Functionalisation of Fe ₃ O ₄ nanoparticles by 2‐((pyrazol‐4‐yl) methylene) hydrazinecarbothioamide enhances the apoptosis of human breast cancer MCF‐7 cells

Abstract

Cancer is a major cause of death. Thus, the incidence and mortality rate of cancer is globally important. Regarding vast problems caused by chemotherapy drugs, efforts have progressed to find new anti-cancer drugs. Pyrazole derivatives are known as components with anti-cancer properties. In here, Fe 3 O 4 nanoparticles were first functionalized with (3-chloropropyl) trimethoxysilane, then 2-((pyrazol-4-yl) methylene) hydrazinecarbothioamide (P) was anchored on the surface of magnetic nanoparticles (PL). The synthesized nano-compounds were characterized using Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, Zeta potential, dynamic light scattering, and energy-dispersive x-ray spectrometry analyses. The cytotoxicity effect was evaluated using MTT assay, apoptosis test by Flow cytometry, cell cycle analysis, Caspase-3 activity assay and Hoechst staining on MCF-7 cell line. The high toxicity for tumor cells and low toxicity on normal cells (MCF10A) was considered as an important feature (selectivity index, 10.9). Based on results, the IC50 for P and PL compounds were 157.80 and 131.84 μM/ml respectively. Moreover, apoptosis inducing, nuclear fragmentation, Caspase 3 activity and induction of cell rest in sub-G1 and S phases, were also observed. The inhibitory effect of PL was significantly higher than P, which could be due to the high penetrability of Fe 3 O 4 nanoparticles.

Co–Sn–Cu oxides/graphene nanocomposites as green catalysts for preparing 1,8‐dioxo‐octahydroxanthenes and apoptosis‐inducing agents in MCF‐7 human breast cancer cells

“…So far, many investigations were done based on metallic nanoparticles (metal oxides, metallic nanocomposites, magnetic nanoparticles, graphene‐based nanoparticles etc.) to find out effective anticancer drugs that play an important role in the apoptosis [ 72 , 73 , 74 , 75 , 76 , 77 ]. The presence of anionic phospholipids in cancer cells causes negative zeta potential that absorb into positively charged nanoparticles by strong electrostatic interaction [ 78 , 79 ].…”

Functionalizing Thiosemicarbazones for Covalent Immobilization on Nanoparticles

“…5H2O to yield a fully covalently linked [NP-TSC-Cu] conjugate with the Cu(II) ions bound by two different anchored 4-oxoacetophenone-TSC moieties [43]. In further recent reports, the surface of NPs was functionalized using materials such as dextran or chitosan before attaching TSCs or TSC complexes to them, but the character of the bonding between the TSCs and NP surface is not clear [49][50][51][52][53][54].…”