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编 号:F036420
分子式:C99H140N20O17
分子量:1882.29
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1mg
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生物活性:
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).

体内研究:
Gramicidin A (0.11 mg/kg; intratumoral injection; twice weekly for 14 days) inhibits the growth of RCC tumor xenografts.Gramicidin A (0.22 mg/kg; intratumoral injection; thrice weekly for 26 days) inhibits the growth and angiogenesis of VHL-expressing RCC tumor xenografts.Animal Model:Female hairless Nu/J mice, 6- to 8-week old, injected subcutaneously with a suspension of SN12C cells (1.0 × 106) in a 50% growth factor–reduced Matrigel solution
Dosage:0.11 mg/kg body weight
Administration:Intratumoral injection, twice weekly for 14 days
Result:The average tumor mass was reduced by approximately 40% without significant toxicity.
Animal Model:Female hairless 6- to 8-week-old Nu/J mice, injected subcutaneously with a suspension of Caki-1-td-Tomato cells (1.5 × 106) in a 50% growth factor-reduced Matrigel solution.
Dosage:0.22 mg/kg
Administration:Intratumoral injection, thrice weekly for 26 days
Result:Inhibited tumor growth. HIF-2α and GAPDH protein expression was substantially reduced.

体外研究:
Gramicidin A displays potent broad-spectrum antibiotic activity against Gram-positive strains, even multidrug-resistant strains.Gramicidin A has the disadvantage of high hemolytic activity.Gramicidin A (0.1 nM-10 μM, 72 h) reduces the viability of RCC cell lines and affects cell viability comparable to Monensin (HY-N4302).Gramicidin A cellular sensitivity is significantly altered by neither VHL nor HIF-1α expression.Gramicidin A (1 and 10 μM, 48 or 72 h) induces nonapoptotic cell death in RCC cells.Gramicidin A (0-10 μM, 24 h) depletes cellular energy and induces metabolic dysfunction in RCC cells.Gramicidin A (0-1 μM, 24-72 h) reduces HIF-1α and HIF-2α protein expression, reduces HIF transcriptional activity and target gene expression (24 h)
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