摘要
目的研究对甲基桂皮丹酚酯(4a)的合成方法及其抗辐射活性。方法通过制备酰氯的方法,在碱性条件下与丹皮酚进行酯化得到目标产物,并确证结构。以6～8周龄ICR小鼠为研究对象,经γ-射线一次性全身照射后,以30 d存活率及保护指数、平均存活天数,以及相关脏器系数、白细胞(WBC)、血小板(PLT)为指标,考察目标化合物4a低、中、高3个剂量的抗辐射损伤效应。结果小鼠经137Csγ-射线8.5 Gy一次性全身照射后,4a低、中、高剂量组的存活率由空白对照组的14.29%分别提高到28.57%、42.86%、35.71%,阳性对照组为28.57%,平均存活天数明显延长,与空白对照组比较,差异均有高度统计学意义(均P<0.01),尤其是中剂量组,和阳性对照组比较差异有统计学意义(P<0.05)。保护指数分别为1.50、2.01、1.60,阳性对照组为1.48,各组间比较,差异无统计学意义(P>0.05);对受6.5 Gyγ-射线全身照射后辐射损伤ICR小鼠生理指标影响的检测,结果显示4a在不同程度上增加PLT和DNA含量及胸腺系数、脾系数。结论本研究表明对甲基桂皮丹酚酯化合物具有一定的抗辐射损伤作用。
Objective To explore the synthetic method and anti-radiation activity of paeonol p-methyl-cinnamate（4a）.Methods The target product was prepared from esterification of p-methyl-cinnamic acid and paeonol in alkaline conditions by the synthesis of acyl chloride,and its structure was confirmed.To investigate the anti-radiation effect of the target product 4a in low,middle and high dose groups,6-8 weeks old ICR mice received Gamma ray irradiation the whole body for once,and then the survival rate in 30 days,protection index,average survival days,relative organ coefficients,WBC and PLT were detected.Results After the irradiation of 8.5 Gy y-rays emitted from 137Cs radiation resource,the survival rates of the mice in the 3 groups used 4a in low,middle,high dose were 28.75%,42.86%,35.71%,respectively,while the blank control group was 14.29%,and the positive control group was 28.57%.The average survival days was longer in 3 dose groups（P 0.01） especially in the middle dose group which had significant difference compared with the positive control group（P 0.05）.The protection index were 1.50,2.01,1.60 in low,middle and high dose groups,while the positive control group was 1.48,there were no significant differences among groups（P 0.05）.ICR mice physiological indexes affect were detected after radiation damage by gamma-irradiation irradiation of 6.5 Gy,the results indicated that 4a could raise the content of PLT and DNA as well as thymus index and spleen index.Conclusion The study exhibits that paeonol p-methyl-cinnamate has radioprotective effects to some degree.
出处
《中国医药导报》
CAS
2013年第1期20-22,共3页
China Medical Herald
关键词
对甲基桂皮酸
丹皮酚
衍生物
辐射防护
功效研究
P-methyl-cinnamic acid
Paeonol
derivative
Radioprotective
Efficacy research
