9/4/2015 Single oral dose pharmacokinetics of decursin, decursinol angelate, and decursinol in rats. ­ PubMed ­ NCBI

http://www.ncbi.nlm.nih.gov/pubmed/23364885 1/2

Planta Med. 2013 Mar;79(3­4):275­80. doi: 10.1055/s­0032­1328202. Epub 2013 Jan 30.

Single oral dose pharmacokinetics of decursin, decursinol angelate, anddecursinol in rats.Li L , Zhang J, Xing C, Kim SH, Lü J.

AbstractDecursin and decursinol angelate are the major components in the alcoholic extract of the root ofAngelica gigas Nakai. Our previous work convincingly demonstrated that both decursin anddecursinol angelate were rapidly converted to decursinol in mice after administration by eitheroral gavage or i. p. injection. In the current study, we compared for the first time the plasmaprofiles of decursinol, when equal moles of decursin/decursinol angelate or decursinol weregiven to rats by oral gavage, and investigated the effect of different formulas and other chemicalsin Angelica gigas extract on the bioavailability of decursinol. Our results show that gavage ofdecursinol led to a faster attainment of plasma decursinol peak (Tmax ~ 0.7 h) and much higherpeak levels than an equal molar amount administered as decursin/decursinol angelate mixture oras Angelica gigas ethanol extract, resulting in 2­3 fold higher bioavailability as estimated by thearea under the curve of the respective regimens (65 012 vs. 27 033 h · ng/mL for decursinol anddecursin/decursinol angelate treatment groups, respectively). Compared to a formula based onethanol­PEG400­Tween80, carboxyl methyl cellulose was a less optimized vehicle. In addition,we detected peak levels of decursin and decursinol angelate in the plasma of rats administeredwith decursin/decursinol angelate or Angelica gigas extract in the nM range (Tmax ~ 0.5 h) with anewly established sensitive UHPLC­MS/MS method. Furthermore, our data support the liver,instead of intestine, as a major organ site where decursin and decursinol angelate werehydrolyzed to decursinol with a S9 microsomal in vitro metabolism assay. Taken together, ourstudy provided important PK, LC­MS/MS methodology, formulation and metabolism insights in arodent model for the rational design of in vivo efficacy studies of the corresponding chemicals inthe future.

Georg Thieme Verlag KG Stuttgart · New York.

PMID: 23364885 [PubMed ­ indexed for MEDLINE]

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9/4/2015 Single oral dose pharmacokinetics of decursin, decursinol angelate, and decursinol in rats. ­ PubMed ­ NCBI

http://www.ncbi.nlm.nih.gov/pubmed/23364885 2/2

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