CAS |
No.3681-99-0 |
中文名称 |
葛根素(10mM in DMSO,无菌) |
英文名称 |
Puerarin(10mM in DMSO,Sterile) |
分子式 |
C21H20O9 |
分子量 |
416.38 |
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. |
运输条件 |
冷冻运输 |
靶点 |
5-HT Receptor |
通路 |
Neuronal Signaling;GPCR & G Protein |
背景说明 |
葛根素是5-HT2C受体拮抗剂。 |
生物活性 |
Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.[1-4] |
In Vitro |
Puerarin 抑制 LPS 诱导的 iNOS、COX-2 和 CRP 蛋白的表达,并抑制 RAW264.7 细胞中 RT-PCR 实验中它们的 mRNA。iNOS、COX-2 和 CRP 表达的抑制是由于 I-κB 磷酸化和降解的剂量依赖性抑制,导致 p65NF-κB 核转位减少。Puerarin 介导的抑制 LPS 诱导的 iNOS、COX-2 和 CRP 表达的作用归因于在转录水平抑制 NF-κB 激活[1]。 Puerarin 是一种新型的 IK1 开放通道阻滞剂,可能是 Puerarin 抗心律失常作用的基础。Puerarin 与 IK1 的开放通道阻滞剂钡竞争抑制 IK1 电流[2]。 |
In Vivo |
染料木黄酮和 Puerarin 均通过潜在的抗氧化、抗炎或抗细胞凋亡机制有效减轻慢性酒精摄入引起的肝损伤。然而,染料木黄酮在降低丙二醛 (1.05±0.0947 vs. 1.28±0.213 nmol/mg pro,p[3]。 Puerarin 可显著改善早期肾损伤,可能是通过抑制糖尿病大鼠肾脏中 ICAM-1 和 TNF-α 的表达[4]。 |
细胞实验 |
RAW264.7 cells are maintained at subconfluence in 95% air and 5% CO2 humidified atmosphere maintained at 37°C. The medium used for routine subculture is Dulbecco’s Modified Eagle’s Medium supplemented with 10% fetal bovine serum, penicillin (100 units/mL) and streptomycin (100 μg/ mL). An MTT assay is used to measure the viability of the cells after treatment with puerarin. After the supernatants are removed for nitrite determination, cells are incubated at 37°C with MTT (0.05 mg/mL) for 4 h, and the optical density is measured at 540 nm. The concentrations of puerarin are10, 20, 40 and 100 μM[1]. |
动物实验 |
Rats: A cohort of healthy male SD rats (7 weeks old) are randomLy divided into a control group, a model group, and a puerarin treatment group with high (H), moderate (M), and low (L) dosage. Puerarin is re-suspended in 0.9% saline and is given by intra-gastric intubation at various concentrations (0.25 mg/(kg×d) for L group, 0.5 mg/(kg×d) for M group, and 1.0 mg/(kg×d) for H group) each day for 8 consecutive days. An equal volume of saline is administered to control and model rats during the same time period[4]. Mice: Forty male ICR mice (weight: 20-22 g) are acclimatized with a daily 12 h light:12 h dark cycle at 22±2 °C room temperature and 55%±5% relative humidity. After 1 week of adaption, the mice are randomLy divided into four groups with ten mice per group. Genistein and puerarin are applied to the mice in sodium carboxymethyl cellulose solution with an equimolar concentration of 0.1 M (gastric volume: 3 mL kg-1 body weight)[3]. |
数据来源文献 |
[1]. Hu W, et al. Puerarin inhibits iNOS, COX-2 and CRP expression via suppression of NF-κB activation in LPS-induced RAW264.7 macrophage cells. Pharmacol Rep. 2011;63(3):781-9. [2]. Zhang H, et al. Puerarin: a novel antagonist to inward rectifier potassium channel (IK1). Mol Cell Biochem. 2011 Jun;352(1-2):117-23. [3]. Zhao L,et al. Protective Effects of Genistein and Puerarin against Chronic Alcohol-Induced Liver Injury in Mice via Antioxidant, Anti-inflammatory, and Anti-apoptotic Mechanisms. J Agric Food Chem. 2016 Sep 28;64(38):7291-7. [4]. Pan X, et al. Effect of Puerarin on Expression of ICAM-1 and TNF-α in Kidneys of Diabetic Rats. Med Sci Monit. 2015 Jul 23;21:2134-40. |
规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
单位 |
瓶 |