CAS |
No.117-39-5 |
中文名称 |
槲皮素(10mM in DMSO,无菌) |
英文名称 |
Quercetin(10mM in DMSO,Sterile) |
分子式 |
C₁₅H₁₀O₇ |
分子量 |
302.24 |
溶解性 |
请根据自己的实验要求使用。 |
外观(性状) |
无菌溶液 |
储存条件 |
Stroe at -20℃,6 months. |
靶点 |
Sirtuin |
通路 |
Cell Cycle;DNA Damage/DNA Repair; Epigenetics |
背景说明 |
是一种黄酮类化合物,可激活 SIRT1,也可抑制 PI3Kγ,PI3Kδ,PI3Kβ。 |
生物活性 |
Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.[1-4] |
In Vitro |
Quercetin 是一种植物性化学物质或植物化学物质,用作补充剂、饮料或食品的成分。在几项研究中,它可能具有抗炎和抗氧化特性,并且正在研究它的广泛潜在健康益处。Quercetin 是一种 PI3K 抑制剂,IC50 为 2.4-5.4 μM。Quercetin 强烈抑制 PI3K 和 Src 激酶,轻度抑制 Akt1/2,并轻微影响 PKC、p38 和 ERK1/2[1]。Quercetin 抑制 TNF 诱导的 LDH% 释放、EC 依赖性中性粒细胞与牛肺动脉内皮细胞 (BPAEC) 的粘附以及 BPAEC DNA 合成和增殖[2]。 |
In Vivo |
Quercetin (75 mg/kg) 和 2-甲氧基雌二醇的组合增强了对人前列腺癌 LNCaP 和 PC-3 细胞异种移植肿瘤生长的抑制[3]。 |
动物实验 |
Mice are inoculated subcutaneously with 5×105?PC-3 cells suspended in 100μL PBS and 2×108?LNCaP cells suspended in 100μL of matrigel and PBS mixture (1:1) on the right back. When xenograft tumors reach a volume of approximately 100 mm3, mice are randomLy assigned to four groups (n=8 each group) and treated intraperitoneally. Therapeutic schedule based on our in vitro results, preliminary experiments and many other researchers‘ studies is as follows: (1) Vehicle control group: vehicle of quercetin on day 1, vehicle of 2-ME on day 2, (2) Quercetin treated group: quercetin 75 mg/kg on day 1, vehicle of 2-ME on day 2, (3) 2-ME treated group: vehicle of quercetin on day 1, 2-ME 150 mg/kg on day 2, (4) Combination treatment group: quercetin 75 mg/kg on day 1, 2-ME 150 mg/kg on day 2. Two days is a treatment cycle and the whole treatment process lasted for 4 weeks. Tumor sizes are monitored every 2 days using caliper and tumor volume are calculated according to the formula: L×S2×0.5, in which L represents the longest diameter and S represents the shortest diameter of tumor. Mice are weighed as well. At the end of treatment procedure, on day 29, mice are anesthetized with chloral hydrate and sacrificed by cervical dislocation. Xenograft tumors are taken out quickly and weighed. One part of it is put into liquid nitrogen immediately for future biomarker analysis and the other part is fixed in 10% neutral buffered formalin for immunohistochemical analysis. Serum biochemical parameters such as ALT, AST, creatinine and urea nitrogen that reflected drug toxicity are also detected. |
数据来源文献 |
[1]. Leyre Navarro-Nú?ez, et al. Effect of quercetin on platelet spreading on collagen and fibrinogen and on multiple platelet kinases. Fitoterapia. 2010 Mar;81(2):75-80. [2]. Yu XB, et al. Inhibitory effects of protein kinase C inhibitors on tumor necrosis factor induced bovine pulmonary artery endothelial cell injuries. Yao Xue Xue Bao. 1996;31(3):176-81. [3]. Yang F, et al. Combination of Quercetin and 2-Methoxyestradiol Enhances Inhibition of Human Prostate Cancer LNCaP and PC-3 Cells Xenograft Tumor Growth. PLoS One. 2015 May 26;10(5):e0128277. [4]. Tao Liu, et al. Quercetin alleviates kidney fibrosis by reducing renal tubular epithelial cell senescence through the SIRT1/PINK1/mitophagy axis. Life Sci. 2020 Jul 20;118116. |
规格 |
1ml |
单位 |
瓶 |