Department of Marine Biotechnology, Stazione Zoologica Anton Dohrn, CAP80121 Naples, Italy.
Marbio, UiT-The Arctic University of Norway, Breivika N-9037 Tromsø, Norway.
Mar Drugs. 2020 Mar 17;18(3):166. doi: 10.3390/md18030166.
Microalgae have been shown to be excellent producers of lipids, pigments, carbohydrates, and a plethora of secondary metabolites with possible applications in the pharmacological, nutraceutical, and cosmeceutical sectors. Recently, various microalgal raw extracts have been found to have anti-inflammatory properties. In this study, we performed the fractionation of raw extracts of the diatom previously shown to have anti-inflammatory properties, obtaining five fractions. Fractions C and D were found to significantly inhibit tumor necrosis factor alpha (TNF-⍺) release in LPS-stimulated human monocyte THP-1 cells. A dereplication analysis of these two fractions allowed the identification of their main components. Our data suggest that lysophosphatidylcholines and a breakdown product of chlorophyll, pheophorbide a, were probably responsible for the observed anti-inflammatory activity. Pheophorbide a is known to have anti-inflammatory properties. We tested and confirmed the anti-inflammatory activity of 1-palmitoyl-sn-glycero-3-phosphocholine, the most abundant lysophosphatidylcholine found in fraction C. This study demonstrated the importance of proper dereplication of bioactive extracts and fractions before isolation of compounds is commenced.
微藻已被证明是生产脂质、色素、碳水化合物和大量具有潜在药理学、营养保健品和化妆品应用的次生代谢产物的优秀生产者。最近，人们发现各种微藻原料提取物具有抗炎特性。在这项研究中，我们对先前显示具有抗炎特性的硅藻进行了原料提取物的分级分离，得到了五个馏分。馏分 C 和 D 被发现可显著抑制 LPS 刺激的人单核细胞 THP-1 细胞中肿瘤坏死因子 alpha（TNF-⍺）的释放。对这两个馏分的去重复分析允许鉴定它们的主要成分。我们的数据表明，溶血磷脂酰胆碱和叶绿素的分解产物脱镁叶绿酸 a 可能是观察到的抗炎活性的原因。脱镁叶绿酸 a 具有抗炎特性。我们测试并证实了在 C 馏分中含量最丰富的溶血磷脂酰胆碱 1-棕榈酰-sn-甘油-3-磷酸胆碱的抗炎活性。这项研究表明，在开始分离化合物之前，对生物活性提取物和馏分进行适当的去重复是很重要的。
