高車前苷作用機制 - Medchemexpress - MCE中國

1、Product Data SheetHomoplantagininCat. No.: HY-N1949CAS No.: 17680-84-1分式: CHO分量: 462.4作靶點: TNF Receptor; NF-B作通路: Apoptosis; NF-B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 : 50 mg/mL (108.13 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 m

2、M 2.1626 mL 10.8131 mL 21.6263 mL5 mM 0.4325 mL 2.1626 mL 4.3253 mL10 mM 0.2163 mL 1.0813 mL 2.1626 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?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保

3、證實驗結果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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 (5.41 mM); Clear solution此案可獲得 2.5 mg/mL (5.41 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 儲備液加到 400 L

4、 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 (5.41 mM); Clear solution此案可獲得 2.5 mg/mL (5.41 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 900 L 20% 的 SBE-CD 理鹽溶液中，混合BIOLO

5、GICAL ACTIVITY物活性 Homoplantaginin來中藥Salvia plebeia的具有抗炎和抗氧化活性的類黃酮。IC & Target p65 TNF-體外研究 Homoplantaginin shows IC50 of reduction level of DPPH radical at 0.35 g/mL. In human hepatocyte HL-7702 cellsexposed to H2O2, the addition of 0.1-100g/mL of homoplantaginin significantly reduces lactate dehydr

6、ogenaseleakage, and increases glutathione, glutathione peroxidase and superoxide dismutase in supernatant1.Homoplantaginin (0.1, 1, 10 M) dose-dependently reduces expression of toll-like receptor-4 evoked by palmitic acid(100 M). Homoplantaginin tightly controlls palmitic acid-induced reactive oxyge

7、n species to prevent nucleotide-binding domain-like receptor 3 (NLRP3) inflammasome activation by suppressing reactive oxygen species-sensitivethioredoxin-interacting protein, NLRP3, and caspase-12. Pre-treatment of homoplantaginin on human umbilical veinendothelial cells significantly inhibits palm

8、itic acid induced TNF- and IL-6 mRNA expression, and IKK and NF-Bp65 phosphorylation. Homoplantaginin significantly modulates the Ser/Thr phosphorylation of IRS-1, improvesphosphorylation of Akt and endothelial nitric oxide synthase, and increases NO production in the presence of insulin3.體內(nèi)研究 Homop

9、lantaginin(25-100mg/kg) significantly reducesthe increase in serum alanine aminotranseferase and aspartateaminotransferase, decreases the levels of TNF- and IL-1. The same treatment also reduces the content of thiobarbituric acid-reactive substances, elevates the levels of GSH, GSH-Px and SOD in hep

10、atic homogenate1.Homoplantaginin is rapidly absorbed (Tmax=16.008.94min), reaching a mean Cmax between 0.77 and 1.27nmol/mL.The absolute oral bioavailability is calculated to be only 0.75%.PROTOCOLCell Assay 3 The viability of cultured cells is determined using the MTT assay. Human umbilical vein en

11、dothelial cells are exposedto various concentrations of homoplantaginin (0.1, 1, 3, 10, 30, 100 M) for 48 h. Subsequently, 20 L of MTT (5mg/mL) is added to each well for an additional 4 h at 37C. The supernatant is removed, and DMSO is added todissolvethe formazan crystals. The optical absorbance is

12、 measured at 540 nm3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Homoplantaginin is dissolved in a solution consistingof DMSO, PEG 400, ethanol and normal saline(2:2:3:3,Administration 14 v/v/v/v) at a concentration of 10 mg/mL. The rat

13、s are randomly divided into three groups to receive oraladministration(150 mg/kg), tail vein injection (15 mg/kg) and peritoneal injectionv (15 mg/kg). Blood samples(approximately 0.5 mL) are collected from the retro-orbital plexus into heparinized microfugetubes at 5, 10, 20, 30,45, 60, 90, 120, an

14、d 180 min after administration. The plasma samples, separated by centrifuging the blood samplesat 10,000 rpm4.Mice: Homoplantaginin is dissolved in 5% amylum. Homoplantaginin is administered orally by gastric intubationduring the experimental period at doses of 25, 50, 100 mg/kg/d, respectively. Eig

15、ht hours after injection of LPS, themice are anesthetized with ether and blood samples are collected by exsanguination from the inferior vein. The liveris removed and fixed in formalin for histological analysis1.MCE has not independently confirmed the accuracy of these methods. They are for referenc

16、e only.Page 2 of 3 www.MedChemEREFERENCES1. Qu XJ, et al. Protective effects of Salvia plebeia compound homoplantaginin on hepatocyte injury. Food Chem Toxicol. 2009 Jul;47(7):1710-5.2. He B, et al. Homoplantaginin Inhibits Palmitic Acid-induced Endothelial Cells Inflammation by Suppressing TLR4 and

17、 NLRP3 Inflammasome. J CardiovascPharmacol. 2016 Jan;67(1):93-101.3. Wu F, et al. Homoplantaginin modulates insulin sensitivity in endothelial cells by inhibiting inflammation. Biol Pharm Bull. 2012;35(7):1171-7.4. Cong Y, et al. Pharmacokinetics of homoplantaginin in rats following intravenous, peritoneal injection and oral administration. J Pha