NO-prednisolone 是释放一氧化氮 (NO) 的 Prednisolone 衍生物。NO-prednisolone 有效刺激体内 IL-10 产生。

NO-prednisolone is a nitric oxide (NO)-releasing derivative of Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.

Solid

IL-10

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 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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[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-
[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.

In Vitro: DMSO : 25 mg/mL (46.33 mM; ultrasonic and warming and heat to 60°C)配制储备液