地奧司明作用機(jī)制 - Medchemexpress - MCE中國 - 副本

1、Product Data SheetDiosminCat. No.: HY-N0178CAS No.: 520-27-4分式: CHO分量: 608.54作靶點(diǎn): Aryl Hydrocarbon Receptor作通路: Immunology/Inflammation儲(chǔ)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(shí)驗(yàn) DMSO : 100 mg/mL (164.33 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制

2、備儲(chǔ)備液1 mM 1.6433 mL 8.2164 mL 16.4328 mL5 mM 0.3287 mL 1.6433 mL 3.2866 mL10 mM 0.1643 mL 0.8216 mL 1.6433 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加

3、助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.11 mM); Clear solution此案可獲得 2.5 mg/mL (4.11 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(chǔ)備液加到 900 L

4、20% 的 SBE-CD 理鹽溶液中，混合均勻。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.11 mM); Clear solution; Need ultrasonic此案可獲得 2.5 mg/mL (4.11 mM) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Diosmin在各種柑橘類果中發(fā)現(xiàn)的類黃

5、酮，也是芳烴受體 (AhR) 的激動(dòng)劑。IC & Target AhR1體外研究 Treatment with Diosmin causes a dose dependent increase in the amount of adducts formed (up to a 7-fold increasein adducts at 5 M Diosmin). At 5 M, Diosmin increases the cytotoxicity of 7,12-dimethylbenz(a)anthracene (DMBA),shifting the IC50 of DMBA from an e

6、stimated 1.2 M to 400 nM. Diosmin is not cytotoxic in itself at the concentrationstested. Diosmin causes an increase in CYPIAI activity in MCF-7 cells in a time- and dose-dependent fashion. Diosmincauses a dose-dependent increase in CYPIAI mRNA after 24 h of incubation, causes a long-lasting increas

7、e in CYPIAImRNA accumulation that reaches its peak after 48 h of incubation1.體內(nèi)研究 Diosmin significantly decreases the malondialdehyde (MDA) levels and increases the activities of total-superoxidedismutase (T-SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) in the retina of rats compare with

8、 theischemia group (P0.05), and suppresses the ischemia/reperfusion (I/R)-induced reduction in the a- and b-waveamplitudes of the electroretinograms (ERGs) (P0.05). The thickness of the entire retina, inner nuclear layer, innerplexiform layer, and outer retinal layer and the number of cells in the g

9、anglion cell layer are significantly less after I/Rinjury (P0.05), and Diosmin remarkably ameliorates these changes on retinal morphology. Diosmin also attenuatesthe I/R-induced loss of retinal ganglion cells (RGCs) of the rat retina (P0.05)2.PROTOCOLCell Assay 1 MCF-7 cells are plated at 25,000 cel

10、ls/well in 24-well plates. After 24 h, the medium is changed to medium containing5 M Diosmin. After an additional 24 h, the medium is again changed with medium containing 5 M Diosmin. After 3days, the total cell growth is assessed by sulforhodamine1.MCE has not independently confirmed the accuracy o

11、f these methods. They are for reference only.Animal Healthy male Wistar rats (n=112) weighing 180 to 200 g each are used in this study. The animals are randomlyAdministration 2 assigned to the following 4 groups, which include combinations of the ischemia/reperfusion (I/R) injury model orsham injury

12、 with the i.g. administration of Diosmin or vehicle solution: sham+vehicle (SV) group, sham+Diosmin (SD)group, model+vehicle (MV) group, and model+Diosmin (MD) group. For intragastric administration, 5 mL of 2%Diosmin per kilogram weight of the rat, or the same volume of vehicle solution, is adminis

13、tered intragastrically 30min before the onset of ischemia, and then daily after I/R injury until the animals are sacrificed. Using an overdose ofanesthesia, 8 rats from each group are sacrificed 24 h after I/R injury, and their eyeballs harvested for determinationof the malondialdehyde (MDA) level a

14、nd the activities of total-superoxide dismutase (T-SOD), glutathione peroxidase(GSH-Px), and catalase (CAT). At 7 days post-I/R injury, electroretinograms (ERGs) are recorded in 6 rats per group.Meanwhile, 6 rats in each group are randomly chosen for retrograde labeling of retinal ganglion cells (RG

15、Cs) , andthe remaining 8 rats from each group are histopathologically examined2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ciolino HP, et al. Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affectcytochrome P450 1A1 activity. Cancer Res.Page 2 of 3 www.MedChemE1998 Jul 1;58(13):2754-60.2. Tong N, et al. Diosmin protects rat retina from ischemia/reperfusion injury. J Ocul Pharmacol Ther. 2012 Oct