钒取代杂多钨酸盐抗伪狂犬病病毒的活性

合成了10种钒取代的杂多钨酸盐，采用细胞培养法，测定了各化合物对兔肾（RK）细胞的毒性及在无毒浓度下，抗伪狂犬病病毒（PRV）的活性，结果表明，部分化合物在无毒浓度下，具有较强的抗伪狂犬病病毒的活性．其中3种化合物显示出相当高的效力和选择性，半有浓度为3．5～5.0mg/L，半中毒浓度在400～420mg/L之间，化合物的浓度在25mg/L时，对伪狂犬病病毒的抑制作用达70％～80％，病毒的感染滴度TCID50下降4个对数．对其构效关系以及抗病毒机理也作了初步探讨．     

三唑类化合物研究与应用

综述了三唑类化合物在医药、农药、化学等相关领域的研究与应用。参考文献82篇。     

嘧啶并呋咱核苷衍生物的制备及其活性初探

4H,6H-[1,2,5]噁二唑并[3,4-d]嘧啶-5,7-二酮1-氧化物(1)和6-甲基-4H,6H-[1,2,5]噁二唑并[3,4-d]嘧啶-5,7-二酮1-氧化物(2)是一氧化氮(NO)供体, 将它们分别在无溶剂条件下与高温熔融的全乙酰基保护的核糖、木糖、葡萄糖进行糖基化反应, 分别得到相应的噁二唑并[3, 4-d]嘧啶核苷类化合物7, 9～12, 化合物7经NH₃-MeOH处理, 去O-乙酰基制得8, 这些新型核苷化合物可作为潜在的NO供体. 部分此类化合物的生物活性研究表明, 嘧啶并呋咱核苷衍生物具有抗病毒、抗肿瘤活性, 为研究抗病毒、抗肿瘤药物提供了新结构类型的候选化合物.     

流感病毒唾液酸苷酶抑制剂研究进展

随着近年来高致病性禽流感疫情的出现,历史上曾给人类生命造成严重威胁的大流感有可能再次大面积流行,这引起了世界范围内的普遍关注。作为合理药物设计一个成功范例的抗流感药物达菲,对患禽流感的病人的治疗也有效。它是一个流感病毒唾液酸苷酶抑制剂,可以对病毒感染细胞过程中关键的释放和扩散步骤进行阻断。这一事件促使人们对抗流感药物的研发产生了极大的兴趣。本文在简述唾液酸苷酶功能、催化反应机理的基础上,对近年来流感病毒唾液酸苷酶抑制剂的研究状况进行综述,重点介绍基于过渡态的药物设计、合成糖模拟物的结构骨架类型以及构效关系研究。由于唾液酸苷酶也与许多其它疾病的发生和发展过程密切相关,不同来源的唾液酸苷酶在结构上具有一些共同的特征,因此有关流感病毒唾液酸苷酶抑制剂的研发知识和经验也必将对其它疾病的唾液酸苷酶抑制剂的研究有直接的帮助。     

P2P网络主动免疫联防模型的研究

针对目前对等计算（P2P）网络中越来越严重的病毒传播和感染问题,结合生物免疫系统的工作原理和P2P网络自身的特点,提出一种新的P2P网络主动免疫联防模型。该模型将Peer节点局部免疫系统和以反病毒中心节点（ACP）主导的整体免疫防御体系有机结合在一起,从而对通过网络传播的恶意代码、病毒进行有效的、主动的控制和防御。详细的描述了P2P网络主动免疫联防模型的组成和运作流程,分析了模型中需要解决的关键问题,重点研究了ACP对病毒报告的应答机制和相应策略,并构建实验系统对此研究结果予以验证。     

The effect of infected external computers on the spread of viruses: A compartment modeling study

Inevitably, there exist infected computers outside of the Internet. This paper aims to understand how infected external computers affect the spread of computer viruses. For that purpose, a new virus–antivirus spreading model, which takes into account the effect of infected/immune external computers, is established. A systematic study shows that, unlike most previous models, the proposed model admits no virus-free equilibrium and admits a globally asymptotically stable viral equilibrium. This result implies that it would be practically impossible to eradicate viruses on the Internet. As a result, inhibiting the virus prevalence to below an acceptable level would be the next best thing. A theoretical study reveals the effect of different parameters on the steady virus prevalence. On this basis, a number of suggestions are made so as to contain virus spreading.     

Dereplication and targeted isolation of bioactive sulphur compound from bacteria isolated from a hydrothermal field

Marine micro-organisms in the deep-sea hydrothermal vent systems are considered as potential sources of bioactive natural products. Sixteen bacterial strains were isolated from a deep-sea hydrothermal field and screened for bioactive metabolism studies. After the strains were subjected to bioactive testing at different culture media, chemical dereplication by HPLC coupled to high-resolution mass spectrometer was performed to analyse or determine the main secondary metabolisms in those strains. Strain 06204 was large-scale fermented with relative optimal media, for isolating the desired sulphur compound. Butyrolactone I 3-sulphate was isolated and structurally identified from the extract, guided by dereplication and showed moderate antivirus activities against H3N2 and EV71 viruses. Our study suggests that deep-sea hydrothermal bacteria are good sources of sulphur natural products. Meanwhile, the described approach, mainly bioactive screening, dereplication and targeted isolation, is effective and efficient to discover interesting bioactive compounds in hydrothermal bacteria.     

A new naphthoquinone analogue and antiviral constituents from the root of Rhinacanthus nasutus

Rhinacanthus nasutus (L.) Kurz (Acanthaceae) is known as traditional medicine for the treatment of fungal and herpes virus infections. A new naphthoquinone racemate, rhinacasutone (1) together with seven known compounds, rhinacanthone (2), rhinacanthins C, D, N, Q, and E (3–7), and heliobuphthalmin (8) were isolated from root of R. nasutus. Their structures were determined on the basis of extensive spectroscopic methods, including 1D-, 2D-NMR and MS data. All the isolated compounds were tested for their antiviral activities against PR8, HRV1B, and CVB3-infected vero cells. Compounds 3–6 exhibited significant antiviral activities with the IC₅₀ value ranging from 0.03 to 23.7 μM in all three infections.     

流感病毒唾液酸苷酶抑制剂研究进展

随着近年来高致病性禽流感疫情的出现,历史上曾给人类生命造成严重威胁的大流感有可能再次大面积流行,这引起了世界范围内的普遍关注.作为合理药物设计一个成功范例的抗流感药物达菲,对患禽流感的病人的治疗也有效.它是一个流感病毒唾液酸苷酶抑制剂,可以对病毒感染细胞过程中关键的释放和扩散步骤进行阻断.这一事件促使人们对抗流感药物的研发产生了极大的兴趣.本文在简述唾液酸苷酶功能、催化反应机理的基础上,对近年来流感病毒唾液酸苷酶抑制剂的研究状况进行综述,重点介绍基于过渡态的药物设计、合成糖模拟物的结构骨架类型以及构效关系研究.由于唾液酸苷酶也与许多其它疾病的发生和发展过程密切相关,不同来源的唾液酸苷酶在结构上具有一些共同的特征,因此有关流感病毒唾液酸苷酶抑制剂的研发知识和经验也必将对其它疾病的唾液酸苷酶抑制剂的研究有直接的帮助.