| CAS |
No.520-33-2 |
| 中文名称 |
橙皮素(10mM in DMSO,无菌） |
| 英文名称 |
Hesperitin(10mM in DMSO，Sterile） |
| 分子式 |
C16H14O6 |
| 分子量 |
302.29 |
| 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 |
Others |
| 通路 |
Others |
| 背景说明 |
Hesperetin 是一种黄烷酮类物质，为有效的，广谱的 UGT 抑制剂。 |
| 生物活性 |
Hesperetin is a natural flavanone， and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis.[1-6] |
| In Vitro |
Hesperetin 在自纳米乳化给药系统中具有抗氧化潜力[1]。Hesperetin 和 NGR 显示出对人类 μgT 的广谱抑制作用。此外，Hesperetin 对 μgT1A1、1A3 和 1A9 具有强抑制作用 (IC50 和 Ki 值均低于 10 μM)，中度抑制 μgT1A4、ugT1A7、ugT1A8 (IC 50 值 29.68-63.87 μM)[2]。Hesperetin 与不同类型的蛋白质相互作用，包括氢键、pi-pi 效应、pi-阳离子键合和 pi-sigma 相互作用，具有不同的结合能。Hesperetin 具有类似药物的特性，这表明它具有作为 CHIKV 感染处理选择的潜力[3]。Hesperetin 以剂量依赖性方式降低培养的原代大鼠肝细胞中 GCDCA 诱导的 caspase-3 活性。Hesperetin 还剂量依赖性地降低肝细胞中 CM 诱导的 Nos2 (iNOS) 表达。有趣的是，与单独使用细胞因子混合物相比，Hesperetin 诱导的抗氧化基因血红素加氧酶 1 (HO-1) 的表达增加了约四倍[5]。 |
| In Vivo |
预先给予 Hesperetin (40 mg/kg，口服) 可显著减轻 Cd 诱导的氧化应激和线粒体功能障碍，恢复抗氧化和膜结合酶活性并减少大鼠脑细胞凋亡[4]。Hesperetin (200 mg/kg) 减弱 Con A 诱导的小鼠肝细胞凋亡和肝 Nos2 (iNOS) 表达。Hesperetin 联合处理还减少了凋亡小体、水肿变性、核碎片、自溶和出血的发生。在小鼠模型中，Hesperetin 显著降低了 D-GalN/LPS 诱导的暴发性肝炎小鼠肝组织中浸润的白细胞数量[5]。 |
| 动物实验 |
After 7 days of adjusting， the animals are randomly divided into 10 experimental groups. Control group (n=8): These animals are treated with the equivalent volume of PBS as used for the administration of Con A and D-GalN/LPS. Control hesperetin group (n=8): The mice are treated with hesperetin 400 mg/kg p.o. in 0.5% sodium carboxymethylcellulose (CMC-Na) solution for 10 days. Con A group (n=15): The animals are treated with the same volume of CMC-Na as used for administration of hesperetin for 10 days and are challenged with Con A (i.v.15 mg/kg). Con A + hesperetin groups: The animals receive various doses of hesperetin (100， 200， 400 mg/kg) p.o. for 10 days before Con A injection (each group n=15). D-GalN/LPS group (n=15): The animals are given CMC-Na for 10 days and injected i.p. with D-GalN (700 mg/kg)/LPS (5 μg/kg). D-GalN/LPS + hesperetin groups: Three doses of hesperetin (100， 200， 400 mg/kg) are given to mice once daily for 10 days. D-GalN (700 mg/kg)/LPS (5 μg/kg) are injected i.p. (each group n=15). |
| 激酶实验 |
First， 0.5 mL tissue homogenate is diluted with 1 mL water. Then， to this mixture， 2.5 mL ethanol and 1.5 mL chloroform (all reagents chilled) are added and shaken for 1 min at 4°C， then centrifuged. The enzyme activity in the supernatant is determined. The assay mixture contained 1.2 mL sodium pyrophosphate buffer (0.025 M， pH 8.3)， 0.1 mL 186 mM phenazine methosulfate (PMS)， 0.3 mL 30 mM Nitroblue tetrazolium (NBT)， and 0.2 mL of nicotinamide adenine dinucleotide (NADH)， and appropriately diluted enzyme preparation and water in a total volume of 3 mL. Reaction is initiated by the addition of NADH. After incubation at 30°C for 90 min， the reaction is stopped by the addition of 1 mL glacial acetic acid. The reaction mixture is stirred vigorously and shaken with 4 mL n-butanol. The intensity of the chromogen in the butanol layer is measured at 560 nm against a butanol blank. A system without enzyme served as control. One unit of enzyme activity is defined as 50% inhibition of NBT reduction in 1 min under the assay conditions. |
| 数据来源文献 |
[1]. Arya A， et al. Bioflavonoid hesperetin overcome bicalutamide induced toxicity by co-delivery in novel SNEDDS formulations: Optimization， in vivo evaluation and uptake mechanism. Mater Sci Eng C Mater Biol Appl. 2017 Feb 1;71:954-964
[2]. Liu D， et al. Inhibitory Effect of Hesperetin and Naringenin on Human UDP-Glucuronosyltransferase Enzymes: Implications for Herb-Drug Interactions. Biol Pharm Bull. 2016;39(12):2052-2059.
[3]. Oo A， et al. In silico study on anti-Chikungunya virus activity of hesperetin. PeerJ. 2016 Oct 26;4:e2602. eCollection 2016.
[4]. Shagirtha K， et al. Neuroprotective efficacy of hesperetin against cadmium induced oxidative stress in the brain of rats. Toxicol Ind Health. 2016 Nov 1. pii: 0748233716665301
[5]. Bai X， et al. The protective effect of the natural compound hesperetin against fulminant hepatitis in vivo and in vitro. Br J Pharmacol. 2017 Jan;174(1):41-56
[6]. Li Q， et al. Hesperetin Induces Apoptosis in Human Glioblastoma Cells via p38 MAPK Activation. Nutr Cancer. 2019 Jul 11:1-8. |
| 规格 |
1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号