Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors

Detalhes bibliográficos
Autor(a) principal: Ezzat, S
Data de Publicação: 2018
Outros Autores: El Bishbishy, M, Habtemariam, S, Salehi, B, Sharifi-Rad, M, Martins, N, Sharifi-Rad, J
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: https://hdl.handle.net/10216/127068
Resumo: 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 IC 50 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.
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spelling Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitorsDiabetes 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 IC 50 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.MDPI20182018-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10216/127068eng1420-304910.3390/molecules23123334Ezzat, SEl Bishbishy, MHabtemariam, SSalehi, BSharifi-Rad, MMartins, NSharifi-Rad, Jinfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-29T15:56:10Zoai:repositorio-aberto.up.pt:10216/127068Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T00:35:32.182699Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
title Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
spellingShingle Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
Ezzat, S
title_short Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
title_full Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
title_fullStr Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
title_full_unstemmed Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
title_sort Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors
author Ezzat, S
author_facet Ezzat, S
El Bishbishy, M
Habtemariam, S
Salehi, B
Sharifi-Rad, M
Martins, N
Sharifi-Rad, J
author_role author
author2 El Bishbishy, M
Habtemariam, S
Salehi, B
Sharifi-Rad, M
Martins, N
Sharifi-Rad, J
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Ezzat, S
El Bishbishy, M
Habtemariam, S
Salehi, B
Sharifi-Rad, M
Martins, N
Sharifi-Rad, J
description 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 IC 50 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.
publishDate 2018
dc.date.none.fl_str_mv 2018
2018-01-01T00:00:00Z
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dc.language.iso.fl_str_mv eng
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dc.relation.none.fl_str_mv 1420-3049
10.3390/molecules23123334
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