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Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents
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 activit...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017251/ https://www.ncbi.nlm.nih.gov/pubmed/29495380 http://dx.doi.org/10.3390/molecules23030515 |
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author | Wu, Cheng-Zhu Liu, Da-Chuan Guo, Xing Dai, Yiqun Ma, Tao Li, Hong-Mei Huo, Qiang |
author_facet | Wu, Cheng-Zhu Liu, Da-Chuan Guo, Xing Dai, Yiqun Ma, Tao Li, Hong-Mei Huo, Qiang |
author_sort | Wu, Cheng-Zhu |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-6017251 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-60172512018-11-13 Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents Wu, Cheng-Zhu Liu, Da-Chuan Guo, Xing Dai, Yiqun Ma, Tao Li, Hong-Mei Huo, Qiang Molecules Article 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. MDPI 2018-02-23 /pmc/articles/PMC6017251/ /pubmed/29495380 http://dx.doi.org/10.3390/molecules23030515 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Wu, Cheng-Zhu Liu, Da-Chuan Guo, Xing Dai, Yiqun Ma, Tao Li, Hong-Mei Huo, Qiang Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents |
title | Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents |
title_full | Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents |
title_fullStr | Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents |
title_full_unstemmed | Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents |
title_short | Synthesis and Evaluation of Bakuchiol Derivatives as Potential Anticancer Agents |
title_sort | synthesis and evaluation of bakuchiol derivatives as potential anticancer agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017251/ https://www.ncbi.nlm.nih.gov/pubmed/29495380 http://dx.doi.org/10.3390/molecules23030515 |
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