Podophyllotoxin is a competitive microtubule assembly inhibitor.
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Podophyllotoxin is a naturally occurring aryltetralin lignans extracted from the roots and rhizomes of Podophyllum species. It exhibited antineoplastic effect on P-388, A-549, and HT-29 cell lines with IC50 values of 0.012, 0.012, and 0.024 μM, respectively. Podophyllotoxin also showed anti-proliferative activity against NCI-H460 human non-small cell lung carcinoma cell line with IC50 value of 0.005 μg/mL[3]. The IC50 values for podophyllotoxin against the cell growth of J45.01, U-266B1, HL-60, HL-60/MX1, HL-60/MX2, CCRF-CEM, and CEM/C1 cell lines were 0.0040, 0.0064, 0.0085, 0.0078, 0.0106, 0.0064, and 0.0286 μg/mL, respectively[4]. In a mouse xenograft model inoculated with NCI-H460 cells, the combined treatment of 5 mg/kg podophyllotoxin acetate, a podophyllotoxin derivative, and infrared significantly enhanced cell death via inducing apoptosis as compared to control group[5].
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