lower toxicity in mice than tacrine.
在体外和体内确定石杉碱乙（Hup B）的抗胆碱酯酶特性，并与他克林进行比较。
采用分光光度法测定胆碱酯酶（ChE）活性。
Hup B对乙酰胆碱酯酶（AChE）的抑制作用比他克林更具选择性。Hup B和他克林对丁酰胆碱酯酶（BuChE）：AChE的IC50比值分别为65.8和0.54。Hup B灌胃对脑AChE的抑制作用比他克林更强。在伴有严重外周不良反应的小鼠中，他克林对血清BuChE的抑制作用比Hup B更有效。单次灌胃给予Hup B在4小时内产生AChE抑制的稳态。
Hup B在抑制AChE方面表现出更高的选择性和效力，并且在小鼠中比他克林毒性更低。
