Journal of Pharmacology and Pharmacotherapeutics

RESEARCH PAPER
Year
: 2014  |  Volume : 5  |  Issue : 1  |  Page : 27--32

Diethylentriaminepenta acetic acid glucose conjugates as a cell permeable iron chelator


Mona Mosayebnia1, Mehdi Shafiee-Ardestani2, Parvin Pasalar3, Mojgan Mashayekhi1, Massoud Amanlou1 
1 Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran
2 Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center; Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
3 Department of Biochemistry, Faculty of Medicine, Tehran University of Medical Sciences, Tehran, Iran

Correspondence Address:
Massoud Amanlou
Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran
Iran

Objective: To find out whether DTPA-DG complex can enhance clearance of intracellular free iron. Materials and Methods: Diethylenetriaminepentaacetic acid-D-deoxy-glucosamine (DTPA-DG) was synthesized and examined for its activity as a cell-permeable iron chelator in human hepatocellular carcinoma (HEPG2) cell line exposed to high concentration of iron sulfate and compared with deferoxamine (DFO), a prototype iron chelator. The effect of DTPA-DG on cell viability was monitored using the 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide MTT assay as well. Results: There was a significant increase of iron level after iron overload induction in HEPG2 cell culture. DTPA-DG presented a remarkable capacity to iron burden reducing with estimated 50% inhibitory concentration value of 65.77 nM. In fact, glycosyl moiety was gained access of DTPA to intracellular iron deposits through glucose transporter systems. Conclusion: DTPA-DG, more potent than DFO to sequester deposits of free iron with no profound toxic effect. The results suggest the potential of DTPA-DG in chelating iron and permitting its excretion from primary organ storage.


How to cite this article:
Mosayebnia M, Shafiee-Ardestani M, Pasalar P, Mashayekhi M, Amanlou M. Diethylentriaminepenta acetic acid glucose conjugates as a cell permeable iron chelator.J Pharmacol Pharmacother 2014;5:27-32


How to cite this URL:
Mosayebnia M, Shafiee-Ardestani M, Pasalar P, Mashayekhi M, Amanlou M. Diethylentriaminepenta acetic acid glucose conjugates as a cell permeable iron chelator. J Pharmacol Pharmacother [serial online] 2014 [cited 2020 May 27 ];5:27-32
Available from: http://www.jpharmacol.com/article.asp?issn=0976-500X;year=2014;volume=5;issue=1;spage=27;epage=32;aulast=Mosayebnia;type=0