从来自新型α-葡萄糖酶抑制的查和评估
Xiang Wang1,2, Yejun Deng1, Yang Zhang1
1CAF; National Engineering Laboratory for Biomass Chemical Utilization, Key and Open Laboratory on Forest Chemical Engineering, SFA, Key Laboratory of Biomass Energy and Material, Institute of Chemical Industry of Forest Products, Nanjing, Jiangsu 210042, China.
Journal of agricultural and food chemistry
|June 8, 2023
概括
来自金科比洛巴种子蛋糕的两种新型体显示出2型糖尿病 (T2DM) 治疗的潜力. 这些,FAPSW和MPGPP,有效地抑制α-葡萄糖酶并抵抗消化.
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.
- 食品科学 食品科学 食品科学
背景情况:
- 由于安全性,食品衍生的被探索为2型糖尿病 (T2DM) 管理.
- 阿尔法-葡萄糖酶抑制剂是T2DM治疗的关键标.
研究的目的:
- 识别和描述来自金科比洛巴种子蛋糕 (GBSC) 的新型α-葡萄糖酶抑制.
- 评估已识别的类对α-葡萄糖酶的结合稳定性和抑制潜力.
主要方法:
- 用分子对接和分子动力学模拟来选.
- 在体外进行了α-葡萄糖酶抑制试验.
- 模拟体外消化被用于评估的稳定性.
主要成果:
- 发现了两种新型的,即Met-Pro-Gly-Pro-Pro (MPGPP) 和Phe-Ala-Pro-Ser-Trp (FAPSW),这些新型的被发现.
- FAPSW和MPGPP与α-葡萄糖酶 (3wy1) 形成稳定的复合体,由静电和范德瓦尔斯力驱动.
- 这两种都显示出显著的α-葡萄糖酶抑制 (IC50值:FAPSW的445.34±49.48μM,MPGPP的1025.68±140.78μM).
- FAPSW和MPGPP对体外消化表现出强烈的耐药性.
结论:
- FAPSW和MPGPP是具有良好的稳定性强大的α-葡萄糖酶抑制剂.
- 这些代表了开发功能性食品或T2DM治疗药物的有希望的候选人.
相关概念视频
Glucagon-like Receptor Agonists
370
Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
370
Dipeptidyl Peptidase 4 Inhibitors
216
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
216
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
219
α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
Acarbose and miglitol are...
219


