A Novel Bufalin Derivative Exhibited Stronger Apoptosis-Inducing Effect than Bufalin in A549 Lung Cancer Cells and Lower Acute Toxicity in Mice
文献类型：期刊论文
| 作者 | Liu, Miao; Feng, Li-Xing; Sun, Peng; Liu, Wang; Wu, Wan-Ying ; Jiang, Bao-Hong; Yang, Min; Hu, Li-Hong; Guo, De-An; Liu, Xuan
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| 刊名 | PLOS ONE
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| 出版日期 | 2016-07-26 |
| 卷号 | 11期号:7 |
| ISSN号 | 1932-6203 |
| DOI | 10.1371/journal.pone.0159789 |
| 文献子类 | Article |
| 英文摘要 | BF211 is a synthetic molecule derived from bufalin (BF). The apoptosis-inducing effect of BF211 was stronger than that of BF while the acute toxicity of BF211 was much lower than that of BF. BF211 exhibited promising concentration-dependent anti-cancer effects in nude mice inoculated with A549 cells in vivo. The growth of A549 tumor xenografts was almost totally blocked by treatment with BF211 at 6 mg/kg. Notably, BF and BF211 exhibited differences in their binding affinity and kinetics to recombinant proteins of the a subunits of Na +/K+-ATPase. Furthermore, there was a difference in the effects of BF or BF211 on inhibiting the activity of porcine cortex Na+/K+-ATPase and in their time-dependent effects on intracellular Ca2+ levels in A549 cells. The time-dependent effects of BF or BF211 on the activation of Src, which was mediated by the Na+/K+-ATPase signalosome, in A549 cells were also different. Both BF and BF211 could induce apoptosis-related cascades, such as activation of caspase-3 and the cleavage of PARP (poly ADP-ribose polymerase) in A549 cells, in a concentration-dependent manner; however, the effects of BF211 on apoptosis-related cascades was stronger than that of BF. The results of the present study supported the importance of binding to the Na+/K+-ATPase a subunits in the mechanism of cardiac steroids and also suggested the possibility of developing new cardiac steroids with a stronger anti-cancer activity and lower toxicity as new anti-cancer agents. |
| WOS关键词 | NA+/K+-ATPASE ; HEPATOCELLULAR-CARCINOMA ; CARDIOTONIC STEROIDS ; CARDIAC-GLYCOSIDES ; PANCREATIC-CANCER ; CYCLE ARREST ; DNA-DAMAGE ; K+-ATPASE ; IN-VITRO ; THERAPY |
| 资助项目 | Shanghai Science & Technology Support Program[13431900401] ; Shanghai Science & Technology Innovation Action Program[15140904800] ; National Nature Science Foundation of China[81373964] ; National Science & Technology Major Project of China[2014ZX09301-306-03] |
| WOS研究方向 | Science & Technology - Other Topics |
| 语种 | 英语 |
| 出版者 | PUBLIC LIBRARY SCIENCE |
| WOS记录号 | WOS:000381515600048 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275949]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Hu, Li-Hong; Guo, De-An; Liu, Xuan |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Miao,Feng, Li-Xing,Sun, Peng,et al. A Novel Bufalin Derivative Exhibited Stronger Apoptosis-Inducing Effect than Bufalin in A549 Lung Cancer Cells and Lower Acute Toxicity in Mice[J]. PLOS ONE,2016,11(7). |
| APA | Liu, Miao.,Feng, Li-Xing.,Sun, Peng.,Liu, Wang.,Wu, Wan-Ying.,...&Liu, Xuan.(2016).A Novel Bufalin Derivative Exhibited Stronger Apoptosis-Inducing Effect than Bufalin in A549 Lung Cancer Cells and Lower Acute Toxicity in Mice.PLOS ONE,11(7). |
| MLA | Liu, Miao,et al."A Novel Bufalin Derivative Exhibited Stronger Apoptosis-Inducing Effect than Bufalin in A549 Lung Cancer Cells and Lower Acute Toxicity in Mice".PLOS ONE 11.7(2016). |
入库方式： OAI收割
来源：上海药物研究所
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