Yiwu Central Hospital, Yiwu, Jinhua, Zhejiang, China.
Phytomedicine. 2012 May 15;19(7):603-8. doi: 10.1016/j.phymed.2012.01.003. Epub 2012 Feb 18.
Ardipusilloside I is a triterpene-saponin isolated from the Traditional Chinese Medicine Ardisia pusilla A. DC. Its effects and mechanism on invasion and metastasis of liver cancer cells are unclear.
The human hepatocellular carcinoma cell line HepG2 and SMMC-7721 cells were treated with different doses of Ardipusilloside I. Cellular survival, in vitro migration and invasion were evaluated. In vivo metastatic abilities of the HCC cells were detected. We further investigated expression and phosphorylation of Mek, Erk and Akt by using Western blot. MMP2 and MMP9 activities were evaluated by gelatin zymography. E-cadherin expression, Rac1 and Cdc42 activities were examined by Western blot and pull-down assay.
Ardipusilloside I inhibited invasion and metastasis of HCC cells both in vitro and in vivo by reducing the protein expressions of metalloproteinase (MMP)-9 and MMP2 proteins. Ardipusilloside I activated Rac1 that enhanced E-cadherin activity and resulted in significantly less metastasis.
Our findings indicate that Ardipusilloside I has the potential of inhibition of liver cancer survival, invasion and metastasis both in vitro and in vivo.
Ardipusilloside I 是从传统中药 Ardisia pusilla A. DC 中分离得到的一种三萜皂苷。其对肝癌细胞侵袭转移的作用及其机制尚不清楚。
用不同剂量的 Ardipusilloside I 处理人肝癌细胞系 HepG2 和 SMMC-7721 细胞。评估细胞存活率、体外迁移和侵袭能力。检测 HCC 细胞的体内转移能力。我们进一步通过 Western blot 检测 Mek、Erk 和 Akt 的表达和磷酸化。通过明胶酶谱法评估 MMP2 和 MMP9 的活性。通过 Western blot 和下拉试验检测 E-钙黏蛋白表达、Rac1 和 Cdc42 活性。
Ardipusilloside I 通过降低金属蛋白酶（MMP）-9 和 MMP2 蛋白的表达，在体内外均抑制 HCC 细胞的侵袭和转移。Ardipusilloside I 激活 Rac1，增强 E-钙黏蛋白活性，从而显著减少转移。
我们的研究结果表明，Ardipusilloside I 具有抑制肝癌细胞在体内外生存、侵袭和转移的潜力。
