[Intestional absorption and mechanism of tiliani in Caco-2 cell model].
OBJECTIVE
To observe the uptake of tiliani in Caco-2 Cell.


METHODS
A human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the kinetics of uptake, transport and efflux kinetics of tiliani at small intestine. The effect of time, pH, drug concentration and inhibitors on the uptake of tiliani were investigated. The determination of tiliani was performed by HPLC.


RESULTS
Tiliani in Caco-2 cell uptake was time-dependent. Tiliani in Caco-2 cell uptake was concentration-dependent at 4-16 mg x L(-1) consistent with passive diffusion process. The acid condition was good for the uptake of tiliani at pH 5-8. Compared with the control group, tiliani cell uptake was significantly higher after additional treatmeant with verapamil (1.545 +/- 0.010) mg x g(-1), (P < 0.05), and tiliani cell uptake was significantly lower after additional treatmeanet with sodium azide (0.994 +/- 0.003) mg x g(-1) (P < 0.05), with 2,4-dinitrophenol (1.174 +/- 0.030) mg x g(-1) (P < 0.05), and with phloridzin (1.098 +/- 0.021) mg x g(-1) (P < 0.05). Compared with the control group, tiliani cell uptake was not significantly after additional treatmeant with lactose (1.470 +/- 0.025) mg x g(-1), Papp of Basolateral to Apical was much more than that of Apical to Basolateral (1.10 Fold).


CONCLUSIONS
P-glycoproteins and SGLT1 participate in the conveying process of tiliani in Caco-2 cells. The uptake of tiliani has no relationship to LPH. passive transport and carrier-mediated transport participate in the uptake process of tiliani in Caco-2 cells.
School of Pharmacy, Shihezi University, Shihezi 832008, China.
Zhiqiao
Z
Huang
Jianguo
J
Xing
Xinchun
X
Wang
Sheng
S
Wang
Yong
Y
Yuan
D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D005419:Flavonoids / Q000493:pharmacokinetics*; D006027:Glycosides / Q000493:pharmacokinetics*; D006801:Humans; D007408:Intestinal Absorption; D007700:Kinetics; D014700:Verapamil / Q000494:pharmacology
D005419:Flavonoids; D006027:Glycosides; C426884:tilianin; D014700:Verapamil