Article · Volume 5, Issue 1 · pp. 27–28
Diethylentriaminepenta acetic acid glucose conjugates as a cell permeable iron chelator
Mona Mosayebnia1, Mehdi Shafiee‑Ardestani2, Parvin Pasalar3, Mojgan Mashayekhi3, Massoud Amanlou3
- 1Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
- 2Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
- 3Department of Biochemistry, Faculty of Medicine, Tehran University of Medical Sciences, Tehran, Iran.
Abstract
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.
Keywords: Cell‑permeable; glycosyl moiety; human hepatocellular carcinoma; iron chelation; iron overload
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