生物活性 | |||
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描述 | Salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, both targets on human cancer stem cells and works as an an antibacterial and coccidiostat compound[1][2]. Salinomycin exhibited selective toxicity for mesenchymally transdifferentiated epithelial cells. Salinomycin reduced the proportion of CSCs by >100-fold relative to paclitaxel. Pretreatment with salinomycin resulted in a >100-fold decrease in tumor-seeding ability relative to paclitaxel pre-treatment for both the HMLER and 4T1 cancer lines. Daily intraperitoneal administration of 5mg/kg salinomycin delayed palpable tumor formation by 2 weeks in mice xenograft SUM159 cells, with increased necrosis and apoptosis, and focally expressed E-cadherin protein observed[1]. The killing CSCs activity of salinomycin is most likely by interfering with ABC drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways[2]. The role of salinomycin involving in autophagy may also account for its anticancer effects[3]. | ||
作用机制 | The effect of salinomycin on ABC drug transporters, the Wnt/β-catenin signaling pathway, and other CSC pathways, as well as autophagy, may contribute to the anticancer effects of salinomycin.[1][2][3] |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
BALB/3T3 cells | Cytotoxicity assay | 72 h | Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50=28.08 μM | 23079523 | |
HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.29 μM | 25644674 | |
HL60/Vinc cells | Cytotoxicity assay | 72 h | Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50=3.44 μM | 23079523 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.33mL 0.27mL 0.13mL |
6.66mL 1.33mL 0.67mL |
13.32mL 2.66mL 1.33mL |
参考文献 |
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