生物活性

• 描述Endothelial cells (EC) can regulate the permeability in brain endothelium which is helpful to overcome the restriction of drug delivery into the brain. Dexamethasone Sodium Phosphate is a phosphate form of Dexamethasone. Dexamethasone is a corticosteroid medication used in modulating tight junction permeability and interleukin receptor modulator with different EC50 values and IC50 values in different kind of cells. GPNT cells treated with 1 μM dexamethasone demonstrated no change in transendothelial resistance, which decreased the permeability and reduced the size of the small pore as well. Dexamethasone treatment can lead to IL-6 and RPM18226 repressions with IC50 values of 1.4 and 6.5 nM respectively. The binding Ki of glucocorticoid receptor (GR) and mineralocorticoid (MR) were 2.1 and 7.2 nM respectively. While in human SW1353 cells, dexamethasone treatment showed an IC50 of GR binding of 3.5nM, the IC50 for transrepression of IL-1 induced MMP-13 expression and transrepression HWB-TNFα were 1.8 and 21 nM respectively. In LPS stimulated human PBMCs, DM affected cytokine production with EC50 values ranging from 10 to 72 nM, while the values were ranged from 0.47 to 4.1 nM and from 0.92 to >200 nM in Anti-CD3 and PHA stimulated human PBMCs respectively. In human H13 cells, DM inhibited GR with EC50 of 9.7 nM, all together suggesting a good in vitro and in vivo anti-inflammatory activity of this compound . DM exposure in the 5-month-old ewes demonstrated unchanged blood pressure and eNOS RNA and protein levels, increased sensitivity to endothelin-1 (ET), enhanced acetylcholine-induced relaxation and abolished L-NAME suppressible vasodilatory response to ET, suggesting that DM led to endothelial dysfunction and vasodilatory compensation in these animals.

• 动物研究
  剂量	Rat: 4 mg/kg[3] (i.p.), 10 mg/kg[4] (i.p.)
  给药途径	i.p.