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  • Title: Synthesis and biological evaluation of a novel artesunate-podophyllotoxin conjugate as anticancer agent.
    Author: Zhang L, Chen F, Zhang Z, Chen Y, Wang J.
    Journal: Bioorg Med Chem Lett; 2016 Jan 01; 26(1):38-42. PubMed ID: 26615886.
    Abstract:
    A novel conjugate of artesunate-podophyllotoxin was prepared and evaluated for its cytotoxicity against diverse normal and multidrug resistance human cancer cell lines by CCK-8 assay. The conjugate exhibited good cytotoxicity on all the cell lines with IC50 values of 0.453±0.156-3.011±0.272μM and reduced the resistant factor. The conjugate was further found to disrupt the microtubule network and induce G2/M cell cycle arrest in multidrug resistance K562/ADR cells. Meanwhile, Hoechst staining analysis suggested that conjugate induced cell death by apoptosis. Furthermore, conjugate could downregulate the levels of P-glycoprotein (P-gp) in P-gp overexpressing K562/ADR cells.
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