title: An assessment of potential chemoprotectant activity against ricin toxicity by mechanism based glycosidase inhibitors in macrophage J744A.1 cell cultures.
abstract: The abilities of potential chemoprotectants to inhibit cytotoxicity of ricin have been determined in vitro, using the macrophage cell line J744A.1. Six compounds were tested: alpha- and beta-galactopyranosylamine; N-bromoacetyl-alpha-D-galactopyranosylamine; N-bromoacetyl-beta-D-galactopyranosylamine; N-bromoacetylglucopyranosylamine; and N-bromoacetylmannopyranosylamine. Of the six compounds which were tested, only N-bromoacetyl-alpha-D-galactopyranosylamine and N-bromoacetyl-beta-D-galactopyranosylamine exhibited significant activity against ricin toxicity, as indicated by the release of lactate dehydrogenase (LDH) and aspartate aminotransferase (AST). The alpha-isomer provided greater protection against ricin toxicity and also exhibited less inherent cytotoxicity in the absence of ricin, as compared to the beta-isomer. Neither the alpha- and beta-galactopyranosylamines nor the glucose and mannose analogs were promising as potential chemoprotectants.
authors: Department of Pharmaceutical Sciences, Creighton University Health Sciences Center, Omaha, NE 68178.
authors: E A
authors: EA
authors: Hassoun
authors: D
authors: D
authors: Bagchi
authors: V F
authors: VF
authors: Roche
authors: S J
authors: SJ
authors: Stohs
mesh_terms: D001219:Aspartate Aminotransferases / Q000378:metabolism; D002460:Cell Line; D003470:Culture Media; D006026:Glycoside Hydrolases / Q000037:antagonists & inhibitors*; D007202:Indicators and Reagents; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008264:Macrophages / Q000201:enzymology*; D012276:Ricin / Q000037:antagonists & inhibitors*
chemical_list: D003470:Culture Media; D007202:Indicators and Reagents; D012276:Ricin; D007770:L-Lactate Dehydrogenase; D001219:Aspartate Aminotransferases; D006026:Glycoside Hydrolases