Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent
Abstract With the improvement and advance in cancer diagnosis and treatment, the cancer is still a major cause of morbidity and mortality throughout the world. Obviously, new breakthroughs in therapies remain be urgent needed. In this work, we designed and synthesized the compound 1–4, namely resver...
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| Format: | Article |
| Language: | English |
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BMC
2020-02-01
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| Series: | BMC Chemistry |
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| Online Access: | http://link.springer.com/article/10.1186/s13065-020-00667-5 |
| _version_ | 1818136980427374592 |
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| author | Zhen-Hui Xin Ya-Li Meng Wen-Jing Jiang Ya-Peng Li Li-Ping Ge Cun-Hui Zhang Lian-Na Liu Yan-Fei Kang |
| author_facet | Zhen-Hui Xin Ya-Li Meng Wen-Jing Jiang Ya-Peng Li Li-Ping Ge Cun-Hui Zhang Lian-Na Liu Yan-Fei Kang |
| author_sort | Zhen-Hui Xin |
| collection | DOAJ |
| description | Abstract With the improvement and advance in cancer diagnosis and treatment, the cancer is still a major cause of morbidity and mortality throughout the world. Obviously, new breakthroughs in therapies remain be urgent needed. In this work, we designed and synthesized the compound 1–4, namely resveratrol analogues with methylation of hydroxy distyrene, to further explore its new anti-cancer potential. Encouragingly, compound 1 ((E)-4,4′-(ethene-1,2-diyl)bis(3,5-dimethylphenol)) exhibited cytotoxicity superior to resveratrol in MCF 7 cells. More importantly, the compound 1 showed greater toxicity to tumor cells than that to normal cells, which proved that it could selectively kill tumor cells. The favorable results encouraged us to explore the inhibitory mechanism of compound 1 on MCF 7 cells. The research finding indicated the compound 1 inhibited tumor cell proliferation by both arresting cell cycle in S phase and apoptosis via a prooxidant manner. In addition, the results further verified compound 1 caused cell cycle arrest in S phase and apoptosis by down-regulation of the cycling A1/cycling A2 expression and the rise of Bax/Bcl-2 ratio in a p21-dependant pathway in MCF 7 cells. Therefore, these results are helpful for the effective design of anticancer reagents and the better understanding of their mechanism of action. |
| first_indexed | 2024-12-11T09:49:01Z |
| format | Article |
| id | doaj.art-5fb5a2d88be54d1cbfee296f853ecfbf |
| institution | Directory Open Access Journal |
| issn | 2661-801X |
| language | English |
| last_indexed | 2024-12-11T09:49:01Z |
| publishDate | 2020-02-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Chemistry |
| spelling | doaj.art-5fb5a2d88be54d1cbfee296f853ecfbf2022-12-22T01:12:28ZengBMCBMC Chemistry2661-801X2020-02-0114111010.1186/s13065-020-00667-5Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agentZhen-Hui Xin0Ya-Li Meng1Wen-Jing Jiang2Ya-Peng Li3Li-Ping Ge4Cun-Hui Zhang5Lian-Na Liu6Yan-Fei Kang7Hebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityZhangbei HospitalHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North UniversityAbstract With the improvement and advance in cancer diagnosis and treatment, the cancer is still a major cause of morbidity and mortality throughout the world. Obviously, new breakthroughs in therapies remain be urgent needed. In this work, we designed and synthesized the compound 1–4, namely resveratrol analogues with methylation of hydroxy distyrene, to further explore its new anti-cancer potential. Encouragingly, compound 1 ((E)-4,4′-(ethene-1,2-diyl)bis(3,5-dimethylphenol)) exhibited cytotoxicity superior to resveratrol in MCF 7 cells. More importantly, the compound 1 showed greater toxicity to tumor cells than that to normal cells, which proved that it could selectively kill tumor cells. The favorable results encouraged us to explore the inhibitory mechanism of compound 1 on MCF 7 cells. The research finding indicated the compound 1 inhibited tumor cell proliferation by both arresting cell cycle in S phase and apoptosis via a prooxidant manner. In addition, the results further verified compound 1 caused cell cycle arrest in S phase and apoptosis by down-regulation of the cycling A1/cycling A2 expression and the rise of Bax/Bcl-2 ratio in a p21-dependant pathway in MCF 7 cells. Therefore, these results are helpful for the effective design of anticancer reagents and the better understanding of their mechanism of action.http://link.springer.com/article/10.1186/s13065-020-00667-5ResveratrolCell apoptosisCell cycle arrestROS |
| spellingShingle | Zhen-Hui Xin Ya-Li Meng Wen-Jing Jiang Ya-Peng Li Li-Ping Ge Cun-Hui Zhang Lian-Na Liu Yan-Fei Kang Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent BMC Chemistry Resveratrol Cell apoptosis Cell cycle arrest ROS |
| title | Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent |
| title_full | Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent |
| title_fullStr | Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent |
| title_full_unstemmed | Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent |
| title_short | Finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent |
| title_sort | finding an efficient tetramethylated hydroxydiethylene of resveratrol analogue for potential anticancer agent |
| topic | Resveratrol Cell apoptosis Cell cycle arrest ROS |
| url | http://link.springer.com/article/10.1186/s13065-020-00667-5 |
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