葡糖杀粉蝶菌素 A
葡糖杀粉蝶菌素 A 用途与合成方法
Glucopiericidin A has cytotoxicities against three renal carcinoma cell lines, ACHN (IC
50
=0.21 μM), OS-RC-2 (IC
50
>100 μM), and 786-O (IC
50
>100 μM), as well as a normal renal cell line, HK-2 (IC
50
>100 μM).
Glucopiericidin A (25, 50 nM; 24 h) causes the upregulation of PRDX1 in ACHN cells.
Glucopiericidin A (25, 50 nM; 24 h) not only raises the expression of mRNA and protein of PRDX1 but also forces it into the nucleus.
Glucopiericidin A (25, 50 nM; 24 h) reduces ROS in normal ACHN cells.
Neither Glucopiericidin A (GPA) nor Piericidin A (PA) alone, at concentrations up to 500 nM and 2.3 mM, respectively, shows inhibitory activity. When combined, much lower concentrations of GPA (17 nM) and PA (0.68 nM) produces inhibition of filopodia protrusion.
Western Blot Analysis
| Cell Line: | ACHN cells |
| Concentration: | 25 and 50 nM |
| Incubation Time: | 24 hours |
| Result: | Caused the upregulation of PRDX1 in ACHN cells. |
RT-PCR
| Cell Line: | ACHN cells |
| Concentration: | 25 and 50 nM |
| Incubation Time: | 24 hours |
| Result: | Not only raised the expression of mRNA and protein of PRDX1 but also forced it into the nucleus |
Glucopiericidin A (0.8 mg/kg/day; IP; for three weeks) significantly reduces the final tumor weight of the mice.
| Animal Model: | Nude mice bearing ACHN tumor xenografts |
| Dosage: | 0.8 mg/kg |
| Administration: | IP; daily; for three weeks |
| Result: |
Significantly reduced the final tumor weight of the mice.
Increased the mRNA and protein expression of PRDX1 in tumor tissues. |
