Evaluation of cytotoxic and antibacterial activities of dihydropyrimidon substituted pyrrole

Asieh Khalilpour,1,* Seyede houriye fallah ,2 Abdoliman amouei,3 Hossein ali asgharnia,4

1. Department of Environmental Health Engineering, Faculty of Paramedical Sciences, Babol University of Medical Sciences, Babol, I.R. Iran
2. Department of Environmental Health Engineering, Faculty of Paramedical Sciences, Babol University of Medical Sciences, Babol, I.R. Iran
3. Department of Environmental Health Engineering, Faculty of Paramedical Sciences, Babol University of Medical Sciences, Babol, I.R. Iran
4. Department of Environmental Health Engineering, Faculty of Paramedical Sciences, Babol University of Medical Sciences, Babol, I.R. Iran

Abstract

Introduction

Cancer is one of the leading causes of death among people in the world. chemotherapy is one of the most effective methods used for treating cancer patients. therefore the development of impressible and safe anticancer agents with high activity and less toxicity is a major focus for scientists. heterocycles are an important class of compounds which exhibit useful medicinal chemistry. among heterocycles, n-heterocycles, especially dihydropyrimidones are important compounds have attracted must attention because they exhibit diverse biological activities. dihydropyrimidone substituted pyrrole has been reported as a potential anticancer agent due to its activity on inhibition of cells growth and induction of tumor cell death.

Methods

In vitro cytotoxicity of the dihydropyrimidone substituted pyrrole was evaluated against hela cancer cell lines using mtt assay. in vitro cytotoxicity of dihydropyrimidone substituted pyrrole was evaluated using hela cell line exposed at concentrations 6.25–100 µg/ml at 24, 48 and 72 h. also, this compound was tested for their antibacterial effects against gram positive (staphylococcus aureus and bacillus subtilis) and gram negative (escherichia and pseudomonas aeruginosa).

Results

The cell viability decreased along with the increase of the tested compounds concentration. the cell viability for dihydropyrimidone substituted pyrrole was 65 % after 24 h incubation at least concentration (6.25 µg/ml) and was 5 % in the highest concentration (100 µg/ml). also, the cell viability in the smallest concentration of doxorubicin (positive control) (6.25 µg/ml) was 51.52 %, while it was 8.39 % in the largest concentration (100 µg/ml). therefore, cell viability decreased along with the increase of dihydropyrimidone substituted pyrrole and doxorubicin concentration. furthermore, the cytotoxicity of dihydropyrimidone substituted pyrrole (ic50 value of 18.83±0.40 μm) was lower than doxorubicin (ic50 value of 11.65±0.50 μm). in each concentration, when time increased from 24 to 48, the cell viability reduced. these trends are not observed after 72h. the cell viability for some tested compounds displayed inverse proportional relation to concentration after 72 h. this might be due to lake of cytotoxicity of these compounds after 72 h as it was observed in some reported research works. these compounds, effective against all of the tested gram positive bacteria that exhibited the highest antibacterial activity against b. subtilis.

Conclusion

Our study shows that the dihydropyrimidone substituted pyrrole could have a dose and time-dependent for preventing growth on hela cancer cell line. it seems to come with further research and utilizes its compound in cancer treatment.

Keywords

Dihydropyrimidone substituted pyrrole, cytotoxicity, hela, antibacterial activities