Mülek Melanie, Seefried Lothar, Genest Franca, Högger Petra
Institut für Pharmazie und Lebensmittelchemie, Universität Würzburg, 97074 Würzburg, Germany.
Department of Orthopedics, Orthopedic Center for Musculoskeletal Research, 97074 Würzburg, Germany.
Nutrients. 2017 Apr 28;9(5):443. doi: 10.3390/nu9050443.
The present randomized controlled study aimed to investigate the in vivo distribution of constituents or metabolites of the standardized maritime pine bark extract Pycnogenol. Thirty-three patients with severe osteoarthritis scheduled for a knee arthroplasty were randomized to receive either 200 mg per day Pycnogenol (P+) or no treatment (Co) over three weeks before surgery. Serum, blood cells, and synovial fluid samples were analyzed using liquid chromatography coupled to tandem mass spectrometry with electrospray ionization (LC-ESI/MS/MS). Considerable interindividual differences were observed indicating pronounced variability of the polyphenol pharmacokinetics. Notably, the highest polyphenol concentrations were not detected in serum. Catechin and taxifolin primarily resided within the blood cells while the microbial catechin metabolite δ-(3,4-dihydroxy-phenyl)-γ-valerolactone, ferulic, and caffeic acid were mainly present in synovial fluid samples. Taxifolin was detected in serum and synovial fluid exclusively in the P+ group. Likewise, no ferulic acid was found in serum samples of the Co group. Calculating ratios of analyte distribution in individual patients revealed a simultaneous presence of some polyphenols in serum, blood cells, and/or synovial fluid only in the P+ group. This is the first evidence that polyphenols distribute into the synovial fluid of patients with osteoarthritis which supports rationalizing the results of clinical efficacy studies.
本随机对照研究旨在调查标准化法国滨海松树皮提取物碧萝芷的成分或代谢产物在体内的分布情况。33例计划接受膝关节置换术的重度骨关节炎患者被随机分为两组，在手术前3周内，一组每天服用200毫克碧萝芷（P+组），另一组不接受治疗（对照组）。采用液相色谱-电喷雾电离串联质谱法（LC-ESI/MS/MS）对血清、血细胞和滑液样本进行分析。观察到个体间存在显著差异，表明多酚类药物代谢动力学具有明显的变异性。值得注意的是，血清中未检测到最高的多酚浓度。儿茶素和紫杉叶素主要存在于血细胞中，而微生物儿茶素代谢产物δ-(3,4-二羟基苯基)-γ-戊内酯、阿魏酸和咖啡酸主要存在于滑液样本中。仅在P+组的血清和滑液中检测到紫杉叶素。同样，在对照组的血清样本中未发现阿魏酸。计算个体患者中分析物分布的比率发现，仅在P+组中血清、血细胞和/或滑液中同时存在一些多酚。这是多酚类物质分布到骨关节炎患者滑液中的首个证据，这为临床疗效研究结果的合理化提供了支持。
