Cell membrane-immobilized magnetic fluorescence nanoparticles as a screening platform for drug lead discovery

IF 6 2区 医学 Q2 MATERIALS SCIENCE, BIOMATERIALS
Yi Qin , Xu Jiang , Runuo Wang , Zhi Jia , Yang Liu , Xun Gao , Longshan Zhao , Xuefeng Guan
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引用次数: 0

Abstract

Cell membrane biomimetic screening technology enables nanomaterials to have unique biointerface targeting function and is widely used in the field of drug lead compound discovery. Here, Coronary artery smooth muscle cell (CASMC) membrane camouflaged Nile Red-doped Polyethyleneimine (PEI) functionalized magnetic fluorescent nanomaterials (CMMFNPs) were synthesized based on the covalent coupling method and were employed for the enrichment and screening of anti-coronary heart disease active ingredients targeting CASMC from the Sanwei Tanxiang capsule. Various characterization tools confirmed the CMMFNPs were successfully prepared and possessed strong biocompatibility, good optical properties, magnetic properties and adsorption properties. Eventually, a total of six potential active ingredients were screened from the extract, and the pro-proliferative effects of the screened ligands on the CASMC were preliminarily evaluated by the cellular imaging assay. In addition, molecular docking demonstrated strong binding between these compounds and cell membrane receptors (CD36, AT1); CCK-8 and BrdU kits assay further validated from different perspectives that the screened ligands promoted cell proliferation in a concentration-dependent manner. In conclusion, this method combined the cell membrane bionic screening with cellular imaging, which could realize the rapid screening of active ingredients and at the same time evaluate the pharmacological activities of the screened ligands, is expected to provide an effective tool for the discovery of new drugs.
细胞膜固定化磁性荧光纳米颗粒作为药物先导发现的筛选平台
细胞膜仿生筛选技术使纳米材料具有独特的生物界面靶向功能,在药物先导化合物发现领域得到广泛应用。本研究基于共价偶联法合成了冠状动脉平滑肌细胞(CASMC)膜伪装尼罗红掺杂聚乙烯亚胺(PEI)功能化磁性荧光纳米材料(CMMFNPs),并用于三味淡香胶囊中针对CASMC的抗冠心病活性成分的富集和筛选。各种表征工具证实CMMFNPs制备成功,具有较强的生物相容性、良好的光学性能、磁性能和吸附性能。最终,从提取物中筛选出6种潜在的活性成分,并通过细胞成像实验初步评价了所筛选出的配体对CASMC的促增殖作用。此外,分子对接表明这些化合物与细胞膜受体(CD36, AT1)之间有很强的结合;CCK-8和BrdU试剂盒实验进一步从不同角度验证了筛选的配体以浓度依赖的方式促进细胞增殖。综上所述,该方法将细胞膜仿生筛选与细胞成像相结合,可以实现对活性成分的快速筛选,同时对筛选的配体的药理活性进行评价,有望为新药的发现提供有效的工具。
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来源期刊
CiteScore
17.80
自引率
0.00%
发文量
501
审稿时长
27 days
期刊介绍: Biomaterials Advances, previously known as Materials Science and Engineering: C-Materials for Biological Applications (P-ISSN: 0928-4931, E-ISSN: 1873-0191). Includes topics at the interface of the biomedical sciences and materials engineering. These topics include: • Bioinspired and biomimetic materials for medical applications • Materials of biological origin for medical applications • Materials for "active" medical applications • Self-assembling and self-healing materials for medical applications • "Smart" (i.e., stimulus-response) materials for medical applications • Ceramic, metallic, polymeric, and composite materials for medical applications • Materials for in vivo sensing • Materials for in vivo imaging • Materials for delivery of pharmacologic agents and vaccines • Novel approaches for characterizing and modeling materials for medical applications Manuscripts on biological topics without a materials science component, or manuscripts on materials science without biological applications, will not be considered for publication in Materials Science and Engineering C. New submissions are first assessed for language, scope and originality (plagiarism check) and can be desk rejected before review if they need English language improvements, are out of scope or present excessive duplication with published sources. Biomaterials Advances sits within Elsevier''s biomaterials science portfolio alongside Biomaterials, Materials Today Bio and Biomaterials and Biosystems. As part of the broader Materials Today family, Biomaterials Advances offers authors rigorous peer review, rapid decisions, and high visibility. We look forward to receiving your submissions!
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