中文摘要
奇壬醇系从常用传统中药——豨莶草中分离得到的具有抗风湿、抗炎、免疫抑制活性的先导化合物。本课题组通过“八五”、“九五”攻关课题,尤其是国家自然科学基金课题的资助,十余年来对该植物的有效成分及药理活性做了深入研究。本课题组前期已经对奇壬醇进行了较为系统的抗炎、免疫抑制活性的研究,发现奇壬醇是一个低毒活性强具备类药性质的二萜类化合物,有开发成新型免疫抑制剂的潜能。通过自然科学基金课题对奇壬醇进行了结构修饰研究,结合药理活性筛选发现了活性更强的分子。本课题的主要研究目的是进行奇壬醇的半合成研究,探索合理的合成反应路线,以及深入的免疫性疾病系统性红斑狼疮的相关药理学活性研究,为将其开发为治疗自身免疫性疾病及系统性红斑狼疮的新药奠定理论和应用基础,从具有较好临床基础的传统中药中寻找先导化合物到发现具有类药性质的、合格的临床候选药物是探索创新药物研究的重要途径和方法。
英文摘要
Kirenol, a diterpenoid isolated from traditional Chinese medicine Siegesbeckia pubescens, was tested to be a good lead compound with anti-rheumatism, anti-inflammatory and immunosuppressive activity. Our group have been concentrating on studying the chemical investigation and pharmacological activities of the plant for more than ten years with the help of the foundations like the research of "85" and "95", and the National Natural Science Foundation of China. Previous study showed that kirenol is a promising lead compound for immunosuppressive agents. We have carried out the study on the structure modification of kirenol and found some compounds with better activities in a pharmacological screening. Next, we will study the semisynthesis of kirenol to explore a reasonable synthetic route. And we will conduct the pharmacology study for systemic lupus erythematosus disease. So that we can develop the theory and application foundation for the new drug to treat systemic lupus erythematosus disease. It is an important way to find the qualified clinical candidates from the lead compound which was isolated from traditional Chinese medicine with good clinical basis.
