SCHIZOSTATIN, A NOVEL SQUALENE SYNTHASE INHIBITOR PRODUCED BY THE MUSHROOM, SCHIZOPHYLLUM-COMMUNE .1. TAXONOMY, FERMENTATION, ISOLATION, PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL-ACTIVITIES
T. Tanimoto et al., SCHIZOSTATIN, A NOVEL SQUALENE SYNTHASE INHIBITOR PRODUCED BY THE MUSHROOM, SCHIZOPHYLLUM-COMMUNE .1. TAXONOMY, FERMENTATION, ISOLATION, PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL-ACTIVITIES, Journal of antibiotics, 49(7), 1996, pp. 617-623
In the process of screening for squalene synthase inhibitors from micr
obial fermentation products we have isolated a novel compound, named s
chizostatin (Fig. 1), from the culture broth of the mushroom, Schizoph
yllum commune SANK 17785. Schizostatin inhibited rat liver microsomal
squalene synthase dose dependently and the IC50 value was 0.84 mu M. T
he inhibition was competitive with respect to farnesylpyrophosphate wi
th a Ki value of 0.45 mu M.