Mice's rectum radioprotection: comparative efficacy of a series of aminothiols and aminothiol precursors.
In mice, in a test of rectal gamma irradiation, cysteamine and cysteine are poor radioprotectors relative to thiazolanes or WR 2721. Among the tested prodrugs, 2-isopropyl 1,3-thiazolane was nearly as efficient as WR 2721 as soon as 15 minutes after its administration. The guarantee of radioprotection is the effective presence of the active aminothiols in the intracellular room during the irradiation. In this study, enterocytes of the rectal mucous membrane were not sufficiently permeable to exogenous cysteine or cysteamine. The cell imperviousness to these straight active aminothiols was compensated by the diffusion of their precursors across the membrane.
Schumacher
C
C
Laboratoire de Chimie Organique Pharmaceutique, Faculté de Pharmacie, Montpellier, France.
Paul
K
K
Robbe
Y
Y
Sicart
M T
MT
Chanal
J L
JL
Delard
R
R
Dubois
J B
JB
D004999:Amifostine / Q000494:pharmacology; D000818:Animals; D003543:Cysteamine / Q000494:pharmacology; D003545:Cysteine / Q000494:pharmacology; D005260:Female; D005720:Gamma Rays; D051379:Mice; D008810:Mice, Inbred C57BL; D011837:Radiation-Protective Agents / Q000494:pharmacology*; D012007:Rectum / Q000528:radiation effects*; D013438:Sulfhydryl Compounds / Q000494:pharmacology*; D013844:Thiazoles / Q000494:pharmacology*
D011837:Radiation-Protective Agents; D013438:Sulfhydryl Compounds; D013844:Thiazoles; D003543:Cysteamine; D003545:Cysteine; D004999:Amifostine