Permeability of the flavonoids liquiritigenin and its glycosides in licorice roots and davidigenin, a hydrogenated metabolite of liquiritigenin, using human intestinal cell line Caco-2.
The present investigation focused on the transepithelial flux of liquiritigenin (LG), davidigenin (DG), liquiritin (LQ), and liquiritin apioside (LA) using the human colonic cell line Caco-2 as a model of human intestinal absorption. Apparent permeability coefficients (Papp) for the apical to basolateral flux of LG and DG were (16.0 +/- 0.727) x 10(-6) cm/s and (18.2 +/- 1.67) x 10(-6) cm/s, respectively. These Papp were higher than that of the transcellular transport marker propranolol (13.5 +/- 0.34) x 10(-6) cm/s (P < 0.01). Papp for the apical to basolateral flux of LQ and LA were (0.26 +/- 0.12) x 10(-6) cm/s and (0.075 +/- 0.005) x 10(-6) cm/s, respectively. These Papp were lower than that of the paracellular transport marker mannitol (0.64 +/- 0.04) x 10(-6) cm/s (LG, P < 0.01; LA, P < 0.001). These data suggested excellent absorption of LG and DG through the human intestinal epithelial cell line. On the contrary, poor absorption of LQ and LA was expected due to the little transepithelial flux of these compounds in the human colonic cell line Caco-2.
Asano
Takayuki
T
Department of Drug Metabolism and Disposition, Tsumura Research Institute, Tsumura & Co., 3586 Yoshiwara, Ami-machi, Inashiki-gun, Ibaraki 300-1192, Japan. asano_takayuki2@mail.tsumura.co.jp
Ishihara
Kazuhisa
K
Morota
Takashi
T
Takeda
Shuichi
S
Aburada
Masaki
M
D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D044950:Flavanones; D005419:Flavonoids / Q000493:pharmacokinetics*; D006027:Glycosides / Q000493:pharmacokinetics*; D029882:Glycyrrhiza uralensis / Q000737:chemistry*; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D018517:Plant Roots / Q000737:chemistry; D018514:Plant Structures / Q000737:chemistry
D044950:Flavanones; D005419:Flavonoids; D006027:Glycosides; C083152:liquiritigenin