4-[4″-(2″,2″,6″,6″-四甲基哌啶氮氧自由基)氨基]-4′-去甲表鬼臼毒与其自由基还原物的体外抗肿瘤作用比较

• 作 者: 包金风 王小琦 张晓文
• 机 构: 北京大学药学院药理系,甘肃省医学科学研究院,甘肃省医学科学研究院
• 出 处: 兰州医学院学报
• 发表日期: 2001年01期
• 关键词: 表鬼臼毒 体外抗肿瘤作用 去甲 氮氧自由基 还原物 四甲基哌啶 自由基清除剂 抗肿瘤活性 细胞生长 小鼠移植性肿瘤

Objective To compare the in vit ro antitumor activity of 4-[4″-(2″,2″,6″,6″-tetramethyl-1″ -piperidinyloxy nitroxide radical)amino]-4′-demethylepipodophyllotoxin(GP -7)with its free radical reduced products,4-[4″-(2″,2″,6″,6″ -t etramethyl-1″-piperidinyloxy)amino]-1′-demethylepipodophyllotoxin(GP- 7-H) and 4-[4″-(2″,2″,6″,6″-tetramethyl-1″-hydraxypiper idine)amino]-1′-demethyepipodophyllotoxin(GP-7-OH).Methods The effects of GP-7,GP-7-H a nd GP-7-OH on the proliferation and clonal formation of L 1210 ce lls were observed,and the oil-water partition coefficient of three compounds we re tested. Results GP-7,GP-7-H and GP-7-OH all had a high inhibition rate on L 1210 cells proliferation and clona l formation,the order of inhibition rate is GP-7>GP-7-H>GP-7-OH.T he oil-water partition coefficient of GP-7 was higher than that of GP-7-H and obviously lower than that of GP-7-OH.Couclusion [ WT5”BZ]GP-7 had a more effective in vitro antitumor activity than that of GP-7-H and GP-7-OH,the free redical in GP-7 had an important r ole in increasing antitumor activity,and this was related to oil-water partitio n coefficient of GP-7.

Objective To compare the in vit ro antitumor activity of 4- [4 “- (2”, 2 “, 6”, 6 “-tetramethyl- 1” -piperidinyloxy nitroxide radical amino] -4’-demethylepipodophyllotoxin (GP- 7) with its free radical reduced products, 4- [4 “- (2”, 2 “, 6”, 6 “-t etramethyl- 1” -piperidinyloxy) amino] -1’-demethylepipodophyllotoxin (GP- (GP-7-OH) .Methods The effects of GP-7, GP (2 “, 2”, 6 “, 6” -tetramethyl-1 “-hydraxypiper idine)] -1’-demethyepipodophyllotoxin -7-H a nd GP-7-OH on the proliferation and clonal formation of L 1210 ce lls were observed, and the oil-water partition coefficient of three compounds we re tested. Results GP-7, GP-7-H and GP-7-OH all had a high inhibition rate on L 1210 cells proliferation and clona l formation, the order of inhibition rate is GP-7> GP-7-H> GP-7-OH. of GP-7 was higher than that of GP-7-H and obviously lower than that of GP-7-OH. Cauclusion [WT5 ”BZ] GP-7 had a more effective in v itro antitumor activity than that of GP-7-H and GP-7-OH, the free redical in GP-7 had an important r ole in increasing antitumor activity, and this was related to oil-water partitio n coefficient of GP-7 .