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CAS No. : 908-54-3
MCE 国际站:Diminazene aceturate
产品活性:Diminazene aceturate (Diminazene diaceturate) 是一种抗锥虫活性分子,适用于牲畜。Diminazene aceturate 的锥虫杀虫作用的主要生化机理是通过与富含腺嘌呤-胸腺嘧啶碱基对的位点发生特异性相互作用,以非插入方式与锥虫动子体 DNA (kDNA) 结合。Diminazene aceturate 还是血管紧张素转化酶 2 (ACE2) 的激活剂,并具有强而有效的抗炎特性。
研究领域:Anti-infection | Metabolic Enzyme/Protease
作用靶点:Parasite | Angiotensin-converting Enzyme (ACE)
In Vitro: Pre-treatment of bone marrow-derived macrophages (BMDM) and dendritic cells (BMDC) with Diminazene aceturate (Berenil) downregulats LPS-, CpG- and Poly I:C-induced proinflammatory cytokine production, suggesting that it may be affecting common pathways through which these molecules stimulate proinflammatory cytokine production. Indeed, Diminazene aceturate does not alter the expression of different TLRs (including TLR2, TLR4 and TLR9), on macrophages and DCs when assessed by flow cytometry. Instead, Diminazene aceturate dramatically downregulats the phosphorylation of MAPKs (ERK, p38 and JNK), STATs (STAT1 and STAT3) and NFκB p65 subunit, which are key signaling molecules and transcription factors involved in the production of proinflammatory cytokines.
In Vivo: Diminazene aceturate (14 mg/kg; intraperitoneal injection; female BALB/c mice and C57BL/6 mice) treatment significantly reduces the percentages of CD25+ cells, a concomitant reduction in the percentage of regulatory (CD4+Foxp3+) T cells and a striking reduction in serum levels of disease exacerbating pro-inflammatory cytokines including IL-6, IL-12, TNF and IFN-γ.
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