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来自"Takifugu flavidus"的 ангиотензин转化酶 (ACE) 抑制性的亲和力净化和分子表征

Yongchang Su^1,2, Shicheng Chen³, Shuji Liu²

¹College of Chemical Engineering, Huaqiao University, Xiamen 361021, China.

|October 27, 2023

概括

研究人员发现了一种新型,TLRFALHGME,来自Takifugu flavidus,具有强大的血管酶转化酶 (ACE) 抑制活性. 这种对开发高血压新疗法充满希望.

科学领域:

生物化学生化学
药理学药理学是指药理学的学科.
食品科学食品科学食品科学

背景情况:

高血压仍然是一个重要的全球健康问题.
ангиотензин转化酶 (ACE) 在血压调节中起着至关重要的作用.
自然来源正在探索新的抗高血压化合物.

研究的目的:

为了识别和表征来自Takifugu flavidus蛋白质水解的ACE抑制.
调查一种新型对ACE的结合机制和亲和力.
评估已识别的在高血压治疗中的潜力.

主要方法:

使用CNBr激活的Sepharose 4B固定ACE的亲和性染色体.
液体染色学-双重质谱学 (LC-MS/MS) 用于的识别.
分子对接,分子动力学 (MD) 模拟和表面等离子体共振 (SPR) 用于结合分析.

主要成果:

确定了24种ACE抑制性,并选择了TLRFALHGME进行进一步研究.
TLRFALHGME表现出显著的 ACE 抑制活性 (IC50 = 93.5 μmol·L−1).
分子模拟和SPR证实了TLRFALHGME和ACE (Kd = 80.9μmol) 之间的强结合相互作用.

结论:

一种新型的ACE抑制性,TLRFALHGME,已经成功地从Takifugu flavidus中分离和特征化.
该显示出有利的结合动力学和与ACE活性部位的相互作用.
作为治疗高血压的治疗剂,TLRFALHGME具有相当大的潜力.

关键词:

它具有抑制ACE的活性.塔基夫古 (Takifugu) 是一种色的植物.亲缘关系净化净化它具有抗高血压作用.分子对接的分子对接.

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