产品
编 号:F514954
分子式:C22H29N9O6
分子量:515.52
产品类型
结构图
CAS No: 908-54-3
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产品详情
生物活性:
Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.
体内研究:
Diminazene aceturate aceturate (14 mg/kg;腹膜内注射;雌性 BALB/c 小鼠和 C57BL/6 小鼠) 显著降低 CD25+ 细胞的百分比,同时降低调节性 (CD4+Foxp3+) T 细胞的百分比,也显著降低疾病加重的促炎细胞因子(包括 IL-6、IL-12、TNF 和 IFN-γ)的血清水平。Animal Model:Female BALB/c mice and C57BL/6 mice (6-8 week old) infected with T. congolense variant antigenic type TC1
Dosage:14 mg/kg
Administration:Intraperitoneal injection
Result:Significantly reduced 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.
体外研究:
用 Diminazene aceturate 预处理骨髓来源的巨噬细胞 (BMDM) 和树突状细胞 (BMDC) 可下调 LPS-、CpG-和 Poly I:C 诱导的促炎细胞因子的产生,这表明它可能通过以下途径影响常见途径这些分子刺激促炎细胞因子的产生。事实上,当通过流式细胞术评估时,Diminazene aceturate 不会改变巨噬细胞和树突状细胞上不同 TLR (包括 TLR2、TLR4 和 TLR9) 的表达。相反,Diminazene aceturate 显著下调 MAPK (ERK、p38 和 JNK)、STAT (STAT1 和 STAT3) 和 NFκB p65 亚基的磷酸化,它们是参与促炎细胞因子产生的关键信号分子和转录因子。