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A small molecule for theraNOstic targeting of cancer cells

Govindan Ravikumar1, Meisam Bagheri, Deepak Kumar Saini

  • 1Department of Chemistry, Indian Institute of Science Education and Research, Pune, India. harinath@iiserpune.ac.in.

Chemical Communications (Cambridge, England)
|December 2, 2017
PubMed

Insights

A novel molecule, Thera/NO, generates nitric oxide (NO) and fluorescence. It selectively targets cancer cells, inducing DNA damage and death, while enabling real-time tracking of NO release.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Chemical Biology

Background:

  • Nitric oxide (NO) plays a crucial role in cellular signaling and disease.
  • Targeted delivery of NO to specific cells, particularly cancer cells, remains a challenge.
  • Developing tools to monitor NO production in living systems is essential for understanding its biological functions.

Purpose of the Study:

  • To develop and characterize Thera/NO, a small molecule probe for hydrogen peroxide-activated nitric oxide (NO) generation.
  • To investigate the selective release of NO by Thera/NO in cancer cells compared to primary cells.
  • To assess the potential of Thera/NO-mediated NO release to induce DNA damage and cell death in cancer cells.
  • To utilize the coupled fluorescence signal for real-time tracking of NO release in living cells.

Main Methods:

  • Synthesis and characterization of the Thera/NO small molecule.
  • In vitro studies using cancer cell lines and primary cells.
  • Assessment of NO generation in response to hydrogen peroxide.
  • Confocal microscopy to visualize fluorescence and track NO release.
  • Evaluation of DNA damage markers (e.g., gamma-H2AX) and cell viability assays (e.g., apoptosis assays).

Main Results:

  • Thera/NO was successfully synthesized and demonstrated activation by hydrogen peroxide to produce NO and a fluorescence signal.
  • Thera/NO exhibited preferential NO release in cancer cells over primary cells.
  • The released NO from Thera/NO triggered significant DNA damage and induced cell death in cancer cells.
  • The intrinsic fluorescence signal allowed for non-invasive, real-time monitoring of NO release dynamics within living cells without affecting NO availability.

Conclusions:

  • Thera/NO is a promising chemiluminescent probe for targeted NO generation and imaging.
  • Its selectivity for cancer cells offers a potential strategy for cancer therapy through NO-mediated DNA damage and apoptosis.
  • The coupled fluorescence reporting provides a valuable tool for studying NO signaling in complex biological environments.
  • Thera/NO facilitates the investigation of localized NO production and its downstream effects in living cells.

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