Inclusion of Quercetin in Gold Nanoparticles Decorated with Supramolecular Hosts Amplifies Its Tumor Targeting Properties.
Mustafa YilmazApostolos A KaranastasisMaria V ChatziathanasiadouMehmet OguzAnastasia KougioumtziNausicaa ClementeTahsin F KelliciNikolaos E ZafeiropoulosApostolos AvgeropoulosThomas MavromoustakosUmberto DianzaniSerdar KarakurtAndreas G TzakosPublished in: ACS applied bio materials (2019)
Despite the anticancer potential of natural products (NPs), their limited bioavailability necessitates laborious derivatization or covalent conjugation to delivery vehicles. To unleash their potential, we developed a nanohybrid delivery platform with a noncovalently tunable surface. Initially, the active compound was encapsulated in a macrocycle, p -sulfonatocalix[4]arene, enabling a 62 000-fold aqueous solubility amplification as also a 2.9-fold enhancement in its cytotoxicity with respect to the parent compound in SW-620 colon cancer cells. A pH stimuli responsive behavior was recorded for this formulate, where a programmable release of quercetin from the macrocycle was monitored in an acidic environment. Then, a nanoparticle gold core was decorated with calixarene hosts to accommodate noncovalently NPs. The loaded nanocarrier with the NP quercetin dramatically enhanced the cytotoxicity (>50-fold) of the parent NP in colon cancer and altered its cell membrane transport mode. In vivo experiments in a mouse 4T1 tumor model showed a reduction of tumor volume in mice treated with quercetin-loaded nanoparticles without apparent toxic effects. Further analysis of the tumor-derived RNA highlighted that treatment with quercetin-loaded nanoparticles altered the expression of 27 genes related to apoptosis.
Keyphrases
- drug delivery
- cancer therapy
- gold nanoparticles
- reduced graphene oxide
- oxidative stress
- metabolic syndrome
- quantum dots
- magnetic resonance imaging
- high throughput
- wound healing
- magnetic resonance
- genome wide
- cell death
- human health
- dna methylation
- liquid chromatography tandem mass spectrometry
- insulin resistance
- simultaneous determination
- cell proliferation
- long non coding rna
- silver nanoparticles
- single cell
- contrast enhanced