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Transepithelial transport of microbial metabolites of quercetin in intestinal Caco-2 cell monolayers.
J Agric Food Chem. 2005 Feb 09; 53(3):601-7.JA

Abstract

m-Hydroxyphenylacetic acid (mHPA), 3,4-dihydroxyphenylacetic acid (DHPA), and 4-hydroxy-3-methoxyphenylacetic acid (HMPA) are major microbial metabolites of quercetin. After administration of quercetin to human subjects, these metabolites are readily detected in blood and urine. mHPA, DHPA, and HMPA are thought to exert protective biological activity within the body due to their antioxidant properties. However, very little work has been published concerning their absorption. I have examined the absorption characteristics of the quercetin metabolites in Caco-2 cells by a coulometric detection method using HPLC-ECD. All of them exhibited nonsaturable transport in Caco-2 cells up to 30 mM, whereas HMPA and mHPA also showed proton-coupled polarized absorption. The proton-coupled directional transport of HMPA and mHPA was inhibited by the substrate of the monocarboxylic acid transporter (MCT). A considerable amount of apically loaded HMPA and mHPA was taken up and transported through to the basolateral side, while almost all of the apically loaded DHPA was retained on the apical side. Furthermore, the transepithelial flux of DHPA was inversely correlated with the paracellular permeability of Caco-2 cells, although those of HMPA and mHPA were almost constant. These results indicate that transport of DHPA was mainly via paracellular diffusion, although HMPA and mHPA were absorbed to some extent by the MCT.

Authors+Show Affiliations

Applied Bioresearch Center, Research and Development Department, Kirin Brewery Co., Ltd., 3 Miyaharacho, Takasaki-shi, Gunma 370-1295, Japan. konishiy@kirin.co.jp

Pub Type(s)

Journal Article

Language

eng

PubMed ID

15686408

Citation

Konishi, Yutaka. "Transepithelial Transport of Microbial Metabolites of Quercetin in Intestinal Caco-2 Cell Monolayers." Journal of Agricultural and Food Chemistry, vol. 53, no. 3, 2005, pp. 601-7.
Konishi Y. Transepithelial transport of microbial metabolites of quercetin in intestinal Caco-2 cell monolayers. J Agric Food Chem. 2005;53(3):601-7.
Konishi, Y. (2005). Transepithelial transport of microbial metabolites of quercetin in intestinal Caco-2 cell monolayers. Journal of Agricultural and Food Chemistry, 53(3), 601-7.
Konishi Y. Transepithelial Transport of Microbial Metabolites of Quercetin in Intestinal Caco-2 Cell Monolayers. J Agric Food Chem. 2005 Feb 9;53(3):601-7. PubMed PMID: 15686408.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transepithelial transport of microbial metabolites of quercetin in intestinal Caco-2 cell monolayers. A1 - Konishi,Yutaka, PY - 2005/2/3/pubmed PY - 2005/3/23/medline PY - 2005/2/3/entrez SP - 601 EP - 7 JF - Journal of agricultural and food chemistry JO - J Agric Food Chem VL - 53 IS - 3 N2 - m-Hydroxyphenylacetic acid (mHPA), 3,4-dihydroxyphenylacetic acid (DHPA), and 4-hydroxy-3-methoxyphenylacetic acid (HMPA) are major microbial metabolites of quercetin. After administration of quercetin to human subjects, these metabolites are readily detected in blood and urine. mHPA, DHPA, and HMPA are thought to exert protective biological activity within the body due to their antioxidant properties. However, very little work has been published concerning their absorption. I have examined the absorption characteristics of the quercetin metabolites in Caco-2 cells by a coulometric detection method using HPLC-ECD. All of them exhibited nonsaturable transport in Caco-2 cells up to 30 mM, whereas HMPA and mHPA also showed proton-coupled polarized absorption. The proton-coupled directional transport of HMPA and mHPA was inhibited by the substrate of the monocarboxylic acid transporter (MCT). A considerable amount of apically loaded HMPA and mHPA was taken up and transported through to the basolateral side, while almost all of the apically loaded DHPA was retained on the apical side. Furthermore, the transepithelial flux of DHPA was inversely correlated with the paracellular permeability of Caco-2 cells, although those of HMPA and mHPA were almost constant. These results indicate that transport of DHPA was mainly via paracellular diffusion, although HMPA and mHPA were absorbed to some extent by the MCT. SN - 0021-8561 UR - https://www.unboundmedicine.com/medline/citation/15686408/Transepithelial_transport_of_microbial_metabolites_of_quercetin_in_intestinal_Caco_2_cell_monolayers_ L2 - https://doi.org/10.1021/jf048662l DB - PRIME DP - Unbound Medicine ER -