中文摘要
H5N1 禽流感病毒以其高致病性及高死亡率,突破了宿主的种属屏障,严重威胁了人类的生命健康。现有用于防治禽流感的药物种类较少,毒副作用较大,远不能满足临床和社会的需求,积极研究防治人禽流感的药物,尤其是从中草药中发现新作用机制的药物,已成为当前迫在眉睫的重要课题。爵床是爵床科植物爵床的干燥全草,药理研究表明具有明显抗肿瘤和抗菌抗病毒等多种生物活性。课题组前期研究发现爵床具有明显抗H5N1禽流感病毒活性,并发现了一些结构新颖的木脂素和环肽生物碱化合物,为探明爵床提取物抗H5N1禽流感病毒活性药效基础,拟对活性部位进行系统化学成分研究,并对所得化合物进行抗H5N1禽流感病毒活性筛选,阐明构效关系和作用机制。通过本研究以期能得到具有较好抗H5N1禽流感病毒活性的活性部位或结构新颖活性先导化合物,对阐明爵床抗H5N1禽流感病毒活性物质基础、作用机制及开发新型抗H5N1禽流感病毒药物都具有重要意义。
英文摘要
H5N1 highly pathogenic avian influenza virus can break through species barriers and infect human beings directly, which is a serious threat to human life and health. In addition, the serious problem of few kind of antiviral agents and side effects, which make it extremely urgent to discover new efficient and low toxicity of anti H5N1 drugs. Currently, there is a growing interest to search for anti H5N1 substances with new mechanisms from natural sources. Justicia procumbens L. (Acanthaceae), known as “Jue chuang” in China, is a commonly used traditional herbal medicine embodied in Chinese Pharmacopoeia 1977 version, with clinical effects of reducing fire, removing toxic heat. The whole plant of J. procumbens mainly distributed in South China and Taiwan has long been used to treat cold, fever, cough, pain, inflammation of the throat and indigestion in children, etc. Several arylnaphthalide lignans showing cytotoxic and antivirus activities have been reported as main constituents of this plant. Preliminary tests for anti-H5N1 virus activity in vitro showed that the ethanol extract of J. procumbens exhibited obvious activity of virus-resistance, and some novel lignans and cyclopeptide alkaloids were observed. Based on the research, the herbs are going to be extracted with 60% ethanol, chemical constituents of fractions will be studied systematically and deeply to screen the anti H5N1 activity, the structure-activity relationship and mechanism of lead compounds or active fractions will also be investigated. Through this study, it will be expected to obtain fractions and lead novel compounds of significant anti H5N1 activity. The research is of great significance to clarify the chemical constituents and mechanism of J. procumbens and to develop the novel anti H5N1 drugs.
