糖基化在新型冠状病毒侵染中的机制及药物研发中的应用

冠状病毒(Coronavirus,CoV)是一类具有包膜的正股单链RNA病毒,可感染人类和多种动物.2019年末,一种新的β-冠状病毒SARS-CoV-2(Severe acute respiratory syndrome-coronavirus-2)开始在人际间传播,该病毒引发的疾病“COVID-19”(Corona...     

新型冠状病毒检测以及相关药物研发中的基础药学知识

新型冠状病毒检测以及相关药物研发中涉及到了丰富的基础药学知识,本文进行了详细的总结,为案例教学提供了素材。     

新型冠状病毒检测以及相关药物研发中的基础药学知识

Abundant basic pharmaceutical knowledge is involved in the detection of SARS-CoV-2 and the discovery and development of antiviral drugs. This paper gives detailed summary and provides rich materials for case teaching.     

抗流感病毒药物合成研究纵览

流行性感冒（流感）是一种传染性强和传播速度快的疾病,对人类健康构成严重威胁。为了更好地抵御流感病毒对人类健康的侵害,科学家们一直致力于新型抗流感病毒药物的研究和发现工作。针对已上市抗流感药物以及处于研发阶段的抗流感病毒抑制剂的合成方法进行概述,为抗流感药物的合成工艺研究和药物研发提供参考。     

冠状病毒抑制剂的研究进展

冠状病毒是一类广泛存在且对人及家畜具有严重危害的病原体,其中于2003年全球爆发的严重急性呼吸综合征病毒(SARS-CoV)以及2012年被发现并传播的中东呼吸综合征病毒(MERS-CoV)给人们的生命健康以及全球经济造成了严重威胁以及重大损失,特别是2019年末爆发的新型冠状病毒(SARS-CoV-2),截至目前为止已经造成了几百万的感染病例以及几十万人的死亡。可以看出,冠状病毒具有较高的传播性以及较高的致死率,时刻威胁着人们的健康安全,但是针对冠状病毒的感染目前还没有批准上市的有效药物,也没有用于预防的疫苗。本文围绕目前关于冠状病毒的潜在成药性靶点,详细介绍了针对这些靶点的具有代表性的抑制剂的结构设计及其化学合成方法,以期为目前抗冠状病毒药物的研发提供一些参考。     

用于抗新型冠状病毒的无机表面材料及其作用机制

由新型冠状病毒所导致的新冠肺炎疫情已对人类健康造成严重威胁, 病毒的大范围传播增加了对抗病毒表面材料(尤其是用于公共场所中)的需求. 本文综述了一系列具有抗病毒性能的无机表面材料, 包括金属单质及其衍生物、 石墨烯及其衍生物和沸石, 以及它们各自的抗病毒机制; 最后, 对无机抗病毒表面材料领域所面临的挑战与发展前景进行了总结与展望.     

新型小分子抗凝血药物的合成、作用机制及构效关系研究进展

以达比加群酯为代表的Ⅱa因子抑制剂和以利伐沙班为代表的Xa因子抑制剂在抗凝血药物中起到了重要作用。本文综述了已上市的新型小分子抗凝血药物的的合成、作用机制及其构效关系,并对其进行了深入分析,同时对此类药物的发展趋势和前景进行了展望。     

几种新型锗修饰药物衍生物的合成及其抗癌活性

几种新型锗修饰药物衍生物的合成及其抗癌活性;磺酰基二苯胺;卡马西林;诺氟沙星     

新型冠状病毒疫苗设计原理与研究进展

新型冠状病毒肺炎(COVID-19)已在全球范围内呈大流行趋势,为全球社会带来重大损失。其致病病原体新型冠状病毒(SARS-CoV-2)具有较强传染率和一定的致死率,为疾病治疗带来挑战。疫苗接种是预防传染病的重要手段,目前全球多家研究机构已经启动了新冠疫苗的研发工作。本文介绍了新冠疫苗研发的原理以及国内外最新的疫苗研究进展,希望有助于理解新冠疫苗的研发。     

新型冠状病毒疫苗设计原理与研究进展

The COVID-19 pandemic caused significant losses to the global community. The pathogen, called SARSCoV-2, showed high infection rate and certain case-fatality rate, which bring great challenges to treatments. Vaccination is the major way for epidemic prevention which attracts several developers to conduct COVID-19 vaccine studies. This paper presents the design principle of a COVID-19 vaccine and summarizes the latest research progress on vaccine development. The authors hope to provide insights for understanding vaccine study of COVID-19.     

Development and Validation of a Novel HPLC Method to Analyse Metabolic Reaction Products Catalysed by the CYP3A2 Isoform: In Vitro Inhibition of CYP3A2 Enzyme Activity by Aspirin (Drugs Often Used Together in COVID-19 Treatment)

Aspirin (also known as acetylsalicylic acid) is a drug intended to treat fever, pain, or inflammation. Treatment of moderate to severe cases of COVID-19 using aspirin along with dexamethasone has gained major attention globally in recent times. Thus, the purpose of this study was to use High-Performance Liquid Chromatography (HPLC) to evaluate the in vitro inhibition of CYP3A2 enzyme activity using aspirin in rat liver microsomes (RLMs). In this study, an efficient and sensitive HPLC method was developed using a reversed phase C18 column (X Bridge 4.6 mm × 150 mm, 3.5 µm) at 243 nm using acetonitrile and water (70:30 v/v). The linearity (r² > 0.999), precision (<15%), accuracy and recovery (80–120%), limit of detection (5.60 µM and 0.06 µM), limit of quantification (16.98 µM and 0.19 µM), and stability of the newly developed method were validated for dexamethasone and 6β-hydroxydexamethasone, respectively, following International Conference on Harmonization (ICH) guidelines. This method was applied in vitro to measure CYP3A2 activity. The results showed that aspirin competitively inhibits 6β-hydroxylation (CYP3A2 activity) with an inhibition constant (Ki) = 95.46 µM and the concentration of the inhibitor causing 50% inhibition of original enzyme activity (IC₅₀) = 190.92 µM. This indicated that there is a minimal risk of toxicity when dexamethasone and aspirin are co-administrated and a very low risk of toxicity and drug interaction with drugs that are a substrate for CYP3A2 in healthcare settings.