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Published on: April 16, 2019
Targeted gene silencing using a follicle-stimulating hormone peptide-conjugated nanoparticle system improves its
Shanshan Hong, Xiaoyan Zhang1, Jun Chen
1Obstetrics and Gynecology Hospital, Fudan University, Shanghai 200011, People's Republic of China. xyzhang80@gmail.com.
Background:
RNA interference technology has shown high therapeutic potential for cancer treatment. However, serum instability, poor tissue permeability and non-specific uptake of short interfering RNA (siRNA) limit its administration in vivo. To overcome these limitations and improve the specificity for ovarian cancer, we developed a targeted nanoparticle delivery system for siRNA. This system included follicle-stimulating hormone (FSH) β 33-53 peptide as a targeting moiety that specifically recognized FSH receptor (FSHR) expressed on ovarian cancer cells. Growth regulated oncogene α (gro-α) has been reported to be involved in ovarian cancer development and progression. Thus, siRNA targeted to gro-α was used as an antitumor drug in this delivery system.
Methods:
FSH β 33-53 peptide-conjugated gro-α siRNA-loaded polyethylene glycol (PEG)-polyethylenimine (PEI) nanoparticles (FSH33-G-NP) were prepared and characterized by gel retardation assay and transmission electron microscopy. Particle size and zeta potential were determined. Expression of gro-α mRNA and protein was detected by real-time quantitative RT-PCR, immunocytochemistry and enzyme-linked immunosorbent assay. The proliferation, migration and invasion of the ovarian clear cell carcinoma cell line ES-2 were evaluated by cell counting kit-8 assay, cell scratch assay and transwell migration assay.
Results:
A siRNA sequence that is effective in silencing gro-α expression was obtained and loaded into the targeted delivery system. Compared with gro-α siRNA-loaded nanoparticles without FSH peptide modification (G-NP), FSH33-G-NP significantly down-regulated gro-α expression in ES-2 cells at mRNA and protein levels. Consequently, the aggressive biological behaviors of ES-2 cells, including proliferation, migration and invasion, were suppressed after silencing gro-α expression, and the addition of the FSH β 33-53 peptide enhanced the suppressive effects.
Conclusions:
This study indicated that a FSHR-mediated delivery system could mediate the highly selective delivery of siRNA into ovarian cancer cells and that silencing gro-α expression could be a potential choice for ovarian cancer treatment.
Insights
Targeted nanoparticles deliver short interfering RNA (siRNA) to ovarian cancer cells by targeting the FSH receptor. This approach effectively silences growth regulated oncogene alpha (gro-α), inhibiting cancer progression and offering a promising therapeutic strategy.
Area of Science:
- Biotechnology
- Nanomedicine
- Oncology
Background:
- RNA interference (RNAi) holds therapeutic promise for cancer but faces challenges in serum stability, tissue permeability, and non-specific uptake of short interfering RNA (siRNA).
- Ovarian cancer progression is linked to growth regulated oncogene alpha (gro-α), making it a target for therapeutic intervention.
- Follicle-stimulating hormone receptor (FSHR) is overexpressed on ovarian cancer cells, presenting a specific target for drug delivery.
Purpose of the Study:
- To develop a targeted nanoparticle delivery system for siRNA to overcome limitations of in vivo administration.
- To enhance specificity for ovarian cancer cells using a follicle-stimulating hormone (FSH) β 33-53 peptide targeting moiety.
- To investigate the therapeutic potential of silencing gro-α expression in ovarian cancer using this targeted system.
Main Methods:
- Preparation and characterization of FSH β 33-53 peptide-conjugated gro-α siRNA-loaded polyethylene glycol (PEG)-polyethylenimine (PEI) nanoparticles (FSH33-G-NP).
- Assessment of nanoparticle characteristics including gel retardation, transmission electron microscopy, particle size, and zeta potential.
- Evaluation of gro-α mRNA and protein expression, and assessment of ovarian cancer cell proliferation, migration, and invasion.
Main Results:
- FSH33-G-NP nanoparticles effectively delivered siRNA and significantly down-regulated gro-α expression in ovarian cancer cells (ES-2) at both mRNA and protein levels.
- Silencing gro-α expression suppressed proliferation, migration, and invasion of ES-2 cells.
- The presence of the FSH β 33-53 peptide enhanced the suppressive effects on cancer cell behaviors.
Conclusions:
- A FSHR-mediated nanoparticle delivery system enables highly selective delivery of siRNA into ovarian cancer cells.
- Targeted silencing of gro-α expression represents a potential therapeutic strategy for ovarian cancer treatment.
- The developed targeted delivery system shows promise for improving the efficacy and specificity of siRNA-based cancer therapies.
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