Structure-activity relationships for the direct toxic action of trichothecenes on rat brain.
Three classes of 12,13-epoxytrichothecenes, differing in the number of hydroxy or acetoxy substituents, were implanted or injected into rat brain to establish structure-toxicity relationships. A free 3 alpha-hydroxy group increases toxicity more than 10-fold, when compared to trichothecenes lacking this substituent. The 8 alpha-hydroxy group enhances toxicity about 4-fold.
Bergmann
F
F
Department of Pharmacology, Hebrew University-Hadassah Medical School, Jerusalem, Israel.
Yagen
B
B
D000287:Administration, Topical; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000187:drug effects*; D004121:Dimethyl Sulfoxide / Q000633:toxicity; D004343:Drug Implants; D007279:Injections, Subcutaneous; D007928:Lethal Dose 50; D008297:Male; D051381:Rats; D012717:Sesquiterpenes / Q000633:toxicity*; D013329:Structure-Activity Relationship; D014255:Trichothecenes / Q000633:toxicity*
D004343:Drug Implants; D012717:Sesquiterpenes; D014255:Trichothecenes; D004121:Dimethyl Sulfoxide