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Published on: May 14, 2016

Anticancer agent shikonin is an incompetent inducer of cancer drug resistance

Hao Wu1, Jiansheng Xie, Qiangrong Pan

  • 1Cancer Institute, the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, China.

Plos One
|January 10, 2013
PubMed
Abstract

Insights

Shikonin shows potent anticancer activity and is a weak inducer of cancer drug resistance. This natural compound can bypass existing drug resistance, making it a promising candidate for cancer therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Cancer drug resistance is a significant challenge in chemotherapy.
  • Developing anticancer drugs that do not induce resistance is crucial.
  • Shikonin and its analogs are known for potent tumoricidal effects and ability to bypass certain resistance mechanisms.

Purpose of the Study:

  • To investigate whether shikonin induces cancer drug resistance.
  • To evaluate shikonin's potential as a therapeutic agent that avoids resistance induction.

Main Methods:

  • Long-term (18-month) repeated treatment of cancer cell lines (K562, MCF-7, K562/Adr) with shikonin.
  • Assays for drug resistance development.
  • Gene expression profiling to understand resistance mechanisms.

Main Results:

  • Cells developed only a 2-fold resistance to shikonin and marginal resistance to other agents after 18 months.
  • No cross-resistance was observed with shikonin analogs or other anticancer drugs.
  • Gene expression analysis revealed strong cellular response to shikonin but failure to activate robust drug resistance pathways.
  • Shikonin-induced weak resistance correlated with increased βII-tubulin, which interacts with shikonin.

Conclusions:

  • Shikonin and its analogs exhibit potent anticancer activity and are weak inducers of drug resistance.
  • These compounds can overcome existing cancer drug resistance.
  • Shikonin's properties make it a promising candidate for cancer therapy, offering advantages in overcoming and avoiding drug resistance.

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