Bioacitivities Evaluation and Pharmacokinetics of 5-Hydroxymethyl-2-furoic Acid Derived from the Administration of Liu-Wei-Di-Huang-Wan

5-Hydroxymethyl-2- furoic acid (5-HMFA) (1) is one of the main metabolites detected in blood after oral administration of Liu-Wei-Di-Huang-Wan (LWDHW), a traditional chinese medical formula used to treat the syndrome of kidney deficiency. In order to understand the coherence between the effects of 5-HMFA and the clinical usage of LWDHW, anti-aging and improving hemorrheology activites of 5-HMFA were elucidated, these bioactivitie are in accordance with therapeutical effectes of LWDHW. Pharmacokinetic studies indicated that not only the absorption but also the distribution of 5-HMFA were rapid (t_1/2kα = 0.1h, t_1/2α = 2.62h), but the elimination was very slow (t_1/2β = 32.66h) (2), these properties might result from its multiple origins of 5-HMFA in vivo[1]. The original form of 5-HMFA existed in Radix Rehmanniae, one of the composition herbal drugs of LWDHW, was rapidly absorbed and distributed, subsequently the precursors (5-HMF) existing in Fructus Corni and Rhizoma Alismatis, another two composition herbal drugs of LWDHW, were gradually metabolized into 5-HMFA and be absorbed later. Thus, LWDHW could be considered as natural sustained releaser of 5-HMFA, and this might contribute to the enlasting therapeutical effect of this formula, 5-HMFA is one of effective constituents of LWDHW in vivo.

Acknowledgement: This work was supported by a grant from the National Natural Science Foundation of China (no. 30572300). Reference: [1] Wang XJ, et al. (2007) Chinese Journal of Natural Medicine 5: 277–280.