Cholesterol-directed nanoparticle assemblies based on single amino acid peptide mutations activate cellular uptake and decrease tumor volume

Adding cholesterol to peptides can increase anti-cancer activity

31 January 2018

Effective anti-cancer drug candidates could be found by systematically adding cholesterol to different points along the amino acid chains of naturally occurring peptides.

Researchers at the East China University of Science and Technology, with colleagues in the US and Sweden, modified an anti-microbial peptide found in bee venom, called halictines-2 (HAL-2), with the aim of enhancing it with anti-cancer activity. They added cholesterol units to different points on HAL-2, creating three new versions.

The version called HAL-C self-assembled into stable, evenly-sized nanoparticles that were able to enter ovarian cancer cells. They found the size of subcutaneous ovarian tumour grafts reduced by over 66 per cent when mice were intravenously injected with HAL-C for two weeks. The results suggest a strategy for identifying natural peptides that could be modified to develop potent anti-cancer activity.

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References

1. Chemical Science 8, 7552–7559 (2017). doi: 10.1039/c7sc02616a