Cellular absorption of anthraquinones emodin and chrysophanol in human intestinal Caco-2 cells

• Published in: Bioscience, biotechnology, and biochemistry Vol. 71; no. 7; pp. 1636 - 1643
• Main Authors: Teng, Z.H.(Fourth Military Medical Univ., Shaan'xi (China)), Zhou, S.Y, Ran, Y.H, Liu, X.Y, Yang, R.T, Yang, X, Yuan, C.J, Mei, Q.B
• Format: Journal Article
• Language: English
• Published: Tokyo Japan Society for Bioscience, Biotechnology, and Agrochemistry 01.07.2007; Japan Society for Bioscience Biotechnology and Agrochemistry; Oxford University Press
• Subjects: ABSORCION DIGESTIVA; ABSORPTION DIGESTIVE; ANTHRAQUINONE; ANTHRAQUINONES; Anthraquinones - pharmacokinetics; ANTRAQUINONAS; Biological and medical sciences; Caco-2 cell; Caco-2 Cells; chrysophanol; DIGESTIVE ABSORPTION; emodin; Emodin - pharmacokinetics; ENFERMEDADES HUMANAS; Enzyme Inhibitors - pharmacokinetics; Fundamental and applied biological sciences. Psychology; GENERO HUMANO; GENRE HUMAIN; HUMAN DISEASES; Humans; intestinal absorption; Intestines - cytology; Intestines - metabolism; MALADIE DE L'HOMME; MANKIND; MICOTOXINAS; Mutagens - pharmacokinetics; MYCOTOXINE; MYCOTOXINS; Human; Absorption; Anthraquinone; chrysophanol; Gut; Caco-2 cell; intestinal absorption; emodin
• ISSN: 0916-8451; 1347-6947
• DOI: 10.1271/bbb.70025

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+-11.57nmol/l.mg.protein, respectively. The absorption of each anthraquinone was significantly lower at 4 deg C than that of 37 deg 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.