江西四种菝葜属植物中甾体皂苷的分离纯化、抗肿瘤活性及构效关系的研究

菝葜属植物中含有大量的甾体皂苷，化学结构类型丰富。该属植物分布广泛，野生资源蕴藏量大，具有较大的药用价值及开发潜力。大量文献报导表明，甾体皂苷具有抗肿瘤的活性，效果显著。课题组前期针对菝葜属中其他两种植物（菝葜和小叶菝葜）的化学成分进行了系统的研究，分离得到50多个甾体类化合物，发现了一些新型的化合物。 本研究拟通过"甾体皂苷分离- - -抗肿瘤活性筛选- - -构建抗肿瘤药效团"三个步骤，在系统分离鉴定小果菝葜、黑果菝葜、光叶菝葜和短梗菝葜的甾体皂苷成分的基础上，以抗肿瘤实验为依据，筛选抗肿瘤的有效单体化合物，并采用计算化学的方法构建抗肿瘤的药效团。 本研究将为选择新型的抗肿瘤药物研究提供先导化合物，同时也为设计活性更强的先导化合物提供重要理论基础。

The genus Smilax contains large amounts of steroidal saponins which have rich chemical structure types. This genus with high distribution rate and large reserves of wild resources have high medical value and development potential. Many investigations have revealed that steroidal saponins have significant antitumor activities. Previous systematic studies about the chemical constituents of two other plants in the genus Smilax (Smilax china and Smilax microphylla)have been carried out by our research group. More than 50 steroidal compounds have been isolated and a number of new compounds have been found. The objective of this research is to build a mode like steroidal saponins separation - antitumor activity selection - building antitumor pharmacophore. In other words, to select effective monomers of antitumor compounds and to build antitumor pharmacophore by computational chemistry based on the systematic isolation, identification and antitumor experiments about ingredients of steroidal saponins of Smilax davidiana, Smilax glaucochina, Smilax glabra and Smilax scobinicaulis is our intention. This research will provide lead compounds for selecting new antitumor drugs and important theoretical basis for designing lead compounds with higher activitives.