The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.
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AbstractPaeoniflorin 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 microM, and the absorption was saturated at about 80 microM of the drug. Sinomenine at 16 and 136 microM concentrations could significantly enhance the absorption of paeoniflorin (20 microM) 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.
CitationJournal of ethnopharmacology, 103(3): 425-432
JournalJournal of ethnopharmacology
- Mechanisms responsible for poor oral bioavailability of paeoniflorin: Role of intestinal disposition and interactions with sinomenine.
- Authors: Liu ZQ, Jiang ZH, Liu L, Hu M
- Issue date: 2006 Dec
- [Absorption of extractive Radix Paeoniae Alba in rat everted gut sacs and its interaction with P-glycoprotein].
- Authors: Dong Y, Zhang Y, Yang Q, Li Y, Zhu X
- Issue date: 2009 Apr
- Influence of co-administrated sinomenine on pharmacokinetic fate of paeoniflorin in unrestrained conscious rats.
- Authors: Liu ZQ, Zhou H, Liu L, Jiang ZH, Wong YF, Xie Y, Cai X, Xu HX, Chan K
- Issue date: 2005 May 13
- Pharmacokinetic interaction of paeoniflorin and sinomenine: pharmacokinetic parameters and tissue distribution characteristics in rats and protein binding ability in vitro.
- Authors: Liu ZQ, Jiang ZH, Chan K, Zhou H, Wong YF, Bian ZX, Xu HX, Liu L
- Issue date: 2005 Dec
- [Multi-channel analysis and comparison on absorption difference between paeoniflorin and Paeonia lactiflora extracts].
- Authors: Chen Y, Zhou L, Xin R, Wang J, Jia X
- Issue date: 2012 Jul