Submitted to: Phytochemistry
Publication Type: Peer reviewed journal
Publication Acceptance Date: 3/9/2000
Publication Date: N/A
Citation: Interpretive Summary: Over fifty years after the first medicinal application of the antimitotic activity of podophyllotoxin was proposed, the aryltetralin lignans of Podophyllum continue to be subjects of intense interest and research. Derivatization of podophyllotoxin has produced the potent and widely used antineoplastic drugs etoposide and teniposide. Numerous other analogs have been synthesized in the hope of increasing the usefulness of these drugs, but little improvement has been achieved. These efforts, nevertheless, have generated large amounts of data that may facilitate the design of podophyllotoxin-derived drugs having novel and improved pharmacological properties. This paper briefly reviews the current status of efforts to derivatize and synthesize new podophyllotoxin analogs.
Technical Abstract: Podophyllin, an ethanolic extract of Podophyllum peltatum L. or P. emodi Wall (syn. P. hexandrum Royle), is a good source of the aryltetralin-type lignan, podophyllotoxin. The latter compound as well as its congeners and derivatives exhibit pronounced biological activity mainly as strong antiviral agents and as antineoplastic drugs. The podophyllotoxin derivatives etoposide, etopophos (etoposide phosphate), and teniposide are thus successfully utilized in the treatment of a variety of malignant conditions. Continued research on the Podophyllum lignans is currently focused on structure optimization to generate derivatives with superior pharmacological profiles and broader therapeutic scope, and the development of alternative and renewable sources of podophyllotoxin.