| Description | Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90. |
| In vitro | 方法：白血病细胞 CEM、K562 和 Nalm6 用 Quercetin (10-250 µM) 处理 48 h，使用 MTT 方法检测细胞毒性。结果：Quercetin 剂量依赖诱导细胞毒性，IC50 分别约为 20、40 和 55 μM。[1]方法：肿瘤细胞 CT-26、LNCaP、MOLT-4 和 Raji 用 Quercetin (120 µM) 处理 48 h，使用 Flow Cytometry 方法检测细胞凋亡情况。结果：Quercetin 剂量依赖性诱导四种肿瘤细胞凋亡。[2]方法：人骨肉瘤细胞 HOS 和 MG63 用 Quercetin (25-100 µM) 处理 12-24 h，使用 wound healing assay 测定细胞迁移能力。 结果：Quercetin 以剂量和时间依赖的方式抑制骨肉瘤细胞系的细胞迁移。[3] |
| In vivo | 方法：为检测体内抗肿瘤活性，将 Quercetin (30 mg/kg) 和 Cisplatin (7 mg/kg) 腹腔注射给携带小鼠乳腺肿瘤 EMT6 的 BALB/c 小鼠，每三天一次，给药四次。结果：Quercetin 和 Cisplatin 协同抑制乳腺癌肿瘤的生长，增强了 Cisplatin 的抗肿瘤效果。Quercetin 还降低了肾毒性，这是 Cisplatin 的潜在副作用。[4]方法：为研究抗衰老策略，将 Quercetin (50 mg/kg) 和 Dasatinib (5 mg/kg) 灌胃给药给 21 个月大的 C57BL/6 小鼠，每两周连续给药三天，持续三个月。结果：Quercetin 和 Dasatinib 具有抗衰老作用，减少衰老相关的 β-半乳糖苷酶、p16 和 p21 基因以及 p16 蛋白在性腺周围白色脂肪组织中的表达。[5] |
| Target activity | PI3Kγ:2.4 μM, PI3Kδ:3.0 μM |
| Synonyms | 槲皮素, Sophoretin |
| molecular weight | 302.24 |
| Molecular formula | C15H10O7 |
| CAS | 117-39-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 4 mg/mL(13.2 mM) DMSO: 50 mg/mL (165.43 mM) |
| References | 1. Srivastava S, et al. Quercetin, a Natural Flavonoid Interacts with DNA, Arrests Cell Cycle and Causes Tumor Regression by Activating Mitochondrial Pathway of Apoptosis. Sci Rep. 2016 Apr 12;6:24049. 2. Hashemzaei M, et al. Anticancer and apoptosis‑inducing effects of quercetin in vitro and in vivo. Oncol Rep. 2017 Aug;38(2):819-828. 3. Lan H, et al. Quercetin Inhibits Cell Migration and Invasion in Human Osteosarcoma Cells. Cell Physiol Biochem. 2017;43(2):553-567. 4. Liu H, et al. Effect of quercetin on the anti-tumor activity of cisplatin in EMT6 breast tumor-bearing mice. Obstet Gynecol Sci. 2019 Jul;62(4):242-248. 5. Islam MT, et al. Senolytic drugs, dasatinib and quercetin, attenuate adipose tissue inflammation, and ameliorate metabolic function in old age. Aging Cell. 2023 Feb;22(2):e13767. 6. Liang Y, Xu Z, Wu X, et al. Inhibition of hyperpolarization-activated cyclic nucleotide-gated channels with natural flavonoid quercetin[J]. Biochemical and Biophysical Research Communications. 2020 7. Shim K S, Hwang Y H, Jang S A, et al. . Water Extract of Lysimachia christinae Inhibits Trabecular Bone Loss and Fat Accumulation in Ovariectomized Mice[J]. Nutrients. 2020, 12(7): 1927. 8. Peng D, Chen L, Sun Y, et al. Melanoma suppression by quercein is correlated with RIG-I and type I interferon signaling[J]. Biomedicine & pharmacotherapy= Biomedecine & pharmacotherapie. 2020, 125: 109984. |