中国新药与临床杂志
中國新藥與臨床雜誌
중국신약여림상잡지
CHINESE JOURNAL OF NEW DRUGS AND CLINICAL REMEDIES
2003年
3期
131-135
,共5页
万云峰%贡沁燕%鲁映青%史念慈%姚明辉
萬雲峰%貢沁燕%魯映青%史唸慈%姚明輝
만운봉%공심연%로영청%사념자%요명휘
叶酸拮抗剂%胸苷酸合成酶%甲基噻唑基四唑%肿瘤
葉痠拮抗劑%胸苷痠閤成酶%甲基噻唑基四唑%腫瘤
협산길항제%흉감산합성매%갑기새서기사서%종류
folic acid antagonists%thymidylate synthase%methyl thiazolyl tatrozolium%neoplasms
目的: 研究胸苷酸合成酶抑制剂ZD 1694体外抗肿瘤活性.方法:采用MTT比色法测定8种肿瘤细胞株(神经胶质瘤细胞株、肝癌细胞株、乳腺癌细胞株、胃腺癌细胞株、宫颈癌细胞株、急性髓细胞性白血病细胞株、急性早幼粒细胞白血病细胞株和卵巢癌细胞株)分别对ZD 1694和氟尿嘧啶的敏感性,每种药物设定6个浓度等级,分别是Cmax×100,Cmax×10,Cmax×1,Cmax×0.1,Cmax×0.01,和Cmax×0.001.结果:ZD 1694和氟尿嘧啶对8种肿瘤细胞72 h的生长抑制均呈浓度依赖性增加,ZD 1694对SK-N-SH(神经胶质瘤细胞株),K 562(急性髓细胞性白血病细胞株),Bcap-37(乳腺癌细胞株),HELA(宫颈癌细胞株)和HL-60(急性早幼粒细胞白血病细胞株)5种肿瘤细胞的IC50分别为0.4,0.6,2.2,3.2和0.2 μmol·L-1,氟尿嘧啶对SK-N-SH(神经胶质瘤细胞株),K-562(急性髓细胞性白血病细胞株),Bcap-37(乳腺癌细胞株),SGC-7901(胃腺癌细胞株)和HO 8910(卵巢癌细胞株)5种肿瘤细胞的IC50分别为5.5,253.7,150.7,161.7和371.3 μmol·L-1,这8种肿瘤细胞对ZD 1694和氟尿嘧啶的敏感程度分别为62.5 %和12.5 %.结论:ZD 1694和氟尿嘧啶都能浓度依赖性地抑制多种肿瘤细胞的增殖,同时ZD 1694较氟尿嘧啶具有更高的抗肿瘤活性.
目的: 研究胸苷痠閤成酶抑製劑ZD 1694體外抗腫瘤活性.方法:採用MTT比色法測定8種腫瘤細胞株(神經膠質瘤細胞株、肝癌細胞株、乳腺癌細胞株、胃腺癌細胞株、宮頸癌細胞株、急性髓細胞性白血病細胞株、急性早幼粒細胞白血病細胞株和卵巢癌細胞株)分彆對ZD 1694和氟尿嘧啶的敏感性,每種藥物設定6箇濃度等級,分彆是Cmax×100,Cmax×10,Cmax×1,Cmax×0.1,Cmax×0.01,和Cmax×0.001.結果:ZD 1694和氟尿嘧啶對8種腫瘤細胞72 h的生長抑製均呈濃度依賴性增加,ZD 1694對SK-N-SH(神經膠質瘤細胞株),K 562(急性髓細胞性白血病細胞株),Bcap-37(乳腺癌細胞株),HELA(宮頸癌細胞株)和HL-60(急性早幼粒細胞白血病細胞株)5種腫瘤細胞的IC50分彆為0.4,0.6,2.2,3.2和0.2 μmol·L-1,氟尿嘧啶對SK-N-SH(神經膠質瘤細胞株),K-562(急性髓細胞性白血病細胞株),Bcap-37(乳腺癌細胞株),SGC-7901(胃腺癌細胞株)和HO 8910(卵巢癌細胞株)5種腫瘤細胞的IC50分彆為5.5,253.7,150.7,161.7和371.3 μmol·L-1,這8種腫瘤細胞對ZD 1694和氟尿嘧啶的敏感程度分彆為62.5 %和12.5 %.結論:ZD 1694和氟尿嘧啶都能濃度依賴性地抑製多種腫瘤細胞的增殖,同時ZD 1694較氟尿嘧啶具有更高的抗腫瘤活性.
목적: 연구흉감산합성매억제제ZD 1694체외항종류활성.방법:채용MTT비색법측정8충종류세포주(신경효질류세포주、간암세포주、유선암세포주、위선암세포주、궁경암세포주、급성수세포성백혈병세포주、급성조유립세포백혈병세포주화란소암세포주)분별대ZD 1694화불뇨밀정적민감성,매충약물설정6개농도등급,분별시Cmax×100,Cmax×10,Cmax×1,Cmax×0.1,Cmax×0.01,화Cmax×0.001.결과:ZD 1694화불뇨밀정대8충종류세포72 h적생장억제균정농도의뢰성증가,ZD 1694대SK-N-SH(신경효질류세포주),K 562(급성수세포성백혈병세포주),Bcap-37(유선암세포주),HELA(궁경암세포주)화HL-60(급성조유립세포백혈병세포주)5충종류세포적IC50분별위0.4,0.6,2.2,3.2화0.2 μmol·L-1,불뇨밀정대SK-N-SH(신경효질류세포주),K-562(급성수세포성백혈병세포주),Bcap-37(유선암세포주),SGC-7901(위선암세포주)화HO 8910(란소암세포주)5충종류세포적IC50분별위5.5,253.7,150.7,161.7화371.3 μmol·L-1,저8충종류세포대ZD 1694화불뇨밀정적민감정도분별위62.5 %화12.5 %.결론:ZD 1694화불뇨밀정도능농도의뢰성지억제다충종류세포적증식,동시ZD 1694교불뇨밀정구유경고적항종류활성.
AIM: To investigate the effects of the thymidylate synthase(TS) inhibitor-ZD 1694 against cancer cell lines in vitro. METHODS: The in vitro growth inhibition of eight human cancer cell lines (carcinoma of neuroglioma, liver, breast, gastric gland, cervix, acute myelocytic leukemia, acute promyelocytic leukemia and ovary) of ZD 1694 and fluorouracil (5-FU) using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium blue (MTT) colorimetric assay were tested. The concentrations of drugs were Cmax×100, Cmax×10, Cmax×1,Cmax×0.1, Cmax×0.01, and Cmax×0.001, respectively. RESULTS: Inhibition of growth of the eight cancer cell lines by ZD 1694 and 5-FU was concentration-dependent following 72 h exposure to the two drugs. 50 % inhibiting concentration (IC50) of ZD 1694 to SK-N-SH, K-562, Bcap-37, HELA and HL-60 was 0.4, 0.6, 2.2, 3.2, and 0.2 μmol*L-1, respectively. IC50 of 5-FU to SK-N-SH, K-562, Bcap-37, SGC-7901 and HO-8910 was 5.5, 253.7, 150.7, 161.7, and 371.3 μmol*L-1, respectively. Efficacy rate of these eight cancer cells to ZD 1694 and 5-FU was 62.5 % and 12.5 %, respectively. CONCLUSION: ZD 1694 and 5-FU both inhibit growth of various malignancies, respectively. Compared with 5-FU, ZD 1694 is more effective on these eight cancer cells.