Preparation of 9-hydroxy grayanotoxin derivatives and their acute toxicity in mice

Abstract

Novel 9α and 9 β-hydroxy grayanotoxin II derivatives were prepared by photo-sensitized oxygenation of isograyanotoxin II and oxidation of grayanotoxin II tetraacetate with selenium dioxide respectively. The lethal dosage of 9α and 9 β-hydroxy grayanotoxin II were lower than that of grayanotoxin II. In addition, the lethal dosage of 9 β-hydroxy-dihydro grayanotoxin II was higher than that of dihydro grayanotoxin II. © 2003 Pharmaceutical Society of Japan.