芹菜素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetApigeninCat. No.: HY-N1201CAS No.: 520-36-5分式: CHO分量: 270.24作靶点: Autophagy; Cytochrome P450作通路: Autophagy; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (370.04 mM; Need ultrasonic)H2O : 0.1 mg/mL (insolubl

2、e)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.7004 mL 18.5021 mL 37.0041 mL5 mM 0.7401 mL 3.7004 mL 7.4008 mL10 mM 0.3700 mL 1.8502 mL 3.7004 mL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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选

3、择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 10 mg/mL (37.00 mM); Clear solution此案可获得 10 mg/mL (37.00 mM，饱和度未知) 的澄清溶液。以

4、 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (37.00 mM); Suspended solution; Need ultrasonicPage 1 of 2 www.MedChemE此案可获得 10 mg/mL (37.00 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。以

5、 1 mL 作液为例，取 100 L 100.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。BIOLOGICAL ACTIVITY物活性 Apigenin (4,5,7-Trihydroxyflavone)种竞争性 CYP2C9 抑制剂，Ki 为 2 M。IC & Target Ki: 2 M (CYP2C9)1体外研究 Apigenin (4,5,7-Trihydroxyflavone) inhibits cytochrome P450 2C9 (CYP2C9) with a Ki of 2 M in the CYP2C9 RECOs

6、ystem (a purified, reconstituted enzyme system containing recombinant human CYP2C9, P450 reductase,cytochrome b5, and liposomes)1. Apigenin inhibits the cell proliferation. The growth inhibition rate (IR) of 20, 40, and80 M of Apigenin is 38%, 71%, and 99% respectively on the 7thd. after exposure to

7、 Apigenin for 24 or 48 h, the cloneformation of SGC-7901 cells is suppressed in a dose- and time-dependent manner. The cloning efficiency in 80 M is9.8% and 5% after treatment with Apigenin for 24 and 48 h, while in the control group it is 40.4% and 43.4%2.体内研究 Apigenin (4,5,7-Trihydroxyflavone), a

8、natural flavonoid, possesses a broad spectrum of biological properties,including antioxidative, anti-inflammatory, anticancer, and neuroprotective effects. Apigenin (125 mg/kg and 250 mg/kg) alleviates Adriamycin (ADR) (24 mg/kg)-induced myocardial injury. Apigenin inhibits serum aspartate aminotran

9、sferase (AST) release. Apigenin reduces serum lactate dehydrogenase (LDH) release. Apigenin reduces serumcreatine kinase (CK) contents3.PROTOCOLCell Assay 2 The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of humangastric cancer SGC-7901 cell

10、s are harvested with 0.2% EDTA and plated at a density of 2.5103/well in 96-wellmicrotiter plates. After an overnight incubation to allow cell attachment, the medium is replaced by fresh mediumcontaining different concentrations (0, 20, 40, and 80 M) of Apigenin. Control wells receive DMSO (0.2%). E

11、achconcentration of Apigenin is repeated in four wells. After incubation for 24 h, one plate is assayed with a microplatereader at the wavelength of 570 nm. Before the assay, MTT (5 mg/mL in PBS) is added to each well and incubated for4 h, then MTT solution is removed from the wells by aspiration. A

12、fter careful removal of the medium, 0.1 mL ofDMSO is added to each well, and the plate is shaken for 15 min. The data of 7 d are fed into the computer and thegrowth curve is drawn. The growth inhibition rate (IR) is calculated2.MCE has not independently confirmed the accuracy of these methods. They

13、are for reference only.Animal Mice3Administration 3 Sixty healthy Kunming mice (262 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-doseApigenin (125 mg/kg/day, n=15),

14、and high-dose Apigenin (250 mg/kg/day, n=15). All Apigenin-treated groups aretreated daily via gastric gavage for seventeen days with a 125 or 250 mg/kg/day dose. ADR (3 mg/kg/day) isinjected intraperitoneally into animals at an interval of 48 h (in total, eight times at a cumulative dose of 24 mg/k

15、g).The mice in the control group receive injections of 0.9% sterile saline. On the 17th day after the first treatment, themice are sacrificed, and blood samples are collected. A number of hearts are fixed with 2.5% glutaraldehyde fixativefor electron microscopy analysis, and the others are stored at

16、 -80C for western blot analysis.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. Front Pharmacol. 2018 Jun 13;9:620.See more customer validations on HYPERLINK www.MedChemE

17、www.MedChemEREFERENCES1. 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 Co