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AuNP Pyrazolo[3,4-d]pyrimidine Nanosystem in Combination with Radiotherapy against Glioblastoma
- Source :
- ACS Med Chem Lett
- Publication Year :
- 2020
-
Abstract
- [Image: see text] Gold-nanoparticle (AuNP)-conjugated drugs represent a promising and innovative antitumor therapeutic approach. In our study, we describe the design, the synthesis, the preparation, and the characterization of AuNPs conjugated with the pyrazolo[3,4-d]pyrimidine derivative SI306, a c-Src inhibitor. AuNPs–SI306 showed a good loading efficacy (65%), optimal stability in polar media and in human plasma, and a suitable morphological profile: a ζ-potential of −43.9 mV, a nanoparticle diameter of 48.6 nm, and a 0.441 PDI value. The antitumoral activity of AuNPs–SI306 was evaluated in vitro in the glioblastoma model, by the low-density growth assay, and also in combination with radiotherapy (RT). Results demonstrated that AuNPs had a basal radiosensitization ability and that AuNPs–SI306, when used in combination with RT, were more effective in inhibiting tumor cell growth with respect to AuNPs and free SI306.
- Subjects :
- Pyrimidine
medicine.medical_treatment
Nanoparticle
Conjugated system
01 natural sciences
Biochemistry
chemistry.chemical_compound
Drug Discovery
medicine
Gold nanoparticles
Nanotechnology
Tyrosine kinase Src inhibitor
Radiotherapy
010405 organic chemistry
Chemistry
Organic Chemistry
medicine.disease
In vitro
0104 chemical sciences
Radiation therapy
010404 medicinal & biomolecular chemistry
Human plasma
Colloidal gold
Biophysics
Glioblastoma
Subjects
Details
- Database :
- OpenAIRE
- Journal :
- ACS Med Chem Lett
- Accession number :
- edsair.doi.dedup.....f25cc5fb81adfcd90acb6d0841042ce0