ABSTRACT
【Objective】 To investigate the effects and molecular mechanism of Elafibranor (ELA) on the proliferation, migration and apoptosis of human prostate cancer (PCa) cells. 【Methods】 After PCa DU145 cells were treated with culture media containing different dosages of ELA, the proliferation, migration and apoptosis were determined with MTT assay, wound healing assay and Transwell assay, respectively. The expressions of genes related to lipid metabolism were detected with real-time quantitative polymerase chain reaction (real-time qPCR). 【Results】 The relative cell proliferation rate at 48 h was 100% in the blank control group, (86.9±7.8)% in the low-dose (5 μmol/L) group and (58.5±9.4)% in the high-dose (15 μmol/L) group;the wound healing rate at 24 h was (74.7±3.2)%, (61.8±2.9)% and (53.2±3.3)%;the relative percentage of migrated cells at 24 h was 100%, (32.4±11.2)% and (15.4±3.2)%;the cell apoptosis rate at 48 h was (9.3±1.4)%, (11.3±0.3)%, and (15.2±4.5)%, respectively, all P<0.05. After ELA treatment for 48 h, the genes related to fatty acid intake (SCPX, PLTP) and fatty acid oxidation (PDK1, ACOX2) were significantly down-regulated in the high-dose group, while the gene related to fatty acid deposition (PLIN2) was significantly up-regulated, indicating that the lipid metabolism pathway of DU145 cells was seriously interfered by the ELA treatment. 【Conclusion】 ELA can inhibit the proliferation and migration, and promote the apoptosis of prostate cancer cells by interfering in the lipid metabolism pathway, which exhibits remarkable potential of clinical translation in the field of anti-tumor chemotherapy.
ABSTRACT
A simple assay for detection of phospholipase C (PLC) activity was developed based on a fluorescence liposome probe using the Liss Rhod PE-loaded phospholipid liposomes.The liposome probe was prepared by the coassembly of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and fluorescent lipid (Liss Rhod PE).The probe showed very low background fluorescence due to fluorescence self-quenching effect of Liss Rhod PE.As the PLC enzyme selectively digested lipid, the Rhod fluorescence was recovered from its quenched state, leading to the sensitive detection of PLC.This assay provided a limit of detection (at a signal-to-noise ratio of 3) of 2 U/L for PLC.In the presence of PLC inhibitor, the fluorescent response of the sensor for PLC decreased, indicating that the assay could also be used for screening PLC inhibitors.