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Special Issue "Grand Celebration: 100th Anniversary of the Discovery of Heparin"

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 May 2016)

Special Issue Editors

Guest Editor
Prof. Dr. Madalena M. M. Pinto

Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências, Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira 228, 4050-313, Porto, Portugal; Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR/CIMAR), Universidade do Porto, Rua dos Bragas 289, 4050-123 Porto, Portugal
Website | E-Mail
Interests: medicinal chemistry; drug discovery and drug design; synthesis and bioenantioselectivity studies of chiral bioactive compounds, as well as studies of structure-activity and structure-properties relationships; molecular recognition-artificial receptors as new chiral stationary phases for HPLC
Guest Editor
Prof. Maria Emília de Sousa

1. Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências, Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira 228, 4050-313, Porto, Portugal
2. Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR/CIMAR), Universidade do Porto, Terminal de Cruzeiros do Porto de Leixões, Avenida General Norton de Matos, S/N 4450-208 Matosinhos, Portugal
Website | E-Mail
Interests: medicinal chemistry; organic synthesis; heterocycles, P-glycoprotein; anticancer; anticoagulants; chiral drugs
Guest Editor
Dr. Marta Correia da Silva

Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências, Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira 228, 4050-313, Porto, Portugal; Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR/CIMAR), Universidade do Porto, Rua dos Bragas 289, 4050-123 Porto, Portugal
Website | E-Mail
Interests: medicinal chemistry; synthesis of sulfated and glycosylated small molecules mimetics of heparin; discovery of biological activities for persulfated versus partially sulfated small molecules; antifouling studies of partially sulfated small molecules; antithrombotic studies of persulfated small molecules; structure-activity and structure-properties relationships studies of bioactive small molecules

Special Issue Information

Dear Colleagues,

Heparin has been used clinically as an antithrombotic agent since the 1940s. However, the history of heparin began in 1916, during the World War I. Continued work on structural characterization, synthesis, structure-activity relationship of heparins has expanded their activity/function spectrum and opens new potential applications. To celebrate a century of discoveries and progresses on this field, the journal Pharmaceuticals now invites valuable contributions that report original observations or reviews. Select topics are listed below and you are welcome to generate a unique topic. This collection of manuscripts will be published as a Special Issue in the journal first and hopefully as an eBook later on. Investigators in the Glycosaminoglycans or other related fields are encouraged to participate in this special event. Please email Prof. Madalena Pinto (madalena@ff.up.pt; madalenakijjoa@gmail.com) if you would like to make a contribution.

  1. New heparin mimetics
  2. New therapeutic applications for heparin/heparan sulfate
  3. Improved preparation and synthesis of heparins
  4. Structural characterization of heparin, low molecular weight heparins (LMWHs), and heparin oligosaccharides
  5. Structure-activity relationships of heparin, LMWHs and heparin oligosaccharides for inflammation, cancer and anticoagulant activities
  6. Improving oral bioavailability of heparins

Prof. Dr. Madalena M. M. Pinto
Dr. Maria Emília de Sousa
Dr. Marta Correia da Silva
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access quarterly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 850 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • heparin
  • glycosaminoglycans
  • synthesis
  • structural characterization
  • anticoagulant
  • bioavailability

Published Papers (4 papers)

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Research

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Open AccessArticle 1H and 15N NMR Analyses on Heparin, Heparan Sulfates and Related Monosaccharides Concerning the Chemical Exchange Regime of the N-Sulfo-Glucosamine Sulfamate Proton
Pharmaceuticals 2016, 9(3), 58; doi:10.3390/ph9030058
Received: 7 July 2016 / Revised: 31 August 2016 / Accepted: 3 September 2016 / Published: 7 September 2016
PDF Full-text (1831 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Heparin and heparan sulfate are structurally related glycosaminoglycans (GAGs). Both GAGs present, although in different concentrations, N-sulfo-glucosamine (GlcNS) as one of their various composing units. The conditional fast exchange property of the GlcNS sulfamate proton in these GAGs has been pointed as
[...] Read more.
Heparin and heparan sulfate are structurally related glycosaminoglycans (GAGs). Both GAGs present, although in different concentrations, N-sulfo-glucosamine (GlcNS) as one of their various composing units. The conditional fast exchange property of the GlcNS sulfamate proton in these GAGs has been pointed as the main barrier to its signal detection via NMR experiments, especially 1H-15N HSQC. Here, a series of NMR spectra is collected on heparin, heparan sulfate and related monosaccharides. The N-acetyl glucosamine-linked uronic acid types of these GAGs were properly assigned in the 1H-15N HSQC spectra. Dynamic nuclear polarization (DNP) was employed in order to facilitate 1D spectral acquisition of the sulfamate 15N signal of free GlcNS. Analyses on the multiplet pattern of scalar couplings of GlcNS 15N has helped to understand the chemical properties of the sulfamate proton in solution. The singlet peak observed for GlcNS happens due to fast chemical exchange of the GlcNS sulfamate proton in solution. Analyses on kinetics of alpha-beta anomeric mutarotation via 1H NMR spectra have been performed in GlcNS as well as other glucose-based monosaccharides. 1D 1H and 2D 1H-15N HSQC spectra recorded at low temperature for free GlcNS dissolved in a proton-rich solution showed signals from all exchangeable protons, including those belonging to the sulfamate group. This work suits well to the current grand celebration of one-century-anniversary of the discovery of heparin. Full article
(This article belongs to the Special Issue Grand Celebration: 100th Anniversary of the Discovery of Heparin)
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Review

