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目的研究合成的1-氮杂苯并蒽酮-吖啶类似物杂合体(Ia～Il)与小牛胸腺DNA的相互作用及抗肿瘤活性。方法利用紫外吸收光谱、荧光光谱研究杂合体与小牛胸腺DNA的相互作用;用MTT法评价杂合体对人肺腺癌(SPC-A)、人宫颈癌(Hela)、人肝癌(HepG2)、人胃癌(SGC-7901)、人肺癌(NCI-H460)、人结直肠癌(SW480)和人肾腺癌(786-O)等7种肿瘤细胞株的毒性。结果杂合体能与小牛胸腺DNA发生嵌入结合作用,细胞毒性测试表明杂合体具有较强的抗肿瘤活性,特别是对SGC-7901、NCI-H460、SW480和786-O等细胞系的毒性最强,其中大部分杂合体的IC50<1μmol.L-1。结论杂合体的抗肿瘤活性很可能是因为杂合体能与DNA作用而产生的。
Objective To study the interaction and antitumor activity of synthetic 1-azabenzanthrone-acridine analog hybrids (Ia-II) with calf thymus DNA. Methods The interaction between hybrids and calf thymus DNA was studied by ultraviolet absorption spectroscopy and fluorescence spectroscopy. The effects of heterozygotes on human lung adenocarcinoma (SPC-A), human cervical cancer (Hela), human hepatocellular carcinoma (HepG2) Toxicity of seven tumor cell lines including human gastric cancer (SGC-7901), human lung cancer (NCI-H460), human colorectal cancer (SW480) and human renal adenocarcinoma (786- O) Results Heterozygotes could bind to calf thymus DNA. Cytotoxicity test showed that the hybrids had strong antitumor activity, especially for the cell lines such as SGC-7901, NCI-H460, SW480 and 786-O Strong, most of which hybrids IC50 <1μmol.L-1. Conclusion The antitumor activity of hybrids is likely to be due to the interaction of hybrids with DNA.