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小鼠ip WB_(852)LD_(50)为107.7mg/kg,iv LD_(50)为52.2mg/kg。体外实验,4～8×10~(-4)WB_(852)对HepA癌细胞的赤染率可达86～99%。体内实验,WB_(852)ip,40mg/kg/日,连用9日,平均可使生命延长率提高160.9%,25或60mg/kg均使生命延长率提高为124.2%,说明WB_(852)对HepA癌细胞体内外均有显著杀伤作用。采用同位素体外掺入法证明,WB_(852) 1-4×10~(-4)对~3H-TdR掺入HepA癌细胞DNA的合成均有抑制作用,培养1小时的掺入抑制率分别为64.9%和62.7%,5小时抑制率分别为66.3%和57.9%,说明WB_(852)对肝癌细胞DNA的合成有抑制作用。电镜观察表明,WB_(852)对肝癌细胞膜有损害作用,细胞膜破裂,细胞内容物溢出,但对细胞核、核膜及线粒体等则未见影响。
The mice ip WB_(852)LD_(50) was 107.7 mg/kg, and iv LD_(50) was 52.2 mg/kg. In vitro experiments, 4-8×10-4 WB-(852) HepA cancer cells red dye rate of up to 86 to 99%. In vivo experiment, WB_(852)ip, 40mg/kg/day, for 9 days, the average life extension rate was increased by 160.9%, 25 or 60mg/kg all increased the life extension rate to 124.2%, indicating WB_(852) HepA cancer cells have significant killing effect in vivo and in vitro. The isotope incorporation method was used to demonstrate that WB_(852) 1-4×10~(-4) inhibited the DNA synthesis of ~3H-TdR-incorporated HepA cancer cells, and the inhibition rate of incorporation for 1 hour was: In 64.9% and 62.7%, the 5-hour inhibition rates were 66.3% and 57.9%, respectively, indicating that WB_(852) has an inhibitory effect on the synthesis of hepatoma cell DNA. Electron microscopy showed that WB_(852) had damage to hepatoma cell membrane, cell membrane ruptured, cell contents overflowed, but no effect on nuclear, nuclear membrane and mitochondria.