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French Maritime Pine (Pinus pinaster) Pycnogenol® Inflammation HC 030165-315
Date: October 31, 2006 RE: Anti-inflammatory Effects of French Maritime Pine Bark Extract Ingestion Grimm T, Chovanova Z, Muchova J, et al. Inhibition of NF-kappaB activation and MMP-9 secretion by plasma of human volunteers after ingestion of maritime pine bark extract (Pycnogenol). J Inflamm. 2006;3(1):1–15. The standardized bark extract of French maritime pine (Pinus pinaster), Pycnogenol® (Horphag Research Ltd., Switzerland), has been shown to have anti-inflammatory properties in human studies. For example, double-blind placebo controlled studies have shown decreases in plasma and urine leukotriene concentrations, improved asthma scores in patients with asthma, and reduced pain and improvement in joint mobility in patients with osteoarthritis after Pycnogenol ingestion. It is unclear whether a single compound or a mixture of related compounds is responsible for these effects. Thus, it is important to elucidate the molecular pharmacological basis of these effects. The objective of this study was to determine the molecular pharmacological effects of maritime pine bark, ex vivo, that contribute to the inflammatory process in humans. Plasma samples were obtained from 7 healthy human volunteers (5 women and 2 men aged 18–30 years) before and after oral administration of 200 mg Pycnogenol per day for 5 days. For a 24-hour period before the ingestion of maritime pine bark, the subjects were required to abstain from the consumption of known flavonoid-rich foods (e.g., fruit, vegetables, marmalade, tea, coffee, cocoa, wine, and beer). The potential influence of the plasma samples on the lipopolysaccharide (LPS)–induced release of matrix metalloproteinase 9 (MMP-9) from human monocytes was determined. Because the induction and release of MMP-9 might be initiated by nuclear transcription factor κB (NF-κB), the effect of the plasma samples on LPS-induced NF-κB nuclear translocation was also determined. The number of viable monocytes was counted after stimulation with 10 ng/mL LPS in the MMP9 study and with 1 µg/mL LPS in the NF-κB study. Monocyte viability was not significantly influenced by plasma samples in the MMP-9 or in the NF-κB study. The number of viable monocytes in plasma was 2.49 ± 0.23 × 105 before
and 2.79 ± 0.26 × 105 after Pycnogenol intake in the MMP-9 study. The number of viable monocytes in plasma was 1.49 ± 0.29 × 106 before and 1.70 ± 0.20 × 106 after Pycnogenol intake in the NF-κB study. However, a significant decrease (P < 0.05) in MMP-9 concentrations from baseline (17.06 ± 2.17 ng/mL per 2.5 × 105 viable monocytes) was observed after Pycnogenol intake (12.70 ± 1.24 ng/mL per 2.5 × 105 viable monocytes). Nuclear p65 concentrations also decreased significantly (P < 0.05) from baseline (2.98 ± 0.48 ng per 1.5 × 106 viable monocytes) after Pycnogenol intake (2.51 ± 0.26 ng per 1.5 × 106 viable monocytes). These values correspond to decreases in MMP-9 release and NF-κB activation of approximately 25% and 15%, respectively, in LPS-stimulated monocytes. According to the authors, regular doses of French maritime pine bark extract for 5 days "moderately inhibited NF-κB activation and MMP-9 secretion ex vivo." Because the plasma samples were diluted 1:1 with cell culture medium before incubation with monocytes, the assumption is that the effects of Pycnogenol ingestion may be even more pronounced in vivo. The ex vivo effects observed in this study are consistent with reported antiinflammatory effects in vivo. The focus of future studies should be to link pharmacodynamic and pharmacokinetic data and to identify the active components in plasma responsible for the observed anti-inflammatory effects of pine bark extract. —Brenda Milot, ELS
Enclosure: Referenced article is an Open Access article via BioMed Central.
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