地奥司明作用机制 - Medchemexpress - MCE中国 - 副本

1、Product Data SheetDiosminCat. No.: HY-N0178CAS No.: 520-27-4分式: CHO分量: 608.54作靶点: Aryl Hydrocarbon Receptor作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (164.33 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制

2、备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；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

3、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： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.11 mM); Clear solution此案可获得 2.5 mg/mL (4.11 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L

4、20% 的 SBE-CD 理盐溶液中，混合均匀。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.11 mM); Clear solution; Need ultrasonic此案可获得 2.5 mg/mL (4.11 mM) 的澄 溶液，此案不适于实验周 期在半个以上的实验。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Diosmin在各种柑橘类果中发现的类黄

5、酮，也是芳烃受体 (AhR) 的激动剂。IC & Target AhR1体外研究 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.体内研究 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