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RGD Peptide-Conjugated Selenium Nanocomposite Inhibits Human Glioma Growth by Triggering Mitochondrial Dysfunction
Wenjian Liu1, Jing Su2, Qiang Shi1
1Department of Oncology, Second Affiliated Hospital of Shandong First Medical University, Shandong Academy of Medical Sciences, Taian, China.
Abstract:
Chemotherapy is still one of the most common ways to treat human glioblastoma in clinic. However, severe side effects limited its clinic application. Design of cancer-targeted drugs with high efficiency and low side effect is urgently needed. Herein, silver nanoparticles (Ag NPs) and nano-selenium (Se NPs) conjugated with RGD peptides (Ag@Se@RGD NPs) to target integrin high-expressed glioma were designed. The results found that Ag@Se@RGD NPs displayed stable particle size and morphology in physiological condition, and induced significant integrin-targeted intracellular uptake. Ag@Se@RGD NPs in vitro dose-dependently inhibited U251 human glioma cells growth by induction of cells apoptosis through triggering the loss of mitochondrial membrane potential, overproduction of reactive oxygen species (ROS), and MAPKs activation. However, ROS inhibition dramatically attenuated Ag@Se@RGD NPs-induced MAPKs activation, indicating the significant role of ROS as an early apoptotic event. Importantly, Ag@Se@RGD NPs administration in vivov effectively inhibited U251 tumor xenografts growth by induction of apoptosis through regulation MAPKs activation. Taken together, our findings validated the rational design that Ag-Se NPs conjugated with RGD peptides was a promising strategy to combat human glioma by induction of apoptosis through triggering mitochondrial dysfunction and ROS-dependent MAPKs activation.
Insights
New RGD peptide-conjugated silver-selenium nanoparticles effectively target and inhibit human glioblastoma growth by inducing apoptosis. This targeted nanoparticle approach offers a promising strategy for treating glioblastoma with reduced side effects.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Chemotherapy is a primary treatment for glioblastoma but causes severe side effects, necessitating the development of targeted therapies.
- Designing efficient, low-side-effect cancer drugs is crucial for improving glioblastoma treatment outcomes.
Purpose of the Study:
- To design and evaluate novel RGD peptide-conjugated silver-selenium nanoparticles (Ag@Se@RGD NPs) for targeted glioblastoma therapy.
- To investigate the in vitro and in vivo efficacy of Ag@Se@RGD NPs in inhibiting glioblastoma growth and inducing apoptosis.
Main Methods:
- Synthesis and characterization of Ag@Se@RGD NPs for stability and targeting capabilities.
- In vitro assessment of Ag@Se@RGD NPs' effects on U251 human glioma cells, including uptake, apoptosis induction, and mechanism investigation (ROS, mitochondrial potential, MAPKs).
- In vivo evaluation of Ag@Se@RGD NPs' efficacy in inhibiting U251 tumor xenografts in mice.
Main Results:
- Ag@Se@RGD NPs demonstrated stable physicochemical properties and efficient integrin-targeted uptake in glioma cells.
- In vitro studies showed dose-dependent inhibition of U251 cell growth via apoptosis, involving mitochondrial dysfunction, reactive oxygen species (ROS) overproduction, and MAPKs activation.
- ROS was identified as a key early event in Ag@Se@RGD NPs-induced apoptosis, as ROS inhibition attenuated MAPKs activation.
- In vivo administration of Ag@Se@RGD NPs effectively suppressed U251 tumor xenograft growth by inducing apoptosis through MAPKs pathway regulation.
Conclusions:
- The rational design of RGD peptide-conjugated Ag-Se NPs represents a promising strategy for combating human glioblastoma.
- Ag@Se@RGD NPs induce glioblastoma cell apoptosis through mitochondrial dysfunction and ROS-dependent MAPKs activation.
- This targeted nanoparticle approach holds potential for developing more effective and safer glioblastoma treatments.
