| Description | Quercetin is a natural flavonoid which activates or inhibits the activities of a number of proteins. Quercetin can activate SIRT1 and inhibit PI3K with IC50s of 2.4 μM, 3.0 μM, 5.4 μM for PI3K γ, PI3K δ and PI3K β, respecti |
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| Related Catalog | Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Autophagy >> Mitophagy Signaling Pathways >> PI3K/Akt/mTOR >> PI3K Natural Products >> Flavonoids Research Areas >> Cancer |
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| Target | PI3Kβ:5.4 μM (IC50) PI3Kδ:2.4 μM (IC50) PI3Kγ:3 μM (IC50) Autophagy Mitophagy |
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| In Vitro | Quercetin is a type of plant-based chemical, or phytochemical, used as an ingredient in supplements, beverages or foods. In several studies, it may have anti-inflammatory and antioxidant properties, and it is being investigated for a wide range of potential health benefits. Quercetin is a PI3K inhibitor with IC50 of 2.4-5.4 μM. It strongly abrogates PI3K and Src kinases, mildly inhibits Akt1/2, and slightly affected PKC, p38 and ERK1/2[1]. Quercetin inhibits TNF-induced LDH% release, EC-dependent neutrophils adhesion to bovine pulmonary artery endothelial cells (BPAEC), and BPAEC DNA synthesis and proliferation[2]. |
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| In Vivo | Combination of Quercetin (75 mg/kg) and 2-Methoxyestradiol enhances inhibition of human prostate cancer LNCaP and PC-3 cells xenograft tumor growth[3]. |
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| Animal Admin | 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. [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. |
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