Qiu Shi, Khan Shabana I, Wang Mei, Zhao Jianping, Ren Siyu, Khan Ikhlas A, Steffek Amy, Pfund William P, Li Xing-Cong
National Center for Natural Product Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA.
Department of Biomolecular Sciences, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA.
Molecules. 2020 Feb 26;25(5):1048. doi: 10.3390/molecules25051048.
The green alga var. is a rich source of proteins, polyphenols, and bioactive small-molecule compounds. An approach involving chromatographic fractionation, anti-inflammatory activity testing, ultrahigh performance liquid chromatography-mass spectrometry profiling, chemometric analysis, and subsequent MS-oriented isolation was employed to rapidly identify its small-molecule anti-inflammatory compounds including hydroxylated fatty acids, chlorophyll-derived pheophorbides, carotenoids, and glycoglycerolipids. Pheophorbide a, which decreased intracellular nitric oxide production by inhibiting inducible nitric oxide synthase, was the most potent compound identified with an IC value of 0.24 µM in lipopolysaccharides-induced macrophages. It also inhibited nuclear factor kappaB activation with an IC value of 32.1 µM in phorbol 12-myristate 13-acetate-induced chondrocytes. Compared to conventional bioassay-guided fractionation, this approach is more efficient for rapid identification of multiple chemical classes of bioactive compounds from a complex natural product mixture.
绿藻变种是蛋白质、多酚和生物活性小分子化合物的丰富来源。采用了一种包括色谱分离、抗炎活性测试、超高效液相色谱 - 质谱分析、化学计量分析以及随后基于质谱的分离方法，以快速鉴定其小分子抗炎化合物，包括羟基脂肪酸、叶绿素衍生的脱镁叶绿酸、类胡萝卜素和糖基甘油酯。脱镁叶绿酸a通过抑制诱导型一氧化氮合酶降低细胞内一氧化氮的产生，是在脂多糖诱导的巨噬细胞中鉴定出的最有效的化合物，其IC值为0.24 μM。它在佛波酯12 - 肉豆蔻酸酯13 - 乙酸酯诱导的软骨细胞中也以32.1 μM的IC值抑制核因子κB的激活。与传统的生物测定引导分级分离相比，这种方法对于从复杂的天然产物混合物中快速鉴定多种化学类别的生物活性化合物更有效。
