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目的:利用短期毒性检测方法对3种具有抗HIV活性的DCK系列化合物的一般毒性和特殊毒性进行检测。方法:采用MTT比色法、上下法和Ames波动试验对3种DCK系列化合物3-CH2NO2-4-CH3-DCK(N-DCK),3-CH2CN-4-CH3-DCK(C-DCK),3-F-4-CH3-DCK(F-DCK)的细胞毒性、急性毒性和遗传毒性进行检测。结果:3个化合物中,N-DCK和C-DCK对CHL细胞毒性相似,F-DCK细胞毒性最大,半数抑制浓度(IC50)分别为0.43,0.49,0.18 mg.mL-1;3种化合物对小鼠半数致死剂量(LD50)均>2 000 mg.kg-1;对沙门菌TA100诱变作用均与溶剂对照组相似,无明显致突变作用。结论:3种DCK系列化合物均为低毒物质,无明显遗传毒性。
OBJECTIVE: To determine the general toxicity and specific toxicity of three DCK compounds with anti-HIV activity by using short-term toxicity assay. Methods: MTT colorimetric method, up and down method and Ames wave test were used to investigate the inhibitory effect of three DCK series compounds (3-CH2NO2-4-CH3-DCK, C-DCK) The cytotoxicity, acute toxicity and genotoxicity of 3-F-4-CH3-DCK (F-DCK) were examined. Results: The cytotoxicity of N-DCK and C-DCK was similar to that of CHL in three compounds. F-DCK had the highest cytotoxicity with the IC50 values of 0.43, 0.49 and 0.18 mg.mL-1, respectively. The three compounds The LD50 of mice was> 2000 mg.kg-1. The mutagenicity of Salmonella TA100 was similar to that of the solvent control group, and no obvious mutagenic effect was observed. Conclusion: All the three DCK series compounds are low toxic substances and have no obvious genotoxicity.