Quercetagetin
(Synonyms: 六羟黄酮/栎草亭,6-Hydroxyquercetin) 目录号 : GC65201
A selective Pim-1 inhibitor
Cas No.:90-18-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PIM1 0.34μM(IC50) | PIM2 3.45μM(IC50) | RSK2 2.82μM(IC50) | PKA 21.2μM(IC50) |
The proto-oncogene serine/threonine-protein kinases, Pim-1 and Pim-2, are enzymes involved in cytokine signaling and participate in various signal transduction pathways, including cell growth, differentiation, and apoptosis. Their overexpression has been implicated in prostate cancer, some forms of leukemia, and lymphoma. Quercetagetin is a flavonol that inhibits Pim-1 with an IC50 value of 0.34 ?M.1 It is selective for Pim-1, inhibiting Pim-2, PKA, RSK2, and JNK with IC50 values of 3.45, 21.2, 2.82, and 4.6 ?M, respectively.1,2 Quercetagetin has been shown to inhibit Pim-1 activity in intact RWPE2 prostate cancer cells with an ED50 value of 5.5 ?M, which led to significant growth inhibition.1 It can also inhibit the growth of additional prostate epithelial cell lines at a potency proportionate to their respective level of Pim-1 protein.1
1.Holder, S., Zemskova, M., Zhang, C., et al.Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinaseMol. Cancer Ther.6(1)163-172(2007) 2.Baek, S., Kang, N.J., Popowicz, G.M., et al.Structural and functional analysis of the natural JNK1 inhibitor quercetagetinJ. Mol. Biol.425(2)411-423(2013)
| Cas No. | 90-18-6 | SDF | Download SDF |
| 别名 | 六羟黄酮/栎草亭,6-Hydroxyquercetin | ||
| 分子式 | C15H10O8 | 分子量 | 318.24 |
| 溶解度 | DMSO : 125 mg/mL (392.79 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1423 mL | 15.7114 mL | 31.4228 mL |
| 5 mM | 0.6285 mL | 3.1423 mL | 6.2846 mL |
| 10 mM | 0.3142 mL | 1.5711 mL | 3.1423 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
A novel copigment of Quercetagetin for stabilization of grape skin anthocyanins
Food Chem 2015 Jan 1;166:50-55.PMID:25053027DOI:10.1016/j.foodchem.2014.05.125.
The thermal and light stability of grape skin anthocyanins combined with Quercetagetin was investigated at designed pH values of 3, 4 and 5. The molar ratios of anthocyanins to Quercetagetin were 1:10, 1:20 and 1:40 for thermally treatment at 70 °C, 80 °C and 90 °C, respectively, and the ratios were tested at 5:1, 1:1, 1:5 and 1:10 in the light exposure experiments. The degradation reaction of anthocyanins in the presence of Quercetagetin followed the first-order kinetic model. The half-life (t₁/₂) of anthocyanins was extended significantly with the increase of Quercetagetin concentration (p<0.05). The total colour difference values (ΔE(∗)) for the anthocyanin solutions with Quercetagetin were smaller than those without copigment under the same experimental conditions (pH and light exposure time). Compared with epigallocatechin gallate (EGCG), tea polyphenols (TP), myricitrin and rutin, Quercetagetin was the most effective copigment to stabilize grape skin anthocyanins.
Quercetagetin inhibits macrophage-derived chemokine in HaCaT human keratinocytes via the regulation of signal transducer and activator of transcription 1, suppressor of cytokine signalling 1 and transforming growth factor-β1
Br J Dermatol 2014 Sep;171(3):512-23.PMID:24602010DOI:10.1111/bjd.12938.
Background: Inflammatory chemokines, such as macrophage-derived chemokine (MDC/CCL22), are elevated in the serum and lesioned skin of patients with atopic dermatitis (AD), and are ligands for C-C chemokine receptor 4, which is predominantly expressed on T helper 2 lymphocytes, basophils and natural killer cells. We have previously reported that Quercetagetin has an inhibitory activity on inflammatory chemokines, which is induced by interferon (IFN)-γ and tumour necrosis factor (TNF)-α, occurring via inhibition of the signal transducer and activator of transcription 1 (STAT1) signal. Objectives: To investigate the specific mechanisms of Quercetagetin on the STAT1 signal. Methods: We confirmed the inhibitory activity of Quercetagetin on MDC and STAT1 in HaCaT keratinocytes. The interaction between STAT1 and IFN-γR1 was investigated using immunoprecipitation. The small interfering RNA approach was used to investigate the role of suppressor of cytokine signalling 1 (SOCS1) and transforming growth factor (TGF)-β1 induced by Quercetagetin. Results: Quercetagetin inhibited the expression of MDC at both the protein and mRNA levels in IFN-γ- and TNF-α-stimulated HaCaT human keratinocytes. Moreover, Quercetagetin inhibited the phosphorylation of STAT1 through upregulation of SOCS1. Increased expression of SOCS1 disrupted the binding of STAT1 to IFN-γR1. Furthermore, Quercetagetin augmented the expression of TGF-β1, which is known to modulate the immune response and inflammation. Conclusions: These results suggest that Quercetagetin may be a potent inhibitor of the STAT1 signal, which could be a new molecular target for anti-inflammatory treatment, and may thus have therapeutic applications as an immune modulator in inflammatory diseases such as AD.
