生物活性 | |||
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描述 | Pyrvinium Pamoate (PP), an anthelmintic drug, inhibited proliferation of different subtypes of breast cancer cells (luminal: MCF-7, claudin-low: MDA-MB-231, basal-like: MDA-MB-468 and Her-2 enriched: SkBr-3) as a novel WNT pathway inhibitor. In the xenograft model, Pyrvinium pamoate (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased. Besides, the metastatic potential and expression of EMT markers (such as N-cadherin, vimentin, Snail) were also found suppressed by PP[1]. PP blocked colon cancer cell growth in vitro in a dose-dependent manner with great differences in the inhibitory concentration (IC50), ranging from 0.6 × 10-6 to 65 × 10-6 M for colon cancer cells with mutations in WNT signaling. In addition, PP demonstrated a cytotoxic effect on primary colon cancer samples[2]. Pyrvinium pamoate imposes specific toxicity on cardiac fibroblasts in ischemia (IC50=9.5 nM). The cytotoxic effect of Pyrvinium pamoate on cardiac fibroblasts specifically under glucose- and glutamine-deficient condition[3]. Pyrvinium pamoate remarkably inhibited cell viability and colony formation ability. Treatment with pyrvinium pamoate induced intrinsic pathway-dependent apoptosis accompanied with a decline of anti-apoptotic XIAP and Survivin, and an overt increase of pro-apoptotic Bax. In addition, pyrvinium pamoate significantly inhibited the migration and invasion in vitro[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.87mL 0.17mL 0.09mL |
4.34mL 0.87mL 0.43mL |
8.69mL 1.74mL 0.87mL |
参考文献 |
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