Benzothiazole derivatives augment glucose uptake in skeletal muscle cells and stimulate insulin secretion from pancreatic β-cells via AMPK activation.
نویسندگان
چکیده
Adenosine monophosphate-activated protein kinase (AMPK) has been identified as one of the major targets for antidiabetic drugs. This study describes two AMPK-activating agents 2-(benzo[d]thiazol-2-ylmethylthio)-6-ethoxybenzo[d]thiazole and 2-(propylthio)benzo[d]thiazol-6-ol, that increase the rate of glucose uptake in L6 myotubes and also augment glucose-stimulated insulin secretion in INS-1E β-cells and rat islets. We believe that such unique bi-functional compounds can be further used for the development of a new class of antidiabetic drugs.
منابع مشابه
AMP-activated protein kinase, a metabolic master switch: possible roles in Type 2 diabetes.
Adenosine 5'-monophosphate-activated protein kinase (AMPK) now appears to be a metabolic master switch, phosphorylating key target proteins that control flux through metabolic pathways of hepatic ketogenesis, cholesterol synthesis, lipogenesis, and triglyceride synthesis, adipocyte lipolysis, and skeletal muscle fatty acid oxidation. Recent evidence also implicates AMPK as being responsible for...
متن کاملAnti-diabetic phytochemicals that promote GLUT4 translocation via AMPK signaling in muscle cells
Skeletal muscles are the largest tissue in our body and play an important role in maintaining glucose homeostasis. Cultured L6 myotubes and C2C12 myotubes are useful to construct simple glucose uptake assay systems, to screen various phytochemicals that promote glucose uptake, and to clarify their modes of actions. In skeletal muscles, insulin promotes glucose uptake by activating phosphatidyli...
متن کاملMetformin, but not leptin, regulates AMP-activated protein kinase in pancreatic islets: impact on glucose-stimulated insulin secretion.
Metformin, a drug widely used in the treatment of type 2 diabetes, has recently been shown to act on skeletal muscle and liver in part through the activation of AMP-activated protein kinase (AMPK). Whether metformin or the satiety factor leptin, which also stimulates AMPK in muscle, regulates this enzyme in pancreatic islets is unknown. We have recently shown that forced increases in AMPK activ...
متن کاملPotentiation of neuronal insulin signaling and glucose uptake by resveratrol: the involvement of AMPK.
Resveratrol (RSV), a polyphenolic phytoestrogen, has been shown to activate the serine/threonine kinase 5'-adenosine monophosphate-activated protein kinase (AMPK) and to stimulate insulin signaling and glucose uptake in skeletal muscle cells. A direct effect of RSV on neuronal insulin signaling, however, has not been demonstrated. Here, we report that RSV stimulates glucose uptake and potentiat...
متن کاملبررسی اثر گلیبنکلامید بر ترشح انسولین و فعالیت گلوکوکیناز در جزایر لانگرهانس پانکراس موشهای صحرایی سالم و دیابتی
Background: Sulfonylurea agents such as Glibenclamide (Glyburide) have been widely prescribe in treatment of type 2 diabetic patients for decades, but controversy remains about their precise mechanism of action. On the other hand, glucokinase serves as a glucose sensor in pancreatic β-cells and plays a key role in the regulation of insulin secretion and glucose homeostasis. The aim of the pres...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Chemical communications
دوره 50 76 شماره
صفحات -
تاریخ انتشار 2014