Quercetagetin and Patuletin: Antiproliferative, Necrotic and Apoptotic Activity in Tumor Cell Lines
Molecules 2018 Oct 9;23(10):2579.PMID:30304821DOI:10.3390/molecules23102579.
Quercetagetin and patuletin were extracted by the same method from two different Tagetes species that have multiple uses in folk medicine in Mexico and around the globe, one of which is as an anticancer agent. Their biological activity (IC50 and necrotic, apoptotic and selective activities of these flavonols) was evaluated and compared to that of quercetin, examining specifically the effects of C6 substitution among quercetin, Quercetagetin and patuletin. We find that the presence of a methoxyl group in C6 enhances their potency.
Rutin and Quercetagetin enhance the regeneration potential of young and aging bone marrow-derived mesenchymal stem cells in the rat infarcted myocardium
Mol Cell Biochem 2022 Dec 25.PMID:36566485DOI:10.1007/s11010-022-04628-5.
Myocardial infarction (MI) damages cardiomyocytes permanently and compromises cardiac function. Mesenchymal stem cells (MSCs) with the potential to differentiate into multiple lineages are considered as one of the best options for the treatment of MI. However, aging affects their regeneration capability. With age, reactive oxygen species (ROS) accumulate in cells ultimately causing cell death. To successfully utilize these stem cells in clinic, novel strategies to improve their functional capability should be explored. In this study, we aimed to enhance the cardiac regeneration potential of bone marrow MSCs derived from aging rats by treating them with antioxidants, rutin or Quercetagetin in separate in vivo experiments. Oxidative stress was induced by treating MSCs of young and aging rats with different concentrations of H2O2 which resulted in an increase in the ROS level. MSCs were treated with rutin or Quercetagetin at varying concentrations and exposed to H2O2. It was observed that both antioxidants significantly (P < 0.001) suppressed H2O2-induced intracellular ROS accumulation in a dose-dependent manner. An optimized concentration of 10 µM rutin or Quercetagetin was used for the in vivo experiments. MI models were developed in aging rats by ligation of left anterior descending artery and treated MSCs were transplanted in the MI models. Echocardiography was performed after 2 and 4 weeks of cell transplantation to evaluate the functional status of the infarcted heart and histological analysis was performed after 4 weeks to assess cardiac regeneration. Significant improvement was observed in cardiac parameters including LVEF% (P < 0.001), LVFS% (P < 0.01 and P < 0.001), LVIDd (P < 0.01 and P < 0.001), LVIDs (P < 0.001), LVEDV (P < 0.001) and LVESV (P < 0.001) in the treated young as well as aging MSCs. It is concluded from these findings that rutin and Quercetagetin treatment enhance the regeneration efficiency of young and aging MSCs in vivo. These antioxidants can be effectively utilized to improve cellular therapy for myocardial infarction by suppressing ROS production.
Fabrication and Characterization of Quercetagetin-Loaded Nanoparticles Based on Shellac and Quaternized Chitosan: Improvement of Encapsulation Efficiency and Acid and Storage Stabilities
J Agric Food Chem 2021 Dec 29;69(51):15670-15680.PMID:34923817DOI:10.1021/acs.jafc.1c01830.
Shellac can be used as an ideal delivery vehicle to deliver and protect the hydrophobic Quercetagetin; the barriers such as low acid stability and encapsulation efficiency, however, heavily impede the application of shellac. The purpose of this work is to prepare quercetagetin-loaded shellac-quaternized chitosan nanoparticles (Que-Sh-QCS NPs) to overcome these challenges. Herein, quaternized chitosan, with 14% degree of substitution, was successfully synthesized via a quaternization modification. The concentration of quaternized chitosan over 0.05% can prevent the aggregation of shellac nanoparticles at the acid. The encapsulation efficiency of Quercetagetin obviously increased from 37.92 to 65.48% with the concentration of QCS varying from 0 to 0.05%. Meanwhile, Que-Sh-QCS0.05 NPs possessed good storage stability, antioxidant property, biocompatibility, and controlled release. Therefore, quaternized chitosan can improve the encapsulation efficiency and acid and storage stabilities of nutraceutical-loaded shellac nanoparticles, providing a new insight into the application of shellac in cosmetics, pharmaceuticals, and food.