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

本研究的结果如下：1。从kansui中分离得到的化合物：通过生物测定法分离得到21种含10个新化合物的ingenol型二萜，5种含3个新化合物的麻风烷型二萜，7种含5个新化合物的euphane/tirucallane型三萜，5种甾体，1种香豆素，1种脂肪酸，共38种化合物。在上述化合物中，Ingenol型二萜表现出最强的细胞分裂抑制活性。此外，这些化合物还能控制细胞分裂，使细胞存活。由于烯烷型二萜选择性抑制癌细胞（MMT， LC540和3T3）的生长。20- 0- （2&cent； E, 4&cent； z -十二烯基）ingenol。(2)对正常细胞3T3细胞无抑制作用，但对乳腺癌细胞mmt有替代抑制控制作用。Ingenol型二萜3-O-（2,3 -二甲基丁醇）-13- o -十二烷基Ingenol（20）对Jurkat和HSC-2细胞有明显的细胞生长抑制活性。结果提示20种主要诱导HSC-2细胞早期凋亡5。综上所述，kansui中的ingenol型二萜可诱导部分癌细胞早期凋亡并抑制细胞分裂。认为这些生物活性成分极有可能成为具有新的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.