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巴库醇衍生物的合成与评价及其作为潜在抗癌剂的研究。

Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents.

机构信息

School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China.

出版信息

Molecules. 2018 Feb 26;23(3):515. doi: 10.3390/molecules23030515.

Abstract

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 .

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e81/6017251/7ba81569aa7e/molecules-23-00515-sch001.jpg

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