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关键词： Bimetallic nanodendrites   Protein corona   Fluorescence quenching   Conformational changes   Biocompatibility  

摘要： Bimetallic nanoparticles present a promising therapeutic platform that offers unique potentials in numerous biomedical applications. However, their interaction with proteins upon contact with biofluids may modulate their biological properties due to adsorbed proteins. Herein, we provide insights on the pattern and mechanism of interactions of gold-core palladium shell dendritic-nanoparticles (Au@PdNDs) with excess morphology in the presence of human blood proteins: bovine serum albumin (BSA), fibrinogen (FBG), and gamma-globulin (gamma-GLO). Upon modification with polyethylene glycol (PEG) and protamine sulfate (PS), various techniques such as fluorescence spectroscopy, dynamic light scattering, and circular dichroism spectroscopy were employed to investigate the dynamics of nanodendrite-protein complex formation. It was found that regardless of the surface charge of the bimetallic nanodendrites, FBG was the most adsorbed among the proteins, followed by BSA and gamma-GLO. Furthermore, both types of nanodendrites showed selective affinity towards the different proteins based on the calculated number of binding sites (n) and association constants (K). Interestingly, FBG displayed substantial concentration-dependent conformational changes in the presence of both types of nanodendrites while only PS-modified Au@PdNDs showed alpha-helix and beta-strand distortions with gamma-GLO. Finally, the nanodendrite-protein complex formation significantly improved the biocompatibility upon the exposure to breast (MCF-7), lung (A549), and kidney embryonic (HEK 293) cell lines and was independent of the surface property as well as the concentration of the biocoronation. Our findings highlighted a critical assessment of relevant considerations towards the deployment of nanodendrites for therapeutic applications. (C) 2021 Elsevier B.V. All rights reserved.

关键词： Glioblastoma   2-Aminoquinoline   G2   M phase arrest   Apoptosis  

摘要： Malignant gliomas are the most common brain tumors, with generally dismal prognosis, early clinical deterioration and high mortality. Recently, 2-aminoquinoline scaffold derivatives have shown pronounced activity in central nervous system disorders. We herein reported a series of 2-aminoquinoline-3-carboxamides as novel nonalkylator anti-glioblastoma agents. The synthesized compounds showed comparable activity to cisplatin against glioblastoma cell line U87 MG in vitro. Among them, we found that 6a displayed good inhibitory activity against A172 and U118 MG glioblastoma cell lines and induced cell cycle arrest in the G2/M phase and apoptosis in U87 MG by flow cytometry analysis. Additionally, 6a displayed low cytotoxicity to several normal human cell lines. In silico study showed 6a had promising physicochemical properties and was predicted to cross the blood-brain barrier. Moreover, preliminary structure-activity relationships are also investigated, shedding light on further modifications towards more potent agents on this series of compounds. Our results suggest this compound has a promising potential as an anti-glioblastoma agent with a differential effect between tumor and non-malignant cells.

关键词： 物理化学   教学   过程性考核  

摘要： 物理化学提供应用于化学及相关领域的基本概念和原理,是药学各专业的重要基础理论课程。本文通过教学试验证明过程性考核模式可以提高主、被动学习型学生的物理化学成绩,对消极学习型学生的成绩影响不明显。

关键词： 物理化学   化学热力学   典型习题   知识理解   精准运用  

摘要： 化学热力学是《物理化学》的重要组成部份和学习基础,虽然其中的概念简单易记,但具有知识点多、相互之间关系复杂的特点,造成了易学难懂的矛盾,需要加强学生对化学热力学知识的应用能力。利用对典型习题的研讨,可以将学生带入具体情景、破除他们对化学热力学知识过于抽象的感受,并增加对知识的理解,养成根据问题来精准选择合适知识的能力。

关键词： 创新能力   物理化学   教学改革  

摘要： 物理化学是化学化工类院校本科生必修的一门专业基础课程,是通过物理原理及物理实验技术,研究所有物质体系的化学行为的原理、规律和方法的学科。物理化学课程具有学科交叉和理论性强的特点,在其教学过程中结合创新教学,有利于培养学生的创新思维和创新能力。通过对学生逻辑思维的培养,采取线上线下混合式教学模式,注重理论与实践相结合,提高教师自身素质等改革方式培养出具有具有扎实物理化学基础的人才。

关键词： 物理化学   微课   线上线下   混合式教学  

摘要： 物理化学作为重要的学科基础课,具有逻辑性强,概念抽象,公式多且难等特点。根据个人在微课教学方面的研究及教学实践,将物理化学课程中的重难点制作成微课视频模块,建立基于微课的线上线下混合教学模式,配以更加客观多元的考核体系,注重培养学生的自主学习能力和综合素质,从而弥补了传统课堂教学的不足,提升教学质量,为物理化学教学改革提供参考。

关键词： Polysaccharide   Ultrasound extraction   Frequency   Physicochemical characterization   Biological activity   Okra (Abelmoschus esculentus (L   ) Moench) plus  

摘要： In this study, single- (SFU) and dual-frequency (DFU) ultrasounds were used to extract polysaccharides from okra (Abelmoschus esculentus (L.) Moench) pods (OPSs), and the physicochemical characteristics, functional properties, and in vitro biological activities of the OPSs were comparatively evaluated. Results showed that ultrasonic extractions at different frequencies led to remarkable variations in extraction yields, chemical components, monosaccharide compositions, molecular weights (MWs), surface morphologies, and rheological properties of the OPSs but hardly affected their preliminary structural features and thermal stabilities. The OPS obtained through DFU at 40/60 kHz with the lowest MWs (0.85-14.93 x 105 Da) and highest polyphenol content (7.38%) as well as loosest network structures showed superior antioxidant, cholesterol absorption and nitrite ion absorption capacities than the other OPSs, and the OPS extracted through SFU at 20 kHz with the highest carboxylate content (76.08%), MWs (7.28-32.83 x 105 Da) and degree of esterification (30.7%) exhibited higher bile acid-binding capacity than the other OPSs.

关键词： Polyelectrolyte complexation   Dextran sulfate   Chitosan   Molecular weight   Chitosan oligosaccharide   Nanoparticles  

摘要： Polyelectrolyte complexation is a technique based on interactions between polyelectrolytes of opposite charges driven by supramolecular interactions. Although many studies address the formation of polyelectrolyte complexes (PECs), few explore strategies and tools to select the best working conditions and are often based on empirical choices. This study evaluates the influence of pH, molecular weight, and polymeric proportion on the formation of PECs based on chitosan:dextran sulfate. In addition, it assesses the approaches that study the influence of pH on the zeta potential of polymeric dispersions as a tool in the design of PECs. Results showed that nanoparticles with an excess of polycation formed aggregates, while an excess of dextran sulfate reduced the size of the particles. The graph of zeta potential as a function of pH proved to be a promising tool in the choice of polymers and a better pH condition in the development of PECs.

关键词： 课程思政   物理化学实验   教学改革  

摘要： 为贯彻落实知识传授、能力培养、价值引领三位一体的课程目标,在物理化学实验教学中实施课程思政改革。本文详述了在实施课程思政的过程中,坚持以学生为中心,采用线上线下混合式教学模式,转变教育观念,建设课程思政团队,深入挖掘课程思政元素,探索思政元素融入教学中的方法及载体,促进学生思想道德水平和教学质量的提高,发挥专业课程在思政教育中的作用。