School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China.
Key Laboratory of Natural Medicines of the Changbai Mountain, College of Pharmacy, Yanbian University, Ministry of Education, 977 Gongyuan Road, Yanji 133002, China.
Molecules. 2021 Jul 15;26(14):4302. doi: 10.3390/molecules26144302.
Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound exhibited the best cytotoxic activity against four human cancer cell lines, with IC values ranging from 20.43 to 28.27 μM. Wound-healing and transwell assays showed that compound significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of , demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents.
厚朴酚（MAG）是一种双酚新木脂素，具有多种生物活性，包括抗肿瘤作用。在这项研究中，半合成了 15 种 MAG 衍生物，并评估了它们的体外抗癌活性。在这些衍生物中，化合物 对四种人癌细胞系表现出最好的细胞毒性活性，IC 值范围为 20.43 至 28.27 μM。划痕愈合和 Transwell 分析表明，化合物 显著抑制 MDA-MB-231 细胞的迁移和侵袭。此外，用不同浓度的 进行 Western blot 实验表明，它以浓度依赖的方式下调 HIF-1α、MMP-2 和 MMP-9 的表达。总的来说，这些结果表明，在 MAG 衍生物的结构优化中，用苯甲基取代具有在 C2 位被 F 原子取代的苄基是一种可行的策略。
