PTUPB

PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively[1].

PTUPB (1-10 μM; 24 hours) shows an inhibitory activity against human 5-LOX, exhibits a 83% and 44% inhibition at 10 μM and 1 μM, respectively[1].PTUPB (10-20 μM; 72 hours) has minimal inhibitory effects on cell proliferation in multiple cancer cell lines, including human melanoma cell and a transformed endothelial cell, whereas it potently inhibits HUVEC proliferation after 3 days of application[1].PTUPB (10-20 μM; 72 hours) induces cell cycle arrest at the G0/1 phase at different various. The percentage of cell number of PTUPB are 65.15%, 66.87%,and 65.91% at 10 μM, 15 μM, and 20 μM, respectively[1]. Cell Viability Assay[1] Cell Line: Multiple cancer cell lines: PC-3 cells, Met-1, H-1, A375, and transformed endothelial cell line (bEnd.3)

PTUPB (subcutaneous injection; 30 mg/kg; 4 weeks) inhibits LLC tumor growth by 70-83% and exhibits with no overt toxicity, such as any weight loss when it is compared with the control group. After a period of treatment, the peak plasma concentration of PTUPB is high[1].PTUPB (subcutaneous injection; 5 mg/kg; once daily; 12 weeks) ameliorates high-fat diet-induced non-alcoholic fatty liver disease via inhibiting NLRP3 inflammasome activation. It reduces body weight, liver weight, liver triglyceride and cholesterol content. It also decreases the expression of lipolytic/lipogenic and lipid uptake related genes[2]. Animal Model: C57BL/6 mice with LLC cells[1]

[1]. Sun CC, et al. PTUPB ameliorates high-fat diet-induced non-alcoholic fatty liver disease via inhibiting NLRP3 inflammasome activation in mice. Biochem Biophys Res Commun. 2020 Mar 19;523(4):1020-1026. [2]. Zhang G, et al. Dual inhibition of cyclooxygenase-2 and soluble epoxide hydrolase synergistically suppresses primary tumor growth and metastasis. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):11127-32. [3]. Hwang SH, et al. Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase.J Med Chem. 2011 Apr 28;54(8):3037-50.