葡糖杀粉蝶菌素 A
- CAS号:108073-65-0
- 英文名:glucopiericidin A
- 中文名:葡糖杀粉蝶菌素 A
- CBNumber:CB71378053
- 分子式:C31H47NO9
- 分子量:577.71
- MOL File:108073-65-0.mol
葡糖杀粉蝶菌素 A性质、用途与生产工艺
- 生物活性 Glucopiericidin A 是一种天然的哌啶菌素化合物，从海洋衍生的链霉菌菌株获得。Glucopiericidin A 充当葡萄糖转运蛋白 (GLUT) 的化学探针，可以抑制糖酵解。Glucopiericidin A 与 Piericidin A (PA; HY-114936) 协同可以抑制 ATP 依赖性丝状伪足突起，而单独使用没有作用。Glucopiericidin A 通过增加 PRDX1 降低活性氧 (ROS) 水平来诱导细胞凋亡，同时在 ACHN 小鼠异种移植物中也表现出有效的抗肿瘤功效。
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体外研究
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 -
体内研究
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.
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