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Published on: September 3, 2013
Targeted delivery of nuclear targeting probe for bladder cancer using cyclic pentapeptide c(RGDfK) and acridine
Jiaxin Qin1,2, Qing Liang1,2, Guangyue Wang3
1Department of Urology, Xuzhou Clinical College of Xuzhou Medical University, Jiefang South Road, No. 199, Xuzhou, Jiangsu, China.
Purpose:
Both cyclic pentapeptide c(RGDfK) and acridine orange (AO) exhibit antitumor effects and cell permeability. This study aimed to evaluate the nuclear targeting efficiency and safety of the nuclear targeting probe for bladder cancer (BCa) synthesized by c(RGDfK) and AO.
Methods:
The nuclear targeting probe AO-(cRGDfK)2 was synthesized from AO hydrochloride, azided c(RGDfK), and a near-infrared skeleton synthesized via click chemistry reactions. The effect of the AO-(cRGDfK)2 probe on cell viability was assessed in BCa 5637 cells. The tumor cell targeting efficacy of the AO-(cRGDfK)2 probe was evaluated in BCa cells in vitro and in tumor-bearing mice in vivo. Nuclear-specific accumulation of fluorescence probe in BCa tumor cells was evaluated using laser scanning confocal microscopy (LSCM). Hematoxylin and eosin staining was performed to detect histopathological changes in the spleen, heart, liver, and kidney.
Results:
The AO-(cRGDfK)2 probe did not cause a significant reduction in cell viability. LSCM analysis showed that AO-(cRGDfK)2 exhibited nuclear-specific ambulation in BCa cells and was not accumulated in 293T cells. Also, this probe efficiently targeted tumor cells in the serum and urine samples. In vivo imaging system of tumor-bearing mice showed that ~ 80% percent of fluorescence signal was accumulated in the tumor sites. The probe did not change histopathology in the heart, liver, spleen, and kidney in tumor-bearing mice after the 21-day treatment.
Conclusions:
The AO-(cRGDfK)2 probe exhibited nuclear-specific accumulation in BCa cells without cytotoxicity, which provides an innovative alternative to improve anticancer therapy for BCa.
Insights
A novel nuclear targeting probe, AO-(cRGDfK)2, shows high efficiency and safety for bladder cancer (BCa) therapy. This probe specifically targets BCa cells, accumulating in the nucleus with no observed cytotoxicity or organ damage.
Area of Science:
- Biomedical Engineering
- Molecular Imaging
- Oncology
Background:
- Cyclic pentapeptide c(RGDfK) and acridine orange (AO) possess antitumor properties and cell permeability.
- Developing targeted nuclear probes is crucial for effective bladder cancer (BCa) therapy.
Purpose of the Study:
- To synthesize and evaluate a nuclear targeting probe, AO-(cRGDfK)2, for bladder cancer (BCa).
- To assess the nuclear targeting efficiency and safety of the AO-(cRGDfK)2 probe in BCa.
Main Methods:
- Synthesis of the AO-(cRGDfK)2 probe using click chemistry.
- Assessment of cell viability in BCa 5637 cells.
- In vitro and in vivo evaluation of tumor cell targeting efficacy using laser scanning confocal microscopy and in vivo imaging.
- Histopathological analysis of major organs (spleen, heart, liver, kidney).
Main Results:
- The AO-(cRGDfK)2 probe demonstrated no significant reduction in cell viability.
- Nuclear-specific accumulation of the probe was observed in BCa cells, with minimal uptake in 293T cells.
- In vivo imaging showed approximately 80% fluorescence signal accumulation at tumor sites in mice.
- No adverse histopathological changes were noted in major organs after 21 days of treatment.
Conclusions:
- The AO-(cRGDfK)2 probe exhibits nuclear-specific accumulation in BCa cells without cytotoxicity.
- This probe represents an innovative and safe approach for enhancing bladder cancer (BCa) therapy.
