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修改酵母衍生物的潜在抗糖尿病活性和透性评估,VLSTSFPPW (VW9)
Samira Alahyaribeik1, Saeed Mirdamadi2, Hyunjin Shim3
1Department of Environmental Technology, Food Technology, and Molecular Biotechnology, Ghent University Global Campus, 21985, Incheon, South Korea.
Food chemistry
|June 14, 2025
概括
一种经过修改的酵母,VLSTSFPPW (VW9),通过DPP-IV抑制显示出抗糖尿病潜力. 然而,它在消化过程中降解,活性片段PPW缺乏细胞透性,限制了治疗用途.
科学领域:
- 生物化学 生物化学
- 药理学 药理学是指药理学的学科.
- 酸科学 酸科学
背景情况:
- 酵母衍生的被探索用于治疗应用.
- 双基酸酶-IV (DPP-IV) 抑制是治疗糖尿病的一个关键策略.
- 了解的稳定性和透性对于药物开发至关重要.
研究的目的:
- 为了评估改性酵母衍生物的抗糖尿病活性,胃肠道稳定性和Caco-2细胞透性,VLSTSFPPW (VW9).
- 为了识别在消化过程中产生的活性片段,并评估它们的特性.
- 研究活性片段对DPP-IV抑制的机制.
主要方法:
- 在体外胃肠道消化模型.
- 可可-2 细胞透性测试.
- 液体染色学-并联质谱学 (LC-MS/MS) 用于的识别和量化.
- 酶抑制试验 (IC50的确定).
- 运动研究和分子对接模拟.
主要成果:
- 在模拟消化过程中,VW9被广泛降解成更小的碎片,包括PPW,FPPW,FPP,ST和SFPP.
- 片段PPW在体外和体外表现出最高的DPP-IV抑制活性.
- PPW具有竞争性抑制DPP-IV,主要是通过涉及其C端Trp残留物的键相互作用.
- 在PPW中,表皮细胞的透性很差.
- 检测到PPW的修饰衍生物在顶部和底部侧面,但缺乏DPP-IV抑制活性.
结论:
- 酵母衍生VW9及其活性片段PPW在胃肠道稳定性和上皮膜透性方面面临重大挑战.
- 虽然PPW显示出强大的DPP-IV抑制,但其无法穿越细胞膜限制了其直接的治疗应用.
- 需要进行进一步的研究,以设计增强稳定性和透性的改,以便有效的抗糖尿病治疗.
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