Li Xianfeng, Ai Hongyan, Sun Deke, Wu Tao, He Jian, Xu Zhai, Ding Li, Wang Ling
Neurosurgery Ward 2, Linyi City Yishui Central Hospital, Linyi, Shandong 276400, P.R. China.
Department of Neurological Surgery Unit 1, The First Affiliated Hospital of Liaoning Medical University, Jinzhou, Liaoning 121001, P.R. China.
Oncol Lett. 2016 Nov;12(5):3373-3377. doi: 10.3892/ol.2016.5094. Epub 2016 Sep 5.
The aim of the study was to investigate the anti-tumoral activity of morelloflavone substances with different structures. We also studied the possible link between morelloflavone structure and its function. Various types of chromatographic techniques were used to isolate and screen morelloflavone substances from the extracts of gambogic tree trunk and the morelloflavone structures were identified by analytical techniques such as high resolution mass spectrometry and nuclear magnetism. Anti-tumoral activities of different compounds were investigated and the link between the antitumor activity and the structure of compound was exaimed. Our results showed that the isolated morelloflavone substances demonstrated a certain level of antitumor activity. The compound no. 1 had the strongest effect to inhibit glioma U87 and C6 cells followed by compound no. 2 while compound no. 5 was the weakest among them. We conducted a preliminary analysis on the structure-function relationship through the structure comparison and we concluded that the antitumor effects of morelloflavone substances with different structures were significantly different from each other. Thus, the glucose chain in C4 position of biflavone structure can enhance the antitumor activity of the compound in glioma cells. Additionally, the formation of intramolecular hydrogen bonds in biflavone compounds may also play a role in enhancing the antitumor activity and inhibition rate.
本研究的目的是探究不同结构的藤黄双黄酮类物质的抗肿瘤活性。我们还研究了藤黄双黄酮结构与其功能之间可能存在的联系。采用了各种色谱技术从藤黄树干提取物中分离和筛选藤黄双黄酮类物质，并通过高分辨率质谱和核磁共振等分析技术鉴定藤黄双黄酮的结构。研究了不同化合物的抗肿瘤活性，并考察了抗肿瘤活性与化合物结构之间的联系。我们的结果表明，分离得到的藤黄双黄酮类物质表现出一定程度的抗肿瘤活性。化合物1对胶质瘤U87和C6细胞的抑制作用最强，其次是化合物2，而化合物5的作用最弱。我们通过结构比较对结构 - 功能关系进行了初步分析，得出结论：不同结构的藤黄双黄酮类物质的抗肿瘤作用存在显著差异。因此，双黄酮结构中C4位的葡萄糖链可增强化合物在胶质瘤细胞中的抗肿瘤活性。此外，双黄酮化合物中分子内氢键的形成可能也在增强抗肿瘤活性和抑制率方面发挥作用。
