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鬼臼脂的主要活性成分鬼臼毒素是传统的有丝分裂一纺锤毒素,它竞争性地与微管蛋白(tubulin)结合,并干扰微管蛋白有丝分裂体内的装配,阻止细胞于中期。但其毒性太大,山道士实验室的Stahelin改变了鬼臼毒素结构制成半合成糖甙衍生物。已供市售的一种化合物是4′—脱甲基—表鬼臼毒素—9—4(4,6—0乙叉β-D吡喃葡萄糖甙(VP16-213),亦称鬼臼乙叉甙(etoposide),VM26则仍在临床上进行试验中。
The main active ingredient of podophyllotoxin, podophyllotoxin, is a traditional mitotic-spindle toxin that competitively binds to tubulin and interferes with the assembly of tubulin mitogens, preventing cells from metaphase. However, its toxicity was too great, and the Tadao Institute of Stahelin changed the structure of the podophyllotoxin into a semi-synthetic glycoside derivative. One commercially available compound is 4’-demethyl-epipodophyllotoxin-9-4 (4,6-0 ethylidene β-D glucopyranoside (VP16-213), also known as glycoside 2 Etoposide, VM26 is still in clinical trials.