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目的:研究碘化-3,3’-二乙基-9-甲基-硫杂羰花青(3,3’-Diethyl-9-methylthiacarbocyanineiodide;DMTCCI)对DNA引物酶-多聚酶α复合体的抑制作用,并观察其对多种肿瘤细胞株的细胞毒作用。方法:提取纯化艾氏腹水癌细胞DNA引物酶-多聚酶α复合体,液闪计数法测定其抑酶活性。用MTT法观察化合物对多种肿瘤细胞株的细胞毒作用。结果:18.5nmol/L、37.0nmol/L、111nmol/L、333nmol/L和1000nmol/LDMTCCI对DNA引物酶-多聚酶α复合体活性的抑制率分别为(27.9±1.3)%、(32.2±1.9)%、(39.2±1.5)%、(51.0±2.3)%和(77.8±1.8)%,其IC50值为(168.2±5.5)nmol/L。显示对DNA引物酶-多聚酶α复合体活性有强烈的抑制作用。MTT实验发现DMTCCI对4种肝癌细胞株Bel-7402、HepG2、Hep3B和SMMC的IC50值分别为(2.09±0.10)μmol/L、(3.84±0.08)μmol/L、(7.01±0.08)μmol/L和(4.91±0.08)μmol/L;对四种鼻咽癌细胞株HNE1、CNE1、CNE2和HK的IC50值分别为(5.27±0.03)μmol/L、(4.30±0.07)μmol/L、(1.78±0.05)μmol/L和(6.76±0.03)μmol/L;对人宫颈癌细胞株HeLa和人急性早幼粒细胞性白血病细胞株HL-60的IC50值分别为(3.23±0.02)μmol/L和(0.24±0.04)μmol/L。结论:DMTCCI对DNA引物酶-多聚酶α复合体活性有显著的抑制作用,并?
Objective: To study the inhibition of DNA primer-polymerase α complex by 3,3’-Diethyl-9-methylthiacarbocyanineiodine (DMTCCI) with iodo-3,3’-diethyl-9-methyl-thiacarbocyanine (DMTCCI) Effect, and observe its cytotoxic effect on a variety of tumor cell lines. Methods: The DNA primers-polymerase α complexes of Ehrlich ascites carcinoma cells were extracted and purified, and their enzyme inhibitory activities were determined by liquid scintillation counting. MTT assay was used to observe the cytotoxicity of the compound against various tumor cell lines. RESULTS: The inhibitory rates of 18.7nmol/L, 37.0nmol/L, 111nmol/L, 333nmol/L, and 1000nmol/L MTCCI were (27.9±1.3)% and (32.2±1.9), respectively, for DNA primer enzyme-polymerase α complex activity. %, (39.2±1.5)%, (51.0±2.3)% and (77.8±1.8)%, and the IC50 value was (168.2±5.5) nmol/L. Shows a strong inhibitory effect on DNA primer enzyme-polymerase alpha complex activity. MTT assay found that the IC50 values of DMTCCI on the four hepatoma cell lines Bel-7402, HepG2, Hep3B and SMMC were (2.09±0.10) μmol/L, (3.84±0.08) μmol/L, and (7.01±0.08) μmol/L, respectively. And (4.91±0.08)μmol/L; IC50 values for the four nasopharyngeal carcinoma cell lines HNE1, CNE1, CNE2, and HK were (5.27±0.03) μmol/L, (4.30±0.07) μmol/L, (1.78 (± 0.05) μmol/L and (6.76 ± 0.03) μmol/L; IC50 values for human cervical carcinoma cell line HeLa and human acute promyelocytic leukemia cell line HL-60 were (3.23 ± 0.02) μmol/L, respectively. And (0.24 ± 0.04) μmol/L. Conclusion: DMTCCI has a significant inhibitory effect on the activity of DNA primer enzyme-polymerase α complex, and?