ABSTRACT

Prodrug discovery from natural sources is characterized by identification, elucidation, derivatization and chemical modification of secondary metabolites obtained from natural resources, which undergo biotransformation prior to reaching binding site and cellular receptors so as to produce desired therapeutic effect compensating the limitation of physiological barrier. Drug researchers had investigated numerous prodrugs from natural resources, may be optimum wangling with the technical assistance of hyphenated analytical techniques and clinical protocols, providing feasible pathway of drug research without huge investment. Psilocybin is a psychedelic prodrug that was isolated in 1957 and biosynthesized in Psilocybe semilanceata Psilocybe azurescens and Psilcybe cyanescens. Melatonin, as a hormone prodrug of N1-acetyl-5-methoxykynuramine moiety, is naturally occurring compound biosynthesized in animals, plants and microbes. Allin is a prodrug of allicin, an unstable compound which is converted into diallyl disulfide. This sulfoxide prodrug is a natural constituent of fresh garlic having both carbon- and sulfur-centered stereochemistry.