In the process of screening for squalene synthase inhibitors from microbial fermentation products we have isolated a novel compound, named schizostatin (Fig. 1), from the culture broth of the mushroom, Schizophyllum communeSANK17785. Schizostatin inhibited rat liver microsomal squalene synthase dose dependently and the IC50 value was 0.84/^m. The inhibition was competitive with respect to farnesylpyrophosphate with a Ki value of 0.45 jllm.

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Schizostatin (1) has been isolated as a potent and selective inhibitor of squalene synthase. Its structure has been determined using spectroscopic methods: the compound is shown to be a diterpenoid which has a /r

In search for new zaragozic acids and their derivatives that are potent inhibitors of squalene synthase, discomycetes of the order Leotiales were cultured and their fermentation broth was assayed, Three strains in 2 unidentified species of Mollisia were found to produce zaragozic acid D3 and three new analogs (F-lO863s), Fermentative production, productivity of F-10863s and mycological characteristics of the producers are described. Discomycetes are expected to be a biological resource providing novel bioactive compounds,

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