The absorption and transport of magnolol in Caco-2 cell model.
OBJECTIVE
To investigate the absorption and transport mechanism of magnolol in Caco-2 cell model.


METHODS
A human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the absorption and transport of magnolol, the effects of time, donor concentration, P-gp inhibitor verapamil, pH and temperature on the absorption and transport of magnolol were investigated. The determination of magnolol was performed by high performance liquid chromatography, then the values of apparent permeability coefficient (P app ) and P ratio Basolateral-to-Apical (BL-to-AP)/Apical-to-Basolateral (AP-to-BL) were calculated.


RESULTS
In Caco-2 cell model, comparing the amounts of transport of AP-to-BL and BL-to-AP, the latter was larger. At the same donor concentration, either the amounts of transport of AP-to-BL or BL-to-AP increased with increase in donor concentration and incubation time. Verapamil could significantly improve the amounts of transport of AP-to-BL. The transport of AP-to-BL and BL-to-AP depended on temperature, and there was no significant effect of pH on the transport of AP-to-BL.


CONCLUSIONS
Magnolol could be transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport, at the same time, the efflux mechanism could be involved.
Research Center of New Drug Development, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
An-Guo
AG
Wu
Bao
B
Zeng
Meng-Qiu
MQ
Huang
Sheng-Mei
SM
Li
Jian-Nan
JN
Chen
Xiao-Ping
XP
Lai
D001692:Biological Transport / Q000187:drug effects; D001713:Biphenyl Compounds / Q000378:metabolism*; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D006863:Hydrogen-Ion Concentration / Q000187:drug effects; D007408:Intestinal Absorption / Q000187:drug effects; D017705:Lignans / Q000378:metabolism*; D008954:Models, Biological; D013696:Temperature; D013997:Time Factors; D014700:Verapamil / Q000494:pharmacology
D001713:Biphenyl Compounds; D017705:Lignans; C005498:magnolol; D014700:Verapamil