Graduate School of Pharmaceutical Sciences, University of Tokyo, Tokyo 113-0033, Japan.
Proc Natl Acad Sci U S A. 2011 Oct 18;108(42):17533-7. doi: 10.1073/pnas.1110577108. Epub 2011 Oct 4.
A lipid extract of Perna canaliculus (New Zealand green-lipped mussel) has reportedly displayed anti-inflammatory effects in animal models and in human controlled studies. However, the anti-inflammatory lipid components have not been investigated in detail due to the instability of the lipid extract, which has made the identification of the distinct active components a formidable task. Considering the instability of the active component, we carefully fractionated a lipid extract of Perna canaliculus (Lyprinol) and detected furan fatty acids (F-acids). These naturally but rarely detected fatty acids show potent radical-scavenging ability and are essential constituents of plants and algae. Based on these data, it has been proposed that F-acids could be potential antioxidants, which may contribute to the protective properties of fish and fish oil diets against chronic inflammatory diseases. However, to date, in vivo data to support the hypothesis have not been obtained, presumably due to the limited availability of F-acids. To confirm the in vivo anti-inflammatory effect of F-acids in comparison with that of eicosapentaenoic acid (EPA), we developed a semisynthetic preparation and examined its anti-inflammatory activity in a rat model of adjuvant-induced arthritis. Indeed, the F-acid ethyl ester exhibited more potent anti-inflammatory activity than that of the EPA ethyl ester. We report on the in vivo activity of F-acids, confirming that the lipid extract of the green-lipped mussel includes an unstable fatty acid that is more effective than EPA.
新西兰绿唇贻贝（Perna canaliculus）的脂质提取物据称在动物模型和人类对照研究中表现出抗炎作用。然而，由于脂质提取物的不稳定性，尚未对其抗炎脂质成分进行详细研究，这使得鉴定独特的活性成分成为一项艰巨的任务。考虑到活性成分的不稳定性，我们仔细地对新西兰绿唇贻贝（Lyprinol）的脂质提取物进行了分级，并检测到了呋喃脂肪酸（F-acids）。这些天然但很少被检测到的脂肪酸具有强大的自由基清除能力，是植物和藻类的重要组成部分。基于这些数据，有人提出 F-acids 可能是潜在的抗氧化剂，这可能有助于鱼类和鱼油饮食对慢性炎症性疾病的保护作用。然而，迄今为止，尚未获得支持这一假设的体内数据，这可能是由于 F-acids 的有限可用性。为了证实 F-acids 与二十碳五烯酸（EPA）相比在体内的抗炎作用，我们开发了一种半合成制剂，并在佐剂诱导关节炎的大鼠模型中研究了其抗炎活性。事实上，F-acid 乙酯表现出比 EPA 乙酯更强的抗炎活性。我们报告了 F-acids 的体内活性，证实了绿唇贻贝的脂质提取物中含有一种不稳定的脂肪酸，其效果优于 EPA。
