A Silver(I)-Estrogen Nanocluster: GSH Sensitivity and Targeting Suppression on HepG2 Cell

Small. 2016 Nov;12(44):6153-6159. doi: 10.1002/smll.201601936. Epub 2016 Sep 26.

Abstract

A structure-determined silver nanocluster of [Ag10 (Eth)4 (CF3 COO)6 (CH3 OH)3 ]·3C-H3 OH (Eth = ethisterone) (1), is firstly demonstrated by self-assembly of silver salt and ethisterone. Due to the thiophilicity of silver(I) ions, complex 1 shows reactivity with glutathione (GSH) molecules in solution and induces the fluorescence quenching behavior. Thus, complex 1 can be used as a fluorescent sensor for GSH. In consideration of the higher level of GSH in cancerous cells, complex 1 presents significant tumor suppression reactivity toward the human hepatocellular carcinoma (HepG2) cells with IC50 value of 165 × 10-9 m. Especially, complex 1 displays 3.4-fold higher in vitro cytotoxicity to HepG2 cells than that of the normal CCC-HEL-1 cells, which makes complex 1 a potential targeting suppression agent for cancerous cells. The molecular design of complex 1 not only generates a new medicine-silver(I) cluster family, but also opens a new avenue to the targeting anticancer organosilver(I) materials.

Keywords: HepG2 cells; ethisterone; luminescence; silver nanoclusters; targeting.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Cell Death / drug effects
  • Cell Shape / drug effects
  • Estrogens / pharmacology*
  • Ethisterone / pharmacology
  • Glutathione / metabolism*
  • Hep G2 Cells
  • Humans
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Silver / pharmacology*
  • Spectrometry, Fluorescence

Substances

  • Antineoplastic Agents
  • Estrogens
  • Silver
  • Glutathione
  • Ethisterone