首次在国内系统开展了长尾粗叶木抗类风湿性关节炎药效物质、主要活性单体的作用机理及构效关系的研究，为阐明长尾粗叶木的药效物质，新药研制，合理利用药用资源及更加完整地评价药材质量奠定了坚实基础。本项目在以下方面进行了重点研究：（1）在前期课题研究基础上，继续对长尾粗叶木进行了深入的化学成分研究。分离得到7 个化合物，鉴定了其中5 个化合物，分别是长尾粗叶木素（Ⅰ）、长尾粗叶木内酯B（Ⅱ）、鸡屎藤苷（Ⅲ）、羽扇豆酮（Ⅳ）和蔗糖（Ⅴ）。其中Ⅰ和Ⅱ是新化合物，羽扇豆酮首次从莤草科植物中分得，所有化合物均是首次从该植物中分得。（2）研究了抗RA作用3个主要活性单体- - -车叶草苷、车叶草酸和去乙酰车叶草酸的抗炎活性及作用机理，研究表明3个化合物毒性较小，车叶草苷显示抗炎活性，其抗炎作用机理可能是对脂多糖诱导的小鼠腹腔巨噬细胞生成NO及iNOS蛋白表达有显著抑制作用，且对瞬时转染的NF-KB通路有显著抑制作用。（3）采用支持向量机，研究了车叶草苷、车叶草酸和去乙酰车叶草酸抗炎活性，结果表明3个化合物是Caspase-1抑制剂，是较好抗炎药物。（4）以活性单体车叶草苷为定量指标，建立了药材质量评价方法。

In this project, the systematical investigation on the bioactive constituents, main compounds' mechanisms and a realationship between structure and activity for the treatment of rheumatoid arthritis from Lasianthus acuminatissimus Merr. had been done for the first time. The results provide a solid support to elucidate the effective compounds, develop a new medicine, make a reasonable usage as well as more completely valuate the plant.Several objectives were focused on: First, the project had a deep and systematic study on the constituents of the plant on the base before.By the means of morden scientific and technological methods, seven compounds had been isolated, and five compounds had been identified by the means of spectra data and chemical properties, which were: lasianthurin（Ⅰ）, lasianthuoactone B（Ⅱ）, lupeone（Ⅲ）, scandoside （Ⅳ）and surcose（Ⅴ）. Among them, compound Ⅰ and Ⅱ are novel ones, lupeone is isolated from the Rubiacea for the first time, all the compounds were separated from the plant for the first time, the other two compounds' structural identification are doing now. Second, the project aimed to elucidate the biological activities and action mechanisms of the main constituents from the plant for treating rheumatoid arthritis, including asperuloside, asperulosidic acid and deacetyl asperulosidic acid. The results showed that their toxin effect were low, asperuloside had a significant anti-inflammation activity, which action mechanisms were inhibition of inducible nitric oxide synthase in lipopolysaccharide-stimulated Peritoneal macrophagesas well as down-regulation of mitogenactivated protein kinase-mediated nuclear factor-κB sign-aling. Third, by the means of support vector machine, the project focused on the realationship between the iridiod's structure and target of inflammation action, the results showed that three compounds had an inhibitory effect on Caspase-1, which showed maybe they are good medicines for anti-inflammation. Forth, the project studied on the establishment of a scientific quantitative quality standard of asperuloside on the base of new HPLC/PAD analytical method for the purpose of evaluating the plant successfully, the quantification of asperuloside in alcohol extract of Lasianthus from three different areas as well as different roots and stems were done, the results provided a scientific foundation to evaluate the plant's quality.

首次在国内系统开展了长尾粗叶木抗类风湿性关节炎药效物质、主要活性单体的作用机理及构效关系的研究，为阐明长尾粗叶木的药效物质，新药研制，合理利用药用资源及更加完整地评价药材质量奠定了坚实基础。本项目在以下方面进行了重点研究：（1）在前期课题研究基础上，继续对长尾粗叶木进行了深入的化学成分研究。分离得到7 个化合物，鉴定了其中5 个化合物，分别是长尾粗叶木素（Ⅰ）、长尾粗叶木内酯B（Ⅱ）、鸡屎藤苷（Ⅲ）、羽扇豆酮（Ⅳ）和蔗糖（Ⅴ）。其中Ⅰ和Ⅱ是新化合物，羽扇豆酮首次从莤草科植物中分得，所有化合物均是首次从该植物中分得。（2）研究了抗RA作用3个主要活性单体- - -车叶草苷、车叶草酸和去乙酰车叶草酸的抗炎活性及作用机理，研究表明3个化合物毒性较小，车叶草苷显示抗炎活性，其抗炎作用机理可能是对脂多糖诱导的小鼠腹腔巨噬细胞生成NO及iNOS蛋白表达有显著抑制作用，且对瞬时转染的NF-KB通路有显著抑制作用。（3）采用支持向量机，研究了车叶草苷、车叶草酸和去乙酰车叶草酸抗炎活性，结果表明3个化合物是Caspase-1抑制剂，是较好抗炎药物。（4）以活性单体车叶草苷为定量指标，建立了药材质量评价方法。