| CAS |
No.520-36-5 |
| 中文名称 |
芹菜素(10mM in DMSO,无菌） |
| 英文名称 |
Apigenin(10mM in DMSO，Sterile） |
| 分子式 |
C15H10O5 |
| 分子量 |
270.24 |
| 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 |
Cytochrome P450 |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
Apigenin是一种竞争性 CYP2C9 抑制剂。 |
| 生物活性 |
Apigenin (4‘，5，7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.[1-3] |
| In Vitro |
Apigenin (4‘，5，7-Trihydroxyflavone) 抑制细胞色素 P450 2C9 (CYP2C9)，在 CYP2C9 RECO 系统 (一种含有重组人 CYP2C9、P450 的纯化重组酶系统) 中，Ki 为 2 μM还原酶、细胞色素 b5 和脂质体)[1]。Apigenin 抑制细胞增殖。20、40、80 μM的 Apigenin 7d生长抑制率 (IR) 分别为38%、71%、99%。暴露于 Apigenin 24 或 48 小时后，SGC-7901 细胞的克隆形成以剂量和时间依赖性方式受到抑制。Apigenin 处理 24 和 48 h 后 80 μM 的克隆效率分别为 9.8% 和 5%，而对照组为 40.4% 和 43.4%[2]。 |
| In Vivo |
Apigenin (4‘，5，7-Trihydroxyflavone) 是一种天然类黄酮，具有广泛的生物学特性，包括抗氧化、抗炎、抗癌和神经保护作用。Apigenin (125 mg/kg 和 250 mg/kg) 减轻 Adriamycin (ADR) (24 mg/kg) 诱导的心肌损伤。Apigenin 抑制血清天冬氨酸氨基转移酶 (AST) 的释放。Apigenin 减少血清乳酸脱氢酶 (LDH) 的释放。Apigenin 降低血清肌酸激酶 (CK) 含量[3]。 |
| 细胞实验 |
The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of human gastric cancer SGC-7901 cells are harvested with 0.2% EDTA and plated at a density of 2.5×103/well in 96-well microtiter plates. After an overnight incubation to allow cell attachment， the medium is replaced by fresh medium containing different concentrations (0， 20， 40， and 80 μM) of Apigenin. Control wells receive DMSO (0.2%). Each concentration of Apigenin is repeated in four wells. After incubation for 24 h， one plate is assayed with a microplate reader at the wavelength of 570 nm. Before the assay， MTT (5 mg/mL in PBS) is added to each well and incubated for 4 h， then MTT solution is removed from the wells by aspiration. After careful removal of the medium， 0.1 mL of DMSO is added to each well， and the plate is shaken for 15 min. The data of 7 d are fed into the computer and the growth curve is drawn. The growth inhibition rate (IR) is calculated[2]. |
| 动物实验 |
Mice[3]Sixty healthy Kunming mice (26±2?g) are randomly assigned into two groups: a control group (n=15) and an ADR group (n=45). The ADR group is divided into three subgroups: ADR only without Apigenin (ADR， n=15)， low-dose Apigenin (125?mg/kg/day， n=15)， and high-dose Apigenin (250?mg/kg/day， n=15). All Apigenin-treated groups are treated daily via gastric gavage for seventeen days with a 125 or 250?mg/kg/day dose. ADR (3?mg/kg/day) is injected intraperitoneally into animals at an interval of 48?h (in total， eight times at a cumulative dose of 24?mg/kg). The mice in the control group receive injections of 0.9% sterile saline. On the 17th day after the first treatment， the mice are sacrificed， and blood samples are collected. A number of hearts are fixed with 2.5% glutaraldehyde fixative for electron microscopy analysis， and the others are stored at -80°C for western blot analysis. |
| 数据来源文献 |
[1]. Si D， et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34.
[2]. Wu K， et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4.
[3]. Yu W， et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号