Pharmacokinetics and disposition of procyanidins metabolites in rats

Abstract

Procyanidins are ubiquitous in the diet. They are poorly absorbed and extensively metabolized via phase II and microbial enzymes. However, their distribution in the body is not well characterized. This study investigates the distribution of procyanidins (monomers and dimers) and their phase II metabolites in brain, spleen, heart, and liver and plasma of Wistar rats gavaged with 1 g of cocoa cream (CC), 30 mg rich procyanidin extract produced from mixed nut skins (PE) and 30 mg PE in 1 g CC (PECC). Rats were sacrificed at 0, 1, 1.5, 2, 3, 4, and 18 h after gavage. After the ingestion of CC, epicatechin‐glucuronide was the main metabolite in plasma with Cmax at 423 nM and tmax at 2 h. After PE, methyl catechin‐glucuronide (301 nM, 2 h) was the main metabolite in plasma, followed by catechin‐glucuronide (255 nM, 1.5 h). After PECC, epicatechin‐glucuronide (452 nM, 1.5 h) and catechin‐glucuronide (297 nM, 2 h) were the main metabolites in plasma. Methyl‐catechin‐glucuronide was found in liver after PE (8 nmol/g fresh wt, 4 h) and PECC (8 nmol/g, 1.5 h). Methyl catechin‐sulphate (6.4 nmol/g, 4 h) was quantified in brain only after PE. Catechin metabolites were not found in spleen and heart. Phenolic acids, such as 3‐hydroxyphenylpropionic acid, derived from microbial metabolism, were detected in all tissues. In conclusion, metabolites were deposited in a tissue dependent manner but there were no great differences between CC and PECC.