A novel bioactive nanoparticle synthesized by conjugation of 3-chloropropyl trimethoxy silane functionalized Fe3O4 and 1-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-2-(4-phenylthiazol-2-yl) hydrazine: assessment on anti-cancer against gastric AGS cancer cells

Mol Biol Rep. 2020 Mar;47(3):1637-1647. doi: 10.1007/s11033-020-05251-7. Epub 2020 Jan 13.

Abstract

Gastric cancer is one of the common types of cancer around the world which has few therapeutic options. Nitrogen heterocyclic derivatives such as thiazoles are used as the basis for the progression of the drugs. The objective of this study was to synthesize the 1-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl) methylene)-2-(4-phenylthiazol-2-yl) hydrazine (TP) conjugating with (3-Chloropropyl) trimethoxysilane (CPTMOS)-coated Fe3O4 nanoparticles (NPs) for anti-cancer activities against gastric AGS cancer cell line. The synthesized Fe3O4@CPTMOS/TP NPs were characterized by FT-IR, XRD, EDX, SEM, TEM and Zeta potential analyses. To evaluate the toxicity of the above compound after AGS cell culture in RPMI1640 medium, the cells were treated at different concentrations for 24 h. The viability of the cells was investigated by MTT assay. Moreover, apoptosis induced by Fe3O4@CPTMOS/TP NPs was assessed by Hoechst 33432 staining, oxygen activity specification evaluation, caspase-3 activity assay, cell cycle analysis and annexin V/PI staining followed by flow cytometry analysis. The IC50 value in AGS cells was estimated to be 95.65 µg/ml. The flow cytometry results of Fe3O4@CPTMOS/TP NPs revealed a large number of cells in the apoptotic regions compared to the control cells and the cells treated with TP. In addition, the amount of ROS production and caspase-3 activity increased in the treated cells with Fe3O4@CPTMOS/TP NPs. The percentage of inhibited cancer cells in the G0/G1 phase increased under the treatment in the binding state to the nonionic iron oxide nanoparticles. Overall, this study showed that Fe3O4@CPTMOS/TP NP had effect on induction of apoptosis and inhibiting the growth of AGS cancer cells. Thus, Fe3O4@CPTMOS/TP NP can be considered as a new anti-cancer candid for next phase of studies on mouse models.

Keywords: (3-Chloropropyl) trimethoxysilane; Flow cytometry; Gastric cancer; Iron oxide nanoparticle; MTT; Thiazole.

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Ferric Compounds / chemistry*
  • Humans
  • Hydrazines / chemistry*
  • Hydrazines / pharmacology
  • Microscopy, Electron
  • Models, Chemical
  • Molecular Structure
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Necrosis
  • Reactive Oxygen Species / metabolism
  • Silanes / chemistry*
  • Spectroscopy, Fourier Transform Infrared
  • Stomach Neoplasms / metabolism
  • Stomach Neoplasms / pathology*
  • X-Ray Diffraction

Substances

  • 3-chloropropyltrimethoxysilane
  • Antineoplastic Agents
  • Ferric Compounds
  • Hydrazines
  • Reactive Oxygen Species
  • Silanes