三种草本决明属植物中新颖色酮类化合物的发现及其抗病毒活性研究

Cassia genus is known as Chinese traditional herb medicines in Yunnan whose important active ingredient is chromone compounds. In our previous works, the phytochemical study of Cassia fistula was carried out, and 21 new compounds (including 8 chromone compounds) were isolated from this plant, some new compounds were found to have notable antiviral activities. Taking the herbaceous plants and trees (cassia fistula) obvious differences into account, we continue to conduct exploratory research on the cassia leschenaultiana, Preliminary separation obtained 16 new compounds (including 9 chromone compounds and new skeleton), some new compounds were found to be have notable anti-tobacco mosaic virus activities, and HPLC analysis showed that the great possibility is similar chromone derivatives exist in other herbaceous plants of the cassia genus. The project group selected the cassia leschenaultiana, cassia nomame and cassia pumila samples from cassia herbaceous plants, the chromone compounds of the samples will be carefully studied by modern separation technology, and anti-viral activeness screening shall be carried on the compounds. It is expected that more than 30 novel chromone compounds (including 2-3 compounds with new skeleton) be isolated from the samples, and 3-5 compounds with significantly antiviral activities will be selected out in order to provide scientific basis for the Yunnan ethnic medicine resources utilization and the development of new drugs. The project will choose some activity significantly compounds for antiviral mechanism and structure-activity relationship research, to understand its resistance and structure-activity relationship.

决明属植物为云南民间常用的中药材，色酮类化合物是其重要活性成分。我们前期从该属腊肠树中分离到21个新化合物，其中8个为色酮，部分化合物中有较好的抗病毒活性。考虑到草本植物和乔木(腊肠树)的明显差异，我们继续对该属草本短叶决明进行了试探性研究，初步分离就得到16个新化合物，其中色酮类化合物9个，有4个为新骨架，部分化合物具有突出的抗烟草花叶病毒活性，而且HPLC分析表明该属其它草本植物中存在同类色酮衍生物的可能性也很大。项目组进一步从该属草本植物中精选出短叶决明、豆茶决明和柄腺山扁豆三种样品，拟用现代分离技术对样品中的色酮及其抗病毒活性进行深入研究。预期从样品分离到30个以上的新颖色酮化合物，力争发现2-3个新骨架，并筛选出3-5个活性显著的化合物结构，为云南民族药资源的开发利用及新药开发提供科学依据。项目还将对部分活性显著的化合物进行抗病毒机理和构效关系的研究，了解其抗病和构效关系。

项目组紧扣计划任务书要求，用现代分离技术对样品中抗病毒活性色酮类化合物进行深入研究。共采集了3个不同产地、品种的草本决明属样品，通过植物化学分离的方法，对样品中的酚类化合物进行了分离鉴定。此外，扩展性的对烟草、紫花苜蓿、假地豆等其它植物样品的抗烟草花叶病毒活性成分进行了研究。项目组总共分离到色酮类化合物116个，包括39个新色酮类化合物，其中2个为新骨架分子；所有化合物均通过核磁共振、质谱、红外、紫外光谱等波谱技术对结构进行准确鉴定，尚有部分化学物还未进行结构解析。项目组还完成了45个化合物的抗烟草花叶病毒活性筛选，发现了8个对烟草花叶病毒抑制率显著超过对照(宁南霉素)的化合物结构，并选择活性好的化合物对其抗病毒机理进行了研究。项目成果发表论文21篇（其中SCI收录期刊发表研究论文16篇），所有发表论文均标准了基金资助号；还申请了6件发明专利，超额完成了计划任务书规定的任务。