Transcellular transport of genistein, a soybean-derived isoflavone, across human colon carcinoma cell line (Caco-2).
Genistein, a soybean-derived isoflavone, is thought to have an anticarcinogenic action, but little is known about the cellular mechanisms of its intestinal absorption. This study was designed to investigate the absorption mechanisms of genistein using human colon carcinoma cell line, Caco-2 cells. The apical-to-basolateral transcellular transport of genistein across a Caco-2 cell monolayer was significantly greater than that in the opposite direction. An uptake experiment revealed that cellular uptake of genistein by Caco-2 cells was concentrative. The transcellular transport of genistein was saturable and temperature-dependent, and was inhibited by other flavonoids such as rutin, quercetin, (+)-catechin and (-)-epicatechin. These results suggest that genistein is transported across Caco-2 cells by a carrier-mediated system, located on the apical membrane.
Oitate
M
M
Department of Medico-Pharmaceutical Sciences, Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
Nakaki
R
R
Koyabu
N
N
Takanaga
H
H
Matsuo
H
H
Ohtani
H
H
Sawada
Y
Y
D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D001692:Biological Transport / Q000187:drug effects; D018938:Caco-2 Cells / Q000187:drug effects / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D019833:Genistein / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D007408:Intestinal Absorption; D007529:Isoflavones / Q000737:chemistry / Q000493:pharmacokinetics; D011794:Quercetin / Q000494:pharmacology; D012431:Rutin / Q000494:pharmacology; D013025:Glycine max / Q000737:chemistry
D000970:Antineoplastic Agents; D007529:Isoflavones; D012431:Rutin; D011794:Quercetin; D019833:Genistein