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1.
It was previously reported that a fluorescent marker dye, fluorescein, is transported via the monocarboxylic acid transporter (MCT). Fluorescein transport was competitively inhibited by MCT substrates such as ferulic and salicylic acids. Tea polyphenols, in particular, epigallocatechin gallate (EGCg) and epicatechin gallate (ECg), inhibited the transport of fluorescein. Tea polyphenols also inhibited the transport of salicylic and ferulic acids, suggesting tea polyphenols might be substrates of MCT. However, the transepithelial flux of tea polyphenols was much lower than that of the MCT substrates and was inversely correlated with the paracellular permeability of Caco-2 cell monolayers. These findings suggest that tea polyphenols are not substrates but inhibitors of MCT. Furthermore, the transepithelial transport of these polyphenols is mainly via paracellular diffusion. However, directional transport of ECg and EGCg from the basolateral to the apical side was observed, indicating that the behavior of tea polyphenols in the intestinal epithelium is complex.  相似文献   

2.
Lactic acid (LA) has been proposed to be an enhancer for dietary iron absorption, but contradictory results have also been reported. In the present study, fully differentiated Caco-2 cell monolayers were used to evaluate the effects of LA (1-50 mmol/L) on the cellular retention and transepithelial transport of soluble non-heme iron (as ferric nitrilotriacetate). Our data revealed a linear decline in Fe(III) retention with respect to the concentration of LA added. In the presence of 50 mmol/L LA, retention of Fe(III) and Fe(II) decreased 57% and 58%, respectively. In contrast, transfer of Fe(III) across the cell monolayer was doubled, while Fe(II) transfer across the cell monolayer decreased 35%. We conclude that LA reduces cellular retention and transepithelial transport of Fe(II) by Caco-2 cells in a dose-dependent manner. However, while LA also reduces retention of Fe(III) by Caco-2 cells, the transfer of Fe(III) across cell monolayers is enhanced, possibly due to effects on paracellular transport.  相似文献   

3.
A-type procyanidin oligomers in cranberries are known to inhibit the adhesion of uropathogenic bacteria. B-type procyanidin dimers and trimers are absorbed by humans. The absorption of A-type procyanidins from cranberries in humans has not been demonstrated. This study examined the transport of A-type cranberry procyanidin dimers, trimers, and tetramers on differentiated human intestinal epithelial Caco-2 cell monolayers. Procyanidins were extracted from cranberries and purified using chromatographic methods. Fraction I contained predominantly A-type procyanidin dimer A2 [epicatechin-(2-O-7, 4-8)-epicatechin]. Fraction II contained primarily A-type trimers and tetramers, with B-type trimers, A-type pentamers, and A-type hexamers being minor components. Fraction I or II in solution was added onto the apical side of the Caco-2 cell membranes. The media at the basolateral side of the membranes were analyzed using HPLC-MS(n) after 2 h. Data indicated that procyanidin dimer A2 in fraction I and A-type trimers and tetramers in fraction II traversed across Caco-2 cell monolayers with transport ratio of 0.6%, 0.4%, and 0.2%, respectively. This study demonstrated that A-type dimers, trimers, and tetramers were transported across Caco-2 cells at low rates, suggesting that they could be absorbed by humans after cranberry consumption.  相似文献   

4.
Both chlorogenic and caffeic acids exhibited nonsaturable transport in Caco-2 cells, whereas caffeic acid also showed proton-coupled polarized absorption. Thus, the absorption efficiency of caffeic acid was greater than that of chlorogenic acid. Polarized transport of caffeic acid was inhibited by substrates of MCT such as benzoic and acetic acids. Almost all of the apically loaded chlorogenic and caffeic acid was retained on the apical side, and the transepithelial flux was inversely correlated with the paracellular permeability of Caco-2 cells. These results indicate that transport was mainly via paracellular diffusion, although caffeic acid was absorbed to a lesser extent by the monocarboxylic acid transporter (MCT). Furthermore, m-coumaric acid and 3-(m-hydroxyphenyl)propionic acid, the main metabolites of chlorogenic and caffeic acid by colonic microflora, competitively inhibited the transport of fluorescein, a known substrate of MCT. This suggests that their absorption could also be mediated by MCT. These findings have exemplified the physiological importance of MCT-mediated absorption in both phenolic acids per se and their colonic metabolites.  相似文献   

