title: Evaluation of physicochemical properties and intestinal permeability of six dietary polyphenols in human intestinal colon adenocarcinoma Caco-2 cells.
abstract: Phenolic compounds are common ingredients in many dietary supplements and functional foods. However, data concerning physicochemical properties and permeability of polyphenols on the intestinal epithelial cells are scarce. The aims of this study were to determine the experimental partition coefficient (Log P), and parallel artificial membrane permeability assay (PAMPA), to characterize the bi-directional transport of six phenolic compounds viz. caffeic acid, chrysin, gallic acid, quercetin, resveratrol and rutin in Caco-2 cells. The experimental Log P values of six polyphenols were correlated (R (2) = 0.92) well with the calculated Log P values. The apparent permeability (P app) range of all polyphenols in PAMPA for the apical (AP) to basolateral (BL) was 1.18 ± 0.05 × 10(-6) to 5.90 ± 0.16 × 10(-6) cm/s. The apparent Caco-2 permeability (P app) range for the AP-BL was 0.96 ± 0.03 × 10(-6) to 3.80 ± 0.45 × 10(-6) cm/s. The efflux ratio of P app (BL → AP) to P app (AP → BL) for all phenolics was <2, suggesting greater permeability in the absorptive direction. Six compounds exhibited strong correlations between Log P and PAMPA/Caco-2 cell monolayer permeation data. Dietary six polyphenols were poorly absorbed through PAMPA and Caco-2 cells, and their transepithelial transports were mainly by passive diffusion.
authors.affiliation: Suresh Gyan Vihar University, Mahal, Jagatpura, Jaipur, 302025, India.
authors.forename: Himanshu
authors.initials: H
authors.lastname: Rastogi
authors.affiliation: Laila Nutraceuticals Research and Development Centre, Kanuru, Vijayawada, 520007, India. jana.snehasis@rediffmail.com.
authors.forename: Snehasis
authors.initials: S
authors.lastname: Jana
mesh_terms: D000230:Adenocarcinoma / Q000378:metabolism*; D018938:Caco-2 Cells; D055598:Chemical Phenomena / Q000187:drug effects; D003110:Colonic Neoplasms / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects* / Q000502:physiology*; D007413:Intestinal Mucosa / Q000187:drug effects / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D010539:Permeability / Q000187:drug effects; D059808:Polyphenols / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D059808:Polyphenols
keywords: Caco-2; Parallel artificial membrane permeability; Partition coefficient; Polyphenols