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dc.contributor.authorChan, Kelvin C.
dc.contributor.authorLiu, Zhong Qiu
dc.contributor.authorJiang, Zhi-Hong
dc.contributor.authorZhou, Hua
dc.contributor.authorWong, Yuen Fan
dc.contributor.authorXu, Hong-Xi
dc.contributor.authorLiu, Liang
dc.date.accessioned2008-06-10T09:38:47Z
dc.date.available2008-06-10T09:38:47Z
dc.date.issued2006
dc.identifier.citationJournal of ethnopharmacology, 103(3): 425-432
dc.identifier.issn0378-8741
dc.identifier.pmid16169700
dc.identifier.doi10.1016/j.jep.2005.08.020
dc.identifier.urihttp://hdl.handle.net/2436/29756
dc.description.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.
dc.language.isoen
dc.publisherAmsterdam: Elsevier
dc.relation.urlhttp://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6T8D-4H4T0VC-7&_user=10&_rdoc=1&_fmt=&_orig=search&_sort=d&view=c&_acct=C000050221&_version=1&_urlVersion=0&_userid=10&md5=ba0973ce6bf98e3cac6f31b3e4fb9a4d
dc.subjectMedicine, Chinese Traditional
dc.subjectPaeoniflorin
dc.subjectSinomenine
dc.subjectPharmacokinetics
dc.subjectBioavailability
dc.subjectHerbal medicine
dc.subjectChinese medicine
dc.subjectTraditional Chinese medicine
dc.subjectChinese herbs
dc.subject.meshAnimals
dc.subject.meshAnti-Inflammatory Agents
dc.subject.meshBenzoic Acids
dc.subject.meshBridged Compounds
dc.subject.meshDigoxin
dc.subject.meshDose-Response Relationship, Drug
dc.subject.meshDrugs, Chinese Herbal
dc.subject.meshGlucosides
dc.subject.meshIntestinal Absorption
dc.subject.meshIntestines
dc.subject.meshMale
dc.subject.meshModels, Animal
dc.subject.meshMorphinans
dc.subject.meshP-Glycoprotein
dc.subject.meshPaeonia
dc.subject.meshQuinidine
dc.subject.meshRats
dc.subject.meshRats, Sprague-Dawley
dc.subject.meshSinomenium
dc.subject.meshTime Factors
dc.subject.meshVerapamil
dc.titleThe effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.
dc.typeJournal article
dc.identifier.journalJournal of ethnopharmacology
html.description.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.


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