漆黃素作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetFisetinCat. No.: HY-N0182CAS No.: 528-48-3分式: CHO分量: 286.24作靶點: Sirtuin; PPAR; TNF Receptor作通路: Cell Cycle/DNA Damage; Epigenetics; Apoptosis儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (174.68 mM)* means solu

2、ble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.4936 mL 17.4679 mL 34.9357 mL5 mM 0.6987 mL 3.4936 mL 6.9871 mL10 mM 0.3494 mL 1.7468 mL 3.4936 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存

3、時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.73 mM); Clear

4、solution此案可獲得 2.5 mg/mL (8.73 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.73 mM); Clear solution此案可獲得 2.5 mg/mL (8.73 mM，飽和度未知) 的澄清溶液。以 1 mL

5、作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。BIOLOGICAL ACTIVITY物活性 Fisetin種在許多果和蔬菜中發(fā)現(xiàn)的天然 酮醇，具有多種益處，如抗氧化，抗癌，神經(jīng)保護(hù)作。IC & Target Sirtuin, PPAR, TNF-alpha12體外研究 Fisetin inhibits lipid accumulation and suppresses the expression of PPAR in 3T3-L1 cells. Fiset

6、in suppresses earlystages of preadipocyte differentiation, and induces expression of Sirt1. Fisetin facilitates Sirt1-mediated deacetylationof PPAR and FoxO1, and enhances the association of Sirt1 with the PPAR promoter, leading to suppression of PPAR transcriptional activity, thereby repressing adi

7、pogenesis1. Fisetin binds to tubulin and stabilizes microtubules withbinding characteristics far superior than paclitaxel. Fisetin treatment of human prostate cancer cells results in robustup-regulation of microtubule associated proteins (MAP)-2 and -4. Fisetin significantly inhibits PCa cell prolif

8、eration,migration, and invasion. Nudc, a protein associated with microtubule motor dynein/dynactin complex that regulatesmicrotubule dynamics, is inhibited with Fisetin treatment2.體內(nèi)研究 Fisetin treatment to UVB exposed mice results in decreased hyperplasia and reduces infiltration of inflammatory cel

9、ls.Fisetin treatment also reduces inflammatory mediators such as COX-2, PGE2 as well as its receptors (EP1- EP4), andMPO activity. Furthermore, Fisetin reduces the level of inflammatory cytokines TNF, IL-1 and IL-6 in UVB exposedskin. Fisetin treatment also reduces cell proliferation markers as well

10、 as DNA damage as evidenced by increasedexpression of p53 and p21 proteins3.PROTOCOLCell Assay 1 3T3-L1 cells are transfected with reporter vector, and expression plasmids using TransIT-LT1. After 24 h, media isreplaced with viral supernatant. After 15-18 h of infection, media is replaced with DMI,

11、0.1 M troglitazone andFisetin (50 M). Cells are lysed using cell culture lysis buffer two days after addition of differentiation stimulus.Luciferase activity is determined using an analytical luminescence luminometer1.MCE has not independently confirmed the accuracy of these methods. They are for re

12、ference only.Animal Mice: The mice are divided into six groups of eight animals each. The mice in the first group are topically treated withAdministration 3 0.2 mL acetone and used as vehicle control. The mice in the second and third groups receive topical treatment ofFisetin 250 nmol/0.2 mL acetone

13、/mouse and 500 nmol/0.2 mL acetone/mouse respectively on their dorsal skin andserves as agent controls. The mice in the fourth, fifth and sixth groups are exposed to UVB. The mice in the fourthgroup receive a topical application of 0.2 mL acetone after 15 min of UVB exposure designated as vehicle co

14、ntrol.The mice in the fifth and sixth groups are treated with topical application of Fisetin 250 nmol/0.2 mL acetone/mouseand 500 nmol/0.2 mL acetone/mouse respectively on to their dorsal skin after 15 min of UVB exposure3.MCE has not independently confirmed the accuracy of these methods. They are f

15、or reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Kim SC, et al. Fisetin induces Sirt1 expression while inhibiting early adipogenesis in 3T3-L1 cells. Biochem Biophys Res Commun. 2015 Nov 27;467(4):638-44.2. Mukhtar E, et al. Dietary flavonoid fisetin binds to -tubulin and disrupts microtubule dynamics in prostate cancer cells. Cancer Lett. 2015 Oct28;