PTUPB is a novel dual COX2 and sHE (soluble epoxide hydrolase) inhibitor. Treatment with PTUPB reduced body weight, liver weight, liver triglyceride and cholesterol content, and the expression of lipolytic/lipogenic and lipid uptake related genes (Acc, Cd36, and Cidec) in HFD mice. This made it be a promising potential therapy for liver steatosis associated with obesity.
PTUPB effectively inhibits both sEH and COX-2 enzymes, demonstrating IC50 values of 0.9 nM and 1.26 μM, respectively[1].
体内研究
PTUPB (subcutaneous injection; 30 mg/kg; 4 weeks) suppresses the growth of LLC tumors by 70-83% without manifesting any significant toxicity, like weight loss, in comparison to the control group. After continuous treatment, the peak concentration of PTUPB in the plasma is observed to be high[1].
PTUPB (subcutaneous injection; 5 mg/kg; once daily; 12 weeks) mitigates non-alcoholic fatty liver disease caused by a high-fat diet through the suppression of NLRP3 inflammasome activation. This treatment leads to a reduction in body and liver weight, as well as decreases in liver triglyceride and cholesterol levels. Furthermore, it lowers the expression of genes associated with lipolysis/lipogenesis and lipid uptake[2].
体外研究
PTUPB (1-10 μM; 24 hours) demonstrates inhibitory effects on human 5-LOX, achieving 83% inhibition at 10 μM and 44% inhibition at 1 μM, respectively[1].
PTUPB (10-20 μM; 72 hours) exerts a slight inhibitory action on the growth of various cancer cell types, such as human melanoma cells and transformed endothelial cells. Yet, it strongly impedes the proliferation of HUVEC cells when applied for a duration of three days[1].
PTUPB (10-20 μM; 72 hours) leads to a halt in the cell cycle at the G0/1 phase at various concentrations. The cell number percentages after PTUPB treatment are 65.15%, 66.87%, and 65.91% for concentrations of 10 μM, 15 μM, and 20 μM, respectively[1].
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