CAJ | 학술논문

设计合成了4种N,N-二(8-黄酮甲基)香叶胺类化合物,所有目标化合物的结构均经~1H NMR、MS和元素分析测试技术确证.采用MTT法考察了目标化合物对K562(白血病细胞)和SMMC7721(肝癌细胞)2种肿瘤细胞的体外抑制活性.结果表明,所测化合物对2种肿瘤细胞均有体外抑制活性,其中N,N-二(3',4'-二甲氧基-8-黄酮甲基)香叶胺(1c)的活性最好,IC_(50)值分别为5.78和3.85 μmol/L,N,N-二(4'-氟-8-黄酮甲基)香叶胺(1a)和化合物1c对K562(白血病细胞)的体外抑制活性明显优于商品药物美法仑(Melphalan).以溴化乙锭(EB)为荧光探针观测到化合物1c与鲱魚精DNA有较强的相互作用.
설계합성료4충N,N-이(8-황동갑기)향협알류화합물,소유목표화합물적결구균경~1H NMR、MS화원소분석측시기술학증.채용MTT법고찰료목표화합물대K562(백혈병세포)화SMMC7721(간암세포)2충종류세포적체외억제활성.결과표명,소측화합물대2충종류세포균유체외억제활성,기중N,N-이(3',4'-이갑양기-8-황동갑기)향협알(1c)적활성최호,IC_(50)치분별위5.78화3.85 μmol/L,N,N-이(4'-불-8-황동갑기)향협알(1a)화화합물1c대K562(백혈병세포)적체외억제활성명현우우상품약물미법륜(Melphalan).이추화을정(EB)위형광탐침관측도화합물1c여비어정DNA유교강적상호작용.
Four N,N-bis(8-flavonmethyl)geranylamine derivatives were designed and synthesized. The structures of the synthesized compounds were determined from the results of ~1H NMR, MS and elemental analysis. The prelimilary cytotoxicity was evaluated on K562 and SMMC7721 cell lines by MTT assay. The results demonstrate that all the compounds possess antitumor actitity and compound 1c is the best among them with an IC_(50) value of 5.78 μmol/L or 3.85 μmol/L against K562 or SMMC7721 cell lines, respectively. The in vitro antitumor activities of compounds 1a and 1c against K562 were better than that of the commercial drug Melphalan. The interaction of compound 1c with herring sperm DNA was explored with ethidium bromide(EB) as a fluorescence probe. The result of the study on fluorescence quenching by DNA-EB confirms the strong interaction of compound 1c with Herring Sperm DNA.