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目的:合成桂皮醛衍生物,观测其对心肌细胞的毒性及抗CVB3病毒的作用。方法:化学合成6种桂皮醛衍生物,其中3种进行了红外、质谱等结构表征;MTT法检测被CVB3病毒感染和用桂皮醛衍生物治疗后的心肌细胞活性。结果:α-溴代对氯肉桂醛、α-溴代对甲基肉桂醛、对氯肉桂醛3种桂皮醛衍生物对心肌细胞的半数毒性浓度(TC50)分别为2151.28μg·mL-1,1475.32μg·mL-1,22460.32μg·mL-1;对CVB3病毒的半数抑制浓度(IC50)分别为178.94μg·mL-1、173.35μg·mL-1、6045.25μg·mL-1;对CVB3病毒的治疗指数(TI)分别为12.02,8.51,3.71。结论:桂皮醛3种衍生物具有直接抑制CVB3病毒作用,但对病毒的细胞合成和吸附无明显作用。
OBJECTIVE: To synthesize cinnamaldehyde derivatives and observe their toxicity on cardiomyocytes and the effect of anti-CVB3 virus. METHODS: Six kinds of cinnamic aldehyde derivatives were chemically synthesized. Three of them were characterized by IR and MS. The activity of cardiomyocytes was detected by MTT assay after CVB3 infection and cinnamic aldehyde derivatives treatment. Results: The half toxic concentrations (TC50) of 3 cinnamic aldehyde derivatives of α-bromo-chloro-cinnamaldehyde, α-bromocarboxymethylcinnamaldehyde and p-chlorocinnamaldehyde on myocardial cells were 2151.28 μg · mL- 1475.32μg-mL-1,22460.32μg · mL-1; the median inhibitory concentration (CV50) of CVB3 virus were 178.94μg · mL-1, 173.35μg · mL-1 and 6045.25μg · mL- The therapeutic index (TI) was 12.02, 8.51, 3.71 respectively. CONCLUSION: The cinnamic aldehyde derivatives have a direct inhibitory effect on CVB3 but have no obvious effect on virus synthesis and adsorption.