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Transport of hop bitter acids across intestinal Caco-2 cell monolayers

Ko Cattoor UGent, Marc Bracke UGent, Dieter Deforce UGent, Denis De Keukeleire UGent and Arne Heyerick UGent (2010) JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY. 58(7). p.4132-4140
abstract
Several health-beneficial properties of hop bitter acids have been reported; however, scientific data on the bioavailability of these compounds are lacking. As a first approach to study the bioavailability, the epithelial transport of hop α- and β-acids across Caco-2 monolayers was investigated. Hop acids were added either to the apical or to the basolateral chamber and, at various time points, amounts transported to the receiving compartment were determined. The monolayer integrity control was performed by using marker compounds (atenolol and propranolol), transepithelial electrical resistance (TEER) measurement, and determination of the fluorescein efflux. The TEER and fluorescein efflux confirmed the preservation of the monolayer integrity. The membrane permeability of the α-acids (apparent permeability coefficients for apical to basolateral transport (PappAB) ranged from 14 x 10-6 to 41 x 10-6 cm/s) was determined to be substantially higher than that of the β-acids (PappAB values ranging from 0.9 x 10-6 to 2.1 x 10-6 cm/s). Notably, the β-acids exhibited significantly different bidirectional Papp values with efflux ratios around 10. The involvement of carrier-mediated transport for β-acids (active efflux pathway by P-gp, BCRP, and/or MRP-2 type efflux pumps) could be confirmed by transport experiments with specific inhibitors (verapamil and indomethacin). It appears that R-acids are efficiently absorbed, whereas the permeability of β-acids is low. Limiting factors in the absorption of β-acids could involve P-gp and MRP-2 type efflux transporters and phase II metabolism.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
β-acids, Caco-2 transport, hop bitter acids, α-acids, alpha-acids, beta-acids, ORAL-DRUG ABSORPTION, HUMULUS-LUPULUS L., ISO-ALPHA-ACIDS, LINE CACO-2, IN-VITRO, ALCOHOL-CONSUMPTION, ACTIVE-TRANSPORT, BILE-ACIDS, BEER HOP, PERMEABILITY
journal title
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
J. Agric. Food Chem.
volume
58
issue
7
pages
4132 - 4140
Web of Science type
Article
Web of Science id
000276232700037
JCR category
AGRICULTURE, MULTIDISCIPLINARY
JCR impact factor
2.816 (2010)
JCR rank
2/55 (2010)
JCR quartile
1 (2010)
ISSN
0021-8561
DOI
10.1021/jf904079h
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
954592
handle
http://hdl.handle.net/1854/LU-954592
date created
2010-05-27 09:44:38
date last changed
2010-05-27 14:14:18
@article{954592,
  abstract     = {Several health-beneficial properties of hop bitter acids have been reported; however, scientific data on the bioavailability of these compounds are lacking. As a first approach to study the bioavailability, the epithelial transport of hop \ensuremath{\alpha}- and \ensuremath{\beta}-acids across Caco-2 monolayers was investigated. Hop acids were added either to the apical or to the basolateral chamber and, at various time points, amounts transported to the receiving compartment were determined. The monolayer integrity control was performed by using marker compounds (atenolol and propranolol), transepithelial electrical resistance (TEER) measurement, and determination of the fluorescein efflux. The TEER and fluorescein efflux confirmed the preservation of the monolayer integrity. The membrane permeability of the \ensuremath{\alpha}-acids (apparent permeability coefficients for apical to basolateral transport (PappAB) ranged from 14 x 10-6 to 41 x 10-6 cm/s) was determined to be substantially higher than that of the \ensuremath{\beta}-acids (PappAB values ranging from 0.9 x 10-6 to 2.1 x 10-6 cm/s). Notably, the \ensuremath{\beta}-acids exhibited significantly different bidirectional Papp values with efflux ratios around 10. The involvement of carrier-mediated transport for \ensuremath{\beta}-acids (active efflux pathway by P-gp, BCRP, and/or MRP-2 type efflux pumps) could be confirmed by transport experiments with specific inhibitors (verapamil and indomethacin). It appears that R-acids are efficiently absorbed, whereas the permeability of \ensuremath{\beta}-acids is low. Limiting factors in the absorption of \ensuremath{\beta}-acids could involve P-gp and MRP-2 type efflux transporters and phase II metabolism.},
  author       = {Cattoor, Ko and Bracke, Marc and Deforce, Dieter and De Keukeleire, Denis and Heyerick, Arne},
  issn         = {0021-8561},
  journal      = {JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY},
  keyword      = {\ensuremath{\beta}-acids,Caco-2 transport,hop bitter acids,\ensuremath{\alpha}-acids,alpha-acids,beta-acids,ORAL-DRUG ABSORPTION,HUMULUS-LUPULUS L.,ISO-ALPHA-ACIDS,LINE CACO-2,IN-VITRO,ALCOHOL-CONSUMPTION,ACTIVE-TRANSPORT,BILE-ACIDS,BEER HOP,PERMEABILITY},
  language     = {eng},
  number       = {7},
  pages        = {4132--4140},
  title        = {Transport of hop bitter acids across intestinal Caco-2 cell monolayers},
  url          = {http://dx.doi.org/10.1021/jf904079h},
  volume       = {58},
  year         = {2010},
}

Chicago
Cattoor, Ko, Marc Bracke, Dieter Deforce, Denis De Keukeleire, and Arne Heyerick. 2010. “Transport of Hop Bitter Acids Across Intestinal Caco-2 Cell Monolayers.” Journal of Agricultural and Food Chemistry 58 (7): 4132–4140.
APA
Cattoor, K., Bracke, M., Deforce, D., De Keukeleire, D., & Heyerick, A. (2010). Transport of hop bitter acids across intestinal Caco-2 cell monolayers. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 58(7), 4132–4140.
Vancouver
1.
Cattoor K, Bracke M, Deforce D, De Keukeleire D, Heyerick A. Transport of hop bitter acids across intestinal Caco-2 cell monolayers. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY. 2010;58(7):4132–40.
MLA
Cattoor, Ko, Marc Bracke, Dieter Deforce, et al. “Transport of Hop Bitter Acids Across Intestinal Caco-2 Cell Monolayers.” JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY 58.7 (2010): 4132–4140. Print.