Genotoxic and antigenotoxic assessment of four newly synthesized dihydropyridine derivatives

Abstract

The current study aims to determine the genotoxic and antigenotoxic potential of four newly synthesized dihydropyridine derivatives using Escherichia coli WP2 and Ames/Salmonella bacterial reversion assay systems. The bacterial mutant tester strains, E. coli WP2uvrA with a point mutation and Salmonella typhimurium TA1537 with a frameshift mutation, were used to determine genotoxic potentials of the test compounds. To determine antigenotoxic potentials of the test compounds, the same strains were also used together with positive mutagens N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) for E. coli WP2uvrA and 9-aminoacridine (9-AA) for S. typhimurium TA1537. According to the results, neither of the test compounds showed significant genotoxic activity on both tester strains at the tested concentrations. However, except compound 4, all the test compounds showed significant antigenotoxic activity on MNNG- or/and 9-AA-induced mutations. The inhibition rates of mutagenesis ranged from 27.0% (compound 2: 2.5 mM/plate) to 65.0% (compound 2: 0.5 mM/plate) for MNNG and from 30.6% (compound 2: 2 mM/plate) to 58.5% (compound 1: 1 mM/plate) for 9-AA genotoxicity. According to these results, it is concluded that all the test compounds do not have a mutagenic potential on the bacterial strains at the tested concentrations, and some of them have antigenotoxic potentials against MNNG- and 9-AA-induced mutagenesis.

A solvent-free synthesis of polyhydroquinolines via Hantzsch multicomponent condensation catalyzed by nanomagnetic-supported sulfonic acid

“…The polyhydroquinoline moiety is a fertile source of biologically and pharmacologically important molecules such as vasodilator, bronchodilator, anti-atherosclerotic, hepto-protective, anti-tumor, anti-mutagenic, geroprotective, anti-diabetic agents, HIV protease inhibition and most importantly as calcium channel blockers. [8][9][10][11][12][13][14][15] All mentioned cases demonstrate clearly the remarkable potential of the polyhydroquinoline derivatives as a source of valuable drugs. 16,17 In continuation of our investigation on the use of nano-g-Fe 2 O 3 -SO 3 H as catalyst for MCRs and our interest in synthesis of heterocycles containing a nitrogen atom, 18,19 we report an efficient and facile synthesis of hexahydroquinolines under solvent-free conditions (Scheme 1).…”

In vitro mutagenic, antimutagenic, and antioxidant activities evaluation and biotransformation of some bioactive 4‐substituted 1‐(2‐methoxyphenyl)piperazine derivatives

“…We reported that the presence of the chloride atom positively influenced compounds antimutagenic potency . In the current study, reductions in mutagenicity were concentration independent, which was also stated by other investigators . Interestingly, in some compounds the highest antimutagenic effect was attributed to the lowest concentration tested.…”

“…[29,30] In the current study, reductions in mutagenicity were concentration independent, which was also stated by other investigators. [6,31,32] Interestingly, in some compounds the highest antimutagenic effect was attributed to the lowest concentration tested.…”

In vitro genotoxicity assessment of biosynthesized zinc oxide nanoparticles

“…In this procedure, the mutagenic index was calculated for each concentration, which is the average number of revertants per plate divided by the average number of revertants per plate of the negative (solvent) control. A sample is considered genotoxic when a dose–response relationship and a twofold increase in the number of mutants with at least one concentration are observed (Turhan et al, 2014; Tugcu et al, 2017).…”