Bioactive marine macrolides

Abstract

Publisher Summary The macrolides are macrocyclic lactones. Since a macrocycle is usually defined as a compound having a ring constituted with twelve or more atoms, this chapter emphasizes on the structural features, sources, and biological activities of marine compounds containing a 12- or higher-membered lactonic ring. The first marine macrolides were the aplysiatoxins, which were reported in 1974 by Kato and Scheuer as toxic constituents of the sea hare. More than 200 marine macrolides have been recorded in the two decades since the first report of the aplysiatoxins. The chapter presents all known marine macrolides with emphasis on their structural features, sources, and biological activities. Around 205 marine macrolides are compiled, which are then classified into five main structural groups: prostaglandin lactones and related compounds, polyol macrolides, polyether macrolides, macrodiolides, and alkaloidal macrolides.All nitrogen-containing macrolides are treated as alkaloidal macrolides. Within each group, the macrolides are further classified according to their structural relationship and are presented in order of structural complexity. The majority of marine macrolides exhibit pronounced biological activity such as cytotoxic/antitumor, antiviral, antifungal, or immunomodulatory activity. Some of them are exceedingly potent cytotoxins or in vivo active antitumor compounds which are now under extensive investigation as cancer chemotherapeutic agents.