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Molecules 2018, 23(12), 3334;

Looking at Marine-Derived Bioactive Molecules as Upcoming Anti-Diabetic Agents: A Special Emphasis on PTP1B Inhibitors

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr El-Ainy Street, Cairo 11562, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, October University for Modern Science and Arts (MSA), Cairo 12566, Egypt
Herbal Analysis Services UK & Pharmacognosy Research Laboratories, University of Greenwich, Central Avenue, Chatham-Maritime, Kent ME4 4TB, UK
Student Research Committee, Bam University of Medical Sciences, Bam 44340847, Iran
Department of Medical Parasitology, Zabol University of Medical Sciences, Zabol 61663-335, Iran
Institute for Research and Innovation in Health (i3S), University of Porto, 4200-135 Porto, Portugal
Faculty of Medicine, University of Porto, Alameda Prof. Hernâni Monteiro, 4200-319 Porto, Portugal
Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol 61615-585, Iran
Department of Chemistry, Richardson College for the Environmental Science Complex, The University of Winnipeg, 599 Portage Avenue, Winnipeg, MB R3B 2G3, Canada
Authors to whom correspondence should be addressed.
Received: 30 November 2018 / Revised: 10 December 2018 / Accepted: 13 December 2018 / Published: 15 December 2018
Full-Text   |   PDF [9906 KB, uploaded 15 December 2018]   |  
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Diabetes mellitus (DM) is a chronic metabolic disease with high morbimortality rates. DM has two types: type 1, which is often associated with a total destruction of pancreatic beta cells, and non-insulin-dependent or type 2 diabetes mellitus (T2DM), more closely associated with obesity and old age. The main causes of T2DM are insulin resistance and/or inadequate insulin secretion. Protein-tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling pathways and plays an important role in T2DM, as its overexpression may induce insulin resistance. Thus, since PTP1B may be a therapeutic target for both T2DM and obesity, the search for novel and promising natural inhibitors has gained much attention. Hence, several marine organisms, including macro and microalgae, sponges, marine invertebrates, sea urchins, seaweeds, soft corals, lichens, and sea grasses, have been recently evaluated as potential drug sources. This review provides an overview of the role of PTP1B in T2DM insulin signaling and treatment, and highlights the recent findings of several compounds and extracts derived from marine organisms and their relevance as upcoming PTP1B inhibitors. In this systematic literature review, more than 60 marine-derived metabolites exhibiting PTP1B inhibitory activity are listed. Their chemical classes, structural features, relative PTP1B inhibitory potency (assessed by IC50 values), and structure–activity relationships (SARs) that could be drawn from the available data are discussed. The upcoming challenge in the field of marine research—metabolomics—is also addressed. View Full-Text
Keywords: protein-tyrosine phosphatase 1B; type 2 diabetes mellitus; insulin signaling pathways; marine metabolites protein-tyrosine phosphatase 1B; type 2 diabetes mellitus; insulin signaling pathways; marine metabolites

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Ezzat, S.M.; Bishbishy, M.H.E.; Habtemariam, S.; Salehi, B.; Sharifi-Rad, M.; Martins, N.; Sharifi-Rad, J. Looking at Marine-Derived Bioactive Molecules as Upcoming Anti-Diabetic Agents: A Special Emphasis on PTP1B Inhibitors. Molecules 2018, 23, 3334.

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