从蛋膜中鉴定DPP-IV抑制:结构活动关系,消化稳定性和分子机制
Shasha Wang1, Zuyue Li1, Mahmoud Abou-Elsoud1,2
1National Research and Development Center for Egg Processing, College of Food Science and Technology, Huazhong Agricultural University, Wuhan 430070, China.
蛋膜 (ESM) 产生的生物活性可以抑制二乙酶-IV (DPP-IV),这是葡萄糖调节中的关键酶. 这些新型为开发功能性食品和治疗药物提供了有希望的途径.
科学领域:
- 生物化学 生化学
- 食品科学 食品科学 食品科学
- 药理学 药理学是指药理学的学科.
背景情况:
- 蛋膜 (ESM) 是一个未充分利用的富含蛋白质的副产品.
- 在ESM中包含具有生理学意义的生物活性序列.
- 双基化酶-IV (DPP-IV) 抑制剂对于管理2型糖尿病至关重要.
研究的目的:
- 探索ESM作为DPP-IV抑制的新型来源.
- 来自ESM的生物活性的识别和表征.
- 阐明这些的结构-活性关系和潜在机制.
主要方法:
- 使用各种蛋白酶,ESM的酶性水解.
- 测定水解剂的DPP-IV抑制活性.
- 液体染色学-双重质谱学 (LC-MS/MS) 用于的识别.
- 分子对接和网络药理学用于机械洞察力.
主要成果:
- 性蛋白酶水解产生了最有效的DPP-IV抑制活性.
- 发现了包括APSPWE,LFPVTPN和GPPHFLPF在内的新型.
- APSPWE在Caco-2细胞中表现出强大的DPP-IV抑制 (IC50 = 246μM) 和现场活性.
- 通过TNF,IL-17,AGE-RAGE和胰岛素信号传递,APSPWE可能调节葡萄糖调节途径.
结论:
- 对于发现DPP-IV抑制来说,ESM是一个有价值的来源.
- 体结构,特别是N端疏水残留物和特定的第二氨基酸,与抑制活性相关.
- 已识别的,如APSPWE,显示出功能性食品成分或针对葡萄糖代谢的治疗剂的潜力.
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