Investigation of intestinal absorption and disposition of green tea catechins by Caco-2 monolayer model

Zhang, Li; Zheng, Ying; Chow, Moses S.S.; Zuo, Zhong

doi:10.1016/j.ijpharm.2004.08.020

Cited by 177 publications

(159 citation statements)

References 24 publications

Supporting

Mentioning

142

Contrasting

Order By: Relevance

“…Moreover, efflux transporters, such as multidrug resistance-associated protein 2 (MRP2), a real so likely factors affecting half-life times; catechin metabolites are substrate of MRPs [22]. Li et al demonstrated that non-gallatedcatechins were preferentially effluxed during their absorption across the small intestines using MRPs expressed in a Caco-2 monolayer model, consistent with our observation [23]. Catechins may also be substrates of another transporter, p-glycoprotein (P-gp) [24].…”

Section: Pharmacokinetic Properties Of Green Tea Catechinssupporting

confidence: 89%

Green Tea Catechins -Pharmacokinetic Properties and Health Beneficial Effects

ErisaTomishige¹

2015

Pharm Anal Acta

View full text Add to dashboard Cite

In this review, we provide information on thepharmacokinetic properties of green tea catechins and their beneficial health effects. The major catechins in green tea are (-)-epicatechin (EC), its hydroxyl derivative (-)-epigallocatechin (EGC), and their gallic acid esters, (-)-epicatechin-3-gallate (ECg) and (-)-epigallocatechin-3-gallate (EGCg). We developed an analytical method for determination of the presence of green tea catechins in human serum using ion-pair HPLC with electrochemical detection to estimate the pharmacokinetic parameters of target catechins. The C max values indicated that catechin absorption was relatively low. One of the gallatedcatechins, EGCg, had a longer half-life than the non-gallatedcatechins. Green tea catechins, in particular, have attracted attention as cancer preventive agents in terms of their low toxicity and being readily available to the general population. Several epidemiological studies revealed that green tea consumption reduces cancer incidence. Numerous in vitro cell culture studies have shown that EGCg, which is defined as a major green tea catechin contributing to green tea's anticancer effects, inhibits cell growth concomitant with induction of apoptosis. We have previously found that the cell death-inhibiting gene, Bcl-xL, was decreased by EGCg. These results support the hypothesis that EGCg regulates cytoplasmic NF-κB and subsequently induction of apoptosis. Green tea consumption may also play a role in preventing other lifestyle diseases, such as cardiovascular diseases and stroke, due to its hypocholesterolemic and hypotensive activities. In conclusion, habitual green tea drinking may promote human health by preventing lifestyle-related diseases.

show abstract

Section: Pharmacokinetic Properties Of Green Tea Catechinssupporting

confidence: 89%

Green Tea Catechins -Pharmacokinetic Properties and Health Beneficial Effects

ErisaTomishige¹

2015

Pharm Anal Acta

View full text Add to dashboard Cite

show abstract

“…Although some in vitro studies have described a passive-diffusion transport (Vaidyanathan and Walle, 2001), others reported the relevance of the facilitated mechanism for flavanol absorption (Vaidyanathan and Walle, 2001;Zhang et al, 2004;Chan et al, 2007). With the objective of investigating its transport across Caco-2 cells, (-)-epicatechin was placed either in the apical or basal compartments.…”

Section: Resultsmentioning

confidence: 99%

Modulation of (–)-Epicatechin Metabolism by Coadministration with Other Polyphenols in Caco-2 Cell Model

Sanchez-Bridge¹,

Lévêques²,

Li³

et al. 2014

Drug Metab Dispos

View full text Add to dashboard Cite

Widely consumed beverages such as red wine, tea, and cocoaderived products are a great source of flavanols. Epidemiologic and interventional studies suggest that cocoa flavanols such as (-)-epicatechin may reduce the risk of cardiovascular diseases. The interaction of (-)-epicatechin with food components including other polyphenols could modify its absorption, metabolism, and finally its bioactivity. In the present study we investigate (-)-epicatechin absorption and metabolism when coexposed with other polyphenols in the intestinal absorptive Caco-2 cell model. Depending on the type of polyphenols coadministered, the total amount of 39-O-methyl-epicatechin and 39-O-sulfate-epicatechin conjugates found both in apical and basal compartments ranged from 19 to 801 nM and from 6 to 432 nM, respectively. The coincubation of (-)-epicatechin with flavanols, chlorogenic acid, and umbelliferone resulted in similar amounts of 39-O-methyl-epicatechin effluxed into the apical compartment relative to control. Coincubation with isorhamnetin, kaempferol, diosmetin, nevadensin, chrysin, equol, genistein, and hesperitin promoted the transport of 39-Omethyl-epicatechin toward the basolateral side and decreased the apical efflux. Quercetin and luteolin considerably inhibited the appearance of this (-)-epicatechin conjugate both in the apical and basolateral compartments. In conclusion, we could demonstrate that the efflux of (-)-epicatechin conjugates to the apical or basal compartments of Caco-2 cells is modulated by certain classes of polyphenols and their amount. Ingesting (-)-epicatechin with specific polyphenols could be a strategy to increase the bioavailability of (-)-epicatechin and to modulate its metabolic profile.

show abstract

“…The apparent permeability coefficients (P app ) of the drug were calculated from the slope of the linear portion of the drug permeability-time profiles by the relationship P app =(dX R /dt)×(1/A·C 0 ), where P app is the apparent permeability coefficient, X R is the amount of drug in the receptor side, A is the diffusion area, and C 0 is the initial drug concentration in the donor side. The efflux ratio was used to evaluate the extent of efflux (24)(25)(26)(27).…”

Section: Absorption Experimentsmentioning

confidence: 99%

Enhanced Intestinal Absorption of Daidzein by Borneol/Menthol Eutectic Mixture and Microemulsion

Shen

et al. 2011

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. In the present study, the effect of a borneol/menthol eutectic mixture (25:75) and microemulsion on the absorption of daidzein in rat intestinal membrane was evaluated. The microemulsion formulation was composed of ethyl oleate (oil), Cremophor RH40 (surfactant), PEG400 (co-surfactant), and water. The borneol/menthol eutectic mixture and its microemulsion were found to enhance the intestinal absorption of daidzein in vitro. A diffusion chamber system with isolated rat intestinal membranes was used. In contrast, verapamil (0.3 mM), a typical P-glycoprotein inhibitor, showed no effect on the absorption of daidzein by this system. A pharmacokinetic study was conducted in rats. After oral administration of daidzein at a dose of 10 mg/kg in the form of either borneol/menthol eutectic mixtures or suspension, the relative bioavailability of borneol/menthol eutectic mixtures and microemulsion was enhanced by about 1.5-and 3.65-fold, respectively, compared with a daidzein suspension. In conclusion, a borneol/menthol eutectic mixture can enhance the absorption of daidzein, although the mechanism of absorption enhancement is still unclear.

show abstract

Investigation of intestinal absorption and disposition of green tea catechins by Caco-2 monolayer model

Cited by 177 publications

References 24 publications

Green Tea Catechins -Pharmacokinetic Properties and Health Beneficial Effects

Green Tea Catechins -Pharmacokinetic Properties and Health Beneficial Effects

Modulation of (–)-Epicatechin Metabolism by Coadministration with Other Polyphenols in Caco-2 Cell Model

Enhanced Intestinal Absorption of Daidzein by Borneol/Menthol Eutectic Mixture and Microemulsion

Contact Info

Product

Resources

About