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Molecules. 2018 Feb 26;23(3). pii: E515. doi: 10.3390/molecules23030515.

Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents.

Author information

1
School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China. dcliu1226@outlook.com.
2
School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China. guoxing7010@163.com.
3
School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China. daiyiqun25@126.com.
4
School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China. matao1992@foxmail.com.
5
School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China. athongmei@foxmail.com.
6
School of Pharmacy, Bengbu Medical College, 2600 Donghai Road, Bengbu 233030, China. huoqiang3@sohu.com.

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 (S,E)-4-(7-methoxy-3,7-dimethyl-3-vinyloct-1-en-1-yl)phenol (10) to have the best activity among the tested compounds, which included PX-478. In addition, compound 10 showed greater inhibitory activity than that of bakuchiol in the transwell migration and invasion assays at every dose. In western blotting tests, compound 10 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 10.

KEYWORDS:

bakuchiol derivatives; cytotoxicity; invasion; migration; semi-synthesis

PMID:
29495380
PMCID:
PMC6017251
DOI:
10.3390/molecules23030515
[Indexed for MEDLINE]
Free PMC Article

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