Caco-2 monolayers in experimental and theoretical predictions of drug transport

Artursson, Per; Palm, Katrin; Luthman, Kristina

doi:10.1016/s0169-409x(96)00415-2

Cited by 616 publications

(705 citation statements)

References 89 publications

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“…Due to different culture conditions and different numbers of passages, Caco-2 cells have often acquired different properties. Thus, the expression of differentiation markers typical of enterocytes, change with increasing numbers of passages (Artursson et al 2001 ). Also, parameters like transepithelial electric resistance (TEER) and proliferation rate have been reported to increase with passage number (Briske Andersson et al 1997 ).…”

Section: Stability Consistency and Reproducibilitymentioning

confidence: 99%

Caco-2 Cell Line

Lea

2015

The Impact of Food Bioactives on Health

215

160

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The human epithelial cell line Caco-2 has been widely used as a model of the intestinal epithelial barrier. The Caco-2 cell line is originally derived from a colon carcinoma. However, one of its most advantageous properties is its ability to spontaneously differentiate into a monolayer of cells with many properties typical of absorptive enterocytes with brush border layer as found in the small intestine. The Caco-2 cell line is heterogeneous and contains cells with slightly different properties. Thus, cultivation conditions can be expected to select for the growth of subpopulations of cells resulting in a cellular model system with properties that may differ from the original cell line. Accordingly, results obtained under similar experimental conditions in different laboratories may not be directly comparable. Due to this, a variety of cloned Caco-2 cell lines has been established, and described in the literature. This chapter will however, focus on describing how to handle and cultivate the original Caco-2 cell line as obtained from cell culture collections like American Type Culture Collection and the European Collection of Cell Cultures. Detailed protocols for handling the Caco-2 cells in the laboratory are provided. Furthermore, in Chap. 9 general protocols for measuring barrier function by transepithelial resistance (TEER), and monolayer integrity by Lucifer Yellow fl ux are described. Proper testing of the cell monolayer is absolutely critical in exploiting Caco-2 cells to measure interaction, uptake and cellular transport of drugs and food components.

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Section: Stability Consistency and Reproducibilitymentioning

confidence: 99%

Caco-2 Cell Line

Lea

2015

The Impact of Food Bioactives on Health

215

160

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“…The mannitol permeability assay was performed using D-Mannitol-1-14 C, (Sigma) as described previously (Artursson et al, 2001). …”

Section: Apparent Permeabilitymentioning

confidence: 99%

“…Since A2(D-R18)-C10 had a P app value of 0.97 Â 10 À6 , it should be well absorbed in vivo. Passive transport pathways across the epithelium are through tight junctions and across the apical and basolateral cell membranes (Artursson et al, 2001;Wong et al, 2002). The poorly permeable hydrophilic A2(D-R18) probably diffused through tight junctions, which provide the usual route for water-soluble compounds.…”

Section: Permeability Of Lipoamino Acid-conjugated Peptidesmentioning

confidence: 99%

Functional implications of modifying RyR‐activating peptides for membrane permeability

Dulhunty

Cengia

Young

et al. 2005

British J Pharmacology

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1 Our aim was to determine whether lipoamino acid conjugation of peptides that are high-affinity activators of ryanodine receptor (RyR) channels would (a) render the peptides membrane permeable, (b) alter their structure or (a) reduce their activity. The peptides correspond to the A region of the II-III loop of the skeletal dihydropyridine receptor. 2 The lipoamino acid conjugation increased the apparent permeability of the peptide across the Caco-2 cell monolayer by up to B20-fold. 3 Nuclear magnetic resonance showed that the a-helical structure of critical basic residues, required for optimal activation of RyRs, was retained after conjugation. 4 The conjugated peptides were more effective in enhancing resting Ca 2 þ release, Ca 2 þ -induced Ca 2 þ release and caffeine-induced Ca 2 þ release from isolated sarcoplasmic reticulum (SR) than their unconjugated counterparts, and significantly enhanced caffeine-induced Ca 2 þ release from mechanically skinned extensor digitorum longus (EDL) fibres. 5 The effect of both conjugated and unconjugated peptides on Ca 2 þ release from skeletal SR was 30-fold greater than their effect on either cardiac Ca 2 þ release or on the Ca 2 þ Mg 2 þ ATPase. 6 A small and very low affinity effect of the peptide in slowing Ca 2 þ uptake by the Ca 2 þ , Mg 2 þ ATPase was exacerbated by lipoamino acid conjugation in both isolated SR and in skinned EDL fibres. 7 The results show that lipoamino acid conjugation of A region peptides increases their membrane permeability without impairing their structure or efficacy in activating skeletal and cardiac RyRs.

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“…They are different from the other bioactive ingredients, as their solubility in water is very high, and thus can be readily extracted with water. They may be adsorbed by the transcytosis routes and the active carrier-mediated transcellular [22,36] in human body, and thus have no significant retention on ILC column, which can only mimic the passive transcellular [22]. A large and off-scale peak with weak retention, which might be mainly contributed by polysaccharides, can be observed for the nbutanol extract and remnant water extract as shown in Fig.…”

Section: Fractions Partitioned With Different Solvents From Water Extmentioning

confidence: 99%

“…Liposomes [10][11][12] formed by phosphatidylcholine (PC), the main components found in cell membrane, or unilaminar phospholipids [13][14][15][16], were non-covalently or covalently immobilized on soft gel or porous silica stationary phases to probe the penetration ability of compounds through biological membranes, which has been considered as important parameters to evaluate their bioactivity [17,18]. Initial studies indicated that a good correlation between ILC and intestinal mucosa model was obtained for a series of drugs [19][20][21][22]. Previously, we investigated the application of ILC in separation and analysis of permeable components in single Chinese herb [23].…”

Section: Introductionmentioning

confidence: 99%