Tehran University of Medical Sciences
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Davood Beiki

Synthesis and radioprotective study of novel amino-alkyldithiocarbamic acid derivatives against γ-irradiation in mice

Authors: Hosseinimehr SJ, Beiki D, Kebriaeezadeh A, Khalaj A, Pirali Hamedani M, Akhlaghpoor S, Esmaeili H, Barazesh A,
Iran J Radiat Res , Vol.7, No.2, 2009,Page:91-96

Background: The aim of this study was to evaluate the radioprotective capacity of some novel aminoalkylated dithiocarbamic acid potassium salts against γ-irradiation in mice.

Materials and Methods: Eight compounds containing 2-aminoethyl-, 3-aminopropyl-, 4-aminobutyl-, 5-aminopentyl-, 6-aminohexyl-, 7-aminoheptyl-, 8-aminooctyl and 9-aminononyl of dithiocarbamate derivatives were prepared. Male NMRI mice were injected intraperitoneally (IP) with a geometric progression of doses (300-1000 mg/kg), through the dose response range for lethal toxicity. To evaluate the radioprotecive activity, one-half of the toxic LD50 of each compound were injected IP to groups of twenty mice, 30 minutes prior to γ-irradiation. The treated animals were kept for 30 days, and the lethality was recorded each day.
Results: Among Eight compounds of alkyl dithiocarbamic acid derivatives, 5-aminopentyl, 7-aminoheptyl, 8-aminooctyl and 9-aminononyl dithiocarbamic acid mono potassium salts are new compounds. All evaluated compounds showed a concentration dependent effect on the survival in mice. The LD50 values were found to be more than 599 mg/kg. The percentages of 30-day survival of mice for 2-aminoethyl, 7-aminoheptyl and 8-aminooctyl dithiocarbamic acid derivatives were 7%, 40% and 13.5%, respectively, when injected 30 minutes before γ-irradiation. Other compounds had no radioprotective effects. Statistical analysis showed a significant difference between the treated and control groups for the 7-aminoheptyl derivative (p<0.05).

Conclusion: Among the compounds investigated in this study, 7-aminoheptyl dithiocarbamate derivative showed more radioprotective effects in comparison with the others. Although it seems that the radioprotective effects in these derivatives correlate with the size of the alkyl chain, more experiments are required to support this hypothesis.