姜黄素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetCurcuminCat. No.: HY-N0005CAS No.: 458-37-7分式: CHO分量: 368.38作靶点: Histone Acetyltransferase; Epigenetic Reader Domain; Keap1-Nrf2; Autophagy;Mitophagy; Influenza Virus; Ferroptosis作通路: Epigenetics; NF-B; Autophagy; Anti-infection; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solven

2、t -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (271.46 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.7146 mL 13.5729 mL 27.1459 mL5 mM 0.5429 mL 2.7146 mL 5.4292 mL10 mM 0.2715 mL 1.3573 mL 2.7146 mL请根据产品在不同溶剂中的溶解度选择合适

3、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

4、： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (8.14 mM); Clear solution此案可获得 3 mg/mL (8.14 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 30.0 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)Page 1 of 2 w

5、ww.MedChemESolubility: 3 mg/mL (8.14 mM); Suspended solution; Need ultrasonic此案可获得 3 mg/mL (8.14 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。以 1 mL 作液为例，取 100 L 30.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 3 mg/mL (8.14 mM); Precipitated solution此案可获得 3 mg/mL (8.14

6、 mM，饱和度未知)以 1 mL 作液为例，取 100 L 30.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Curcumin (Diferuloylmethane)， 种天然酚类化合物， 酰转移酶 p300/CREB 结合蛋 特异性抑制剂，抑制组 蛋/组蛋的酰化和组蛋酰转移酶依赖的染质转录。Curcumin 对 NF-b 和 MAPKs 有抑制作，并具有抗炎、抗氧化、抗增殖和抗管成等多种药理作。IC & Target Keap1-Nrf21, Histone acetyltransferase6体外研究 Curcumi

7、n exerts its chemopreventive effects partly through the activation of nuclear factor (erythroid-2 related) factor2 (Nrf2) and its antioxidant and phase II detoxifying enzymes1. Curcumin inhibits T47D cells growth, with IC50s of 25,19 and 17.5 M for 24, 48 and 72 h MTT assays respectively. IC50s of c

8、urcumin and silibinin mixture against T47Dcells, are 17.5, 15, and 12 M for 24, 48, and 72 h exposure times, respectively2. Curcumin (2.5-80 M) inducesapoptotic cell death in AGS and HT-29 cell lines, and the IC50 is 21.90.1, 40.70.5 M, respectively, in both AGS andHT-29 cell lines. Curcumin-induced

9、 apoptosis requires caspase activities in AGS and HT-29 cells. Curcumin induces ERCa2+ decline and mitochondrial Ca2+ overloading3. Curcumin induces the G2/M cell cycle arrest of LNCaP and PC-3cells in a dose dependent manner. Curcumin upregulates the protein level of NF-kappaB inhibitor IkappaBalph

10、a anddownregulates protein levels of c-Jun and AR5.体内研究 Curcumin (10 mg/kg, p.o.) significantly prevents decrease in the percentage of sucrose consumption, as compared tothe CMS-exposed rats. Curcumin treatment results in significant prevention of increase in TNF- and IL-6 levels instressed rats4. C

11、urcumin decreases binding of p300/CREB-binding protein (CBP) at the brain-derived neurotrophicfactor (BDNF) promoter at 20 mg/kg (i.p.), reduces binding of P300/CBP at the BDNF promoter at 40 mg/kg, anddecreases binding all the four proteins of p300/CBP and H3K9ac/H4K5ac at the BDNF promoter at 60 m

12、g/kg inchronic constriction injury (CCI) rats6.PROTOCOLCell Assay 2 T47D breast cancer cell line is grown in RPMI 1640 supplemented with 10% FBS, 2 mg/mL sodium bicarbonate, 0.05mg/mL penicillin G, 0.08 mg/mL streptomycin. Culture is maintained on plastic flask and incubated at 37C in 5% CO2. After

13、growing sufficient amount of cells, cytotoxic effect of silibinin and curcumin is studied by 24, 48 and 72 h MTTassays in which 1000 cell/well are cultivated in a 96 well plate. After 24 h incubation in 37C with humidifiedatmosphere containing 5% CO2, the cells are treated with serial concentrations

14、 of curcumin (5, 10, 20, 30, 40, 50, 60,80, 100 M), silibinin (20, 40, 60, 80, 100, 120, 140, 180, 200 M), and curcumin-silibinin mixture (each of them 5, 10,20, 30, 40, 50, 60, 80, 100 M) for 24, 48 and 72 h in the quadruplicate manner, in addition to cells with 200 L culturemedium containing 10% D

15、MSO for control. After incubation, the medium of all wells of the plate are exchanged withfresh medium and the cells are leaved for 24 h in incubator. Then, medium of all wells are removed carefully and 50 L of 2 mg/mL MTT dissolved in PBS is added to each wells and the plate is covered with aluminu

16、m foil and incubatedPage 2 of 3 www.MedChemEfor 4.5 h again. After removing content of the wells, 200 L pure DMSO is added to the wells. Then, 25 L Sorensensglycine buffer is added and immediately absorbance of each wells is read in 570 nm using EL800 MicroplateAbsorbance Reader with reference wavel

17、ength of 630 nm.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Curcumin (10 mg/kg), freshly suspended in saline, is administrated by oral gavage once a day for 3 weeks. Forty ratsAdministration 4 are randomLy assigned to 4 groups (n=10/each grou

18、p): group I receives saline and serves as control, group IIreceives curcumin, group III is exposed to CMS andreceive saline and group IV are subjected to CMS andreceivecurcumin.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Syst. 2018

19、Apr 25;6(4):424-443.e7. J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. FASEB J. 2017 Sep;31(9):3800-3815. Eur J Immunol. 2020 Apr 27. Int J Mol Sci. 2019 Jan; 20(1): 28.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Gao S, et al. Curcumin attenuates arsenic-induced h

20、epatic injuries and oxidative stress in experimental mice through activation of Nrf2 pathway,promotion of arsenic methylation and urinary excretion. Food Chem Toxicol. 2013 Jul 18. pii: S0278-6915(13)0042. Nasiri M, et al. Curcumin and Silibinin Inhibit Telomerase Expression in T47D Human Breast Can

21、cer Cells. Asian Pac J Cancer Prev. 2013;14(6):3449-53.3. Cao A, et all. Curcumin induces apoptosis in human gastric carcinoma AGS cells and colon carcinoma HT-29 cells through mitochondrial dysfunction andendoplasmic reticulum stress. Apoptosis. 2013 Jul 24. Epub ahead of print4. Jiang H, et al. An

22、tidepressant-like effects of curcumin in chronic mild stress of rats: Involvement of its anti-inflammatory action. ProgNeuropsychopharmacol Biol Psychiatry. 2013 Jul 20. pii: S0278-5846(13)00150-4.5. Guo H, et al. Curcumin induces cell cycle arrest and apoptosis of prostate cancer cells by regulating the expression of IkappaBalpha, c-Jun and androgenreceptor.