Packer L, Rimbach G, Virgili F
Department of Molecular and Cell Biology, University of California, Berkeley 94720-3200, USA.
Free Radic Biol Med. 1999 Sep;27(5-6):704-24. doi: 10.1016/s0891-5849(99)00090-8.
There is growing interest in the biologic activities of plant extracts such as that obtained from the bark of the French maritime pine Pinus maritima, Pycnogenol. Pycnogenol (PYC) is a standardized extract composed of a mixture of flavonoids, mainly procyandins and phenolic acids. Studies indicate that PYC components are highly bioavailable. Uniquely PYC displays greater biologic effects as a mixture than its purified components do individually indicating that the components interact synergistically. PYC has been reported to have cardiovascular benefits, such as a vasorelaxant activity, angiotensin-converting enzyme (ACE) inhibiting activity, and the ability to enhance the microcirculation by increasing capillary permeability. Investigations of the cellular mechanisms of these therapeutic effects have demonstrated that PYC has strong free radical-scavenging activity against reactive oxygen and nitrogen species. The oligomeric components of PYC contribute significantly to the ESR free radical signal. PYC also participates in the cellular antioxidant network as indicated by its ability to regenerate the ascorbyl radical and to protect endogenous vitamin E and glutathione from oxidative stress. PYC modulates NO metabolism in activated macrophages by quenching the NO radical and inhibiting both iNOS mRNA expression and iNOS activity. The spectrum of different effects of NO in the circulation and the nervous system suggest the potential applications of PYC in immune and circulatory disorders as well as in neurodegenerative disease. PYC can bind to proteins, altering their structure and thereby modulating the activity of key enzymes and proteins involved in metabolic pathways. PYC effects redox-sensitive signal transduction pathways and alters gene expression. Aspects of PYC's activity are presented and discussed together with possible future implications and directions in the field of flavonoid research.
人们对植物提取物的生物活性越来越感兴趣，比如从法国滨海松（Pinus maritima）树皮中提取的碧萝芷（Pycnogenol）。碧萝芷（PYC）是一种标准化提取物，由类黄酮混合物组成，主要是原花青素和酚酸。研究表明，PYC的成分具有很高的生物利用度。独特的是，PYC作为一种混合物比其纯化成分单独显示出更大的生物学效应，这表明这些成分具有协同作用。据报道，PYC对心血管有益，如具有血管舒张活性、抑制血管紧张素转换酶（ACE）的活性，以及通过增加毛细血管通透性来增强微循环的能力。对这些治疗作用的细胞机制的研究表明，PYC对活性氧和氮物种具有强大的自由基清除活性。PYC的低聚成分对电子自旋共振自由基信号有显著贡献。PYC还参与细胞抗氧化网络，这体现在它能够再生抗坏血酸自由基，并保护内源性维生素E和谷胱甘肽免受氧化应激。PYC通过淬灭NO自由基并抑制诱导型一氧化氮合酶（iNOS）mRNA表达和iNOS活性来调节活化巨噬细胞中的NO代谢。NO在循环系统和神经系统中的不同作用谱表明PYC在免疫和循环系统疾病以及神经退行性疾病中的潜在应用。PYC可以与蛋白质结合，改变其结构，从而调节参与代谢途径的关键酶和蛋白质的活性。PYC影响氧化还原敏感的信号转导途径并改变基因表达。本文介绍并讨论了PYC的活性方面，以及黄酮类研究领域未来可能的影响和方向。
