Isoquercetin是一种具有多样生物活性的类黄酮，具有抗氧化、抗增殖和抗炎等特性。
Cas No.:482-35-9
Sample solution is provided at 25 µL, 10mM.
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Isoquercetin is a flavonoid with diverse biological activities, including antioxidant, antiproliferative, and anti-inflammatory properties[1, 2]. Due to its high bioavailability and low toxicity, Isoquercetin is a promising candidate for preventing congenital defects in diabetic pregnancy[3].
In vitro, pretreatment of primary cultured rat cortical neurons with Isoquercetin (20, 40, 80µg/mL) for 24h reduced the increase in intracellular calcium concentration and lactate dehydrogenase (LDH) release induced by oxygen-glucose deprivation/reperfusion (OGD/R) injury, and prevented the decrease in cell viability[4]. Pretreatment of HepG2 cells with Isoquercetin (10μM) for 1h significantly downregulated ethanol-induced iNOS protein expression levels in the cells[5].
In vivo, intravenous administration of Isoquercetin (50mg/kg) for 7 days to rats subjected to middle cerebral artery occlusion (MCAO) injury reduced the cerebral infarct volume and mitigated the decrease in Nrf2 expression levels in hippocampal tissue[6]. Oral administration of Isoquercetin (20mg/kg) for 3 days to rats subjected to middle cerebral artery occlusion/reperfusion (MCAO/R) injury reduced the cerebral infarct volume, improved neurological deficits, and decreased the production of reactive oxygen species (ROS) and malondialdehyde (MDA) in brain tissue[7].
References:
[1] Mbikay M, Chrétien M. Isoquercetin as an anti-COVID-19 medication: A potential to realize[J]. Frontiers in Pharmacology, 2022, 13: 830205.
[2] Azeem M, Hanif M, Mahmood K, et al. An insight into anticancer, antioxidant, antimicrobial, antidiabetic and anti-inflammatory effects of quercetin: A review[J]. Polymer Bulletin, 2023, 80(1): 241-262.
[3] Cao L, Tan C, Meng F, et al. Amelioration of intracellular stress and reduction of neural tube defects in embryos of diabetic mice by phytochemical quercetin[J]. Scientific Reports, 2016, 6(1): 21491.
[4] Wang C P, Li J L, Zhang L Z, et al. Isoquercetin protects cortical neurons from oxygen–glucose deprivation–reperfusion induced injury via suppression of TLR4–NF-кB signal pathway[J]. Neurochemistry international, 2013, 63(8): 741-749.
[5] Lee S, Lee J, Lee H, et al. Relative protective activities of quercetin, quercetin‐3‐glucoside, and rutin in alcohol‐induced liver injury[J]. Journal of food biochemistry, 2019, 43(11): e13002.
[6] Chen M, Dai L H, Fei A, et al. Isoquercetin activates the ERK1/2-Nrf2 pathway and protects against cerebral ischemia-reperfusion injury in vivo and in vitro[J]. Experimental and Therapeutic Medicine, 2017, 13(4): 1353-1359.
[7] Dai Y, Zhang H, Zhang J, et al. Isoquercetin attenuates oxidative stress and neuronal apoptosis after ischemia/reperfusion injury via Nrf2-mediated inhibition of the NOX4/ROS/NF-κB pathway[J]. Chemico-biological interactions, 2018, 284: 32-40.
Isoquercetin是一种具有多样生物活性的类黄酮，具有抗氧化、抗增殖和抗炎等特性[1, 2]。Isoquercetin具有高生物利用度和低毒性，是预防糖尿病妊娠先天缺陷的有前景候选药物[3]。
在体外，Isoquercetin（20, 40, 80µg/mL）预处理原代培养的大鼠皮层神经元24h，降低了氧糖剥夺损伤（OGD/R）诱导的细胞内钙离子浓度升高和乳酸脱氢酶（LDH）释放，防止了细胞活力下降[4]。Isoquercetin（10μM）预处理HepG2细胞1h，显著下调了细胞中乙醇诱导的iNOS蛋白表达水平[5]。
在体内，Isoquercetin（50mg/kg）通过静脉注射给药治疗接受大脑中动脉闭塞（MCAO）损伤的大鼠7天，减轻了大鼠脑梗死体积，减轻了海马组织中Nrf2表达水平下降程度[6]。Isoquercetin（20mg/kg）通过灌胃给药治疗接受大脑中动脉闭塞/再灌注（MCAO/R）损伤的大鼠3天，减轻了大鼠脑梗死体积，改善了大鼠的神经功能缺损，降低了大鼠脑组织中活性氧（ROS）和丙二醛（MDA）的产生[7]。
| Cell experiment [1]: | |
Cell lines | Primary culture of rat cortical neurons |
Preparation Method | The primary culture of rat cortical neurons were pretreated with 20, 40 and 80µg/mL Isoquercetin and 2.5, 5µg/mL nimodipine, respectively, for 24h, followed by exposure to oxygen-glucose deprivation (OGD) for 6h, then reperfusion for 24h. The cortical neurons cultured in plain medium served as control. |
Reaction Conditions | 20, 40, 80µg/mL; 24h |
Applications | Isoquercetin administered prior to the insult could prevent OGD/R-induced intracellular calcium concentrations ([Ca2+]i) increase, lactate dehydrogenase (LDH) release and cell viability decrease. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley (SD) rats |
Preparation Method | The rats were randomly allocated to one of four groups: Control, sham, model and Isoquercetin. In the model group, rats were anesthetized via the intraperitoneal injection of 10% chloral hydrate. The rectal temperature was monitored and maintained at 37.0±0.5˚C by the use of a feedback‑regulated heating system during surgery. Permanent focal ischemia was induced by occluding the right middle cerebral artery (MCA) via an intraluminal technique. Briefly, a 4‑0 nylon monofilament suture with a slightly enlarged rounded tip was inserted into the stump of the external carotid artery and advanced into the lumen of the internal carotid artery until it reached and occluded the MCA. The distance from the bifurcation of the common carotid artery (CCA) to the tip of the inserted suture averaged 18‑20mm. Sham operated animals were subjected to the aforementioned procedures, with the exception of suture insertion. Rats in the Isoquercetin group were subjected to MCAO surgery and treated with intravenous 50mg/kg Isoquercetin once a day for 7 days. Rats that did not undergo any surgery served as the control group. |
Dosage form | 50mg/kg; 7 days; i.v. |
Applications | The rats treated with Isoquercetin exhibited a lower degree of neurological dysfunction and smaller infarct volume than the vehicle‑treated rats. In the hippocampal tissue, the expression of Nrf2 at the mRNA and protein levels was decreased in the model group 7 days after ischemia, and the reduction in expression levels was significantly attenuated in the Isoquercetin treated-group. |
References: | |
| Cas No. | 482-35-9 | SDF | |
| 别名 | 槲皮素-3-葡萄糖苷; Quercetin 3-glucoside | ||
| Canonical SMILES | OC1=CC(O)=C(C(C(O[C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)=C(C3=CC=C(O)C(O)=C3)O4)=O)C4=C1 | ||
| 分子式 | C21H20O12 | 分子量 | 464.4 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,PBS (pH 7.2): 0.3 mg/ml | 储存条件 | 4°C, protect from light |
| 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1533 mL | 10.7666 mL | 21.5332 mL |
| 5 mM | 430.7 μL | 2.1533 mL | 4.3066 mL |
| 10 mM | 215.3 μL | 1.0767 mL | 2.1533 mL |
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| 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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工作液浓度： mg/ml；
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2.
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