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

2.50
Hdl Handle:
http://hdl.handle.net/2436/29756
Title:
The effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.
Authors:
Chan, Kelvin C.; Liu, Zhong Qiu; Jiang, Zhi-Hong; Zhou, Hua; Wong, Yuen Fan; Xu, Hong-Xi; Liu, Liang
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 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.
Citation:
Journal of ethnopharmacology, 103(3): 425-432
Publisher:
Amsterdam: Elsevier
Journal:
Journal of ethnopharmacology
Issue Date:
2006
URI:
http://hdl.handle.net/2436/29756
DOI:
10.1016/j.jep.2005.08.020
PubMed ID:
16169700
Additional Links:
http://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
Type:
Article
Language:
en
ISSN:
0378-8741
Appears in Collections:
Pharmacy and Natural Products Research Group

Full metadata record

DC FieldValue Language
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): 425-432en
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.en
dc.language.isoenen
dc.publisherAmsterdam: Elsevieren
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=ba0973ce6bf98e3cac6f31b3e4fb9a4den
dc.subjectPaeoniflorinen
dc.subjectSinomenineen
dc.subjectPharmacokineticsen
dc.subjectBioavailabilityen
dc.subjectHerbal medicineen
dc.subjectChinese medicineen
dc.subjectTraditional Chinese medicineen
dc.subjectChinese herbsen
dc.subjectMedicine, Chinese Traditional-
dc.subject.meshAnimalsen
dc.subject.meshAnti-Inflammatory Agentsen
dc.subject.meshBenzoic Acidsen
dc.subject.meshBridged Compoundsen
dc.subject.meshDigoxinen
dc.subject.meshDose-Response Relationship, Drugen
dc.subject.meshDrugs, Chinese Herbalen
dc.subject.meshGlucosidesen
dc.subject.meshIntestinal Absorptionen
dc.subject.meshIntestinesen
dc.subject.meshMaleen
dc.subject.meshModels, Animalen
dc.subject.meshMorphinansen
dc.subject.meshP-Glycoproteinen
dc.subject.meshPaeoniaen
dc.subject.meshQuinidineen
dc.subject.meshRatsen
dc.subject.meshRats, Sprague-Dawleyen
dc.subject.meshSinomeniumen
dc.subject.meshTime Factorsen
dc.subject.meshVerapamilen
dc.titleThe effects of sinomenine on intestinal absorption of paeoniflorin by the everted rat gut sac model.en
dc.typeArticleen
dc.identifier.journalJournal of ethnopharmacologyen

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