Synthesis and biological evaluation of matrine derivatives containing benzo-α-pyrone structure as potent anti-lung cancer agents
文献类型：期刊论文
| 作者 | Wu LC1; Wang GZ2; Li M4; Zhou GB[*]2; Wang LS[*]1; Liu SB1; Wei JR3; Zhang S1 |
| 刊名 | SCIENTIFIC REPORTS
 |
| 出版日期 | 2016 |
| 卷号 | 6期号:X页码:e35918 |
| 通讯作者 | gbzhou@ioz.ac.cn ; w_lsheng@163.com |
| 合作状况 | 其它 |
| 英文摘要 | Matrine, an active component of root extracts from Sophora flavescens Ait, is the main chemical ingredient of Fufang Kushen injection which was approved by Chinese FDA (CFDA) in 1995 as an anticancer drug to treat non-small cell lung cancer and liver cancer in combination with other anticancer drugs. Owning to its druggable potential, matrine is considered as an ideal lead compound for modification. We delineate herein the synthesis and anticancer effects of 17 matrine derivatives bearing benzo-α-pyrone structures. The results of cell viability assays indicated that most of the target compounds showed improved anticancer effects. Further studies showed that compound 5i could potently inhibit lung cancer cell proliferation in vitro and in vivo with no obvious side effects. Moreover, compound 5i could induce G1 cell cycle arrest and autophagy in lung cancer cells through up-regulating P27, down-regulating CDK4 and cyclinD1 and attenuating PI3K/Akt/mTOR pathway. Suppression of autophagy attenuated 5i induced proliferation inhibition. Collectively, our results infer that matrine derivative 5i bears therapeutic potentials for lung cancer. |
| 资助信息 | The present study was financially supported by the Natural Science Foundation of China (No. 21262005), the high level innovation team and outstanding scholar project of Guangxi institutions of higher education (gui jiao ren [2014] 49 hao), the Postdoctoral Science Foundation of Guangxi Province of China (Y304001912), the National Natural Science Funds for Distinguished Young Scholar (81425025), and Special Financial Grant from the China Postdoctoral Science Foundation (2016T90135). |
| 收录类别 | SCI |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/10617]  |
| 专题 | 昆明动物研究所_转化基因组 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.School of Chemistry and Chemical Engineering, Guangxi University, Nanning, Guangxi 530004, PR China 2.State Key Laboratory of Membrane Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing, China 3.Guangxi Scientific Research Center of Traditional Chinese Medicine, Guangxi University of Chinese Medicine, Nanning, Guangxi 530200, PR China 4.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Kunming, Yunnan, People’s Republic of China |
| 推荐引用方式 GB/T 7714 | Wu LC,Wang GZ,Li M,et al. Synthesis and biological evaluation of matrine derivatives containing benzo-α-pyrone structure as potent anti-lung cancer agents[J]. SCIENTIFIC REPORTS,2016,6(X):e35918. |
| APA | Wu LC.,Wang GZ.,Li M.,Zhou GB[*].,Wang LS[*].,...&Zhang S.(2016).Synthesis and biological evaluation of matrine derivatives containing benzo-α-pyrone structure as potent anti-lung cancer agents.SCIENTIFIC REPORTS,6(X),e35918. |
| MLA | Wu LC,et al."Synthesis and biological evaluation of matrine derivatives containing benzo-α-pyrone structure as potent anti-lung cancer agents".SCIENTIFIC REPORTS 6.X(2016):e35918. |
入库方式： OAI收割
来源：昆明动物研究所
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