Intestinal absorption and first-pass metabolism of polyphenol compounds in rat and their transport dynamics in Caco-2 cells

• Published in: PloS one Vol. 7; no. 1; p. e29647
• Main Authors: Teng, Zenghui, Yuan, Chengjun, Zhang, Feng, Huan, Menglei, Cao, Weidong, Li, Kangchu, Yang, Jingyue, Cao, Dayong, Zhou, Siyuan, Mei, Qibing
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 13-01-2012; Public Library of Science (PLoS)
• Subjects: Absorption; Absorptivity; Administration, Oral; Animals; Biological Transport; Biology; Caco-2 Cells; Cell Membrane Permeability; Chemistry; Chinese medicine; Chrysophanic acid; Diet; Emodin; Epithelial cells; Glycoproteins; Humans; In vivo methods and tests; Intestinal Absorption; Intestine; Intestine, Small - metabolism; Male; Medicine; Metabolism; Metabolites; Monomolecular films; Oral administration; P-Glycoprotein; Perfusion; Pharmacology; Physiological aspects; Polyphenols; Polyphenols - administration & dosage; Polyphenols - chemistry; Polyphenols - metabolism; Polyphenols - pharmacokinetics; Rats; Rats, Sprague-Dawley; Resveratrol; Rodents; Small intestine; Time Factors; Transport; China
• ISSN: 1932-6203; 1932-6203
• DOI: 10.1371/journal.pone.0029647

Polyphenols, a group of complex naturally occurring compounds, are widely distributed throughout the plant kingdom and are therefore readily consumed by humans. The relationship between their chemical structure and intestinal absorption, transport, and first-pass metabolism remains unresolved, however.
Here, we investigated the intestinal absorption and first-pass metabolism of four polyphenol compounds, apigenin, resveratrol, emodin and chrysophanol, using the in vitro Caco-2 cell monolayer model system and in situ intestinal perfusion and in vivo pharmacokinetic studies in rats, so as to better understand the relationship between the chemical structure and biological fate of the dietary polyphenols.
After oral administration, emodin and chrysophanol exhibited different absorptive and metabolic behaviours compared to apigenin and resveratrol. The differences in their chemical structures presumably resulted in differing affinities for drug-metabolizing enzymes, such as glucuronidase and sulphatase, and transporters, such as MRP2, SGLT1, and P-glycoprotein, which are found in intestinal epithelial cells.