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目的：比较鬼臼毒氮氧自由基衍生物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）及其自由基还原物ＧＰ－７－Ｈ和ＧＰ－７－ＯＨ的抗肿瘤活性和急性毒性。方法：采用小鼠移植性肿瘤Ｓ１８０、ＨｅＰＳ和腹腔注射ＬＤ５０值。结果：ＧＰ－７、ＧＰ－７－Ｈ、ＧＰ－７－ＯＨ５～１０ｍｇ·ｋｇ－１给药１０ｄ，对Ｓ１８０肉瘤的抑制率分别为３９．７％～４６．８％、１７．３％～２９．５％和１９．９％～２２．４％，对ＨｅＰＳ的抑制率分别为３８．７％～４８．８％、１５．５％～３５．１％和１８．４％～３３．３％。昆明种小鼠腹腔注射一次给药，ＬＤ５０分别为２３１．２、８９．７和１２９．５ｍｇ·ｋｇ－１。结论：ＧＰ－７对Ｓ１８０、ＨｅＰＳ生长抑制作用均较其还原物ＧＰ－７－Ｈ、ＧＰ－７－ＯＨ强，急性毒性较其还原物ＧＰ－７－Ｈ和ＧＰ－７－ＯＨ小；提示ＧＰ－７中的自由基在加强抗肿瘤作用和降低毒性方面起着重要的作用。
OBJECTIVE: To compare the effects of podophyllotoxynin 4 - [4 “- (2”, 2 “, 6”, 6 "- tetramethylpiperidine nitroxide) Antitumor activity and acute toxicity of podophyllotoxin (GP-7) and its GP-7-H and GP-7-OH free radicals.METHODS: Mouse transplanted tumors S180, HePS and intraperitoneal injection of LD50 were used. Results: The inhibitory rates of GP-7, GP-7-H and GP-7-OH 5 ~ 10 mg · kg-1 for 10 days on S180 sarcoma were 39.7% -46.8%, 17.3% 29.5% and 19.9% ~ 22.4%, respectively. The inhibition rate to HePS was 38.7% ~ 48.8%, 15.5% ~ 35.1% and 18.4% ~ 33.3 %. Kunming mice were injected intraperitoneally with LD50 of 231.2, 89.7 and 129.5 mg · kg -1, respectively.Conclusion: GP-7 can inhibit the growth of S180 and HePS Compared with GP-7-H and GP-7-OH, GP-7-H and GP-7-OH, GP-7-H and GP-7-OH showed less acute toxicity than GP- Role and reduce toxicity plays an important role.