| 中文名称 | 异鼠李素 |
| 英文名称 | Isorhamnetin |
| CAS号 | 480-19-3 |
| 分子式 | C16H12O7 |
| 分子量 | 316.26 |
| EINECS号 | 207-545-5 |
| 熔点 | 307°C |
| 沸点 | 599.4±50.0 °C(Predicted) |
| 密度 | 1.634±0.06 g/cm3(Predicted) |
| LogP | 1.760 (est) |
| 溶解度 | DMF:10mg/mL; DMSO:20mg/mL; DMSO:PBS (pH 7.2) (1:1):0.5 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 6.31±0.40(Predicted) |
| 颜色 | 淡黄色至琥珀色至深绿色 |
| BRN | 44723 |
| 稳定性 | 吸湿性 |
| 危险品标志 | Xi,Xn |
| 危险类别码 | 36/37/38-40 |
| 安全说明 | 22-36-26-36/37 |
| WGK Germany | 3 |
| RTECS号 | LK9275450 |
| 海关编码 | 29329990 |

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PI3-K
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MEK1
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Human Endogenous Metabolite
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Isorhamnetin is a plant flavonoid that occurs in fruits and medicinal herbs. Isorhamnetin binds directly to MEK1 in an ATP-noncompetitive manner and to PI3-K in an ATP-competitive manner. In vitro and ex vivo kinase assay data show that Isorhamnetin inhibits the kinase activity of MAP/ERK kinase (MEK) 1 and PI3-K and the inhibition is due to direct binding with Isorhamnetin. Isorhamnetin inhibits the Akt/mTOR and MEK/ERK signaling pathways, and promotes the activity of the mitochondrial apoptosis signaling pathway. The inhibitory effects of Isorhamnetin on breast cancer cells are determined using the CCK-8 method. Isorhamnetin inhibits the proliferation of numerous breast cancer cells (IC 50 , ~10 µM), including MCF7, T47D, BT474, BT-549, MDA-MB-231 and MDA-MB-468, whereas less inhibitory activity is observed in the MCF10A normal breast epithelial cell line (IC 50 , 38 µM).
Photographic data shows that Isorhamnetin treatment suppresses tumor development in mice. The average volume of tumors in untreated mice increases over time and reaches a volume of 623 mm 3 at 4 weeks post-inoculation; however, at this time, in mice treated with 1 or 5 mg/kg Isorhamnetin, the average tumor volume is only 280 or 198 mm 3 , respectively. At the end of the study, Isorhamnetin treatment (1 or 5 mg/kg) reduces tumor weight compared with the untreated control group.