title: Transport of Schisandra chinensis extract and its biologically-active constituents across Caco-2 cell monolayers - an in-vitro model of intestinal transport.
abstract: We have determined the intestinal transport of Schisandra chinensis extract and its lignans (gomisin A, gomisin N and schisandrin C) in the Caco-2 cell monolayer model. The transport across monolayers was examined for 2 h in absorptive and secretory directions. Quantitation of lignans was performed by HPLC. Out of the three lignans, gomisin A exhibited bi-directional transport, with P(app) values in the range of 25-29 x 10(-6) cm s(-1), indicating a passive diffusion. Gomisin N, mixture and Schisandra extract displayed a higher transport in the secretory direction with efflux ratios in the range of 2.2-5.2. The efflux was decreased in the presence of inhibitors of multidrug resistance protein (MRP) transporter (MK-571) and P-glycoprotein (verapamil) indicating a possible involvement of an efflux pump and MRP in the transport of Schisandra lignans. Poor transport of schisandrin C was observed which could not be quantitated. The permeability of gomisin A in the isolated form was significantly different compared with the mixture or extract.
authors.affiliation: National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, MS 38677, USA.
authors.forename: Vamsi L M
authors.initials: VL
authors.lastname: Madgula
authors.forename: Bharathi
authors.initials: B
authors.lastname: Avula
authors.forename: Young W
authors.initials: YW
authors.lastname: Choi
authors.forename: Srinivas V
authors.initials: SV
authors.lastname: Pullela
authors.forename: Ikhlas A
authors.initials: IA
authors.lastname: Khan
authors.forename: Larry A
authors.initials: LA
authors.lastname: Walker
authors.forename: Shabana I
authors.initials: SI
authors.lastname: Khan
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D001682:Biological Availability; D001692:Biological Transport; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D034242:Cyclooctanes / Q000493:pharmacokinetics*; D004058:Diffusion; D004149:Dioxoles / Q000493:pharmacokinetics*; D004347:Drug Interactions; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000737:chemistry; D017705:Lignans / Q000493:pharmacokinetics*; D008516:Medicine, Chinese Traditional; D008954:Models, Biological; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000378:metabolism; D010539:Permeability; D010936:Plant Extracts / Q000493:pharmacokinetics; D011083:Polycyclic Compounds / Q000493:pharmacokinetics*; D032141:Schisandra / Q000737:chemistry*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D034242:Cyclooctanes; D004149:Dioxoles; D017705:Lignans; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D010936:Plant Extracts; D011083:Polycyclic Compounds; C015499:schizandrin B; C033585:schizandrol B; C031409:schizandrin C