Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai, PR China.
J Ethnopharmacol. 2011 Jan 7;133(1):213-9. doi: 10.1016/j.jep.2010.09.032.
The root of Acanthopanax senticosus (also called Eleutherococcus senticosus or Siberian ginseng) has been used extensively in China, Russia and Japan as an adaptogen to fight against stress and fatigue.
The present study was designed to ascertain the anti-fatigue property of Acanthopanax senticosus by load-weighted swimming test, sleep deprivation test, also to isolate and characterize the active constituents.
Animals were orally administered with the extract of Acanthopanax senticosus. The anti-fatigue effects of the four fractions with different polarities from the 80% ethanol extract, and the different eluates collected from D101 macroporous resin chromatography and eleutheroside E, were examined based on the weight-loaded swimming capacity (physical fatigue) and the change of biochemical parameters in ICR mice. Moreover, the active fraction was later submitted to sleep-deprived mice (mental fatigue).
The results shown that the n-butanol fraction significant extends the swimming time of mice to exhaustion. Furthermore, the 60% ethanol-water eluate, more purified eleutherosides (including eleutheroside E, E(2) and derivatives), were the exactly active constituents. Two compounds were isolated, which were identified as eleutheroside E, E(2).
The eleutherosides possess the potent abilities to alleviate fatigue both in physical and mental fatigue. Eleutheroside E may be responsible for the pharmacological effect of anti-fatigue. Furthermore, the possible mechanisms were reduced the level of TG by increasing fat utilization, delayed the accumulation of blood urea nitrogen (BUN), and increased the LDH to reduce the accumulation of lactic acid in muscle and then protect the muscle tissue.
刺五加（又名西伯利亚人参或刺五加）的根在中国、俄罗斯和日本被广泛用作适应原，以对抗压力和疲劳。
本研究旨在通过负重游泳试验、睡眠剥夺试验来确定刺五加的抗疲劳特性，并分离和鉴定其活性成分。
动物经口给予刺五加提取物。根据 ICR 小鼠的负重游泳能力（体力疲劳）和生化参数的变化，考察 80%乙醇提取物的四个不同极性部分以及 D101 大孔树脂层析的不同洗脱液和刺五加苷 E 的抗疲劳作用。此外，活性部分随后用于睡眠剥夺小鼠（精神疲劳）。
结果表明，正丁醇部分显著延长了小鼠的游泳时间直至力竭。此外，60%乙醇-水洗脱液，更纯的刺五加苷（包括刺五加苷 E、E(2)及其衍生物）是确切的活性成分。分离得到两种化合物，鉴定为刺五加苷 E、E(2)。
刺五加苷具有缓解体力和精神疲劳的强大能力。刺五加苷 E 可能是其抗疲劳作用的药理学基础。此外，其可能的作用机制是通过增加脂肪利用来降低 TG 水平，延缓血尿素氮（BUN）的积累，并增加 LDH 以减少肌肉中乳酸的积累，从而保护肌肉组织。
