Virgili F, Pagana G, Bourne L, Rimbach G, Natella F, Rice-Evans C, Packer L
National Institute of Nutrition, Rome, Italy.
Free Radic Biol Med. 2000 Apr 15;28(8):1249-56. doi: 10.1016/s0891-5849(00)00244-6.
French maritime pine (Pinus maritima) bark extract (PBE) is a polyphenol-rich food supplement patented under the name of Pycnogenol and known to have strong antioxidant activity and different beneficial effects on human health. Although its biological properties have begun to be extensively studied both in vitro, in laboratory animals and more recently in humans, little is known about its bioavailability. The present study investigated the urinary excretion of free and conjugated ferulic acid, present in quantitatively detectable amounts in PBE, after oral PBE administration to human subjects. Eleven healthy adult subjects (4 women and 7men) consumed either a single dose (200 mg PBE) or two doses of PBE (100 and 200 mg, respectively) within a 48-h interval. Two days before the oral administration of PBE and during the urine sample collection period volunteers adhered to a diet low in polyphenols. Aliquots of all urine production were collected over 24 h. Free and conjugated ferulic acid was assessed in urine by HPLC using diode array detection. A close association between the dietary intake of PBE and the urinary excretion of ferulic acid was detected. Moreover, the results indicate that a considerable proportion of ferulic acid is excreted as glucuronide or sulfate after PBE consumption, varying over the range 2 to 20% between individuals. The kinetics of excretion associated with the administration of 100 mg PBE was quite similar to that obtained after 200 mg PBE. A a biphasic trend was evident in a number of subjects. All subjects studied here displayed a significant, although variable level of excretion of ferulic acid after supplementation with PBE, Thus, the data provide evidence that at least a part of the phenolic components of PBE are absorbed, metabolized, and eliminated by humans.
法国滨海松（Pinus maritima）树皮提取物（PBE）是一种富含多酚的食品补充剂，以碧萝芷（Pycnogenol）为名获得专利，已知具有强大的抗氧化活性，并对人体健康有多种有益作用。尽管其生物学特性已开始在体外、实验动物以及最近在人体中进行广泛研究，但其生物利用度却鲜为人知。本研究调查了在向人类受试者口服PBE后，PBE中定量可检测量的游离和结合阿魏酸的尿排泄情况。11名健康成年受试者（4名女性和7名男性）在48小时内服用了单剂量（200毫克PBE）或两剂PBE（分别为100毫克和200毫克）。在口服PBE前两天以及尿液样本收集期间，志愿者遵循低多酚饮食。在24小时内收集所有尿液产物的等分试样。通过使用二极管阵列检测的高效液相色谱法评估尿液中的游离和结合阿魏酸。检测到PBE的饮食摄入量与阿魏酸的尿排泄之间存在密切关联。此外，结果表明，食用PBE后，相当一部分阿魏酸以葡萄糖醛酸苷或硫酸盐的形式排泄，个体之间的变化范围在2%至20%之间。与服用100毫克PBE相关的排泄动力学与服用200毫克PBE后获得的排泄动力学非常相似。在一些受试者中明显呈现双相趋势。这里研究的所有受试者在补充PBE后均显示出阿魏酸排泄水平显著，尽管存在差异。因此，数据提供了证据，表明PBE的至少一部分酚类成分被人体吸收、代谢和消除。
