生物活性 | |||
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描述 | Crotonoside is isolated from Chinese medicinal herb, Croton and inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. In vivo, crotonoside treatment at 70 and 35 mg/kg/d produced significant AML tumor inhibition rates of 93.5% and 73.6%, respectively. Crotonoside (0 - 200 μM) selectively inhibits the viability of AML cell line MV4-11, MOLM-13 (with FLT3-ITD mutant) and KG-1 (without FLT3-ITD mutant) in a dose-dependent manner with an IC50 of 11.6 μM, 12.7 μM and 17.2 μM, respectively. Crotonoside (0 – 100 μM; 7 hours) inhibits the phosphorylation of FLT3. Erk1/2, Akt/mTOR and STAT5 is strongly inhibited by crotonoside at higher concentration of 12.5 μM in a concentration-dependent manner. Crotonoside (0 - 100 μM; 12 hours) exhibits a dose-dependent increase in the percentage of G0/G1 phase and a dose-dependent decrease in the percentage of G2/M and S phases cells[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.53mL 0.71mL 0.35mL |
17.65mL 3.53mL 1.77mL |
35.31mL 7.06mL 3.53mL |
参考文献 |
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