Synthesis of [123I] iodoantipyrine to study the high-LET characteristics of Auger electrons in mammalian cells

Slabbert, J.P.; Langenhoven, J. H.; Smit, B. S.

doi:10.1007/bf02349403

Cited by 10 publications

(5 citation statements)

References 18 publications

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“…14)/Be neutrons. Reduced variation in radiosensitivity can easily be demonstrated for particles like Auger electrons with very high ionization densities comparable to that of α-particles [30].…”

Section: Resultsmentioning

confidence: 99%

Potential for Therapeutic Gain - 29 MeV Neutrons versus 6 MeV Neutrons

Slabbert

Vral²

2015

AMR

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When a cancer type proves to be radioresistant to treatment with X-rays, the use of neutrons may constitute therapeutic gain provided the cells are relatively sensitive to high-LET radiation. In this work studies with different tumor cell types are reported following exposure to either photons or different neutron energies used in clinical radiation therapy. Potential for therapeutic gain is clearly noted for neutrons with a mean energy of 6 MeV whilst that for 29 MeV neutrons is dependent on the cell types used in the study.

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Section: Resultsmentioning

confidence: 99%

Potential for Therapeutic Gain - 29 MeV Neutrons versus 6 MeV Neutrons

Slabbert

Vral²

2015

AMR

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“…The [ 123 I]NaI used was carrier-free and was produced at NAC and 4-[ 123 I]iodoantipyrine was synthesised from [ 123 I] NaI as previously described [4]. Counting of the radioactivity was done by means of an intrinsic Ge detector, coupled to a PC based Silena 16 kchannel analyser.…”

Section: Radionuclides and Radioactivity Countingmentioning

confidence: 99%

“…We have previously shown that 4-[ 123 I]iodoantipyrine is a suitable iodine carrier which can be synthesised by iodination of antipyrine with chloramine-T and isotope exchange with [ 123 I]NaI in alkaline solution [4]. The availability of 4-[ 123 I]iodoantipyrine prompted us to compare intra-and extracellular Auger decay from the two reagents [ 123 I]NaI and 4-[ 123 I]iodoantipyrine.…”

Section: Introductionmentioning

confidence: 99%

Comparison of cell inactivation by Auger electrons using the two reagents 4-[ 123 I]iodoantipyrine and [ 123 I]NaI

Smit

Slabbert

Reinecke

et al. 2001

Radiation and Environmental Biophysics

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The Auger electron emitter 123I was examined in the form of 4-[123I]iodoantipyrine and as [123I]NaI for its effectiveness in killing cells of different sensitivity to photon irradiation. Micronucleus assays showed that 4-[123I]iodoantipyrine is 2-3 times more effective in cell inactivation than [123I]NaI. This can be attributed to the fact that antipyrine, for reason of its lipid solubility, can enter cells and can reach the nucleus, whereas [123I]NaI is excluded from the cytoplasm. In the nucleus Auger decay is conceivably located on the DNA where it may invoke high-LET irradiation damage. Irradiation damage by [123I]NaI is by long range Auger and internal conversion electrons and hence less densely ionising. Results of the present study demonstrate, however, that the enhancement of micronuclei frequency (MNF) seen with 4-[123I]iodoantipyrine as compared to [123I]NaI is similar for all cell lines and that the ratio of 4-[123I]iodoantipyrine/[123I]NaI MN response remains the same. Experiments with the free radical scavenger DMSO, indicated nearly identical dose reduction factors for both 123I carriers. These two observations strongly suggest that the cell inactivation by 4-[123I]iodoantipyrine is not by direct high-LET ionisation of DNA, but is due to an indirect effect. The indirect radiation effect of Auger decay in the nucleus could arise because 4-[123I]iodoantipyrine is not incorporated into the DNA, but is only associated with chromatin where the DNA is shielded by histones.

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“…Most of the radiochemical procedures used to make radio-iodine labelled molecules are quite simple, being based on iodine for X exchange; often X is iodine itself. Recent examples are the labelling of zopiclone 150 with iodine-131, the preparation of [ 123 I]iodoantipyrine 151 (useful because it can carry the radionuclide across a cell membrane) and the synthesis of 152 used in the investigation of Alzheimer's disease. Nucelophilic exchange is usually catalysed by copper(I) ions, and [ 123 I]iodoproxyfan, 153 4-[ 123/125 I]iodo-N-(2-morpholinoethyl) benzamide 154 and m-[ 131 I]iodobenzylguanidine 155 have all been made in this way.…”

Section: Iodinementioning

confidence: 99%

27 Radiochemistry

Urch¹

2000

Annu. Rep. Prog. Chem., Sect. A

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Synthesis of [123I] iodoantipyrine to study the high-LET characteristics of Auger electrons in mammalian cells

Cited by 10 publications

References 18 publications

Potential for Therapeutic Gain - 29 MeV Neutrons versus 6 MeV Neutrons

Potential for Therapeutic Gain - 29 MeV Neutrons versus 6 MeV Neutrons

Comparison of cell inactivation by Auger electrons using the two reagents 4-[ 123 I]iodoantipyrine and [ 123 I]NaI

27 Radiochemistry

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