文献：Rapid Screening and Identification of Antitumor Ingredients from the Mangrove Endophytic Fungus Using an Enzyme-Immobilized Magnetic Nanoparticulate System

文献链接：

作者：Nan Wei , Jun Zhao , Guimei Wu , Wenjuan Cao , Pei Luo , Zhifeng Zhang , Gang Chen and Lu Wen

相关产品：NH2-PEG-NH2（氨基-聚乙二醇-氨基）

原文摘要：

As a consequence of recent progression in biomedicine and nanotechnology, nanoparticlebased systems have evolved as a new method with extensive applications in responsive therapy,multimodal imaging, drug delivery and natural product separation. Meanwhile, the magnetic nanoparticulate system has aroused great interest for separation and purification because of its excellent magnetic properties. Phospholipase A2(PLA2) is a highly expressed regulator to promote the growth of various cancers and is an ideal target to treat cancers. In this study, a novel strategy based on ligand–receptor interactions to discover novel PLA2 inhibitors was established, in which PLA2-functionalized Fe3O4@PLGA-PEG-NH2 magnetic nanoparticles were used as a supporting material combined with high-performance liquid chromatography–mass spectrometry, aiming to accelerate the discovery of novel PLA2 inhibitors from natural sources such as mangrove endophytic fungi. Under the optimized ligand fishing conditions, six target compounds were ultimately fished and identified to be cyclic peptides (1–3) and sterols (4–6), which compounds 1, 2 and 4–6 have well-documented cytotoxicities. Compound 3 exerted better inhibitory effect on A549 cells by experiment. In conclusion, PLA2-functionalized Fe3O4@PLGA-PEG-NH2 magnetic nanoparticlesbased ligand fishing provided a feasible, selective and effective platform for the efficient screening and identification of antitumor components from natural products.  

NH2-PEG-NH2：NH₂（氨基）：两端的氨基是这个化合物的关键官能团。氨基是一种活性很高的官能团，能参与多种化学反应。例如，它可以与羧酸发生酰胺化反应，与醛或酮发生缩合反应等。这些反应特性使得该化合物能够方便地与其他含有合适官能团的分子进行连接，从而构建各种功能复杂的分子结构。PEG（聚乙二醇）：聚乙二醇是一种由乙二醇单体聚合而成的聚合物。在 NH₂- PEG - NH₂结构中，PEG 起到连接两个氨基的作用。PEG 具有良好的水溶性、生物相容性和低poison性。其分子链具有一定的柔韧性，在溶液中能够自由伸展，这种特性有助于减少蛋白质吸附和降低免疫原性。NH₂- PEG - NH₂是一种双端氨基修饰的聚乙二醇化合物。这种结构赋予了它在化学合成和生物医学等多个领域应用的潜力，因为双端的氨基可以作为连接点，方便地与其他分子进行化学结合。基于NH2-PEG-NH2的性质，PLA2功能化Fe3O4@PLGA-PEG-NH2磁性纳米颗粒的合成如下：

图：合成方案

Fe3O4@PLGA-PEG-NH2 MNPs的合成：

将Fe3O4 MNPs和PLGA-PEG-NH2通过涡旋悬浮在二氯甲烷中，得到一个油相，然后加入 PVA水溶液中，超声。随后将乳化液加入到PVA溶液中，通过减压蒸发去除有机相。将分散物离心，以去除未封装的Fe3O4 MNPs。将制备的Fe3O4@PLGA-PEG-NH2 MNPs产物冻干，在4◦C下保存。在Fe3O4@PLGA-PEG-NH2 MNPs的合成过程中，考察了不同反应条件对MNPs磁性能的影响，包括制备方法和四氧化三铁MNPs的含量。

图：表征图像

结论：

该文献成功制备出基于NH2-PEG-NH2合成的PLA2功能化Fe3O4@PLGA-PEG-NH2磁性纳米颗粒。该物质作为支持材料结合高效液相色谱质谱，能加快发现新型PLA2抑制剂从自然来源如红树林内生Fungi 。实验表明，化合物对A549细胞有较好的抑制作用。综上，PLA2功能化的Fe3O4@PLGA-PEG-NH2磁性纳米材料提供了一个可行、选择性和有效的平台。