5.
The intestinal absorption characteristics of phenolic acids (PAs) have been elucidated in terms of their affinity for the monocarboxylic acid transporter (MCT). Recently, the involvement of the stomach has been implicated in the absorption of polyphenols. The present work demonstrates that the gastric absorption efficiency of each PA is apparently different between various PAs. Various PAs with different affinities for MCT were administered (2.25 mumol) to rat stomach, and then the plasma concentration of the PA was measured. The plasma concentration of ferulic acid (FA) peaked 5 min after administration in the stomach. At 5 min after administration, the plasma concentration of each PA increased in the order: gallic acid = chlorogenic acid < caffeic acid < p-coumaric acid = FA. This order matches their respective affinity for MCT in Caco-2 cells, which we have demonstrated in previous studies. These results indicated that MCT might be involved in the gastric absorption of PAs, similar to the intestinal absorption.  相似文献   

6.
The effect of three plant lectins, soybean lectin (SBA), Japanese jack bean lectin (CGA), and wheat germ lectin (WGA), on the transport of various food factors, such as isoflavones, quercetin, dipeptides, and calcium ions, were investigated by use of an intestinal tract model, Caco-2 cell monolayers. The lectins increased the isoflavone transport but had no effect on aglycon transport. SBA increased the transport of quercetin glycosides, whereas CGA and WGA had no effect. The lectins increased the transport of calcium ions but showed no effect on the transport of dipeptides, carnosine, and anserine. Although SBA did not change the transepithelial electrical resistance (TER) value of the Caco-2 cell monolayers, CGA and WGA decreased the TER value. These results indicate that plant lectins affect the transport of food factors in different manners, presumably due to their specific sugar binding activity.  相似文献   

7.
We have investigated the absorption rates of two purified major allergen 2S albumins, Ber e 1 from Brazil nuts (Bertholletia excelsa Humb. & Bonpl.) and Ses i 1 from white sesame seeds (Sesamum indicum L.), across human intestinal epithelial Caco-2 cell monolayers following gastrointestinal digestion in vitro. The transport from apical to basolateral side in cell monolayers was evaluated by RP-HPLC-UV and indirect competitive ELISA methods, being confirmed by western-blotting analysis. Significant amounts (approximately 15-25 nmol micromol(-1) initial amount/h) of intact Ber e 1 and Ses i 1 were found in the basolateral side. The absorption rates of both plant allergens through the cell monolayer were shown to be constant during the whole incubation period (4 h at 37 degrees C), verifying that the permeability of the membrane was not altered by the allergen digests. Our findings revealed that both purified 2S albumin allergens may be able to survive in immunologically reactive forms to the simulated harsh conditions of the gastrointestinal tract to be transported across the Caco-2 cell monolayers, so that they would be able to sensitize the mucosal immune system and/or elicit an allergic response.  相似文献   

8.
Angiotensin converting enzyme (ACE) inhibitory peptides are biologically active peptides that play a very important role in blood pressure regulation. In previous experiments, we obtained an ACE inhibitory peptide Val-Leu-Pro-Val-Pro (VLPVP) by DNA recombinant technology. The purpose of this study was to examine the bidirectional transport of VLPVP by using the human intestinal Caco-2 monolayers. The permeability coefficient ( P app) values of VLPVP over 4-8 mmol/L ranged from 7.44 x 10(-8) to 1.35 x 10(-6) cm/s for apical (AP) to basolateral (BL) transport, while the P app values for BL to AP flux were significantly lower than those for the AP to BL flux, with efflux ratio values of 0.74-0.13 over 4-8 mM. Preincubation of the paracellular transport enhancer (sodium deoxycholate), the inhibitor of multidrug resistant protein (MK-571), or sodium azide stimulated efflux of VLPVP significantly ( p < 0.01); these results indicate that the transport of VLPVP across Caco-2 monolayers was involved in paracellular diffusion and MRP2 transport.  相似文献   

9.
The aim of this study is to illustrate the in vivo and in vitro absorption of theasinensins B and A that are (-)-epigallocatechin-3-O-gallate (EGCG)-(-)-epigallocatechin (EGC) dimer and EGCG dimer, respectively, and their transport pathway across the intestinal membrane. Our animal study by a single oral administration to rats demonstrated the intact absorption of theasinensins into the blood system, which was estimated to be a >10-fold lower absorption amount than EGCG. The in vitro absorption study indicated that theasinensins can be transported across Caco-2 cell monolayers, while their permeability coefficients were also >10-fold lower than those of EGCG and EGC. Transport experiments using cytochalasin D or quercetin as a tight junction (TJ) modulator and a non-saturable permeation revealed that theasinensins were transported across Caco-2 cells in a TJ paracellular diffusion route. In conclusion, the dimers of condensed catechins, theasinensins B and A, can be absorbed intact into rat blood and transported across Caco-2 cell monolayers probably through a TJ paracellular pathway.  相似文献   

