10-取代1-氮杂苯并蒽酮衍生物的抗肿瘤和抗菌活性研究

Antitumor and antimicrobial activity of 10-substituted 1-azabenzanthrone derivatives

目的研究10-取代1-氮杂苯并蒽酮衍生物与小牛胸腺DNA的相互作用及其抗肿瘤和抗菌活性。方法利用紫外吸收光谱法研究衍生物与小牛胸腺DNA的相互作用;运用MTT法检测化合物对肺癌细胞（NCI-H460）、人肝癌细胞（HepG2）和肝癌细胞7404的毒性;运用滤纸片扩散法测试化合物对金黄色葡萄球菌、巨大芽孢杆菌、伤寒沙门氏菌和枯草芽孢杆菌的抑菌能力。结果化合物能与小牛胸腺DNA发生嵌入结合作用;大多数的化合物对上述3种肿瘤细胞有较强的毒性,其IC50〈10μmol·L^-1;大部分化合物对上述4种菌具有较强的抑制作用,其抑菌圈直径为13.5～25.0 mm。结论化合物具良好的肿瘤细胞毒性和抑菌活性,在抗肿瘤药物和抗菌药物领域具有潜在的研究价值。

OBJECTIVE To study the interaction of hybrids of the 10 - substituted 1 - azabenzanthrone derivatives with calf thymus DNA and their antitumor and antimicrobial activities. METHODS The interaction of the derivatives with calf thymus DNA was performed by UV spectra. The toxicity effect of the compounds on NCI - H460, HepG2 and hepatocarcinoma 7404 were detected by MTT colorimetric assay. The inhibitory effect of the compounds on Staphylococcus aureus, Salmonella typhi, Bacillus magaterium and Bacillus subtilis were also evaluated by filter paper diffusion method. RESULTS Results indicated that the compounds could intercalate calf thymus DNA. Major synthetical compounds showed potent eytotoxicity against three tumor cell with IC_50 values less than 10 μmol·L^-1 ,and most of them also exhibited obvious inhibitory potency toward four bacteria, the diameter of inhibition zone being 13.5-25.0 mm. CONCLUSION Compounds are worth further researching in the field of antitumor and antimicrobial due to their potent eytotoxieity against tumor cell lines and antimicrohial activity.