Abstract

Podophyllotoxin is a nonalkaloid toxin aryltetralin lactone lignan, occurring naturally and extracted from the rhizomes and roots of Podophyllum species. Podophyllotoxin and its derivatives have been shown to possess a broad spectrum of pharmacological activities, mainly antineoplastic and antiviral properties. Podophyllotoxin serves as a potential anticancer agent and also the precursor for the chemical synthesis of some clinically important anticancer agents. The chemical modification and pharmacological investigation of podophyllotoxin derivatives have become a concern nowadays. Research interest has been stimulated towards the innovation of podophyllotoxin derivatives as the semi-synthetic anticancer agents, especially etoposide and teniposide. Podophyllotoxin and its derivatives are available in several formulations and also found to be effective in combination therapy. This review article aims to provide an overview of the role of podophyllotoxin, its mechanism of action, pharmacological activities, pharmacokinetics, available formulations, and its effects in combination therapy. This article also reviews the biosynthesis, structure and modifications of podophyllotoxin and its derivatives as an anticancer agent.

Keywords: Podophyllotoxin, anticancer agents, etoposide, teniposide, lignan, structure-activity relationship.