Bufalin, a component in Chansu, inhibits proliferation and invasion of hepatocellular carcinoma cells.
Bufalin, a component in Chansu, inhibits proliferation and invasion of hepatocellular carcinoma cells.
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蟾酥成分蟾蜍灵抑制肝癌细胞增殖和侵袭
DOI：
10.1186/1472-6882-13-185
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发表时间：
2013-07-19
影响因子：
--
通讯作者：
Yang YK
中科院分区：
文献类型：
--
作者：
Qiu DZ;Zhang ZJ;Wu WZ;Yang YK
背景肝细胞癌是一种常见的侵袭性癌症，晚期肝细胞癌患者的治疗选择有限。蟾酥是中药蝉苏中主要的地高辛样成分，在许多肿瘤细胞系中显示出显著的抗肿瘤活性。在本研究中，我们研究了蟾酥对AKT相关信号通路的抑制作用，并探讨了调控蛋白与肝癌细胞抗肿瘤作用的关系。方法对人肝癌细胞株HCCLM3和HepG2进行增殖、伤口愈合、跨孔迁移/侵袭和黏附实验。免疫印迹法检测PACT、AKT、pGSK3β、GSK3β、pβ-连环蛋白、β-连环蛋白、E-钙粘蛋白、基质金属蛋白酶-9和基质金属蛋白酶-2的蛋白表达水平。免疫荧光法检测E-钙粘连蛋白和β-连环蛋白的表达。结果蟾酥能抑制肝癌细胞的增殖、迁移、侵袭和黏附。此外，蟾酥能显著降低肝细胞癌组织中PAKT、pGSK3β、MMP9和MMP2的水平，增加GSK3β和E-钙粘蛋白的表达，抑制β-连环蛋白的核转位。结论蟾酥能抑制AKT/GSK3β/β-连环蛋白/E-钙粘蛋白信号通路，是一种潜在的抗肝癌药物。对肝细胞癌患者，特别是晚期患者，有必要对蟾酥进行进一步的研究。
BackgroundHepatocellular carcinoma (HCC) is a common and aggressive cancer, and the treatment options are limited for patients with advanced HCC. Bufalin, the major digoxin-like component of the traditional Chinese medicine Chansu, exhibits significant anti-tumor activities in many tumor cell lines. In the present study, we investigated the effect of bufalin on the inhibition of an AKT-related signaling pathway, and examined the relationship between regulatory proteins and anti-tumor effects in hepatoma cells.MethodsProliferation, wound healing, transwell-migration/invasion and adhesion assays were performed in HCCLM3 and HepG2 cell lines. The protein levels of pAKT, AKT, pGSK3β, GSK3β, pβ-catenin, β-catenin, E-cadherin, MMP-9, and MMP-2 were measured by western blot analysis. E-Cadherin and β-catenin expression levels were also evaluated by immunofluorescence.ResultsBufalin inhibited hepatoma cell proliferation, migration, invasion and adhesion. In addition, treatment with bufalin significantly decreased the levels of pAKT, pGSK3β, MMP-9, and MMP-2, while increasing the levels of GSK3β and E-cadherin and suppressing the nuclear translocation of β-catenin.ConclusionsBufalin is a potential anti-HCC therapeutic candidate through its inhibition of the AKT/GSK3β/β-catenin/E-cadherin signaling pathway. Further studies with bufalin are warranted in patients with HCC, especially those with the disease at advanced stages.
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影响因子：
6.2
作者：
Meng, Zhiqiang;Yang, Peiying;Shen, Yehua;Bei, Wenying;Zhang, Ying;Ge, Yongqian;Newman, Robert A.;Cohen, Lorenzo;Liu, Luming;Thornton, Bob;Chang, David Z.;Liao, Zongxing;Kurzrock, Razelle
通讯作者：
Kurzrock, Razelle
影响因子：
11.2
作者：
Baryawno, Ninib;Sveinbjornsson, Baldur;Johnsen, John Inge
通讯作者：
Johnsen, John Inge
影响因子：
2.9
作者：
Newman, Robert A.;Kondo, Yasuko;Yang, Peiying
通讯作者：
Yang, Peiying
PI3K/Akt 参与蟾蜍灵诱导的胃癌细胞凋亡
影响因子：
2.3
作者：
Li, Dan;Qu, Xiujuan;Liu, Yunpeng
通讯作者：
Liu, Yunpeng
影响因子：
4.3
作者：
Qin, Tian-Jie;Zhao, Xin-Han;Pan, Bo-Rong
通讯作者：
Pan, Bo-Rong