Mutagenicity of Bisbenzimidazole Derivatives

2010 ◽  
Vol 65 (1-2) ◽  
pp. 10-14 ◽  
Author(s):  
Filiz Susuz Alanyalı ◽  
Merve Arıcı ◽  
Öge Artagan ◽  
İlhan Işıkdağ ◽  
Yusuf Özkay

The mutagenicities of 2,2’-(di-3-hydroxyphenyl)-1H,1H’-[5,5’]-bisbenzimidazole, 2,2’-(di- 4-hy droxyphenyl)-1H,1H’-[5,5’]-bisbenzimidazole, 2,2’-(di-3-methoxyphenyl)-1H,1H’-[5,5’]- bisbenzimidazole, 2,2’-bis-(4-nitrophenyl)-1H,1H’-[5,5’]-bisbenzimidazole, 2,2’-bis-(3-nitrophenyl)- 1H,1H’-[5,5’]-bisbenzimidazole, 2,2’-bis-(4-methylphenyl)-1H,1H’-[5,5’]-bisbenzimidazole, 2,2’-(di-4-methoxyphenyl)-1H,1H’-[5,5’]-bisbenzimidazole, and 2,2’-bis-(3-me thylphenyl)- 1H,1H’-[5,5’]-bisbenzimidazole were studied in vitro using two strains of Salmonella typhimurium with frameshift mutation (TA98) and base-pair substitution mutation (TA100) as the plate incorporation assay in the absence of metabolic activation. These compounds are currently used to treat cancer. 4-Nitrophenyl and 3-nitrophenyl compounds were found to be mutagenic on both strains of Salmonella. A clear mutagenic response was seen in nitro-bound derivatives. The mutagenic response in Salmonella test strains (TA98, TA100) and structures of molecules suggest that nitro-bound molecules could be mutagenic.

2019 ◽  
Vol 4 (2) ◽  
pp. 68-77
Author(s):  
Anifowoshe T Abass ◽  
Oladipo S Olayinka ◽  
Adebayo O Mutolib ◽  
Eboh O Solomon ◽  
Abdussalam A Rasheedat ◽  
...  

AbstractAsa river is a major river designated to supply millions of people of Ilorin, Kwara State, Nigeria potable water for drinking but its managements is of grave concern due to anthropogenic activities. Thus, evaluation of genotoxicity of this river was carried out by subjecting the water samples and fish therein to three bioassays (Micronucleus (MN) assay, Ames test and SOS-chromo test). Physicochemical parameters and heavy metals were analysed at three different stations (Aliara (SI), Unity (SII) and Tuyil (SIII)) of the river. In SII, most of the heavy metals analysed were above the acceptable limits compare to SI and SIII. The peripheral erythrocyte of the fishes (Oreochromis niloticus, Synodontis batensoda, Synodontis eupterus, Clarias gariepinus and Clarias angullaris) at SI and SII stations showed a significant (p<0.05) induction of MN and different nuclear abnormalities (NA). Water samples from the three stations subjected to Ames test (Salmonella typhimurium TA100) and SOS chromotests (Escherichia coli PQ37) at 25%, 50% and 100% concentrations showed statistically significant (p<0.05) induction of DNA damage at all concentrations in the two tester strains, thus indicating base-pair substitution mutation and excision-repairdeficient, respectively, by the water samples. Therefore, drinking of this water and/or consumption of fish from this river should be taken with caution to avoid a carcinogenic risk.


2008 ◽  
Vol 6 (4) ◽  
pp. 29-33 ◽  
Author(s):  
Nazira S Karamova ◽  
Alexandra P Denisova ◽  
Zenon Stasevski

The mutagenic activity of five pesticides actara, sencor, mospilan, pencozeb, fastac widely used for treatment of potato plant lands in Tatarstan was tested in the Ames test. The non toxic concentrations of the pesticides determined in preliminary cytotoxicty test were used in the Ames assay. Pesticides actara, mospilan, pencozeb, fastac did not show mutagenic effect in Salmonella typhimurium TA 100 without rat liver S9 fraction. The weak mutagenic effect of herbicide sencor was established at concentration 1 ug/plate. Metabolic activation in vitro using rat liver S9 fraction decreased the mutagenic activity of sencor and did not alter the mutagenicity rate of the pesticides actara, mospilan, pencozeb and fastac.


