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The lignans of Podophyllum

2002; Elsevier BV; Linguagem: Inglês

10.1016/s1572-5995(02)80007-2

2542-6621

Rita M. Moraes, Franck E. Dayan, Camilo Canel,

Traditional and Medicinal Uses of Annonaceae

Lignans are a widely distributed class of dimeric phenylpropanoid derivatives, many of which have strong antimicrobial, antiviral, or antifeedant activity and thus play important roles in plant defense. Of more restricted taxonomic distribution, the aryltetralin lignans have been found in highest abundance in plants of the genus Podophyllum (Berberidaceae). Foremost among these lignans, podophyllotoxin is a particularly cytotoxic inhibitor of microtubule assembly and astrong antiviral agent. Semisynthetic epimeric derivatives of podophyllotoxin having inhibitory activity against DNA-topoisomerase II have been developed as effective antineoplastic drugs. Current work on Podophyllum lignans is focused on two fronts: 1) Structure optimization to generate derivatives with superior pharmacological profiles and broader therapeutic use, and 2) Development of alternative sources of podophyllotoxin. Numerous variations of the basicaryltetralin structure have been created. Some of the new compounds have shown promising activity profiles, but practically little has been achieved besides improvement in solubility. Interest in new derivatives remains strong, which, along with the formulation of existing drugs for new indications, is increasing the demand for podophyllotoxin. While intense collection has severely reduced the natural stocks of Indian Podophyllum, the primary source of podophyllotoxin, a North American species has emerged as a rich and renewable source of this compound.