Meroterpenoids with various biological activities produced by fungi

Abstract

Acyl-CoA:cholesterol acyltransferase inhibitors (pyripyropenes), acetylcholinesterase inhibitors (arisugacins), and protein farnesyltransferase inhibitors (andrastins) have been isolated from fungi. They are all biosynthesized from terpene and polyketide and called meroterpenoids (mixed polyketide-terpenoids). Although pyripyropenes and arisugacins have the same skeleton, they showed highly selective inhibition against the respective target enzymes. Pyripyropene A is biosynthesized from a sesquiterpene, a diketide, and a nicotinic acid. Andrastin A is biosynthesized from a sesquiterpene and a tetraketide. It enhanced drug accumulation and is suggested to interact with P-glycoprotein. © 1999 IUPAC.