地胆草倍半萜内酯化合物的结构修饰

Structure modification on sesquiterpene lactones from Elephantopus scaber

为寻找毒性低、活性强的化合物,对地胆草倍半萜内酯化合物进行结构修饰。本文首先从地胆草全草中分离得到去氧地胆草内酯（deoxyelephantopin）和地胆草种内酯（scabertopin）,再对这两个化合物进行氧化和氢化反应,制备不同结构修饰产物。共得到5个大环化合物,通过IR、1HNMR和MS等方法确定其结构。其中4个化合物（2~5）为新化合物,部分化合物有一定的抗肿瘤活性。

In order to look for lower toxic and strongly active compounds, the structure of sesquiterpene lactones from Elephantopus scaber was modified. Deoxyelephantopin and scabertopin were isolated from the whole plant of Elephantopus scaber and hydrogenated and epoxidated. Five sesquiterpenoide derivatives were prepared and their structures were identified by IR, NMR and MS spectra analysis. Four sesquiterpenoides are new compounds. Part of the compounds show definite antitumor activity.