Quercetin
(Synonyms: 槲皮素) 目录号 : GN10266
Quercetin 是一种天然类黄酮，是重组 SIRT1 的刺激剂，也是 PI3K 抑制剂，对 PI3K γ、PI3K δ 和 PI3K β 的 IC50 分别为 2.4 μM、3.0 μM 和 5.4 μM。
Cas No.:117-39-5
Sample solution is provided at 25 µL, 10mM.
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Animal experiment: |
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. |
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References: [1]. Navarro-Nú ez L, et al. Effect of quercetin on platelet spreading on collagen and fibrinogen and on multiple platelet kinases. Fitoterapia. 2010 Mar;81(2):75-80. |
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Quercetin is an important dietary flavonoid, present in vegetables, fruits, seeds, nuts, tea and red wine. It has various biological functions in terms of tumor prevention. Quercetin is a strong inhibitor of PI3K, NF-κB, and other kinases involved in intracellular signaling. It can also mildly inhibit Akt1/2, and slightly affect PKC, p38 and ERK1/2 [1].
A number of reports have demonstrated that Quercetin possessed anti-inflammatory, anti-oxidant and pro-apoptotic functions in cancer cells and inhibited tumor progress with different mechanisms. Quercetin increased cytosolic Ca2+ levels and disrupted the mitochondrial membrane potential (MMP), which in turn promoted the release of cytochrome c in the cytoplasm, thus activating multiple caspases such as caspase-3, -8 and -9 and subsequently inducing apoptosis via mitochondrial pathway [2]. Quercetin induced cell-cycle arrest and apoptosis, which was associated with the function of p53. Quercetin could promote p53 phosphorylation and therefore stabilize p53 both at the mRNA and protein level [3]. However, several studies investigated that cells with impaired p53 became more sensitive to Quercetin mediated cytotoxicity and apoptosis [4].
In vivo studies showed that administration of Quercetin before the initiation stage of carcinogenesis dramatically reduced various chemical agents induced tumor burden in mice models, including benzo(a)pyrene-induced lung tumor burden, azoxymethane-induced preneoplastic lesions in rat colon and N-nitrosodiethylamine-induced hepatocarcinoma etc. [5].
槲皮素是一种重要的膳食类黄酮，在蔬菜、水果、种子、坚果、茶叶和红酒中均有分布。它在肿瘤预防方面具有各种生物学功能。槲皮素是PI3K、NF-κB和其他参与细胞内信号转导的激酶的强力抑制剂。它也能轻微抑制Akt1/2，并轻微影响PKC、p38和ERK1/2等 [1]。
许多报告已经证明，槲皮素在癌细胞中具有抗炎、抗氧化和促凋亡等功能，并通过不同的机制抑制肿瘤进展。槲皮素提高了细胞质中Ca2+水平并破坏了线粒体膜电位(MMP)，从而促进了细胞质中细胞色素c的释放，激活多种半胱氨酸蛋白酶如半胱氨酸蛋白酶-3、-8和-9，并随后通过线粒体途径诱导细胞凋亡[2]。槲皮素诱导细胞周期停滞和凋亡，与p53的功能有关。槲皮素可以促进p53磷酸化，因此在mRNA和蛋白质水平上稳定p53 [3]。然而，一些研究表明，p53功能受损的细胞对槲皮素介导的细胞毒性和凋亡更为敏感[4]。
体内研究表明，在癌变发生前期给予槲皮素，能显著降低小鼠模型中各种化学物质引起的肿瘤负担，包括苯并(a)芘诱导的肺肿瘤负担、氧化甲基异腺嘌呤诱导的大鼠结肠癌前病变和N-亚硝基二乙胺诱导的肝癌等[5]。
References:
[1].Quercetin and cancer chemoprevention. Evid Based Complement Alternat Med. 2011;2011:591356. doi: 10.1093/ecam/neq053. Epub 2011 Apr 14.
Food-derived polyphenols inhibit pancreatic cancer growth through mitochondrial cytochrome C release and apoptosis. Int J Cancer. 2002 Apr 10;98(5):761-9.
[2].Stabilization of p53 is involved in quercetin-induced cell cycle arrest and apoptosis in HepG2 cells. Bioscience, Biotechnology and Biochemistry. 2008;72(3):797–804.
[3].Survivin and p53 modulate quercetin-induced cell growth inhibition and apoptosis in human lung carcinoma cells. The Journal of Biological Chemistry. 2004
[4].The effects of quercetin on antioxidant status and tumor markers in the lung and serum of mice treated with benzo(a)pyrene. Biological and Pharmaceutical Bulletin. 2007
| Cas No. | 117-39-5 | SDF | |
| 别名 | 槲皮素 | ||
| 化学名 | 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxychromen-4-one | ||
| Canonical SMILES | C1=CC(=C(C=C1C2=C(C(=O)C3=C(C=C(C=C3O2)O)O)O)O)O | ||
| 分子式 | C15H10O7 | 分子量 | 302.24 |
| 溶解度 | ≥ 15.1mg/mL in DMSO | 储存条件 | Store at RT |
| 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 | 3.3086 mL | 16.5431 mL | 33.0863 mL |
| 5 mM | 0.6617 mL | 3.3086 mL | 6.6173 mL |
| 10 mM | 0.3309 mL | 1.6543 mL | 3.3086 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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1. 首先保证母液是澄清的；
2.
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