Graphene nanocomposites
have gained significant interest in a variety
of biological applications due to their unique properties. Herein,
we have studied the apoptosis-inducing ability and anticancer properties
of functionalized highly reduced graphene oxide (HRG) and gold nanoparticles
(Au NPs)-based nanocomposites (AP-HRG-Au). Samples were prepared under
facile conditions via simple stirring and ultrasonication. All the
samples were tested for their anticancer properties against different
human cancer cell lines including lung (A549), liver (HepG2), and
breast (MCF-7) cancer cells using doxorubicin as a positive control.
In order to enhance the solubility and bioavailability of the sample,
HRG was functionalized with 1-aminopyrene (1-AP) as a stabilizing
ligand. The ligand also facilitated the homogeneous growth of Au NPs
on the surface of HRG by offering chemically specific binding sites.
The synthesis of nanocomposites and the surface functionalization
of HRG were confirmed by UV–Vis, powder X-ray diffraction,
and Fourier transform infrared spectroscopy. The structure and morphology
of the as-prepared nanocomposites were established by high-resolution
transmission electron microscopy. Because of the functionalization,
the AP-HRG-Au nanocomposite exhibited enhanced physical stability
and high dispersibility. A comparative anticancer study of pristine
HRG, nonfunctionalized HRG-Au, and 1-AP-functionalized AP-HRG-Au nanocomposites
revealed the enhanced apoptosis ability of functionalized nanocomposites
compared to the nonfunctionalized sample, whereas the pristine HRG
did not show any anticancer ability against all tested cell lines.
Both HRG-Au and AP-HRG-Au have induced a concentration-dependent reduction
in cell viability in all tested cell lines after 48 h of exposure,
with a significantly higher response in MCF-7 cells compared to the
remaining cells. Therefore, MCF-7 cells were selected to perform detailed
investigations using apoptosis assay, cell cycle analysis, and reactive
oxygen species measurements. These results suggest that AP-HRG-Au
induces enhanced apoptosis in human breast cancer cells.