橙皮素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetHesperetinCat. No.: HY-N0168CAS No.: 520-33-2分式: CHO分量: 302.28作靶點: p38 MAPK; Apoptosis; Autophagy作通路: MAPK/ERK Pathway; Apoptosis; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (330.82 mM; Need ultrasonic)SolventMass1 mg 5

2、 mg 10 mgConcentration制備儲備液1 mM 3.3082 mL 16.5410 mL 33.0819 mL5 mM 0.6616 mL 3.3082 mL 6.6164 mL10 mM 0.3308 mL 1.6541 mL 3.3082 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。-80C 儲存時，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?。以下溶解案都請先按?

3、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 (8.27 mM); Clear solution此案可獲得 2.5 mg/mL (8.27 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L

4、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 (8.27 mM); Clear solution此案可獲得 2.5 mg/mL (8.27 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 90

5、0 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.27 mM); Clear solution此案可獲得 2.5 mg/mL (8.27 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Hesperetin亡。種天然 烷酮類物質(zhì)，為有效的，譜的 UGT 抑制劑。Hesperetin 可通過激活

6、 p38 MAPK 來誘導(dǎo)凋體外研究 Hesperetin has the retention of antioxidant potential in self nano-emulsifying drug delivery system1. Hesperetin andNGR display broad-spectrum inhibition against human UGTs. Besides, Hesperetin exhibits strong inhibitory effects onUGT1A1, 1A3 and 1A9 (both IC50 and Ki values lower

7、 than 10 M) and moderately inhibits UGT1A4, UGT1A7, UGT1A8(IC50 values 29.68-63.87 M)2. Hesperetin interacts with different types of proteins involving hydrogen bonds, pi-pieffects, pi-cation bonding and pi-sigma interactions with varying binding energies. Hesperetin exhibits drug-likeproperties whi

8、ch projects its potential as a therapeutic option for CHIKV infection3. Hesperetin dose-dependentlyreduces GCDCA-induced caspase-3 activity in cultured primary rat hepatocytes. Hesperetin also dose-dependentlyreduces CM-induced Nos2 (iNOS) expression in hepatocytes. Interestingly, hesperetin-induced

9、 expression of theantioxidant gene haem oxygenase 1 (HO-1) about fourfold compared with cytokine mixture alone5.體內(nèi)研究 Preadministration of Hesperetin (40 mg/kg b.w., oral) significantly attenuates the Cd-induced oxidative stress andmitochondrial dysfunction, restores the antioxidant and membrane-boun

10、d enzyme activities and decreases apoptosisin the brain of rats4. Hesperetin (200 mg/kg) attenuates Con A-induced hepatocyte apoptosis and hepatic Nos2(iNOS) expression in mice. Hesperetin co-treatment also decreases the occurrence of apoptotic bodies, hydropicdegeneration, nuclear fragments, autoly

11、sis and haemorrhage. The number of leukocytes infiltrated in liver tissue ofmice with D-GalN/LPS-induced fulminant hepatitis are significantly decreased by hesperetin in a murine model5.PROTOCOLKinase Assay 4 First, 0.5 mL tissue homogenate is diluted with 1 mL water. Then, to this mixture, 2.5 mL e

12、thanol and 1.5 mLchloroform (all reagents chilled) are added and shaken for 1 min at 4C, then centrifuged. The enzyme activity in thesupernatant is determined. The assay mixture contained 1.2 mL sodium pyrophosphate buffer (0.025 M, pH 8.3), 0.1mL 186 mM phenazine methosulfate (PMS), 0.3 mL 30 mM Ni

13、troblue tetrazolium (NBT), and 0.2 mL of nicotinamideadenine dinucleotide (NADH), and appropriately diluted enzyme preparation and water in a total volume of 3 mL.Reaction is initiated by the addition of NADH. After incubation at 30C for 90 min, the reaction is stopped by theaddition of 1 mL glacial

14、 acetic acid. The reaction mixture is stirred vigorously and shaken with 4 mL n-butanol. Theintensity of the chromogen in the butanol layer is measured at 560 nm against a butanol blank. A system withoutenzyme served as control. One unit of enzyme activity is defined as 50% inhibition of NBT reducti

15、on in 1 min underthe assay conditions.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal After 7 days of adjusting, the animals are randomly divided into 10 experimental groups. Control group (n=8): TheseAdministration 4 animals are treated with the

16、 equivalent volume of PBS as used for the administration of Con A and D-GalN/LPS.Control hesperetin group (n=8): The mice are treated with hesperetin 400 mg/kg p.o. in 0.5% sodiumcarboxymethylcellulose (CMC-Na) solution for 10 days. Con A group (n=15): The animals are treated with the samePage 2 of

17、3 www.MedChemEvolume of CMC-Na as used for administration of hesperetin for 10 days and are challenged with Con A (i.v.15mg/kg). Con A + hesperetin groups: The animals receive various doses of hesperetin (100, 200, 400 mg/kg) p.o. for10 days before Con A injection (each group n=15). D-GalN/LPS group

18、 (n=15): The animals are given CMC-Na for 10days and injected i.p. with D-GalN (700 mg/kg)/LPS (5 g/kg). D-GalN/LPS + hesperetin groups: Three doses ofhesperetin (100, 200, 400 mg/kg) are given to mice once daily for 10 days. D-GalN (700 mg/kg)/LPS (5 g/kg) areinjected i.p. (each group n=15).MCE has

19、 not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Cell Signal. 2020 Mar 18:109606. Eur J Pharmacol. 2019 Jun 5;852:151-158. Nutr Cancer. 2019 Jul 11:1-8.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Arya A, et al. B

20、ioflavonoid hesperetin overcome bicalutamide induced toxicity by co-delivery in novel SNEDDS formulations: Optimization, in vivoevaluation and uptake mechanism. Mater Sci Eng C Mater Biol Appl. 2017 Feb 1;71:954-9642. Liu D, et al. Inhibitory Effect of Hesperetin and Naringenin on Human UDP-Glucuronosyltransferase Enzymes: Implications for Herb-Drug Interactions.Biol Pharm Bull. 2016;39(12):2052-2059.3. Oo A, et al. In silico study on anti-Chikungunya virus activity of hesperetin. PeerJ. 2016 Oct 26;4:e2602. eCollection 2016.4. Sha