Biologia ◽  
2007 ◽  
Vol 62 (1) ◽  
Author(s):  
Gözde Aydoğan ◽  
Mehtap Kutlu

AbstractTen imidazole derivatives were tested for mutagenicity in Salmonella typhimurium strains TA98 and TA100 both in the absence and presence of metabolic activation by the microsomal fraction S9 mix. In a general manner, derivatives tested exhibited a greater mutagenic activity in the TA100 strain comparing to the responses in TA 98. In the standard plate incorporation assay, 8 of these substances (80%) were found to be mutagenic for at least one of the two strains in the presence or absence of metabolic activation. Two compounds showed positive results in TA98 and 6 compounds were also mutagenic in TA100 without S9. In the presence of S9 mix, all of the 10 substances were non-mutagenic in TA98, whereas 4 compounds were positive in TA100. The results suggested the mutagenic potentials of the imidazole derivatives particularly inducing the reversion of base-pair substitutions. According to the structure-activity relationships phenyl groups in position 2 with different substituents can confer the mutagenic activity of the tested compounds. Methyl groups in different positions of these phenyl substituents can cause different types of mutations. This mutagenic effect is observed more clearly when the phenyl group is inhibited with a nitro group.


1998 ◽  
Vol 21 (4) ◽  
pp. 567-572 ◽  
Author(s):  
Marcos Antonio de Morais Jr. ◽  
Rita de Cássia Café Ferreira ◽  
Luiz Carlos de Souza Ferreira

CL64,855 is a nitroimidazole-thiodiazole derivate with high anti-Trypanosoma cruzi activity. CL64,855-induced mutagenesis in the Salmonella/microsome test was detected by TA98 and TA98dnp6 strains, but not by the nitroreductase I-deficient TA98nr strain. The lack of mutagenic response of TA98nr was connected with its extreme resistance to the killing effect of the drug. Presence of S9 mix did not restore mutagenic activity of CL64,855 to the TA98nr strain. Additionally, CL64,855 was reduced in vitro by the nitroreductase I-proficient TA98 strain, mainly in the presence of oxygen, but not by the TA98nr strain. Mutagenic activity was detected in serum samples of treated guinea pigs by nitroreductase-proficient strains TA98 and TA98dnp6, but not by nitroductase-deficient strain TA98nr. In the case of urine, mutagenic activity was observed with all three tested strains, suggesting an in vivo metabolic activation of the drug by a distinct metabolic pathway.


1974 ◽  
Vol 27 (2) ◽  
pp. 231 ◽  
Author(s):  
DG MacPhee ◽  
F Paula Imray

The tranquilizer chlorpromazine, in combination with visible light or near-u.v. radiation, can cause base-pair substitution mutations and frameshift mutations in Salmonella typhimurium. The mutagenic damage is subject to repair by the bacterial excision~repair system.


2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Vyoma Singla ◽  
Tripti Pachauri ◽  
Aparna Satsangi ◽  
K. Maharaj Kumari ◽  
Anita Lakhani

In the present study, the concentrations of three volatile organic compounds (VOCs), namely, acronym for benzene, toluene, and xylenes (BTX) were assessed because of their role in the tropospheric chemistry. Two representative sites, a roadside and a petrol pump, were chosen for sample collection. VOCs were collected using SKC-activated charcoal tubes and SKC personal sampler and characterized by gas chromatograph using flame ionization detector. Among BTX, benzene had the highest concentration. At the roadside, mean concentration of benzene, toluene, o-,m-xylene, and p-xylene were 14.7 ± 2.4 μgm−3, 8.1 ± 1.2 μgm−3, 2.1 ± 0.8 μgm−3, and 5.1 ± 1.2 μgm−3, respectively. At the petrol pump, the mean concentrations of benzene, toluene, o-,m-xylene and p-xylene were 19.5 ± 3.7 μgm−3, 12.9 ± 1.1 μgm−3, 3.6 ± 0.5 μgm−3and 11.1 ± 1.5 μgm−3, respectively, and were numerically higher by a fraction of 2. Monthly variation of BTX showed maximum concentration in winter. Inter-species ratios and inter-species correlation indicated traffic as the major source of BTX. Extracts of samples were positive in both Salmonella typhimurium tester strains TA98 and TA100 without metabolic activation suggesting the presence of direct mutagens in ambient air that can cause both frame-shift and base-pair mutation. The mutagenic response was greater for TA100 than TA98 suggesting greater activity for base-pair mutagenicity than frame-shift mutagenicity and was found to be statistically significant.


1996 ◽  
Vol 59 (3) ◽  
pp. 244-248 ◽  
Author(s):  
P. B. RASTOGI ◽  
R. E. LEVIN

Among a variety of experimental protocols used, the combined use of 0.5% dextrose in bottom agar and 1 μmol of flavin mononucleotide (FMN) in preincubation mixtures without fraction S9 mix resulted in the highest level of induced Salmonella typhimurium his− reversions with both dyes metanil yellow and orange II with strain TA100. Strain TA98 yielded notably lower levels of reversions under the same conditions. The presence of uninduced hamster liver S9 fraction resulted in a weak mutagenic response while Aroclor 1254-induced rat liver S9 fraction resulted in the complete absence of mutagenicity with both strains and with both dyes.


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