Abstract

French maritime pine bark extract (Pycnogenol®) displays a variety of anti-inflammatory effects in vivo. Aim of this study was to determine whether human plasma after oral intake of Pycnogenol contains sufficient concentrations of active principles to inhibit key mediators of inflammation. Blood samples from seven healthy volunteers were obtained before and after five days administration of 200 mg Pycnogenol per day. Plasma samples statistically significantly inhibited matrix metalloproteinase 9 (MMP-9) release from human monocytes and NF-κB activation. Thus, we provide evidence that bioavailable active principles of Pycnogenol exert anti-inflammatory effects by inhibition of proinflammatory gene expression which is consistent with documented clinical observations. We suggest that our ex vivo method is suitable to substantiate molecular pharmacological mechanisms of complex plant extracts in a more focussed and rational way compared to in vitro studies by taking into account the processes of absorption and metabolism.

Highlights

  • Pycnogenol is a standardized bark extract of the French maritime pine Pinus pinaster (Pycnogenol®, Horphag Research Ltd., UK)

  • We investigated a potential influence of the plasma samples on LPS-induced release of matrix metalloproteinase 9 (MMP-9) from human monocytes

  • The upper panel shows concentrations of p65 was determined in nuclear extracts of 1.5 × 106 viable human monocytes after ex vivo incubation with the individual volunteers' plasma

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Summary

Introduction

Pycnogenol is a standardized bark extract of the French maritime pine Pinus pinaster (Pycnogenol®, Horphag Research Ltd., UK). It comprises of a concentrate of pine bark constituents such as polyphenolic monomers, procyanidins and phenolic or cinnamic acids and their glycosides [1]. About 65–75 % of the Pycnogenol extract are procyanidins that consist of catechin and epicatechin subunits of varying chain lengths [1]. The quality of this extract is specified in the United States Pharmacopeia (USP 28) [2]. Oral [6] and topical [7] application of Pycnogenol reduced inflammation and delayed skin-cancer formation following UV-radiation in controlled experiments in mice

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