染料木苷作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetGenistinCat. No.: HY-N0595CAS No.: 529-59-9分式: CHO分量: 432.38作靶點(diǎn): Autophagy作通路: Autophagy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 (231.28 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1

2、mM 2.3128 mL 11.5639 mL 23.1278 mL5 mM 0.4626 mL 2.3128 mL 4.6256 mL10 mM 0.2313 mL 1.1564 mL 2.3128 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，再依次添加助溶劑：為

3、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 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.78 mM); Clear solution此案可獲得 2.5 mg/mL (5.78 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 400

4、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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.78 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.78 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 20% 的 SBE-CD 理鹽溶液中，混合均勻。3.

5、請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.78 mM); Clear solution此案可獲得 2.5 mg/mL (5.78 mM，飽和度未知) 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)。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 Genistin和產(chǎn)品的主要異黃酮。體外研究 Genistin is the major isoflavonoid of soybeans and soy prod

6、ucts. Genistin shows a dose-dependent superoxidescavenging effect and exhibits major effect at 200 M, corresponding in activity to 0.08 U/mg protein superoxidedismutase (SOD). Results demonstrate that Genistin exhibits a significantly (P0.01) and a dose-dependent inhibitoryeffect on the human cancer

7、 cell examined, and at higher concentration (100 M), the cell viability is 59%. Genistin alsoinduces a significant and dose-dependent increase in ROS formation when compare with the untreated control1.體內(nèi)研究 Myocardial infarct is markedly diminished by pretreatment with Genistin, particularly at the h

8、igh dose. After 1 h ofreperfusion, preconditioning with Genistin at dosages of 20 to 60 mg/kg significantly attenuats the release of lactate dehydrogenase (LDH), creatine kinase (CK) in a dose-dependent manner compare with the I/R group. Results showthat the level of malondialdehyde (MDA) is decreas

9、ed and the activities of superoxide dismutase (SOD) and catalase(CAT) are increased as well as an increased glutathione (GSH) level in a dose-dependent manner by Genistintreatment in I/R. Pretreatment with Genistin (20, 40 and 60 mg/kg) also prevents the expression of P2X7, p-IB, andp-NF-B p65 compa

10、re with the model group2.PROTOCOLCell Assay 1 M14 human melanoma cells are used and grown in RPMI containing 10% fetal calf serum, 100 U/mL penicillin, 100 g/mL streptomycin, and 25 g/mL fungizone. After 24 h of incubation at 37C under a humidified 5% carbon dioxideto allow cell attachment, the cell

11、s are treated with different concentrations (12, 25, 50, and 100 M) of Genistin anddaidzin, and incubated for 72 h under the same conditions1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Sprague-Dawley rats (male, 250 to 300 g) are used to est

12、ablish the I/R injury animal model and used in thisAdministration 2 experiment. Rats are randomly apportioned in equal animals (n=10) to five experimental groups: (1) sham group: ratsare subjected to the entire surgical procedure but without the induction of I/R; (2) model group: I/R injury animalmo

13、del is constructed by left anterior descending coronary artery (LAD) ligation for 30 min, and then the LAD isallowed 1 h reperfusion; and (3) three Genistin-treated groups: different doses (20, 40, and 60 mg/kg body weight,resp.) of Genistin dissolved in 0.5% sodium carboxyl methyl cellulose (CMC-Na

14、) solution are given intragastrically for5 days before operation2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Russo A, et al. Genistin inhibits UV light-induced plasmid DNA damage and cell growth in human melanoma cells. J Nutr Biochem. 2006 Feb;17(2):103-8.Page 2 of 3 www.MedChemE2. Gu M, et al. Cardioprotective Effects of Genistin in Rat Myocardial Ischemia-Reperfusion Injury Studies by Regulation of P2X7/NF-B Pathway. Evid BasedComplement Alternat Med. 2016;2016:5381290.