合成抗菌肽TachyplesinⅠ的体外生物活性及其降解规律  

In Vitro Bioactivity and Degradation Regularity of Synthetical Tachyplesin Ⅰ

作　　者：谢海伟[1] 王娣[1] 杨贤松[1] 孙兰萍[1] 张斌[1] 许晖[1] 

机构地区：[1]蚌埠学院生物与食品工程系,安徽蚌埠233030

出　　处：《中国生物制品学杂志》2011年第3期270-275,共6页Chinese Journal of Biologicals

基　　金：安徽省高校自然科学研究资助项目(KJ2009B014);安徽省食品科学与工程教学团队项目资助(20101094);高校省级优秀人才基金项目(2011SQRL166)

摘　　要：目的探讨合成抗菌肽TachyplesinⅠ在体外的生物活性及在模拟消化环境中的降解规律。方法采用不同温度、pH值、阳离子浓度、溶剂极性、模拟消化环境分别处理TachyplesinⅠ,通过检测TachyplesinⅠ生物活性的变化分析其稳定性;检测TachyplesinⅠ对小鼠血细胞的溶血活性;通过HPLC图谱变化评定TachyplesinⅠ在模拟消化环境中的降解情况。结果 TachyplesinⅠ在低于100℃、pH值小于10.3的情况下具有稳定性,阳离子浓度和溶液极性对TachyplesinⅠ的抗菌活性具有一定影响;在TachyplesinⅠ浓度大于80 mg/L时,作用时间大于30 min时,表现出一定的溶血活性;TachyplesinⅠ在模拟胃液、胃黏膜匀浆和血浆系统中表现出很高的稳定性,色谱峰型基本未改变,几乎无降解作用,TachyplesinⅠ的最小抑菌浓度为5.0～20.0 mg/L;在模拟小肠液和小肠黏膜匀浆系统中稍微敏感,色谱峰型降低,出现小杂峰,生物活性明显降低,最小抑菌浓度在80～160 mg/L之间。结论 TachyplesinⅠ具有较强的高温耐受性,在酸性条件下稳定,同时具有一定的耐受体内蛋白酶降解的能力。Objective To investigate the in vitro bioactivity of synthetical tachyplesinⅠas well as its degradation regularity in mimic digestive environment.Methods TachyplesinⅠwas treated at various temperatures,pH values,cation concentrations,polarities of solvent and mimic digestive environments,then determined for bioactivity to evaluate the stability,and for hemolytic activity to mouse blood cells.The degradation of tachyplesinⅠin mimic digestive environment was evaluated by HPLC profile.Results TachyplesinⅠwas stable at temperatures less than 100℃ and pH values less than 10.3.Cation concentration and polarity of solvent showed certain effects on the antibacterial activity of tachyplesinⅠ.The tachyplesinⅠat a concentration of more than 80 mg / L showed a certain hemolytic activity after treatment for more than 30 min.TachyplesinⅠwas highly stable in mimic gastric juice,gastric mucosa homogenate and plasma,of which the chromatographic pattern showed no significant change,and little degradation was observed.The minimum bacteriostatic concentration of tachyplesinⅠwas 5.0 ～ 20.0 mg/L.However,tachyplesinⅠ was slightly sensitive in mimic intestine juice and intestine mucosa homogenate,expressed as decreased peak height,appearance of foreign protein peak and significantly decreased bioactivity,of which the minimum bacteriostatic concentration was 80～160 mg / L.Conclusion TachyplesinⅠshowed high thermotolerance,stability to acidic condition as well as a certain resistance to degradation with protease in vivo.

关 键 词：抗菌肽 TachyplesinⅠ 生物活性 模拟消化液 降解规律 

分 类 号：R977.6[医药卫生—药品]