tetraphenylethylene

四苯基乙烯
  • 文章类型: Journal Article
    间充质干细胞(MSCs),由于他们的肿瘤嗜性,被各种实体瘤强烈募集,并被肿瘤微环境中的炎症信号动员。然而,有效的细胞摄取对于基于MSC的药物递送是关键的。在这项研究中,我们合成了一种球形共聚物,聚乙烯亚胺-聚(ε-己内酯),与聚集诱导发射(AIE)材料和抗癌药物,紫杉醇,涂在它的内核上。随后添加转录反式激活因子(TAT)肽,一种细胞穿透肽,以修饰纳米粒子(NPs)。最后,MSCs用于将TAT修饰的AIE-NP药物携带至肿瘤部位,并协助同时进行癌症诊断和靶向肿瘤治疗.体外,TAT修饰的AIE-NP表现出良好的生物相容性,瞄准,以及在水溶液中的稳定性,除了高的载药量和包封效率。体外,AIE-NP在弱酸性环境下表现出可控的释放。体内和体外研究表明,AIE-NP药物具有较高的抗肿瘤功效和较低的细胞毒性,而生物分布证实了MSCs的肿瘤嗜性。总结一下,基于MSC的负载TAT的AIE-NP药物通过增强的NP-药物摄取具有良好的生物相容性和高抗肿瘤功效。此外,MSCs的肿瘤嗜性提供了肿瘤细胞的选择性药物摄取,从而减少了全身副作用。
    Mesenchymal stem cells (MSCs), due to their tumor tropism, are strongly recruited by various solid tumors and mobilized by inflammatory signals in the tumor microenvironment. However, effective cellular uptake is critical for MSC-based drug delivery. In this study, we synthesized a spherical copolymer, polyethylenimine-poly(ε-caprolactone), with aggregation-induced emission (AIE) material and the anticancer drug, paclitaxel, coloaded onto its inner core. This was followed by the addition of a transactivator of transcription (TAT) peptide, a type of cell-penetrating peptide, to modify the nanoparticles (NPs). Finally, the MSCs were employed to carry the TAT-modified AIE-NPs drug to the tumor sites and assist in simultaneous cancer diagnosis and targeted tumor therapy. In vitro, the TAT-modified AIE-NPs showed good biocompatibility, targeting, and stability in an aqueous solution besides high drug-loading and encapsulation efficiency. In vitro, the AIE-NPs exhibited a controllable release under a mildly acidic environment. The in vivo and in vitro studies showed high antitumor efficacy and low cytotoxicity of the AIE-NP drug, whereas biodistribution confirmed the tumor tropism of MSCs. To summarize, the MSC-based AIE-NP drugs loaded with TAT possessed good biocompatibility and high antitumor efficacy via the enhanced NP-drug uptake. In addition, the tumor tropism of MSCs provided selective drug uptake by the tumor cells and thus reduced the systemic side effects.
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  • 文章类型: Journal Article
    在过去的一百年里,高分子科学取得了巨大的发展。高分子科学的发展与表征技术和方法的发展密切相关,从分子量测定中的粘度测定法到包括差示扫描量热法在内的先进技术,核磁共振,和扫描电子显微镜。然而,这些技术通常局限于繁琐的样品制备,高成本,苛刻的实验条件,或异位表征。荧光技术具有灵敏度高、可视化直观等优点。与常规引起聚集的猝灭荧光团相反,那些具有聚集诱导发射(AIE)特性的染料在聚集状态下显示出高发射效率。基于AIE性质的分子内运动的限制,由于扭曲的螺旋桨状结构,AIE材料对周围的微环境非常敏感,因此在聚合物研究中具有巨大的潜力。AIE概念已成功用于聚合物科学,并提供了对聚合物结构和性能的更深入的了解。在这次审查中,AIEgens在聚合物科学中可视化聚合的应用,玻璃化转变,溶出度,结晶,凝胶化,自组装,相分离,cracking,和自我修复的例子和总结。最后,解决了使用AIEgens研究聚合物科学的挑战和观点。
    The past one hundred years have witnessed the great development of polymer science. The advancement of polymer science is closely related with the development of characterization techniques and methods, from viscometry in molecular weight determination to advanced techniques including differential scanning calorimetry, nuclear magnetic resonance, and scanning electron microscopy. However, these techniques are normally constrained to tedious sample preparation, high costs, harsh experimental conditions, or ex situ characterization. Fluorescence technology has the merits of high sensitivity and direct visualization. Contrary to conventional aggregation-causing quenching fluorophores, those dyes with aggregation-induced emission (AIE) characteristics show high emission efficiency in aggregate states. Based on the restriction of intramolecular motions for AIE properties, the AIE materials are very sensitive to the surrounding microenvironments owing to the twisted propeller-like structures and therefore offer great potential in the study of polymers. The AIE concept has been successfully used in polymer science and provides a deeper understanding on polymer structure and properties. In this review, the applications of AIEgens in polymer science for visualizing polymerization, glass transition, dissolution, crystallization, gelation, self-assembly, phase separation, cracking, and self-healing are exemplified and summarized. Lastly, the challenges and perspectives in the study of polymer science using AIEgens are addressed.
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  • 文章类型: Journal Article
    Fluorogens with aggregation-induced emission (AIEgens) have emerged as a powerful and versatile platform for the development of novel biosensors. In this study, a series of water-soluble fluorescent probes based on tetraphenylethylene (TPE) were designed and synthesized for the detection of monoamine oxidases (MAOs) based on specific interactions between the probes and the proteins. Among the six probes developed, t-TPEM displays a significant fluorescence increase upon introduction of MAOs. Of particular significance is that the fluorescence of t-TPEM in the presence of MAO-A is 21-fold higher than other proteins including MAO-B. Lineweaver-Burk plots reveal that t-TPEM acts as an uncompetitive inhibitor of MAO-A with Ki = 17.1 μM, which confirms its good binding affinity toward MAO-A. Furthermore, a cell imaging experiment reveals that t-TPEM is able to selectively monitor the activity of MAO-A which is localized in mitochondria of MCF-7 cells.
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