Gamabufotalin, a bufadienolide compound from toad venom, suppresses COX-2 expression through targeting IKKβ/NF-κB signaling pathway in lung cancer cells
文献类型：期刊论文
| 作者 | Liu,Quentin1,2; Yu,Zhenlong2; Guo,Wei2; Ma,Xiaochi2; Zhang,Baojing2; Dong,Peipei2; Huang,Lin2; Wang,Xiuli2; Wang,Chao2; Huo,Xiaokui2 |
| 刊名 | Molecular Cancer
 |
| 出版日期 | 2014-08-31 |
| 卷号 | 13期号:1 |
| 关键词 | Gamabufotalin NSCLC COX-2 NF-κB p300 IKKβ |
| ISSN号 | 1476-4598 |
| DOI | 10.1186/1476-4598-13-203 |
| 通讯作者 | Ma,Xiaochi(maxc1978@163.com) ; Deng,Wuguo(dengwg@sysucc.org.cn) |
| 英文摘要 | AbstractBackgroundGamabufotalin (CS-6), a major bufadienolide of Chansu, has been used for cancer therapy due to its desirable metabolic stability and less adverse effect. However, the underlying mechanism of CS-6 involved in anti-tumor activity remains poorly understood.MethodsThe biological functions of gamabufotalin (CS-6) were investigated by migration, colony formation and apoptosis assays in NSCLC cells. The nuclear localization and interaction between transcriptional co-activator p300 and NF-κB p50/p65 and their binding to COX-2 promoter were analyzed after treatment with CS-6. Molecular docking study was used to simulate the interaction of CS-6 with IKKβ. The in vivo anti-tumor efficacy of CS-6 was also analyzed in xenografts nude mice. Western blot was used to detect the protein expression level.ResultsGamabufotalin (CS-6) strongly suppressed COX-2 expression by inhibiting the phosphorylation of IKKβ via targeting the ATP-binding site, thereby abrogating NF-κB binding and p300 recruitment to COX-2 promoter. In addition, CS-6 induced apoptosis by activating the cytochrome c and caspase-dependent apoptotic pathway. Moreover, CS-6 markedly down-regulated the protein levels of COX-2 and phosphorylated p65 NF-κB in tumor tissues of the xenograft mice, and inhibited tumor weight and size.ConclusionsOur study provides pharmacological evidence that CS-6 exhibits potential use in the treatment of COX-2-mediated diseases such as lung cancer. |
| 语种 | 英语 |
| WOS记录号 | BMC:10.1186/1476-4598-13-203 |
| 出版者 | BioMed Central |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/167102]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 通讯作者 | Ma,Xiaochi; Deng,Wuguo |
| 作者单位 | 1.Collaborative Innovation Canter of Cancer Medicine; Sun Yat-sen University Cancer Center; State Key Laboratory of Oncology in South China 2.Dalian Medical University; Institute of Cancer Stem Cell; College of Pharmacy |
| 推荐引用方式 GB/T 7714 | Liu,Quentin,Yu,Zhenlong,Guo,Wei,et al. Gamabufotalin, a bufadienolide compound from toad venom, suppresses COX-2 expression through targeting IKKβ/NF-κB signaling pathway in lung cancer cells[J]. Molecular Cancer,2014,13(1). |
| APA | Liu,Quentin.,Yu,Zhenlong.,Guo,Wei.,Ma,Xiaochi.,Zhang,Baojing.,...&Deng,Wuguo.(2014).Gamabufotalin, a bufadienolide compound from toad venom, suppresses COX-2 expression through targeting IKKβ/NF-κB signaling pathway in lung cancer cells.Molecular Cancer,13(1). |
| MLA | Liu,Quentin,et al."Gamabufotalin, a bufadienolide compound from toad venom, suppresses COX-2 expression through targeting IKKβ/NF-κB signaling pathway in lung cancer cells".Molecular Cancer 13.1(2014). |
入库方式： OAI收割
来源：大连化学物理研究所
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