Α-NETA
Α-NETA 用途与合成方法
IC50: 9 μM (ChAT); 0.04 µM (ALDH1A1); CMKLR1; 84 µM (ChE); 300 µM (AChE)
α-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner.
α-NETA (2.5-10.0 µg/mL; 24 hours) leads to epithelial ovarian cancer (EOC) cell death associated with membrane blistering and cytoplasm leakage.
α-NETA treatment increases EOC cell expression of pyroptosis-associated proteins.
α-NETA is most potent in inhibiting aldehyde dehydrogenase 1 family, member A1 (ALDH1A1; IC
50
=0.04 µM; purified enzymes assay), followed by CMKLR1 (IC
50
=0.375 µM for β-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC
50
=0.50 µM; purified enzymes assay). α-NETA selectively inhibits chemerin-stimulated CMKLR1 association with β-arrestin2.
α-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety.
Cell Viability Assay
| Cell Line: | Ho8910, Ho8910PM, A2780, and Iose80 cells |
| Concentration: | 50, 100, 150 nM |
| Incubation Time: | 24 hours |
| Result: | Decreased all cell lines viability in a dose-dependent manner. |
Apoptosis Analysis
| Cell Line: | Epithelial ovarian cancer (EOC) cell |
| Concentration: | 2.5, 7.5, 10.0 µg/mL |
| Incubation Time: | 24 hours |
| Result: | Led to EOC cell death associated with membrane blistering and cytoplasm leakage. |
α-NETA (i.p.; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight.
α-NETA (s.c. injection; 3 mg/kg or 10 mg/kg; daily; for 30 days) significantly delays the onset of EAE with 3 mg/kg, and completely suppresses clinical signs for an average of nine days with 10 mg/kg beyond the first appearance of disease in control female C57BL/6 mice.
| Animal Model: | BALB/c nude mice with skov3 cells |
| Dosage: | 0.125 mg/kg |
| Administration: | IP; once every other day for 20 days |
| Result: | Significantly decreased tumor volume and tumor weight. |
