Chapter Two - Metabolic Activation and Toxicities of Furanoterpenoids

Abstract

Abstract This chapter introduces the bioactivation and toxicity of furanoterpenoids, particularly their hepatotoxicity. It starts with a brief description of biosynthesis of furanoterpenoids, followed by mechanisms of metabolic activation of furan-containing compounds and the interactions of reactive metabolites of furanoids with proteins. A total of five furanoterpenoids, i.e., 4-ipomeanol, teucrin A, diosbulbin B, 8-epidiosbulbin E acetate, and toosendanin, are discussed as examples. The chapter covers (1) the natural source and toxicities of the furanoterpenoids; (2) identification of reactive metabolites and major cytochromes P450 involved in the metabolic activation of the furan-containing compounds; and (3) protein modifications induced by the reactive metabolites of the furanoids. It also describes a newly developed approach to screen potentially harmful furan-containing compounds from complicated mixtures.