Icaritin (Anhydroicaritin) 是淫羊藿中的异戊二烯类黄酮衍生物，有效抑制 K562 细胞 (IC50为 8 μM) 和原代 CML 细胞 (对 CML-CP 的IC50值为 13.4 μM，对 CML-BC 的IC50值为 18 μM) 的增殖。Icaritin 可以调节MAPK/ERK/JNK和JAK2/STAT3/AKT信号传导，并具有增强成骨的作用。
| 生物活性 | Icaritin (Anhydroicaritin) is a prenylflavonoid derivative fromEpimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC50of 8 μM) and primary CML cells (IC50of 13.4 μM for CML-CP and 18 μM for CML-BC). Icaritin can regulateMAPK/ERK/JNKandJAK2/STAT3 /AKTsignalings, also enhances osteogenesis[1][2][3. |
体外研究
(In Vitro) | Icaritin (4-64 μM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells[1].
Icaritin (0-64 μM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner[1].
Icaritin (32 μM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells[1].
Icaritin (0-64 μM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1[1].
Cell Proliferation Assay[1] | Cell Line: | K562, imatinib-resistant cells and primary CML cells | | Concentration: | 4 μM, 8 μM, 16 μM, 32 μM and 64 μM | | Incubation Time: | 48 hours | | Result: | Inhibited cell proliferation. |
Apoptosis Analysis[1] | Cell Line: | K562 or primary cells | | Concentration: | 0 μM, 4 μM, 8 μM, 16 μM, 32 μM and 64 μM | | Incubation Time: | 48 hours | | Result: | Induced K562 or primary cells apoptosis. |
Cell Cycle Analysis[1] | Cell Line: | K562 cells | | Concentration: | 32 μM | | Incubation Time: | | | Result: | Cell population in the sub-G1 phase was increased. |
Western Blot Analysis[1] | Cell Line: | K562 cells | | Concentration: | 0 μM, 4 μM, 8 μM, 16 μM, 32 μM and 64 μM | | Incubation Time: | 48 hours | | Result: | Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. |
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体内研究
(In Vivo) | Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia model[1].
| Animal Model: | Female NOD-SCID nude mice (6-8 weeks old) with K562 cells[1] | | Dosage: | 4 mg/kg and 8 mg/kg | | Administration: | Intraperitoneal injection; daily; for 10 weeks | | Result: | Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow. |
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| 来源 | - Plants
- Berberidaceae
- Epimedium brevicornuMaxim.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 15.62 mg/mL(42.40 mM;Need ultrasonic) H2O : 1.2 mg/mL(3.26 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL | | 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL | | 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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此方案可获得 ≥ 1.56 mg/mL (4.23 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 50%PEG300 50% saline Solubility: 1.51 mg/mL (4.10 mM); Suspended solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
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