10.
Previous studies have shown that organic acids have an impact on both Fe(II) and Fe(III) uptake in Caco-2 cell. However, to what extent this effect is correlated with the anion of organic acids per se, or with the resulting decrease in pH, has not yet been clarified. Therefore, we studied the effect of five organic acids (tartaric, succinic, citric, oxalic, and propionic acid) on the absorption of Fe(II) and Fe(III) in Caco-2 cells and compared this with sample solutions without organic acids but set to equivalent pH by HCl. The results showed that the mechanisms behind the enhancing effect of organic acids differed for the two forms of iron. For ferric iron the organic acids promoted uptake both by chelation and by lowering the pH, whereas for ferrous iron the promoting effect was caused only by the lowered pH.  相似文献   

11.
Oxidative stress is involved in the initiation and propagation of chronic intestinal pathologies. Bioactive peptides such as egg yolk-derived phosvitin phosphopeptides (PPP3) have been previously shown to reduce in vitro oxidative stress by up-regulating glutathione synthesis and antioxidant enzyme activities. Peptide and gene expression profile analysis of the PPP3 peptides can provide insight into structures involved in signal transduction mechanisms in the antioxidative stress response. The objectives of this research were to identify the PPP3 amino acid sequences before and after simulated gastrointestinal digestion and to assess the genes influenced by PPP3. Peptide sequences were analyzed using ESI Q-TOF-MS/MS, and the expression profile of 84 human oxidative stress and antioxidant defense genes were analyzed. Undigested PPP3 was composed of three main peptides: GTEPDAKTSSSSSSASSTATSSSSSSASSPNRKKPMDE (phosvitin-PV residues 4-41), NSKSSSSSSKSSSSSSRSRSSSKSSSSSSSSSSSSSSKSSSSR (PV residues 155-197), and EDDSSSSSSSSVLSKIWGRHEIYQ (PV residues 244-257) and their fragments. There was limited degradation of PPP3 after gastrointestinal digestion as deduced from the fragment sizes of digested PPP3, which ranged from 5 to 32 amino acids. These fragments were rich in contiguous serines and, in some cases, monoesterified with phosphate. Both undigested and digested PPP3 significantly reduced IL-8 secretion in H(2)O(2)-induced Caco-2 cells, indicating that antioxidative stress bioactivity is retained upon digestion. After PPP3 pretreatment, antioxidant genes associated with oxygen and reactive oxygen species (ROS) metabolism and cellular responses to chemical stimulus, oxidative stress, and ROS are up-regulated in the presence and absence of oxidative stress, thereby contributing to the prevention of intestinal oxidative stress and the promotion of gut health.  相似文献   

12.
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.  相似文献   

13.
p-Coumaric and ferulic acid are actively taken up by monocarboxylic acid transporter (MCT), whereas gallic acid, caffeic acid (CA), and rosmarinic acid (RA) are absorbed by paracellular diffusion in human intestinal Caco-2 cells, although CA has low affinity for MCT. We previously demonstrated that p-coumaric acid has a much higher absorption efficiency than gallic acid in rats, owing to the MCT-mediated absorption of p-coumaric acid in vivo (J. Agric. Food Chem. 2004, 52, 2527-2532). Here, absorption of orally administered CA and RA in rats has been studied to investigate their intestinal absorption characteristics and pharmacokinetics in vivo and to compare the results with those of p-coumaric and gallic acids obtained under identical conditions. Rats were given 100 micromol/kg body weight of CA and RA, and blood was collected from the portal vein and abdominal artery after administration. CA, RA, and their metabolites were quantified by a coulometric detection method using HPLC-ECD. The serum concentration of intact CA and RA in the portal vein peaked at 10 min after administration, with a C(max) of 11.24 micromol/L for CA and 1.36 micromol/L for RA. The area under the curve (AUC) for intact CA and RA in the portal vein was calculated from the serum concentration-time profile to be 585.0 and 60.4 micromol min L-1, respectively. The absorption efficiency of CA was about 9.7-fold higher than that of RA. Overall, the absorption efficiency of these compounds in vivo increases in the order: gallic acid = RA < CA < p-coumaric acid, which is in good agreement with results obtained in Caco-2 cells in vitro.  相似文献   

