CAJ | 학술논문

设计合成了系列吖啶-多胺类衍生物(ACP1~ ACP6)，并通过四甲基偶氮唑蓝(MTT)染色法研究了化合物对 K562(人白血病细胞)、 A549(人肺癌细胞)和 Hela(人宫颈癌细胞)细胞株的体外抗肿瘤活性。结果显示，化合物对肿瘤细胞具有一定的抑制作用，尤其是化合物 ACP2的抗肿瘤活性优于阳性对照顺铂。通过 UV-Vis 光谱、荧光光谱、圆二色谱和热变性实验研究了合成化合物与小牛胸腺 DNA(Ct-DNA)的键合作用。结果表明，三乙烯四胺修饰的化合物 ACP2具有较好的抗肿瘤活性，与 DNA 分子具有较强的结合能力。
설계합성료계렬아정-다알류연생물(ACP1~ ACP6)，병통과사갑기우담서람(MTT)염색법연구료화합물대 K562(인백혈병세포)、 A549(인폐암세포)화 Hela(인궁경암세포)세포주적체외항종류활성。결과현시，화합물대종류세포구유일정적억제작용，우기시화합물 ACP2적항종류활성우우양성대조순박。통과 UV-Vis 광보、형광광보、원이색보화열변성실험연구료합성화합물여소우흉선 DNA(Ct-DNA)적건합작용。결과표명，삼을희사알수식적화합물 ACP2구유교호적항종류활성，여 DNA 분자구유교강적결합능력。
A series of novel acridine-polyamine conjugates(ACP1-ACP6) was designed and synthesized. Their antitumor activities were evaluated against Leukemia cells(K562), human lung cancer cells(A549) and human cervical carcinoma cells(Hela) in vitro using MTT assay. The results showed that compound ACP2 ex-hibited potent anticancer activities, which was better than the positive control drug(cis-platin). Furthermore, their DNA binding properties were investigated by UV-Vis, fluorescence and circular dischroism(CD) spec-troscopies and thermal denaturation experiment, which showed that the acridine-polyamine conjugates as the DNA intercalator had strong binding interaction with Ct-DNA.