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Supramolecular alleviation of cardiotoxicity of a small-molecule kinase inhibitor

Xue Yang1, Qiaoxian Huang, David Bardelang

  • 1State Key Laboratory of Quality Research in Chinese Medicine, and Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau, China. rwang@umac.mo.

Organic & Biomolecular Chemistry
|August 11, 2017
PubMed

Insights

Small-molecule kinase inhibitors (SMKIs) like sorafenib can cause cardiotoxicity. Encapsulating sorafenib with cucurbit[7]uril (CB[7]) reduced toxicity in zebrafish while maintaining anti-cancer efficacy.

Area of Science:

  • Oncology
  • Supramolecular Chemistry
  • Pharmacology

Background:

  • Small-molecule kinase inhibitors (SMKIs) are vital cancer therapeutics.
  • Sorafenib (SO), a widely used SMKI, exhibits significant cardiotoxicity.
  • Managing SMKI-induced side effects is crucial for patient outcomes.

Purpose of the Study:

  • To investigate the potential of cucurbit[7]uril (CB[7]) encapsulation to mitigate sorafenib's cardiotoxicity.
  • To evaluate if CB[7] encapsulation preserves the anti-cancer efficacy of sorafenib.
  • To explore a novel supramolecular strategy for improving SMKI safety.

Main Methods:

  • In vivo zebrafish model for assessing cardiotoxicity.
  • In vitro and in vivo cancer and angiogenesis models for evaluating anti-cancer activity.
  • Supramolecular complex formation between sorafenib and cucurbit[7]uril.

Main Results:

  • Encapsulation of sorafenib with CB[7] significantly alleviated cardiotoxicity in a zebrafish model.
  • The anti-cancer and anti-angiogenesis activities of sorafenib were retained after CB[7] encapsulation.
  • Demonstrated preserved therapeutic efficacy alongside reduced toxicity.

Conclusions:

  • Cucurbit[7]uril encapsulation offers a promising strategy to reduce the cardiotoxicity of sorafenib.
  • Supramolecular complexation can enhance the safety profile of small-molecule kinase inhibitors.
  • This approach may lead to improved therapeutic options for cancer patients.

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