The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model

Kelvin Chan, Zhong Qiu Liu, Zhi Hong JIANG, Hua Zhou, Yuen Fan Wong, Hong Xi Xu, Liang LIU*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

64 Citations (Scopus)

Abstract

Paeoniflorin and sinomenine, derived from the root of Paeonia lactiflora Pall. (family Ranunculaceae) and the stem of Sinomenium acutum Rehder & Wilson (family Menispermaceae), respectively, have been, and are currently, widely used for treatment of rheumatic and arthritic diseases in China and Japan. Our previous studies demonstrated that sinomenine could significantly improve the bioavailability of paeoniflorin in rats, but the underlying mechanisms remain unknown. The present study aims to investigate the intestinal kinetic absorptive characteristics of paeoniflorin as well as the absorptive behavior influenced by co-administration of sinomenine using an in vitro everted rat gut sac model. The results showed a good linear correlation between the paeoniflorin absorption in sac contents and the incubation time from 0 to 90 min. However, the concentration dependence showed that a non-linear correlation exists between the paeoniflorin absorption and its concentrations from 10 to 160 μM, and the absorption was saturated at about 80 μM of the drug. Sinomenine at 16 and 136 μM concentrations could significantly enhance the absorption of paeoniflorin (20 μM) by 1.5- and 2.5-fold, respectively. Moreover, two well-known P-glycoprotein inhibitors, verapamil and quinidine, could significantly elevate the absorption of paeoniflorin by 2.1- and 1.5-fold, respectively. Furthermore, sinomenine in a pattern, which influenced paeoniflorin's absorption, manifested as similar to that of P-glycoprotein inhibitors. In conclusion, sinomenine significantly enhance the intestinal absorption of paeoniflorin, subsequently improve the bioavailability of paeoniflorin. The mechanism underlying the improvement of paeoniflorin's bioavailability was proposed that sinomenine could decrease the efflux transport of paeoniflorin by P-glycoprotein.

Original languageEnglish
Pages (from-to)425-432
Number of pages8
JournalJournal of Ethnopharmacology
Volume103
Issue number3
DOIs
Publication statusPublished - 20 Feb 2006

Scopus Subject Areas

  • Pharmacology
  • Drug Discovery

User-Defined Keywords

  • Absorption
  • Bioavailability
  • Everted rat gut sacs
  • P-glycoprotein inhibitor
  • Paeoniflorin
  • Sinomenine

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