Cellular absorption of anthraquinones emodin and chrysophanol in human intestinal Caco-2 cells.
The intestinal absorption characteristics of anthraquinones emodin and chrysophanol were observed by measuring the intracellular accumulation across Caco-2 cells by the reverse-phase high performance liquid chromatography. The intracellular accumulation of chrysophanol was much greater than that of emodin, the maximum absorption of emodin and chrysophanol being 414.02+/-15.28 and 105.56+/-11.57 nmol/l x mg x protein, respectively. The absorption of each anthraquinone was significantly lower at 4 degrees C than that of 37 degrees C. The effects of the transport inhibitors, verapamil, cyclosporine and phloridzin, on the intracellular accumulation were also examined. Verapamil and cyclosporine increased the absorption of emodin and chrysophanol, while phloridzin inhibited their absorption, all in a dose-dependent manner. These results suggest that the absorption characteristics of emodin and chrysophanol were closely related to their special structure with the hydroxy groups. It is also likely that a specific transport system mediated the intracellular accumulation of emodin and chrysophanol across the Caco-2 cells.
Teng
Zeng-hui
ZH
Department of Pharmacology, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaan'xi, China.
Zhou
Si-yuan
SY
Ran
Yu-hua
YH
Liu
Xin-you
XY
Yang
Run-tao
RT
Yang
Xi
X
Yuan
Cheng-jun
CJ
Mei
Qi-bing
QB
D000880:Anthraquinones / Q000493:pharmacokinetics*; D018938:Caco-2 Cells; D004642:Emodin / Q000493:pharmacokinetics*; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics*; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism*; D007422:Intestines / Q000166:cytology; D009153:Mutagens / Q000493:pharmacokinetics*
D000880:Anthraquinones; D004791:Enzyme Inhibitors; D009153:Mutagens; D004642:Emodin; C027113:chrysophanic acid