陈佳丽;杨胜涛;萧振邦;千忠吉;

• 1:广东海洋大学食品科技学院
• 2:广东海洋大学化学与环境学院
• 3:广东海洋大学深圳研究院

摘要(Abstract)：

【目的】分析罗非鱼鱼皮多肽LSGYGP的ACE抑制活性、胃肠道消化稳定性以及与降压药卡托普利在分子对接的对比。【方法】用HHL法测定多肽的IC50值和抑制模式,测定多肽在模拟胃肠道消化中的稳定性,MTT法检测细胞活力,Western blot法检测诱导型一氧化氮合酶(i NOS)、环氧合酶-2(COX-2)、内皮素-1(ET-1)等蛋白表达情况,将多肽、卡托普利分别与ACE进行分子对接对比分析。【结果】LSGYGP的半抑制率(IC50)值为2.57μmol/L,表现为混合非竞争性抑制,4 h内模拟胃肠道消化较为稳定;MTT法验证多肽LSGYGP对HUVEC细胞无毒性作用(P> 0.05),且能明显提高Ang Ⅱ诱导组的HUVEC细胞活力(P <0.01);与对照组相比,随实验组多肽浓度增加,i NOS、COX-2和ET-1的表达明显逐渐减少(P<0.001)。对接结果表明,氢键是LSGYGP与ACE结合结构中的支撑力,而卡托普利通常与ACE的Zn⁽²⁺⁾离子形成紧密结合的相互作用。【结论】消化稳定的罗非鱼鱼皮多肽可明显抑制血管收缩因子和炎症因子的表达,展现了较好ACE抑制活性,LSGYGP与卡托普利的活性差异可能是由于ACE分子对接的作用力不同,这些可作为研发少副作用ACE抑制剂的药理基础。

关键词(KeyWords)： 罗非鱼鱼皮多肽;HUVEC;模拟胃肠道消化;分子对接

Abstract:

Keywords:

基金项目(Foundation): 广东省“扬帆起航”紧缺人才引进项目(201433009);; 广东海洋大学“创新强校”科研启动基金项目(2013050204)

作者(Authors): 陈佳丽;杨胜涛;萧振邦;千忠吉;

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