2. Academic Validation
  3. Synthesis and biological evaluation of a novel artesunate-podophyllotoxin conjugate as anticancer agent

Synthesis and biological evaluation of a novel artesunate-podophyllotoxin conjugate as anticancer agent

  • Bioorg Med Chem Lett. 2016 Jan 1;26(1):38-42. doi: 10.1016/j.bmcl.2015.11.042.
Lei Zhang 1,  Fan Chen 2,  Zeguo Zhang 2,  Yongzheng Chen 2,  Jing Wang 3
Affiliations

Affiliations

  • 1 School of Pharmacy, Zunyi Medical University, 201 Dalian Road, Zunyi 563003, PR China. Electronic address: lzhang@zmc.edu.cn.
  • 2 School of Pharmacy, Zunyi Medical University, 201 Dalian Road, Zunyi 563003, PR China.
  • 3 School of Pharmacy, Zunyi Medical University, 201 Dalian Road, Zunyi 563003, PR China. Electronic address: wangjing@zmc.edu.cn.
PMID: 26615886 DOI: 10.1016/j.bmcl.2015.11.042
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.

Keywords

Apoptosis; Artesunate; Cell cycle; Cytotoxicity; Microtubule; Podophyllotoxin.

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