14.
It was previously reported that m-coumaric acid, m-hydroxyphenylpropionic acid (mHPP), and 3,4-dihydroxyphenylpropionic acid (DHPP) are major metabolites of ingested caffeic acid formed by gut microflora and would be transported by the monocarboxylic acid transporter (MCT). We have directly measured their absorption characteristics in Caco-2 cells using a coulometric detection method involving HPLC-ECD. The proton-coupled directional transport of m-coumaric acid, mHPP, and DHPP was observed, and the transport was inhibited by an MCT substrate. The permeation of m-coumaric acid and mHPP was concentration-dependent and saturable: The Michaelis constant for m-coumaric acid and mHPP was 32.5 and 12.9 mM, respectively, and the maximum velocity for m-coumaric acid and mHPP was 204.3 and 91.2 nmol (min)(-1) (mg protein)(-1), respectively. By contrast, the permeation of DHPP was nonsaturable even at 30 mM and was inversely correlated with the paracellular permeability of Caco-2 cells. Our results demonstrate that these compounds are absorbed by the MCT, although DHPP is mainly permeated across Caco-2 cells via the paracellular pathway. MCT-mediated absorption of phenolic compounds per se and their colonic metabolites would exert significant impact on human health.  相似文献   

15.
Polyphenolic compounds are known to possess many beneficial health effects, including the antioxidative activities of scavenging reactive oxygen species and chelating metals, such as iron and zinc. Tea and red wine are thought to be important sources of these compounds. However, some polyphenolic compounds can also reduce the absorption of iron, and possibly other trace metals, when included in a diet. There is very little information on the effect of dietary polyphenolic compounds on the status of trace elements other than iron. The effects of epigallocatechin-3-gallate (EGCG), green tea extract (GT), and grape seed extract (GSE) on the absorption of (65)Zn were examined and compared with their effects on (55)Fe absorption in human intestinal Caco-2 cells grown on microporous membrane inserts. The levels of EGCG, GT, and GSE used in this study were within physiological ranges and did not affect the integrity of the Caco-2 cell monolayers. GSE significantly (P < 0.05) reduced zinc transport across the cell monolayer, and the decreased zinc transport was associated with a reduction in apical zinc uptake. However, EGCG and GT did not alter zinc absorption. In contrast, the polyphenolic compounds in EGCG, GT, and GSE almost completely blocked transepithelial iron transport across the cell monolayer. The effect of GSE on zinc absorption was very different from that on iron absorption. Whereas GSE decreased zinc absorption by reducing apical zinc uptake, the polyphenolic compounds inhibited iron absorption by enhancing apical iron uptake. GSE inhibited zinc absorption similarly to that observed for phytate. Phytate significantly (P < 0.05) decreased transepithelial zinc transport by reducing apical zinc uptake. The inhibition of zinc absorption may be due to the presence of procyanidins in GSE, which bind zinc with high affinity and block the transport of zinc across the apical membrane of enterocytes. Further research on the absorption of zinc as zinc-polyphenol complexes and free zinc should provide further insight into the process of dietary zinc absorption in the presence of GSE and other bioactive dietary polyphenols. The present study suggests that some individuals should consider their zinc status if they regularly consume procyanidin-containing foods in their diet. However, further studies, especially in vivo studies, are needed to confirm these results.  相似文献   

16.
Consumption of polyphenols is associated with health promotion through diet, although many are poorly absorbed in animals and humans alike. Lipid peroxides may reach the intestine and initiate deleterious oxidation. Here we measured inhibition of the oxidation of linoleic acid (LA) in authentic fluid from rat small intestine (RIF) by two dietary polyphenols, a flavonoid, epicatechin (EC), and a stilbene, resveratrol (RV), and by gallic (GA) and caffeic (CA) acids, and their partition coefficients. Both polyphenols inhibited 80%, and CA inhibited 65%, of the production of hexanal. GA was the weakest antioxidant in this assay. Interestingly, measuring peroxides production in RIF showed that only epicatechin inhibited the first stage of oxidation. The oxidizing agent, the antioxidant comound, the solution pH and lipophilicity are known to affect the total antioxidative activity. We suggest that the mechanism of this activity changes in accord with the environment: i.e., RV may act as a free radial scavenger, but here, in protecting lipids in intestinal fluid from oxidation, it acts as a hydrogen atom donor. Since the concentration of phenolics is much higher in the intestinal fluid than is ever achieved in plasma or other body tissues, it is suggested that their antioxidant activity could be exerted in the gastrointestinal tract (GIT), breaking the propagation of lipid peroxides oxidation and production of toxic compounds.  相似文献   

