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

• Published in: Small (Weinheim an der Bergstrasse, Germany) Vol. 12; no. 44; pp. 6153 - 6159
• Main Authors: Shen, De-Feng, Wu, Shan-Shan, Wang, Rui-Rui, Zhang, Qiang, Ren, Zhong-Juan, Liu, Hong, Guo, Hua-Dong, Gao, Guang-Gang
• Format: Journal Article
• Language: English
• Published: Germany Blackwell Publishing Ltd 01.11.2016; Wiley Subscription Services, Inc
• Subjects: Antineoplastic Agents - pharmacology; Cell Death - drug effects; Cell Shape - drug effects; Displays; Estrogens - pharmacology; ethisterone; Ethisterone - pharmacology; Fluorescence; Glutathione; Glutathione - metabolism; Hep G2 Cells; HepG2 cells; Humans; In vitro testing; luminescence; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Nanostructure; Nanotechnology; Particle Size; Quenching; Self assembly; Silver - pharmacology; silver nanoclusters; Spectrometry, Fluorescence; targeting; Toxicity; silver nanoclusters; targeting; HepG2 cells; luminescence; ethisterone
• ISSN: 1613-6810; 1613-6829
• DOI: 10.1002/smll.201601936

A structure‐determined silver nanocluster of [Ag10(Eth)4(CF3COO)6(CH3OH)3]·3C­H3OH (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. A structure‐determined silver nano­­­cluster of [Ag10(Eth)4(CF3COO)6(CH3OH)3]·3CH3OH (Eth = ethisterone) (1), demonstrated for the first time, shows reactivity with glutathione molecules in solution and induces the fluorescence quenching behavior. Complex 1 displays 3.4‐fold higher in vitro cytotoxicity to HepG2 cells than that of the normal CCC‐HEL‐1 cells, which makes 1 a potential targeting suppression agent for cancerous cells.