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新合成的鬼臼毒素氮氧自由基衍生物4-[4”-(2”,2”,6”,6”-四甲基哌啶氮氧自由基)氨基]-4’-去甲表鬼臼毒(GP-7)显著抑制小鼠移植性肿瘤S180、实体型HePS和Lewis肺癌生长;7.5～20mg/kg,给药10d,抑瘤率分别为36.0％～58.4%、29.6%～60.0%和27.2%～46.5%;抑制作用和鬼臼乙叉甙(VP-16)相似。GP-7小鼠一次ip,LD_(50)为231.2mg/kg,是VP-16的3.3倍;连续给药10d,对小鼠脾和胸腺指数的影响较VP-16小,对小鼠WBC的影响和VP-16相同。GP-7和VP-165mg/L处理L1210细胞24h,抑瘤率分别为75.5%和73.6%;处理SGC-7901细胞72h,抑瘤率分别为81.4%和84.2%。
Newly synthesized Podophyllotoxin nitroxide derivatives 4-[4“-(2”,2“,6”,6"-tetramethylpiperidine nitroxyl)amino]-4’-demethylamine GP-7 significantly inhibited the growth of transplanted tumor S180, solid HePS, and Lewis lung cancer in mice; 7.5-20 mg/kg, for 10 days, the tumor inhibition rates were 36.0%-58.4%, 29.6%-60.0, respectively. % and 27.2% to 46.5%; The inhibitory effect was similar to that of VP-16. The ip,LD_(50) of GP-7 mice was 231.2 mg/kg, which was 3.3 times that of VP-16. After 10 days of administration, the effect of spleen and thymus index on mice was smaller than that of VP-16, and the effect on WBC of mice was the same as that of VP-16. The treatment of GP-7 and VP-165 mg/L of L1210 cells for 24 h was the tumor inhibition rates were 75.5% and 73.6%; treatment of SGC-7901 cells for 72 hours, the tumor inhibition rates were 81.4% and 84.2%, respectively.