Study of the Cytotoxic and Bactericidal Effects of Sila‐substituted Thioalkyne and Mercapto‐thione Compounds based on 1,2,3‐Triazole Scaffold

Abstract

A series of sila-organosulphur compounds containing 1,2,3-triazole cores were screened for their cytotoxic activity on human breast cancer cell line MCF-7. Most of the tested compounds exhibited moderate-to-good activity against the cancer cells. Especially, the compound 4-((2-(trimethylsilyl)ethynylthio)methyl)-1-benzyl-1H-1,2,3-triazole (3a) from series of sila-substituted thioalkyne 1,2,3-triazoles (STATs) and the compounds 3-(1-benzyl-1H-1,2,3-triazol-4-yl)-1-mercapto-1,1-bis(trimethylsilyl)propane-2-thione (4a) and 1-mercapto-1,1-bis(trimethylsilyl)-3-(1-phenethyl-1H-1,2,3-triazol-4-yl)propane-2-thione (4e) from series of sila-substituted mercapto-thione 1,2,3-triazoles (SMTTs) exhibited promising cytotoxicity against MCF-7 with IC values of 35.17, 32.63 and 30.3 μg/mL, respectively. In addition, the possible mechanisms for inhibition of cell growth and induction of apoptotic cell death were explored by DAPI staining, cell cycle analysis and qRT-PCR. The synthetic compounds were evaluated for their in vitro antibacterial activities, and as a result, the most prominent effects were observed for 3e and 4e. Especially, 3e was found to be quite active against all the tested strains with the MIC values ranging from 15 to 62 μg/mL, except P. aeruginosa. The results of the time-kill assay suggested that the compound of 3e completely inhibited the growth of both gram-negative bacteria, A. baumannii, and gram-positive bacteria, S. aureus. In addition, SEM analysis confirmed morphostructural damage of the bacteria. Our findings could be applicable for developing dual-targeting anticancer/antibacterial therapeutics.

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“…For the cDNA synthesis, an appropriate proportion of RNA was taken from each sample and reverse transcribed through RevertAid Firststrand cDNA synthesis Kit (Fermentas, St Leon-Rot, Germany). A Real-Time PCR system was followed using Syber Green Master Mix (BioMolecular Systems, Australia) for the target genes relating to the stated primers as described previously [29].…”

The effect of SiO2/Au core–shell nanoparticles on breast cancer cell’s radiotherapy

“…The fixed cells then, transferred to 4 C for two days. For FACS studies the cells were washed with PBS, incubated for 45 min by Ribonuclease A (Cinaclon), and were stained b Propidium Iodide (Sigma) in dark place [21] to measure fluorescent intensity by Flowcytometer (Becton Dikinson, Franklin Lakes, NJ, USA).…”

Histone Deacetylase Inhibitor (Trapoxin A) Enhances Stemness Properties in Adipose Tissue Derived Mesenchymal Stem Cells

“…After 72 h' incubation, the fixation of cells was performed using 70 % cold ethanol for 2 or 3 days in 0-4 °C, then Ribonuclease A (CinnaGen, Tehran, Iran) was added, incubated at 37 °C for 45 min and finally the cells were stained using the Propidium Iodied (PI) in the dark. The percentage of cells at each phases of cell cycle was reported utilizing a FACS system (Beckton Dicinson, USA) [19].…”