Bioactivity-guided fractionation for anti-fatigue property of Acanthopanax senticosus

Ethnopharmacological relevance: 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. Aim of the study: 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. Materials and methods: 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). Results: 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. Conclusions: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. (C) 2010 Elsevier Ireland Ltd. All rights reserved.