Transport of Schisandra chinensis extract and its biologically-active constituents across Caco-2 cell monolayers - an in-vitro model of intestinal transport.
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.
Madgula
Vamsi L M
VL
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, MS 38677, USA.
Avula
Bharathi
B
Choi
Young W
YW
Pullela
Srinivas V
SV
Khan
Ikhlas A
IA
Walker
Larry A
LA
Khan
Shabana I
SI
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*
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