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Synthesis of Core-shell Lanthanide-doped Upconversion Nanocrystals for Cellular Applications
Published on: November 10, 2017
Bifunctional up-converting lanthanide nanoparticles for selective in vitro imaging and inhibition of cyclin D as
Chi-Fai Chan1, Ming-Kiu Tsang, Hongguang Li
1Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong. klwong@hkbu.edu.hk.
Abstract:
Inhibition of the CDK4/cyclin D complex through the substrate recruitment site on the cyclin positive regulatory subunit is recognised as being a promising anti-cancer target. Specific peptide sequences can be used to selectively disrupt this target, but the development of peptides as anti-tumor agents in vitro/in vivo presents several obstacles. Poor cell internalization, low sensitivity towards enzymatic degradation in vivo, and ineffectiveness in monitoring via indirect screening are all issues which must be overcome. Herein, we describe the surface functionalization of lanthanide nanoparticles with cyclin D-specific peptides to prepare novel nanomaterials (UCNPs-P1) which can target the CDK4/cyclin D complex. The nanomaterials prepared (UCNPs-P1) are cell permeable and they display parallel emission spectra in vitro and in an aqueous biological environment. They can also be used in low dose concentrations under harmless NIR excitation and emission via upconversion. Uniquely, in addition to acting as a bioimaging probe, UCNPs-P1 also exhibits promising cytotoxicity towards cancer cells. In light of the aforementioned properties, the prepared functionalized nanomaterials (UCNPs-P1) offer the first real dual acting system for cyclin D imaging and simultaneous inhibition of cancer cell division.
Insights
Researchers developed novel lanthanide nanoparticles functionalized with cyclin D-specific peptides. These nanoparticles target the CDK4/cyclin D complex, enabling dual bioimaging and cancer cell inhibition.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- The CDK4/cyclin D complex is a key anti-cancer target, but peptide-based inhibitors face challenges like poor cell penetration and degradation.
- Developing effective therapeutic and diagnostic agents for cancer remains a significant challenge.
Purpose of the Study:
- To create novel nanomaterials targeting the CDK4/cyclin D complex for dual bioimaging and anti-cancer therapy.
- To overcome the limitations of traditional peptide-based cancer treatments.
Main Methods:
- Surface functionalization of lanthanide nanoparticles (UCNPs) with cyclin D-specific peptides (P1) to create UCNPs-P1.
- Characterization of UCNPs-P1 for cell permeability, spectral properties, and upconversion luminescence.
- Evaluation of UCNPs-P1's cytotoxicity against cancer cells.
Main Results:
- UCNPs-P1 demonstrated cell permeability and stable emission spectra in vitro and biological environments.
- The nanomaterials function effectively at low doses under near-infrared (NIR) excitation via upconversion.
- UCNPs-P1 exhibited significant cytotoxicity towards cancer cells, acting as a dual-action agent.
Conclusions:
- Functionalized lanthanide nanoparticles (UCNPs-P1) offer a promising dual-acting system for cyclin D imaging and cancer cell inhibition.
- This novel approach addresses key limitations of peptide-based anti-cancer agents, paving the way for new cancer therapies.
