Hypoglycemic activity of 6-bromoembelin and vilangin in high-fat diet fed-streptozotocin-induced type 2 diabetic rats and molecular docking studies

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• 作者：Antony Stalin^a ; Santiagu Stephen Irudayaraj^b ; Gopalsamy Rajiv Gandhi^b ; Kedike Balakrishna^b ; Savarimuthu Ignacimuthu^a ; ^b ; ^c ; ^{eriloyola@hotmail.com" class="auth_mail" title="E-mail the corresponding author} ; Naif Abdullah Al-Dhabi^d
• 关键词：6-Bromoembelin ; Vilangin ; Type 2 diabetes mellitus ; PPARγ ; Biochemical analysis ; Molecular-docking
• 刊名：Life Sciences
• 出版年：2016
• 出版时间：15 May 2016
• 年：2016
• 卷：153
• 期：Complete
• 页码：100-117
• 全文大小：3763 K

文摘

This paper investigates the hypoglycemic activity of two derivatives of embelin (1) viz. 6-bromoembelin (2) and vilangin (3), in high-fat diet - STZ induced diabetic rats.

2">Main methods

The effects of 6-bromoembelin (2) and vilangin (3) on insulin resistance, β-cell dysfunction and glucose transport in high-fat diet (HFD) fed-streptozotocin (STZ) (40 mg/kg) induced type 2 diabetic rats were evaluated. The binding modes of 6-bromoembelin (2) and vilangin (3) into PPARγ, PI3K, Akt, and GLUT4 were also studied using Autodock 4.2 and ADT 1.5.6 programs.

Key findings

At the dose of 30 mg/kg, the plasma glucose, plasma insulin and body weight were reduced by both embelin derivatives in diabetic rats. Additionally the altered lipid profiles and hexokinase, glucose-6-phosphatase and fructose-1,6-bisphosphatase levels were brought to normal. Compared to diabetic control group, there was a significant increase in the expression of PPARγ in epididymal adipose tissue. Inhibition of adipogenic activity and mild activation of PPARγ levels in the skeletal muscle and liver were observed. In epididymal adipose tissue, the compounds increased the insulin-mediated glucose uptake through the activation and translocation of GLUT4 in PI3K/p-Akt signaling cascade.

Significance

The derivatives of embelin such as 6-bromoembelin (2) and vilangin (3) may be useful in the prevention and treatment of obesity-linked type 2 diabetes mellitus.