CAS NO: | 327610-87-7 |
规格: | 98% |
分子量: | 539.57 |
包装 | 价格(元) |
100mg | 电议 |
50mg | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
20mg | 电议 |
Background:
NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo. IL-10[1]
NO-prednisolone (NCX-1015), an NO-releasing derivative of Prednisolone, is demonstrated to be more effective than Prednisolone in reducing inflammation, inhibiting cytokine and chemokine generation, and up-regulating the expression of the steroid-sensitive cell-surface marker CD163 in human peripheral blood mononuclear cells[1] Incubation of PBMCs with NO-prednisolone (NCX-1015) and Prednisolone produces a concentration-dependent activation of CD163. NO-prednisolone is more potent than Prednisolone at inducing CD163 cell surface expression. The increased efficacy of NO-prednisolone, compared with the parent molecule Prednisolone, is also observed when assessing inhibition of LPS induced IL-1β production[2].
In vivo treatment with NO-prednisolone (NCX-1015) potently stimulates IL-10 production, suggesting that the NO steroid induces a regulatory subset of T cells that negatively modulates intestinal inflammation. The two doses of NO-prednisolone tested, 0.5 and 5 mg/kg/day (equivalent to 0.33 and 3.3 mg/kg/day prednisone, respectively) effectively attenuates the severity of the wasting syndrome, ameliorates the colitis score, and reduces the colonic myeloperoxidase (MPO) activity. NO-prednisolone administration also reduces the colonic mRNA and protein content of tumor necrosis factor-α, IL-12, and IFN-γ. NO-prednisolone also reduces the expression of inducible NO synthase and cyclooxygenase-2 but in contrast does not inhibit colonic expression of IL-10 mRNA or protein. In fact, IL-10 expression is enhanced in mice treated with NO-prednisolone[1].
[1]. Fiorucci S, et al. NCX-1015, a nitric-oxide derivative of prednisolone, enhances regulatory T cells in the lamina propria and protects against 2,4,6-trinitrobenzene sulfonic acid-induced colitis in mice. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15770-5. [2]. Paul-Clark M, et al. 21-NO-prednisolone is a novel nitric oxide-releasing derivative of prednisolone with enhanced anti-inflammatory properties. Br J Pharmacol. 2000 Dec;131(7):1345-54.