Licochalcone D 是存在于Glycyrrhiza uralensis中的黄酮类化合物，是具有口服活性的NF-κB p65的有效抑制剂。Licochalcone D 具有抗氧化、抗炎、抗癌等作用。
| 生物活性 | Licochalcone D, a flavonoid compound mainly existing in the root ofGlycyrrhiza uralensis, is a potent and orally active inhibitor ofNF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties[1][2]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Licochalcone D (10 μM; 1 h) negatively regulatesLipopolysaccharides(LPS) (HY-D1056)-induced NF-κB activation by inhibiting the phosphorylation and transactivation of NF-κB p65, inhibits the LPS-induced activation of protein kinase A (PKA), and significantly inhibits the LPS-induced expression of TNFα and MCP-1[1].
Licochalcone D (10 μM; 24 h) significantly inhibits LPS-induced iNOS expression and NO production[1].
Licochalcone D (0-90 μM; 24 h) inhibits the proliferation of human melanoma cells, induces the apoptosis of A375 cells, decreases the mitochondrial membrane potential and increases ROS production in A375 cells[2].
Licochalcone D (0-25 μM; 24 h) decreases the migration and invasion ability of the A375 cells, decreased the protein levels of MMP-2 and MMP-9[2].
Western Blot Analysis[1] | Cell Line: | RAW264.7 cells | | Concentration: | 10 μM | | Incubation Time: | 1 h or 24 h (iNOS), following LPS stimulation (1 μg/mL) for 30 min | | Result: | Inhibited the phosphorylation of NF-κB at serine 276 but not at serine 536.
Inhibited the LPS-induced expression of TNFα mRNA and MCP-1 mRNA.
Strongly inhibited the expression of iNOS. |
Cell Viability Assay[2] | Cell Line: | A375 cells or SK-MEL-5 | | Concentration: | 0, 1, 2.5, 5, 15, 30, 45, 60, 75 and 90 μM (A375) or 0, 20, 40, 60 and 80 μM (SK-MEL-5) | | Incubation Time: | 24 h | | Result: | Inhibited the proliferation of A375 and SK-MEL-5 in a concentration dependent manner. |
Apoptosis Analysis[2] | Cell Line: | A375 | | Concentration: | 0, 30, 60 and 90 μM | | Incubation Time: | 24 h | | Result: | Cells exhibited obvious apoptotic characteristics after the treatment. |
RT-PCR[2] | Cell Line: | A375 | | Concentration: | 0, 30, 60 and 90 μM | | Incubation Time: | 24 h | | Result: | Downregulated the mRNA level of Bcl-2 and upregulated the mRNA levels of caspase-3, caspase-9 and Bax. |
Cell Invasion Assay[2] | Cell Line: | A375 | | Concentration: | 25 μM | | Incubation Time: | 24 h | | Result: | Significantly suppressed cell invasion. |
Cell Migration Assay[2] | Cell Line: | A375 | | Concentration: | 25 μM | | Incubation Time: | 24 h | | Result: | Significantly suppressed cell migration in the A375 cells. |
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体内研究
(In Vivo) | Licochalcone D (25 and 50 mg/kg; i.g.; daily for a week) inhibits the tumor growth in a mouse xenograft model of murine melanoma B16F0 cells[2].
| Animal Model: | C57BL/6 mice, B16F0 tumor model[2] | | Dosage: | 25 and 50 mg/kg | | Administration: | Intragastric administration, daily for a week | | Result: | Obviously lowered the tumor growth rates, the tumor growth inhibition rates were calculated to be 32.0 and 54.1% at 25 and 50 mg/kg, respectively. |
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| 来源 | - Plants
- Leguminosae
- Glycyrrhiza uralensisFisch.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(352.71 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8217 mL | 14.1084 mL | 28.2167 mL | | 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | | 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.87 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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