Jump to: Research

Open AccessReview Heparin: Past, Present, and Future
Pharmaceuticals 2016, 9(3), 38; doi:10.3390/ph9030038
Received: 29 May 2016 / Revised: 23 June 2016 / Accepted: 27 June 2016 / Published: 4 July 2016
Cited by 11 | PDF Full-text (702 KB) | HTML Full-text | XML Full-text
Abstract
Heparin, the most widely used anticoagulant drug in the world today, remains an animal-derived product with the attendant risks of adulteration and contamination. A contamination crisis in 2007–2008 increased the impetus to provide non-animal-derived sources of heparin, produced under cGMP conditions. In addition,
[...] Read more.
Heparin, the most widely used anticoagulant drug in the world today, remains an animal-derived product with the attendant risks of adulteration and contamination. A contamination crisis in 2007–2008 increased the impetus to provide non-animal-derived sources of heparin, produced under cGMP conditions. In addition, recent studies suggest that heparin may have significant antineoplastic activity, separate and distinct from its anticoagulant activity, while other studies indicate a role for heparin in treating inflammation, infertility, and infectious disease. A variety of strategies have been proposed to produce a bioengineered heparin. In this review, we discuss several of these strategies including microbial production, mammalian cell production, and chemoenzymatic modification. We also propose strategies for creating “designer” heparins and heparan-sulfates with various biochemical and physiological properties. Full article
(This article belongs to the Special Issue Grand Celebration: 100th Anniversary of the Discovery of Heparin)
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Open AccessFeature PaperReview Strategies to Overcome Heparins’ Low Oral Bioavailability
Pharmaceuticals 2016, 9(3), 37; doi:10.3390/ph9030037
Received: 22 April 2016 / Revised: 15 June 2016 / Accepted: 23 June 2016 / Published: 29 June 2016
PDF Full-text (1783 KB) | HTML Full-text | XML Full-text
Abstract
Even after a century, heparin is still the most effective anticoagulant available with few side effects. The poor oral absorption of heparins triggered the search for strategies to achieve oral bioavailability since this route has evident advantages over parenteral administration. Several approaches emerged,
[...] Read more.
Even after a century, heparin is still the most effective anticoagulant available with few side effects. The poor oral absorption of heparins triggered the search for strategies to achieve oral bioavailability since this route has evident advantages over parenteral administration. Several approaches emerged, such as conjugation of heparins with bile acids and lipids, formulation with penetration enhancers, and encapsulation of heparins in micro and nanoparticles. Some of these strategies appear to have potential as good delivery systems to overcome heparin’s low oral bioavailability. Nevertheless, none have reached the market yet. Overall, this review aims to provide insights regarding the oral bioavailability of heparin. Full article
(This article belongs to the Special Issue Grand Celebration: 100th Anniversary of the Discovery of Heparin)
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Open AccessReview Marine Non-Glycosaminoglycan Sulfated Glycans as Potential Pharmaceuticals
Pharmaceuticals 2015, 8(4), 848-864; doi:10.3390/ph8040848
Received: 9 October 2015 / Revised: 30 November 2015 / Accepted: 8 December 2015 / Published: 10 December 2015
Cited by 8 | PDF Full-text (1501 KB) | HTML Full-text | XML Full-text
Abstract
Sulfated fucans (SFs) and sulfated galactans (SGs) are currently the marine non-glycosaminoglycan (GAG) sulfated glycans most studied in glycomics. These compounds exhibit therapeutic effects in several pathophysiological systems such as blood coagulation, thrombosis, neovascularization, cancer, inflammation, and microbial infections. As analogs of the
[...] Read more.
Sulfated fucans (SFs) and sulfated galactans (SGs) are currently the marine non-glycosaminoglycan (GAG) sulfated glycans most studied in glycomics. These compounds exhibit therapeutic effects in several pathophysiological systems such as blood coagulation, thrombosis, neovascularization, cancer, inflammation, and microbial infections. As analogs of the largely employed GAGs and due to some limitations of the GAG-based therapies, SFs and SGs comprise new carbohydrate-based therapeutics available for clinical studies. Here, the principal structural features and the major mechanisms of action of the SFs and SGs in the above-mentioned pathophysiological systems are presented. Discussion is also given on the current challenges and the future perspectives in drug development of these marine glycans. Full article
(This article belongs to the Special Issue Grand Celebration: 100th Anniversary of the Discovery of Heparin)
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