Studies on the Components and Bioactivities of Euphorbiacea plants wbich influencing Cell Cycle and Cell Differentiation

本研究的研究结果如下。从甘遂中分离得到化合物：在生测分离的基础上，共分离鉴定出21种吲哚二萜化合物，其中包括10个新化合物，5个麻疯烷型二萜化合物，其中包括3个新化合物，7个安非他烷型三萜化合物，其中包括5个新化合物，5个甾体化合物，1个孜然糖素化合物，1个脂肪酸化合物，共38个化合物。在上述化合物中，吲哚二萜类化合物具有最强的细胞分裂抑制活性。此外，这些化合物还控制了细胞分裂和细胞存活。由于金刚烷型二萜类化合物选择性地抑制癌细胞(MMT、LC540和3T3)的生长。20-O-(2-Cent；E，4&Cent；Z-Decadienoyl)吲哚。(2)对正常细胞3T3细胞没有显示抑制控制作用，但对乳腺癌细胞MMT表现出交替抑制控制作用。吲哚醇型二萜化合物3-O-(2，3-二甲基丁酰基)-13-O-十二酰基吲哚(20)对Jurkat和HSC-2细胞具有显著的生长抑制活性。研究结果表明，20主要诱导HSC-2细胞早期凋亡。在上述结果中，甘遂中的吲哚醇型二萜类化合物诱导了一些癌细胞的早期凋亡并抑制了细胞分裂。人们认为这些生物活性成分很有可能成为一种具有新作用机制的抗癌药物。

The result in this research is as follows.1. Compound separated from kansui :On the basis of a bioassay-guided fractination, 21 sorts of ingenol type diterpenes which containing ten new compounds, five jatrophane type diterpenes which containing three new compounds, seven euphane/tirucallane type triterpenes which containing five new compounds, five steroid, one cumarin, one fatty acid, a total of 38 sorts of compounds were isolated and identified.2. Ingenol type diterpenes showed the strongest cell division inhibitory activity in the above-mentioned compounds. Moreover, these compounds controlled cell division and the cells survived.3. As a result of the selective inhibition of the growth of cancer cells (MMT, LC540, and 3T3) by ingenane-type diterpenes. 20-O-(2&cent ; E, 4&cent ; Z-decadienoyl) ingenol. (2) did not show a inhibition control to 3T3 cell which is a normal cell, but it showed the alternative inhibitory control action to the breast cancer cell MMT.4. Ingenol type diterpene 3-O-(2, 3-dimethylbutanoyl)-13-O-dodecanoylingenol (20) showed a cell growth inhibitory -activity remarkably to Jurkat and the HSC-2 cell. And the findings suggest 20 mainly induced early apoptosis in HSC-2 cells5. In the above results, ingenol type diterpene in kansui induced the early apotosis and inhibited cell division of some cancer-cells. It is thought that these bioactive components have a highly possibility to be an anti-cancer drug with a new action mechanism.