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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENeohesperidin dihydrochalconeCat. No.: HY-N0154CAS No.: 20702-77-6Synonyms: Neohesperidin DC; NHDC分式: CHO分量: 612.58作靶點(diǎn): Reactive Oxygen Species作通路: Immunology/Inflammation; Metabolic Enzyme/Protease; NF-B儲(chǔ)存式: Powder -20C 3 years
2、4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31 mg/mL (50.61 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6324 mL 8.1622 mL 16.3244 mL5 mM 0.3265 mL 1.6324 mL 3.2649 mL10 mM 0.1632 mL 0.8162 mL 1.6324 mL請(qǐng)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(chǔ)備液
3、,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Neohesperidin dihydrochalcone種合成的糖苷查酮,作為低熱量造甜味劑添加到各種品和飲料中。體外研究Neohesperidin dihydrochalcone shows remarkable radical scavenging activity against stable radical andreactive oxygen species (ROS) in concentration dependent manner. Especially, neohesperidin1/3 Mast
4、er of Small Molecules 您邊的抑制劑師www.MedChemEdihydrochalcone is the most potent inhibitor of H2O2 and HOCl. Neohesperidin dihydrochalcone shows HOClscavenging activity of 93.5% and H2O2 scavenging property of 73.5%. Neohesperidin dihydrochalconeshows extensive inhibitory effect especially on non-radical
5、 ROS H2O2 and HOCl with IC50 values of 205.1,25.5 M 1. Neohesperidin dihydrochalcone is found to be an activator of porcine pancreatic alpha-amylase(PPA) with an IC50 of 389 M 2.體內(nèi)研究 Neohesperidin dihydrochalcone administration results in significant reduction in activities of two usefulmarkers of l
6、iver damage, AST and ALT. The relative levels of NF-B, IL-6, IL-1 and TNF- protein in theliver of PQ-treated mice are inhibited by neohesperidin dihydrochalcone 3. The embryotoxicity/teratogenicityof neohesperidin dihydrochalcone is examined in Wistar Crl:(WI)WU BR rats. No adverse effects areobserv
7、ed at neohesperidin dihydrochalcone levels of up to 5% of the diet, the highest dose level tested, atwhich the rats consumed about 3.3 g/kg body weight/day 4.PROTOCOLCell Assay 1 WST-8 dye is used in the cell viability assay. HIT-T15 and HUVEC cells are grown and maintained inDulbeccos modified Eagl
8、es medium, supplemented with 10% fetal bovine calf serum. 1000 cells in eachwell are incubated with various concentrations of neohesperidin dihydrochalcone (50, 100, 500 M, 1 mM)and other compounds. After treating HIT-T15 and HUVEC cells with 500 M HOCl, WST-8 dye is added toeach well, and the absor
9、bance is detected at 420 nm with microplate reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: The embryotoxicity/teratogenicity of neohesperidin dihydrochalcone is examined in Wistar Crl:(WI)WUAdministration 34 BR rats. The study is
10、comprised of four groups of 28 mated female rats each, i.e., a control group (0%neohesperidin dihydrochalcone) and three treatment groups (1.25, 2.5, and 5% neohesperidindihydrochalcone). The general condition and behavior of the animals are observed twice daily. Body weightis determined on days 0,
11、7, 14, and 21 of gestation. Food consumption is determined during threeconsecutive periods (days 0-7, 7-14, and 14-21 of gestation) 4.3Mice: Neohesperidin dihydrochalcone is dissolved in a 0.5% CMC vehicle. Mice are randomized into fourgroups. The control group receives equal volume of vehicles thro
12、ughout. The PQ group receives saline oncedaily for 6 consecutive days. One hour after final saline treatment, mice are injected with PQ (75 mg/kg bodyweight). The neohesperidin dihydrochalcone group receives a daily dose of 200 mg/kg body weight by oralgavage for 6 consecutive days. One hour after f
13、inal neohesperidin dihydrochalcone treatment, mice areinjected with PQ (75 mg/kg body weight) 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Choi JM, et al. Antioxidant properties of neohesperidin dihydrochalcone: inhibition of hypochlor
14、ous acid-induced DNA strand breakage,protein degradation, and cell death. Biol Pharm Bull. 2007 Feb;30(2):324-30.2. Kashani-Amin E, et al. Neohesperidin dihydrochalcone: presentation of a small molecule activator of mammalian alpha-amylase as anallosteric effector. FEBS Lett. 2013 Mar 18;587(6):652-
15、8.3. Shi Q, et al. Artificial sweetener neohesperidin dihydrochalcone showed antioxidative, anti-inflammatory and anti-apoptosis effects2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEagainst paraquat-induced liver injury in mice. Int Immunopharmacol. 2015 Dec;29(2):722-9.4. Waalkens-Berendsen DH, et al. Embryotoxicity and teratogenicity study with neohesperidin dihydrochalcone in rats. Regul ToxicolP
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