^(60)Co辐照与高温对多肽药物GCIP-27抗心肌肥大作用的影响  

Influence of ^(60)Co radiation and heating on anti-cardiac hypertrophy activity of the polypeptide drug GCIP-27

作　　者：杨华[1] 卢小岚[1] 李晓辉[1] 张海港[1] 

机构地区：[1]第三军医大学药学院药剂学教研室与新药研究中心,重庆400038

出　　处：《中国新药杂志》2010年第12期1022-1025,共4页Chinese Journal of New Drugs

基　　金：国家重大新药创制科技重大专项(2009ZX09103-052);国家自然科学基金(30973524);重庆市科技攻关项目(CSTC2009AB5034)

摘　　要：目的:研究60Coγ射线和高温对G蛋白抑制性多肽(GCIP)-27抗心肌肥大活性的影响,为其灭菌方法的选择提供实验依据。方法:采用ProtParam和ProtScale工具预测GCIP-27的不稳定性指数、脂肪族侧链指数与亲水性、柔韧性、残基隐藏性。去甲肾上腺素腹腔注射复制小鼠心肌肥大模型,观察25kGy辐照和115℃加热对GCIP-27(100μg·kg-1)抗心肌肥大作用的影响。结果:预测显示GCIP-27为稳定多肽,具有较好的耐热性。GCIP-27经辐照和加热处理后仍可明显降低心脏指数和左心室指数,与病理模型空白对照组相比无显著差异。结论:常规辐照和高温灭菌对GCIP-27抗心肌肥大活性无明显影响。Objective：To study the influence of ^60Co radiation and heating on anti-cardiac hypertrophy activity of the polypeptide drug （GCIP）-27,and provide experimental evidence for the choice of best degerming method. Methods：The instability index,aliphatic index,the grand average of hydropathicity,average flexibility and buried residues of peptide GCIP-27 were predicted respectively by bioinformatics tool ProtParam and ProtScale. Observe the influence of ^60Co radiation 25 kGy and heating 115 ℃ independently on anti-cardiac hypertrophy activity of GCIP-27（100 μg·kg^-1） when rat modle with cardiac hypertrophy was induced by norepinephrine（NE）. Results：The prediction showed that GCIP-27 is a stabile polypeptide and has good thermostability. Compared with the NE control,both radiated drug and heated drug significantly decreased the heart index and left ventricular index in mice,while there was no significant difference between treated drug and untreated drug groups,respectively. Conclusion：Conventional radiation and megatemperature degerming have no harmful influence on anti-cardiac hypertrophy activity of GCIP-27.

关 键 词：肽类药物 加热 辐照 心肌肥大 

分 类 号：R96[医药卫生—药理学]