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编 号:F618247
分子式:C43H67Cl2NO12
分子量:860.9
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生物活性:
AlbA-DCA is a conjugate formed by the attachment of Albiziabioside A (AlbA) to a dichloroacetate acid (DCA) subunit. AlbA-DCA can induce a marked increase in intracellular ROS and alleviate the accumulation of lactic acid in tumor microenvironment (TME), and also selectively kills cancer cells and induce apoptosis.

体内研究:
AlbA-DCA (2 mg/kg; subcutaneous injection; every 2 days; for 2 weeks; nude mice) treatment displays antitumor efficacy and almost completely suppresses tumor progression, and no mouse deaths and no significant changes in body weight are observed. AlbA-DCA has no obvious toxicity of liver and kidney and no major abnormality is observed in heart, liver, spleen, lung, and kidney.Animal Model:Nude mice bearing MCF-7 tumors
Dosage:2 mg/kg
Administration:Subcutaneous injection; every 2 days; for 2 weeks
Result:Displayed the best antitumor efficacy and almost completely suppressed tumor progression.

体外研究:
AlbA-DCA exhibits the cytotoxicity against the MCF-7 cells, HCT116 cells, A375 cells, 4T1 cells, HBMEC cells and LO2 cells with IC50 values of 0.43 μM, 3.87 μM, 3.78 μM, 1.31 μM, 38.20 μM and 53.14 μM, respectively.AlbA-DCA (2 μM; 24 hours; MCF-7 cells) treatment induces apoptotic cell death in MCF-7 cells.AlbA-DCA (2 μM; MCF-7 cells) treatment could significantly up-regulate the expression of cytochrome c and down-regulate the expression of antiapoptotic protein Bcl-2. AlbA-DCA significantly enhances the expression of caspase-9.
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