Abstract
Angelicae Pubescentis Radix (APR) is a widely-used traditional Chinese medicine. Pharmacological studies have begun to probe its biological activities on neurological disorders recently. To assess the brain penetration and distribution of APR, a validated ultra-performance liquid chromatography tandem mass spectrometry method was applied to the simultaneous determinations of the main coumarins from APR in the rat cerebrospinal fluid (CSF) and brain after oral administration of APR extract, including psoralen, xanthotoxin, bergapten, isoimperatorin, columbianetin, columbianetin acetate, columbianadin, oxypeucedanin hydrate, angelol B, osthole, meranzin hydrate and nodakenetin. Most of the tested coumarins entered the rat CSF and brain quickly, and double-peak phenomena in concentration-time curves were similar to those of their plasma pharmacokinetics. Columbianetin had the highest concentration in the CSF and brain, while psoralen and columbianetin acetate had the largest percent of CSF/plasma and brain/plasma, indicating that these three coumarins may be worthy of further research on the possible nervous effects. Correlations between the in vivo brain distributions and plasma pharmacokinetics of these coumarins were well verified. These results provided valuable information for the overall in vivo brain distribution characteristics of APR and also for its further studies on the active substances for the central nervous system.
Highlights
Angelicae Pubescentis Radix (APR), the dried roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan, is well known as Duhuo in traditional Chinese medicines
Daidzein was used as the internal standarddetermine (IS)
A validated UPLC-MS/MS method was applied for the distribution assessments of twelve coumarins in the rat cerebrospinal fluid (CSF) and brain after oral administration of APR extract (APRE)
Summary
Angelicae Pubescentis Radix (APR), the dried roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan, is well known as Duhuo in traditional Chinese medicines. F. biserrata Shan et Yuan, is well known as Duhuo in traditional Chinese medicines. It has been widely used as an analgesic and anti-rheumatic drug for centuries in China [1]. The in vitro intestinal absorptions across the human intestinal epithelial Caco-2 cell monolayer of main coumarins from APR [3,4,5] have been carried out in our group. The in vivo pharmacokinetics of sixteen coumarins in rat plasma after oral administration of APR extract (APRE) [6] have been studied.
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