In Vivo Bioavailability, Absorption, Excretion, and Pharmacokinetics of [¹⁴C]Procyanidin B2 in Male Rats

Abstract

ABSTRACT:Procyanidins are important biologically active compounds, but the pathway and extent of absorption and metabolism are controversial. We conducted a mass balance study to evaluate the total radioactivity excreted in urine and feces after oral administration of

Pine Bark Extracts: Nutraceutical, Pharmacological, and Toxicological Evaluation

“…In male rats, extensive enterohepatic cycling of flavonoids and their conjugated metabolites has been reported (Coldham and Sauer, 2000;Silberberg et al, 2006), and 28% of intravenously administered procyanidin B2 was excreted in feces, which is consistent with biliary excretion and enterohepatic recycling (Stoupi et al, 2010).…”

“…After intravenous administration of procyanidin B2, 76% was excreted in the urine, reflecting extensive renal clearance (Stoupi et al, 2010). Several procyanidin metabolites were present in the kidney, which further indicated that urine was the main procyanidin excretion pathway in the rat (Serra et al, 2011).…”

“…Most in vivo studies suggest that procyanidin dimers can be absorbed (Baba et al, 2002;Tsang et al, 2005;Shoji et al, 2006;Prasain et al, 2009). The gut is the predominant location for absorption, a large percentage of the parent compound may be transformed by gut microflora, and the resulting metabolites may constitute the predominant form of absorption (Stoupi et al, 2010).…”

Insights into the metabolism and microbial biotransformation of dietary flavan-3-ols and the bioactivity of their metabolites

“…29 Recently, it has been reported that after oral administration of [ 14 C]procyanidin B2, 63% of the total radioactivity was excreted via urine, indicating that a large quantity of the parent compound is degraded by the gut microflora. 51 The recognition that the colon is a very active organ for the metabolism of flavan-3-ols, particularly proanthocyanidins, has led to a resurgence in the study of the biotransformation of these compounds and other polyphenols by the intestinal Fig. 3 Metabolic pathway tentatively proposed for the catabolism of monomeric flavan-3-ols and dimeric procyanidins by the intestinal microbiota.…”

Cinnamtannin A2, a Tetrameric Procyanidin, Increases GLP-1 and Insulin Secretion in Mice

“…29,30) In vivo bioavailability of procyanidin B2 has been reported using a radioactively labeled molecule in male rats. 31) Radioactivity was observed to increase, and its T max in blood was approximately 6 h after oral administration, indicating that the parent compound and its microbial metabolites are incorporated into the body. Using an apple polyphenol extract containing abundant procyanidin oligomers, dimeric and trimeric procyanidins were detected by LC-MS/MS in rat plasma 2 h after administration.…”