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Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts[1][2]. | [in vivo]
Glucopiericidin A (0.8 mg/kg/day; IP; for three weeks) significantly reduces the final tumor weight of the mice[2].
| Animal Model: | Nude mice bearing ACHN tumor xenografts[2] | | 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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| [References]
[1] Mitsuhiro Kitagawa, et al. Metabolomic identification of the target of the filopodia protrusion inhibitor glucopiericidin A. Chem Biol. 2010 Sep 24;17(9):989-98. DOI:10.1016/j.chembiol.2010.06.017
[2] Xuefeng Zhou, et al. Exploring the Natural Piericidins as Anti-Renal Cell Carcinoma Agents Targeting Peroxiredoxin 1. J Med Chem. 2019 Aug 8;62(15):7058-7069. DOI:10.1021/acs.jmedchem.9b00598 |
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