School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China.
Molecules. 2018 Feb 26;23(3):515. doi: 10.3390/molecules23030515.
A series of bakuchiol derivatives were synthesized and evaluated for their anti-proliferative and the inhibitory activities on SMMC7721 cell line migration using PX-478 as a positive control. The results showed (,)-4-(7-methoxy-3,7-dimethyl-3-vinyloct-1-en-1-yl)phenol () to have the best activity among the tested compounds, which included PX-478. In addition, compound showed greater inhibitory activity than that of bakuchiol in the transwell migration and invasion assays at every dose. In western blotting tests, compound showed a promising ability to downregulate the expression of HIF-1α and its associated downstream proteins MMP-2 and MMP-9. Moreover, this effect was dose-dependent and could represent a possible mechanism of action for the anticancer activity of compound .
合成了一系列补骨脂酚衍生物，并以 PX-478 为阳性对照，评估它们对 SMMC7721 细胞系增殖和迁移的抑制活性。结果表明，在所测试的化合物中，（,）-4-（7-甲氧基-3,7-二甲基-3-乙烯基辛-1-基）苯酚（）具有最佳活性，包括 PX-478。此外，化合物在每个剂量下的 Transwell 迁移和侵袭实验中显示出比补骨脂酚更强的抑制活性。在 Western blotting 试验中，化合物显示出下调 HIF-1α及其相关下游蛋白 MMP-2 和 MMP-9 表达的有希望的能力。此外，这种作用呈剂量依赖性，可能代表化合物的抗癌活性的一种可能作用机制。
