کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8529187 | 1558854 | 2018 | 27 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The potential role of glucokinase activator SHP289-04 in anti-diabetes and hepatic protection
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موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The potential role of glucokinase activator SHP289-04 in anti-diabetes and hepatic protection The potential role of glucokinase activator SHP289-04 in anti-diabetes and hepatic protection](/preview/png/8529187.png)
چکیده انگلیسی
Glucokinase was glucose sensor in hepatocytes and islet beta cells. It not only promoted glucose metabolism, but also advanced glucose-stimulated insulin secretion. Glucokinase activators had been reported as one kind of new potential drugs for treatment of type 2 diabetes. Compound 6-(5-(3-fluorobenzyloxy)â2-ethoxybenzamido) pyridine-3-carboxylic acid (SHP289-04) was found to increase glucokinase activity effectively by our lab. In order to demonstrate its effect of anti-diabetes, in vitro, human liver carcinoma cell line HepG2 was used to glucose consumption test, and pancreatic cell line NIT-1 was used to assess insulin secretion in response to different concentration of glucose (5â¯mmol/l and 20â¯mmol/l). Type 2 diabetes model KKAy mice were chose to evaluate the pharmacodynamics of SHP289-04 in vivo. In hepatocytes, SHP289-04 could accelerate glucose consuming. In NIT cell line, it promoted glucose-stimulated insulin secretion at the 20â¯mmol/l of glucose. Moreover, it normalized oral glucose tolerance test and down-regulated blood lipid level in KKAy mice. At the same time, it ameliorated function of islets and accelerated the ratio of beta cell/alpha cell mass, and also alleviated the fatty liver of KKAy mice. Therefore, SHP289-04 as a glucokinase activator had the potential effect of diabetes treatment.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 826, 5 May 2018, Pages 17-23
Journal: European Journal of Pharmacology - Volume 826, 5 May 2018, Pages 17-23
نویسندگان
Lei Lei, Shuainan Liu, Yongqiang Li, Huipeng Song, Lianchao He, Quan Liu, Sujuan Sun, Yan Li, Zhiqiang Feng, Zhufang Shen,