Sm. Kuo et Cp. Lin, 17 beta-estradiol inhibition of ascorbic acid accumulation in human intestinal Caco-2 cells, EUR J PHARM, 361(2-3), 1998, pp. 253-259
We investigated the effect of estrogen on the accumulation of ascorbic acid
by human intestinal Caco-2 cells. 17 beta-estradiol, synthetic estrogen di
ethylstilbestrol, and partial agonist tamoxifen were found to inhibit ascor
bic acid accumulation in a dose-dependent fashion. The inhibitory effect of
estrogens can be observed at as short as 5 min of incubation. An additive
effect was observed when they were used in combination. Similar to dietary
flavonoids, inhibition was also observed in two other intestinal cell lines
, HT-29 and IEC-6. These chemicals affected both Na+-dependent and Na+-inde
pendent (K+ substituting Na+) accumulation of ascorbic acid and did not aff
ect the efflux of accumulated ascorbic acid. Kinetic analysis of diethylsti
lbestrol showed a non-competitive inhibition with an apparent K-i of 23 mu
M. The hormone-ascorbic acid interaction in the intestinal cell could help
to explain the known reduction in blood ascorbic acid level among oral cont
raceptive users and female guinea pigs given contraceptive hormones. (C) 19
98 Elsevier Science B.V. All rights reserved.