Transport of trans-tiliroside (kaempferol-3-β-D-(6"-p-coumaroyl-glucopyranoside) and related flavonoids across Caco-2 cells, as a model of absorption and metabolism in the small intestine.

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Zijun LuoAndrea J Day

Abstract

1. Absorption and metabolism of tiliroside (kaempferol 3-β-D-(6"-p-coumaroyl)-glucopyranoside) and its related compounds kaempferol, kaempferol-3-glucoside and p-coumaric acid were investigated in the small intestinal Caco-2 cell model. Apparent permeation (Papp) was determined as 0.62 × 10(-6) cm/s, 3.1 × 10(-6) cm/s, 0 and 22.8 × 10(-6) cm/s, respectively. 2. Mechanistic study showed that the transportation of tiliroside, kaempferol-3-glucoside and p-coumaric acid in Caco-2 model were transporter(s) involved, while transportation of kaempferol was solely by passive diffusion mechanism. 3. Efflux transporters, multi-drug-resistance-associated protein-2 (MRP2), were shown to play a role in limiting the uptake of tiliroside. Inhibitors of MRP2, (MK571 and rifampicin) and co-incubation with kaempferol (10 μM), increased transfer from the apical to the basolateral side by three to five fold. 4. Metabolites of kaempferol-3-glucoside and p-coumaric acid were not detected in the current Caco-2 model, while tiliroside was metabolised to a limited extent, with two tiliroside mono-glucuronides identified; and kaempferol was metabolised to a higher extent, with three mono-glucuronides and two mono-sulfates identified. 5. In conclusion, t...Continue Reading

References

Jan 6, 1999·Journal of Pharmaceutical Sciences·J D IrvineJ R Grove
Jul 30, 1999·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·N G SchipperP Artursson
Dec 19, 2000·Free Radical Biology & Medicine·A J DayG Williamson
Dec 29, 2000·Phytochemistry·G G LeitãoF Delle Monache
Feb 6, 2003·European Journal of Pharmacology·Araceli SalaJosé Luis Rosí
Jun 6, 2003·Bioscience, Biotechnology, and Biochemistry·Yutaka Konishi, Makoto Shimizu
Apr 29, 2004·Journal of Agricultural and Food Chemistry·Yutaka Konishi, Shoko Kobayashi
May 28, 2004·European Journal of Clinical Nutrition·M S DuPontP A Kroon
Jan 11, 2005·The American Journal of Clinical Nutrition·Gary Williamson, Claudine Manach
Apr 3, 2007·Bioorganic & Medicinal Chemistry Letters·Kiyofumi NinomiyaMasayuki Yoshikawa
Oct 24, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Laure PoquetGary Williamson
Nov 24, 2007·Fundamental & Clinical Pharmacology·Nathalie MaubonOlivier Fardel
Feb 19, 2011·Journal of Agricultural and Food Chemistry·Zijun LuoAndrea J Day

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Citations

Jul 28, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Virgilio Alfonso Juárez RamírezEnrique Jiménez-Ferrer
Sep 1, 2018·Comprehensive Reviews in Food Science and Food Safety·Daniel M GrochowskiMichał Tomczyk
Apr 21, 2021·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Xiongwei YinZhining Xia

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