Cynaroside (Luteolin 7-glucoside) 是一种具有抗氧化能力的黄酮类化合物。Cynaroside 还是一种流感依赖的RNA 聚合酶抑制剂，IC50为 32 nM。Cynaroside 也是一种应对2O2诱导的细胞凋亡的抑制剂，对氧化应激诱导的心血管疾病具有细胞保护作用。Cynaroside 还具有抗细菌、真菌和抗癌活性，以及抗氧化和抗炎活性。
| 生物活性 | Cynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependentRNA polymeraseinhibitor with anIC50of 32 nM. Cynaroside also is a promising inhibitor for H2O2-inducedapoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities[1][3][4][5]. |
| IC50& Target | IC50:32 nM (RNA polymerase inhibitor)[2] |
体外研究
(In Vitro) | Cynaroside promots macrophage phenotypic transition from pro-inflammatory M1 to anti-inflammatory M2, and mitigates sepsis-associated liver inflammatory damage.
Cynaroside reduces binding of PKM2 to hypoxia-inducible factor-1α (HIF-1α) by abolishing translocation of PKM2 to the nucleus and promoting PKM2 tetramer formation, as well as suppressing phosphorylation of PKM2 at Y105 in vivo and in vitro.
Cynaroside restores pyruvate kinase activity, inhibits glycolysis-related proteins including PFKFB3, HK2 and HIF-1α, and inhibits glycolysisrelated hyperacetylation of HMGB1 in septic liver.
Cynaroside protects H9c2 cells against H2O2-induced apoptosis by decreasing ROS generation and inhibiting caspase activation in both the mitochondrial and death receptor pathways.
Cynaroside maintains mitochondrial function by regulating Bcl-2 protein expression, as well as JNK and P53 expression[2][3].
Western Blot Analysis[2] | Cell Line: | RAW264.7 cell | | Concentration: | 5μM, 10μM | | Incubation Time: | 2 h | | Result: | Reduced expression levels of IL-1β, IL-6 and TNF-α and HMGB1, suppressed M1 polarized phenotype in RAW264.7 cells. |
Immunofluorescence[2] | Cell Line: | RAW264.7 cell | | Concentration: | | | Incubation Time: | 4 h | | Result: | Decreased PKM2 nuclear translocation in hepatic macrophages of septic mice. |
RT-PCR[2] | Cell Line: | RAW264.7 cell | | Concentration: | 2.5μM, 5μM, 10μM | | Incubation Time: | | | Result: | Increased increased expression levels of M2 markers Arg-1, IL-10 andCD206. |
Cell Viability Assay[3] | Cell Line: | H9c2 cells | | Concentration: | 25, 50, 100 μg/mL | | Incubation Time: | 4 h | | Result: | Protected H9c2 cells from oxidative stress-induced cell injury. |
Apoptosis Analysis[3] | Cell Line: | H9c2 cells | | Concentration: | 25, 50, 100 μg/mL | | Incubation Time: | 4 h | | Result: | Decreased H2O2-induced apoptosis in H9C2 cells. |
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体内研究
(In Vivo) | Cynaroside (i.p.; 5mg/kg) reduces binding of PKM2 to hypoxia-inducible factor-1α (HIF-1α) by abolishing translocation of PKM2 to the nucleus and promoting PKM2 tetramer formation, as well as suppressing phosphorylation of PKM2 at Y105[2].
| Animal Model: | Mice model of sepsis[2] | | Dosage: | 5mg/kg | | Administration: | Cynaroside (i.p.; 5mg/kg) | | Result: | Inhibited PKM2 dimer formation in liver of septic mice. |
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| 来源 | - Plants
- Umbelliferae
- Anthriscus sylvestris
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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 : 83.33 mg/mL(185.85 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2303 mL | 11.1513 mL | 22.3025 mL | | 5 mM | 0.4461 mL | 2.2303 mL | 4.4605 mL | | 10 mM | 0.2230 mL | 1.1151 mL | 2.2303 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： 50%PEG300 50% saline Solubility: 16.67 mg/mL (37.18 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.64 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.64 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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