Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest
Resveratrol has been extensively studied as the anti-cancer agent. A variety of resveratrol analogues have been developed with structural modification to improve its bioactivity. In this work, resveratrol analogues, compound 1-4, were designed and synthesized with the Stille–Heck reaction. These res...
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2020-07-01
|
| Series: | Journal of Pharmacological Sciences |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1347861320300347 |
| _version_ | 1817986971756134400 |
|---|---|
| author | Zhen-Hui Xin Hui-Hui Yang Yu-Han Gan Ya-Li Meng Ya-Peng Li Li-Ping Ge Cun-Hui Zhang Lian-Na Liu Yan-Fei Kang |
| author_facet | Zhen-Hui Xin Hui-Hui Yang Yu-Han Gan Ya-Li Meng Ya-Peng Li Li-Ping Ge Cun-Hui Zhang Lian-Na Liu Yan-Fei Kang |
| author_sort | Zhen-Hui Xin |
| collection | DOAJ |
| description | Resveratrol has been extensively studied as the anti-cancer agent. A variety of resveratrol analogues have been developed with structural modification to improve its bioactivity. In this work, resveratrol analogues, compound 1-4, were designed and synthesized with the Stille–Heck reaction. These results showed compound 1–4 had better anticancer effect than that of parent resveratrol. Especially compound 1 ((E)-4,4′-(ethene-1,2-diyl)bis(3-methylphenol)) displayed the excellent cytotoxicity and high selectivity. The mechanism research indicated compound 1 inhibited cell proliferation by binary paths of cell cycle arrest in S phase regulated by cyclin A1/A2 and apoptosis induction mediated by Bax/Bcl2 in a prooxidant manner. |
| first_indexed | 2024-04-14T00:16:04Z |
| format | Article |
| id | doaj.art-5d8058b6ef0a4b3dbed0cac96d984305 |
| institution | Directory Open Access Journal |
| issn | 1347-8613 |
| language | English |
| last_indexed | 2024-04-14T00:16:04Z |
| publishDate | 2020-07-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Pharmacological Sciences |
| spelling | doaj.art-5d8058b6ef0a4b3dbed0cac96d9843052022-12-22T02:23:08ZengElsevierJournal of Pharmacological Sciences1347-86132020-07-011433238241Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrestZhen-Hui Xin0Hui-Hui Yang1Yu-Han Gan2Ya-Li Meng3Ya-Peng Li4Li-Ping Ge5Cun-Hui Zhang6Lian-Na Liu7Yan-Fei Kang8Hebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaZhangbei Hospital, Guangchang Alley, Garden Street, Zhangbei Country, Zhangjiakou, 076450, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of ChinaHebei Key Laboratory of Quality & Safety Analysis-Testing for Agro-Products and Food and College of Laboratory Medicine, Hebei North University, 11 Diamond Street South, Zhangjiakou, 075000, Hebei, People's Republic of China; Corresponding author. Fax: +86 313 4029275.Resveratrol has been extensively studied as the anti-cancer agent. A variety of resveratrol analogues have been developed with structural modification to improve its bioactivity. In this work, resveratrol analogues, compound 1-4, were designed and synthesized with the Stille–Heck reaction. These results showed compound 1–4 had better anticancer effect than that of parent resveratrol. Especially compound 1 ((E)-4,4′-(ethene-1,2-diyl)bis(3-methylphenol)) displayed the excellent cytotoxicity and high selectivity. The mechanism research indicated compound 1 inhibited cell proliferation by binary paths of cell cycle arrest in S phase regulated by cyclin A1/A2 and apoptosis induction mediated by Bax/Bcl2 in a prooxidant manner.http://www.sciencedirect.com/science/article/pii/S1347861320300347ResveratrolCell apoptosisCell cycle arrest |
| spellingShingle | Zhen-Hui Xin Hui-Hui Yang Yu-Han Gan Ya-Li Meng Ya-Peng Li Li-Ping Ge Cun-Hui Zhang Lian-Na Liu Yan-Fei Kang Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest Journal of Pharmacological Sciences Resveratrol Cell apoptosis Cell cycle arrest |
| title | Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest |
| title_full | Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest |
| title_fullStr | Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest |
| title_full_unstemmed | Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest |
| title_short | Finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest |
| title_sort | finding a resveratrol analogue as potential anticancer agent with apoptosis and cycle arrest |
| topic | Resveratrol Cell apoptosis Cell cycle arrest |
| url | http://www.sciencedirect.com/science/article/pii/S1347861320300347 |
| work_keys_str_mv | AT zhenhuixin findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT huihuiyang findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT yuhangan findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT yalimeng findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT yapengli findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT lipingge findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT cunhuizhang findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT liannaliu findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest AT yanfeikang findingaresveratrolanalogueaspotentialanticanceragentwithapoptosisandcyclearrest |