Introduction | epipodophyllotoxin is a lignan-like compound isolated from the rhizomes of podophyllaceae, has significant anti-tumor activity, mainly through the role of tubulin and DNA topoisomerase II to produce cytotoxic activity to play an anti-tumor effect, but because of its stomach and intestinal toxicity, therefore, it is not suitable for direct clinical application. |
clinical research | in recent years, epipodophyllotoxin derivatives with better pharmacological and pharmacokinetic properties have been found, such as NK-611, GL-331, TOP-53, F11782 and F14512, etc., of which GL-331 can overcome the multi-drug resistance caused by a variety of tumor cell lines, has now entered the phase 2 clinical trials; TOP-53 has shown a strong inhibitory effect on the highly resistant mutant yeast type 2 enzyme, which has entered the phase 1 clinical trial. |
biological activity | (-)-Epipodophyllotoxin is a cancer cell antiproliferative agent isolated from Podophyllum peltatum, GI50 values in HeLa cells and MCF-7 cells were 0.36 and 0.24 μm, respectively. (-)-Epipodophyllotoxin inhibits mitotic spindle assembly in vitro. |