相关实验视频
Updated: Jul 9, 2025

06:09
An In Ovo Model for Testing Insulin-mimetic Compounds
Published on: April 23, 2018
10.6K
来自药用植物的四胺激活了人类的葡萄糖激酶,以调节葡萄糖恒温
Sweta Singh1,2, Payel Ghosh3, Shilpy Sharma4
1Department of Zoology, Savitribai Phule Pune University, Pune, India.
Biotechnology and applied biochemistry
|December 1, 2023
概括
天然的类化合物 - - 甲基胺激活葡萄糖激酶 (GK) 并改善葡萄糖平衡. 这种化合物通过调节GK活性和基因表达,显示出作为一种新型抗糖尿病治疗药物的潜力.
科学领域:
- 药理学 药理学是指药理学的学科.
- 生物化学 生化学
- 药用化学 医学化学
背景情况:
- 针对糖尿病的合成葡萄糖激酶激活剂 (GKA) 在临床试验中遭遇了失败.
- 自然产品数据库为药物发现提供了替代性支架.
研究的目的:
- 使用in silico方法从天然产品中识别新的葡萄糖激酶激活剂.
- 为了研究抗糖尿病潜力和Tetrahydropalmatine的作用机制.
主要方法:
- 在天然产品数据库中搜索GKA的in silico结构相似性.
- 使用复合人类GK的结合亲和力和酶动力学的实验验证.
- 在HepG2细胞中进行基于细胞的测试,以评估葡萄糖吸收和基因表达.
主要成果:
- 十种天然化合物显示出有利的结合分数和GK激活;确定了四基胺.
- 甲基胺激活了GK (EC50 = 71.7μM),改变了S0.5和Vmax,并表现出混合的,非基本的激活动力学.
- 微尺度热泳表明对GK的亲和力很好 (Kd = 3.8 μM). 在HepG2细胞中,它增强了葡萄糖的吸收,并调节了参与葡萄糖平衡的关键基因.
结论:
- 甲基皮氨酸显示出显著的葡萄糖激酶激活特性,并改善葡萄糖平衡.
- 它调节GK活性和相关基因表达的能力表明,单独或组合治疗糖尿病的治疗潜力.
相关概念视频
Hormones Regulating Blood Glucose
3.4K
Insulin is released by beta cells of the pancreas when blood glucose levels are high. It facilitates glucose absorption and utilization in insulin-dependent cells with insulin receptors on their plasma membranes. Insulin promotes glucose uptake by increasing the number of glucose transport proteins in the cell membrane, allowing glucose to enter the cell. As a result, glucose utilization and ATP production are enhanced.
In addition to accelerating glucose uptake and utilization, insulin has...
In addition to accelerating glucose uptake and utilization, insulin has...
3.4K
Glucagon-like Receptor Agonists
329
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...
329
Glucose Homeostasis: Regulation of Blood Glucose
1.7K
Carbohydrates consumed through foods are converted into glucose, a crucial energy source for the body. In the prandial state, high blood glucose levels stimulate the secretion of insulin from the pancreas. Insulin inhibits hepatic glucose production and stimulates glucose uptake and metabolism by muscle and adipose tissue. The excess glucose is converted into glycogen and stored in the liver and muscles.
During fasting, when blood glucose levels are low, the pancreas secretes glucagon. it...
During fasting, when blood glucose levels are low, the pancreas secretes glucagon. it...
1.7K
Dipeptidyl Peptidase 4 Inhibitors
190
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...
190
Glucose Homeostasis: Pancreatic Islets and Insulin Secretion
1.3K
The pancreatic islets comprising only 1%-2% of the volume are highly vascularized and innervated mini-organs. They contain five endocrine cell types, including β cells that secrete insulin, which is synthesized as a single polypeptide chain, preproinsulin, processed to proinsulin, and finally to insulin and C-peptide. This process is complex and regulated, involving the Golgi complex, the endoplasmic reticulum, and the secretory granules of the β cell.
Insulin and C-peptide are...
Insulin and C-peptide are...
1.3K
Oral Hypoglycemic Agents: Glinides
157
Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
157