17.
Ferulic acid (FA) and p-coumaric acid (CA) are absorbed by the monocarboxylic acid transporter (MCT) in Caco-2 cells, although gallic acid (GA) is not. Therefore, the MCT is selective for certain phenolic acids. Absorption of orally administered CA and GA in rats was studied to obtain serum pharmacokinetic profiles and to investigate their intestinal absorption characteristics in vivo. Rats were administered 100 micromol/kg body weight of CA and GA, and blood was collected from the portal vein and abdominal artery after administration. CA, GA, and their metabolites were quantified with a highly selective and sensitive coulometric detection method using high-performance liquid chromatography-electrochemical detection. Ingested CA was rapidly absorbed in the gastrointestinal tract in an intact form. The serum concentration of intact CA in the portal vein peaked 10 min after dosing (C(max) was 165.7 micromol/L). In contrast, GA was slowly absorbed, with a t(max) for intact GA of 60 min and a C(max) of 0.71 micromol/L. The area under the curve for intact CA and GA was calculated from the serum concentration profile in the portal vein to be 2991.3 and 42.6 micromol min L(-)(1), respectively. The relative bioavailability of CA against GA was about 70. This is the first demonstration that absorption efficiency of CA is much higher than that of GA in vivo. The absorption characteristics of CA are clearly different from those of GA. These findings are in good agreement with the results obtained in vitro using a Caco-2 cell system.  相似文献   

18.
The solubility and bioavailability of cadmium (Cd) in infant foods, three cereal- and milk-based diets and two ready-to-use baby dishes, were studied after in vitro digestion and by using human intestinal Caco-2 cells. The solubility of Cd after in vitro digestion varied between diets; liver casserole had the highest solubility and was lower after infant as compared to adult digestion conditions. Generally, more Cd was soluble in infant intestinal than gastric juice in contrast to the results from the adult digestion. Caco-2 cells were incubated with supernatants of infant digests that had been equilibrated with (109)Cd during the in vitro digestion procedure, and cellular uptake and transport of (109)Cd were measured after 180 min. Statistically significant differences in both uptake and transport of Cd were detected between some of the diets and a control solution containing only digestive enzymes and (109)CdCl(2). Uptake of soluble Cd in the cells varied between diets from 4 to 6%, and the transport over the monolayers was 1-2% of the dose. We conclude that age specific digestion conditions as well as composition of diets affect both solubility and bioavailability of Cd.  相似文献   

19.
Considering the importance of the oral route for human exposure to atrazine, we have investigated the possible effect of this herbicide on the human intestinal cells and the integrity of the epithelial barrier, using Caco-2 cells as the intestinal model in vitro. We evaluated possibile cytotoxic and genotoxic effects of atrazine in concentrations ranging from 1 to 250 μM on the Caco-2 cells at different stages of growth after short- and long-term exposure. Results from the tetrazolium blue (MTT) test and the Trypan blue exclusion assay showed that atrazine cytotoxicity was dose- and time-dependent. Obtained data indicated that atrazine at high concentrations (50 and 250 μM) was able to induce effects on Caco-2 proliferation and viability. Moreover, it was found that the long-term exposure to atrazine at the non-cytotoxic dose caused inhibition of the intestinal cell maturation and decreased the transepithelial electrical resistance, the indicator of the epithelial barrier integrity. Studies on the atrazine genotoxicity determined using the single cell microelectrophoresis assay indicated that atrazine did not induce DNA damages in the Caco-2 cells at concentrations of up to 50 μM, whereas enhancement in the DNA damage was observed at 250 μM. Altogether, our results indicate that atrazine at expected human oral exposure concentrations is not able to induce effects on the Caco-2 cell proliferation and viability, but may suppress the intestinal cell differentiation and reduce the cell monolayer integrity. We suggest that chronic exposure on low levels of atrazine may lead to alteration in the expression of the morphological and functional features of the Caco-2 cells related to the transport and barrier function of small intestinal enterocytes. In consequence, this may lead to alterations in the intestinal absorption process.  相似文献   

20.
Calcium transport from mineral waters across caco-2 cells.   总被引：1，自引：0，他引：1  
In the present study the absorption of calcium from 13 different mineral waters has been examined. For this purpose the mineral waters were first digested in vitro by simulating gastric and intestinal digestion. Afterward, the absolute and fractional transport rates of calcium from these digested solutions across human colon adenocarcinoma (Caco-2) cell monolayers grown on bicameral filters were measured. Results showed that the fractional transport rates for calcium lie between 1.65 and 6.72% after 90 min of incubation time. The absolute transport values varied between 90.4 and 624.7 pmol/(min x cm(2)). The transport values [pmol/(min x cm(2))] for calcium from the mineral waters were in general not concentration dependent, showing neither signs of saturation kinetics nor unsaturable uptake mechanisms. In addition, the fractional transport rates from mineral waters with similar calcium concentrations were greatly different in some cases. On the basis of these results, it can be concluded that calcium bioavailability from mineral waters could vary dependent on probably several factors.  相似文献   

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