4'-Hydroxychalcone 是从甘草根中分离的一种查尔酮，具有保护肝脏的作用。4'-Hydroxychalcone 能通过抑制蛋白酶体 (proteasome)，抑制TNFα 诱导的 NF-κB 活性。4'-Hydroxychalcone 能诱导大鼠离体肝线粒体囊泡快速释放钾，并引起其线粒体呼吸控制和氧化磷酸化衰退。
| 生物活性 | 4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-inducedNF-κBactivation viaproteasomeinhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria[1][2][3]. |
体外研究
(In Vitro) | 4'-Hydroxychalcone (20-40 μM ; 2 hours) inhibits TNFα-induced (20 ng/mL; 6 hours) NF-kB pathway activation in a dose-dependent manner[3].
4'-Hydroxychalcone (0.1-25 μM ; 8 hours) inhibits proteasome activity in a dose-dependent manner but has no effect on IKK activity[3].
4'-Hydroxychalcone inhibits TNFα-dependent degradation of IkBα and subsequently prevents p50/p65 nuclear translocation leading to 4'-Hydroxychalcone-inhibited expression of NF-kB target genes[3].
4'-Hydroxychalcone affects cancer cell viability but has no significant effect on non-transformed cell viability[3].
Cell Viability Assay[3] | Cell Line: | K562 cells, Jurkat cells, U937 cells, PBMCs | | Concentration: | 5 μM, 10 μM, 20 μM, 24 μM, 28 μM, 32 μM, 40 μM, 60 μM | | Incubation Time: | 24 hours | | Result: | Affected cancer cell viability but has no significant effect on non-transformed cell viability. |
Western Blot Analysis[3] | Cell Line: | Jurkat cells | | Concentration: | 60 μM (followed by TNFα 20 ng/mL ) | | Incubation Time: | 2 hours | | Result: | Inhibited TNFα -dependent degradation of IkBα and prevents p50/p65 nuclear translocation. |
|
体内研究
(In Vivo) | 4'-Hydroxychalcone has hepatoprotective activity against Acetaminophen induced hepatotoxicity in mice[2].
| Animal Model: | Male albino mice(5-30 g)[2] | | Dosage: | 25 mg/kg, 50 mg/kg, 100 mg/kg | | Administration: | Oral administration, 12h intervals, 4 doses | | Result: | Significantly reduced the mortality rate induced by Acetaminophen (1 g/kg). |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 结构分类 | |
| 来源 | - Plants
- Leguminosae
- Glycyrrhiza uralensisFisch.
|
| 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 |
|
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(1114.83 mM;Need ultrasonic) 配制储备液 | 1 mM | 4.4593 mL | 22.2965 mL | 44.5931 mL | | 5 mM | 0.8919 mL | 4.4593 mL | 8.9186 mL | | 10 mM | 0.4459 mL | 2.2297 mL | 4.4593 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。-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 (9.28 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.28 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 (9.28 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.28 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (9.28 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 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 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
