Podophyllotoxin is a naturally occurring lignin from the rhizomes of Podophyllum hexandrum Royle (Berberidaceae), have important antineoplastic and antiviral properties. Podophyllotoxin and their glycosidic derivatives (Etoposide and Teniposide) have different mode of action. Podophyllotoxin inhibit the microtubules but its glycosidic derivatives like Etoposide and Teniposide inhibit DNA topoisomerase II by stabilising the covalent topo II- DNA cleavable complex. So glycosidic derivatives of podophyllotoxin reduce the side effect. Podophyllotoxin have been widely used in traditional herbal medicine of many diverse cultures as remedies for purgative, snakebites, periodontitis, skin disorders, coughs, various intestinal worm disease, veneral wart condyloma acuminatum, lymphadenopathy and certain tumours, but its glycosidic derivatives are mainly used in the treatment of cancer disease.