Absorption and Metabolism of Chlorogenic Acids in Cultured Gastric Epithelial Monolayers

Abstract

ABSTRACT:Gastric absorption of feruloylquinic acid and di-O-caffeoylquinic acid analogs has never been investigated despite their potential contribution to the proposed beneficial health effects leading to reduced risk of type 2 diabetes. Using a cultured gastric epithelial model, with an acidic apical pH, the relative permeability coefficients (P app ) and metabolic fate of a series of chlorogenic acids (CGAs) were investigated. Mechanistic studies were performed in the apical to basal direction and demonstrated differential rates of absorption for different CGA subgroups. For the first time, we show intact absorption of feruloylquinic acids and caffeoylquinic acid lactones across the gastric epithelium (P app ϳ 0.2 cm/s). Transport seemed to be mainly by passive diffusion, because good linearity was observed over the incubation period and test concentrations, and we speculate that a potential carrier-mediated component may be involved in uptake of certain 4-acyl CGA isomers. In contrast, absorption of intact di-O-caffeoylquinic acids was rapid (P app ϳ 2-10 cm/s) but nonlinear with respect to time and concentration dependence, which was potentially limited by interaction with an efflux transporter and/or pH gradient dependence. For the first time, methylation is shown in gastric mucosa. Furthermore, isoferulic acid, dimethoxycinnamic acid, and ferulic acid were identified as novel gastric metabolites of CGA biotransformation. We propose that the stomach is the first location for the release of hydroxycinnamic acids, which could explain their early detection after coffee consumption.

In vitrostudies on the stability in the proximal gastrointestinal tract and bioaccessibility in Caco-2 cells of chlorogenic acids from spent coffee grounds

“…Despite different functions and morphology between gastric epithelial and Caco-2 cell monolayers, similar absorptive patterns were observed among both cellular lines. The absorption percentage of spent coffee CQAs was 0.3% of the apical dose, in agreement with the findings of Farrell et al (2011a). In their study, Farrell et al found that the percentage of FQAs and CQLs transported across the gastric cell monolayer was slightly higher than that of CQAs.…”

“…In their study, Farrell et al found that the percentage of FQAs and CQLs transported across the gastric cell monolayer was slightly higher than that of CQAs. The only difference between gastric and intestinal cells was the percentage of diCQAs transported, due to the high permeability observed in gastric cells (Farrell et al, 2011a).…”

Dose‐dependent absorption of chlorogenic acids in the small intestine assessed by coffee consumption in ileostomists

“…). Considering a possible gastric residence time from 0.2 up to 3.8 h , a CGA uptake and methylation in the stomach is conceivable . Plasma appearance is linearly correlated to the most compounds within the different ingested doses (Fig.…”

Pharmacokinetics and Tissue Distribution Study of Chlorogenic Acid from Lonicerae Japonicae Flos Following Oral Administrations in Rats

“…Furthermore, it can be inferred that ChA might target liver and induce a protective effect. Farrell et al have studied the absorption and metabolism of ChA in cultured gastric epithelial monolayers [14], but cell experiment has its intrinsic limits. Pharmacokinetics of ChA extracted from Shuang-Huang-Lian [15], Yin-Huang granules [16], Aidi lyophilizer [17], or Daqingye [18] was also studied, while little in LJF.…”