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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 biological activity of synthetic antimicrobial peptide Tachyplesin Ⅰ in vitro and its degradation in simulated digestive environment. Methods The Tachyplesin Ⅰ was treated with different temperature, pH value, cation concentration, solvent polarity and simulated digestion environment. The stability of Tachyplesin Ⅰ was detected by detecting the changes of Tachyplesin Ⅰ biological activity. The hemolysis activity of Tachyplesin Ⅰ was detected by the change of Tachyplesin Ⅰ Degradation in a simulated digestive environment. Results Tachyplesin Ⅰ had stability below 100 ℃ and pH value less than 10.3. Cation concentration and solution polarity had some effects on the antibacterial activity of Tachyplesin Ⅰ. When Tachyplesin Ⅰ concentration was more than 80 mg / L, the action time was longer than 30 min , Showing some hemolytic activity; Tachyplesin Ⅰ in the simulated gastric juice, gastric mucosa homogenates and plasma system showed high stability, the chromatographic peak basically unchanged, almost no degradation, Tachyplesin Ⅰ minimum inhibitory concentration of 5.0 ~ 20.0 mg / L. In the simulated intestinal fluid and small intestinal mucosa homogenate system was slightly sensitive, peak shape decreased, small miscellaneous peak appeared, biological activity decreased significantly, the minimum inhibitory concentration of 80 ~ 160 mg / L. Conclusion Tachyplesin I has high temperature tolerance, is stable under acidic conditions, and has certain ability to resist protease degradation in vivo.