Author:
Hsing Ho Yueng,Rathnasamy Selestin,Dianita Roza,Wahab Habibah A.
Abstract
Introduction: Growing incidence of type-2 diabetes mellitus (T2DM), together with obesity, shows the complexity and progressive nature of these metabolic disorders and alarms the necessity to explore new and alternative therapeutic pathways and drugs. Diabetes has also been proven to be a key cause of premature aging through different mechanisms. Understanding these mechanisms could lead us to manage diabetes more efficiently, thus curtailing its age-related complications. Insulin and leptin resistance are the most common pathophysiological link between T2DM and obesity. Protein tyrosine phosphatase 1B (PTP1B) is thought to interfere with glucose homeostasis and satiety through down-regulation of insulin and leptin signaling pathways. Thus, drugs that are potent to impede this enzyme should be effective in treating T2DM and obesity.
Method: In line with that, our current study involved screening of potent PTP1B inhibitors from the Natural Product Discovery System (NADI) database using in silico virtual screening and in vitro PTP1B inhibition study. The compounds that showed promising interaction with PTP1B catalytic site were traced down to their plant of origin. Further, the extracts of the plants were tested in vitro for PTP1B inhibition activity.
Results: Our results showed promising PTP1B inhibition activity of Pandanus amaryllifolius, Vitex negundo and Piper nigrum with 94.38%, 89.03% and 81.39% inhibition, respectively.
Conclusion: Therefore, the compounds of these plants might be an attractive option to develop drugs for T2DM and obesity.
Publisher
Biomedical Research and Therapy
Subject
General Biochemistry, Genetics and Molecular Biology
Cited by
8 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献