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编 号:F406867
分子式:C5H8O3
分子量:116.12
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生物活性:
Ethyl pyruvate is a simple derivative of the endogenous metabolite pyruvate. Ethyl pyruvate is an HMGB1 release inhibitor. Ethyl pyruvate can induce apoptosis by autophagy. Ethyl pyruvate has anti-inflammatory, antioxidant and anti-tumor activity. Ethyl pyruvate can be used in the study of neurodegenerative diseases such as Alzheimer's and Parkinson's disease.

体内研究:
Ethyl pyruvate (80 mg/kg, 腹腔注射, 连续 9 天) 在小鼠肝脏肿瘤模型中可抑制肿瘤生长。Ethyl pyruvate (2 或40 mg/kg, 腹腔注射) 在百草枯中毒大鼠模型中具有降低脂质过氧化和抗炎作用。Animal Model:Liver tumor model in mice
Dosage:80 mg/kg
Administration:i.p., 30 min before tumor injection and daily up to 9 days and daily from 7 to 10 days after infusion of tumor cells.
Result:Decreased innate immune cells (NK cells, monocytes) and T and B cell lymphocytic infiltrates.Inhibited the release of HMBG1.
Animal Model:Paraquat-intoxicated rats
Dosage:2 or 40 mg/kg
Administration:30 min before or 1 h after paraquat (50 mg/kg i.p.)
Result:Decreased the MDA concentrations at 6 and 24 h.Decreased NO concentrations significantly at 6 h and GSH concentrations in the lung.

体外研究:
Ethyl pyruvate (10 mM, 1 h) 在 1-10 mM 范围内对 N9 microglial 细胞没有毒性作用,通过抑制 HMGB1/ NF-κB /miR-223 信号通路减弱小胶质 NLRP3 炎性体的激活。Ethyl pyruvate (10-40 mM, 6, 24 h) 在 MC38 细胞中可诱导细胞凋亡。Ethyl pyruvate (5-15 mM, 2 h) 对小鼠腹腔巨噬细胞的 IC50 值为 28.83 mM,通过抑制 caspase-11 依赖性细胞焦亡来预防内毒素血症和败血症。
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