Development and validation of a LC–MS/MS method for the quantification of phenolic compounds in human saliva after intake of a procyanidin-rich pine bark extract

Bayer, Jasmin; Högger, Petra

doi:10.1016/j.jpba.2023.115914

Cited by 4 publications

(3 citation statements)

References 33 publications

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“…Until recently, it was not known whether dietary polyphenols circulating in blood would be transferred into saliva. After developing an analytical method to quantify polyphenol concentrations in saliva, a saliva sample and a simultaneously obtained serum sample of a single volunteer were analyzed after intake of Pycnogenol ® ( 70 ). Gallic acid, protocatechuic acid, taxifolin, p-coumaric acid, caffeic acid and 5-(3′,4′-dihydroxyphenyl)-γ-valerolactone were detected in saliva.…”

Section: Biodistributionmentioning

confidence: 99%

“…This confirmed the metabolism of procyanidins and bioavailability of the valerolactone metabolites. Subsequently, the formation and bioavailability of 5-(3′,4′-dihydroxyphenyl)-γ-valerolactone after intake of Pycnogenol ® has been demonstrated for human plasma ( 32 ), serum ( 34 ), blood cells ( 34 ), synovial fluid ( 34 ), and saliva ( 70 ). In addition to the valerolactone, 4-hydroxy-5-(3′,4′-dihydroxyphenyl)-valeric acid and 4-hydroxy-5-phenyl-valeric acid were detected as well in serum samples after intake of Pycnogenol ® ( 33 ).…”

Section: Metabolismmentioning

confidence: 99%

“…After intake of Pycnogenol ® , a compartment-specific deconjugation of phase II metabolites has been observed in a human volunteer (see section “5.5 Distribution into saliva”). In saliva, but not in serum, various polyphenols, and the microbial metabolite 5-(3′,4′-dihydroxyphenyl)-γ-valerolactone were exclusively present as unconjugated molecules ( 70 ). This might be the first report of metabolite deconjugation in humans.…”

Section: Metabolismmentioning

confidence: 99%

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Review of the pharmacokinetics of French maritime pine bark extract (Pycnogenol®) in humans

Bayer,

Högger

2024

Front. Nutr.

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The French maritime pine bark extract Pycnogenol® is a proprietary product from Pinus pinaster Aiton. It complies with the quality specifications in the United States Pharmacopeia monograph “Pine extract” in the section of dietary supplements. Pycnogenol® is standardized to contain 65–75% procyanidins which are a variety of biopolymers consisting of catechin and epicatechin monomeric units. The effects of Pycnogenol® have been researched in a multitude of human studies. The basis for any in vivo activity is the bioavailability of constituents and metabolites of the extract. General principles of compound absorption, distribution, metabolism and elimination as well as specific data from studies with Pycnogenol® are summarized and discussed in this review. Based on plasma concentration profiles it can be concluded that low molecular weight constituents of the extract, such as catechin, caffeic and ferulic acid, taxifolin are readily absorbed from the small intestine into systemic circulation. Procyanidin oligomers and polymers are subjected to gut microbial degradation in the large intestine yielding small bioavailable metabolites such as 5-(3′,4′-dihydroxyphenyl)-γ-valerolactone. After intake of Pycnogenol®, constituents and metabolites have been also detected in blood cells, synovial fluid and saliva indicating a substantial distribution in compartments other than serum. In studies simultaneously investigating concentrations in different specimen, a preferential distribution of individual compounds has been observed, e.g., of ferulic acid and 5-(3′,4′-dihydroxyphenyl)-γ-valerolactone into synovial fluid compared to serum. The main route of elimination of constituents and metabolites of the French pine bark extract is the renal excretion. The broad knowledge accumulated regarding the pharmacokinetics of compounds and metabolites of Pycnogenol® constitute a rational basis for effects characterized on a cellular level and observed in human clinical studies.

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Section: Biodistributionmentioning

confidence: 99%