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Investigational New Drugs

, Volume 37, Issue 4, pp 784–790 | Cite as

An orally antitumor chalcone hybrid inhibited HepG2 cells growth and migration as the tubulin binding agent

  • Wang Yan
  • Chen Xiangyu
  • Li Ya
  • Wang Yu
  • Xu FengEmail author
SHORT REPORT
  • 145 Downloads

Summary

Liver cancer is a kind of high mortality cancer due to the difficulty of early diagnosis. It is necessary to develop the anticancer agents to treat liver cancer. Here, a novel chalcone derivative was synthesized and evaluated for anticancer activity in vitro against liver cancer cell lines (HepG2, SNU-423, SMMC7221, and SNU-398). The chalcone hybrid 9 displayed the antiproliferative effect against HepG2, SNU-423, SMMC7221 and SNU-398 cells with IC50 values of 0.9 μM, 2.7 μM, 6.2 μM and 4.6 μM, respectively. Cellular mechanisms showed that derivative 9 could obviously inhibit HepG2 cells growth and colony formation in a concentration-dependent manner. Analogue 9 inhibited the migration by regulating the expression levels of migration-releated markers and transcription factors (Snail and Slug). Tubulin polymerization inhibition assay illustrated that chalcone hybrid 9 might be a potent tubulin polymerization inhibitor. Importantly, compound 9 displayed the antitumor activity against liver cancer HepG2 cells in vivo with the low toxicity toward mice. Therefore, compound 9 as a novel tubulin polymerization inhibitor deserves further investigation to treat liver cancer.

Graphical abstract

Compound 9 displayed the antitumor activity against liver cancer HepG2 cells in vivo and low toxicity toward mice Figure: Orally antitumor chalcone hybrid 9 inhibited HepG2 cells growth and migration as the tubulin binding agent.

Keywords

Chalcone Liver cancer Cell growth Migration Tubulin 

Notes

Acknowledgments

So thanks the supports from The First Affiliated Hospital of Zhengzhou University.

Author’s contribution

Wang Yan., Chen Xiangyu., Li Ya., and Wang Yu. performed the design work and experiments. Wang Yan., and Xu Feng. witten the paper. All authors read and approved the final manuscript.

Funding

This work was supported by the fund of The First Affiliated Hospital of Zhengzhou University.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Ethical approval

This article does not contain any studies with human participants or animals performed by any of the authors.

Informed consent

Informed consent was obtained from all individual participants included in the study.

Supplementary material

10637_2019_737_MOESM1_ESM.pdf (299 kb)
ESM 1 (PDF 298 kb)

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • Wang Yan
    • 1
  • Chen Xiangyu
    • 1
  • Li Ya
    • 1
  • Wang Yu
    • 1
  • Xu Feng
    • 1
    Email author
  1. 1.Department of GastroenterologyThe First Affiliated Hospital of Zhengzhou UniversityZhengzhouChina

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