Recent Advances in Drug Discovery Based on β-Glucans

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Biopharmaceuticals".

Deadline for manuscript submissions: closed (5 July 2023) | Viewed by 6209

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Guest Editor
Department of Galenic Pharmacy and Food Technology, Universitad Complutense de Madrid, Madrid, Spain
Interests: bioactive compound extraction; metabolic syndrome; bioactive polysaccharides; phenolic compounds; biological rhythms; mushrooms
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Special Issue Information

Dear Colleagues,

β-glucans constitute a highly diverse group of polysaccharides composed of β-linked glucose monomers that can be mainly found in plants, fungi, bacteria, and seaweed cell walls. In addition to the different nature of the sources, their particular structure is varied depending on the specific linkages (β 1,3, β 1,4, β 1,6), the branching and polymerization degree, the molecular weight, etc. In recent decades, interest in these molecules has noticeably increased because of their relevant biological activities that have led to a plethora of studies to develop novel drugs and food supplements based on β-glucans. Among these bioactivities, hypocholesterolemic ability has been described by reducing cholesterol intestinal absorption, scavenging bile acids, or stimulating microbiota short-fatty acid production. Moreover, a potent immune-modulatory action has been observed for β-glucans, being associated in many cases with anti-inflammatory and antitumoral activities. In addition, antimicrobial, antiviral, antioxidant, and wound-healing effects have been reported. In this sense, pharmaceutical approaches have been carried out exploring the effectiveness of β-glucans considering administration routes, side effects, mechanisms of actions, etc. The versatility of these polysaccharides places them not only as active ingredients but also as biodegradable carriers for other bioactive compounds targeting controlled release and bioavailability enhancement. The aim of this Special Issue is to investigate the latest findings and insights related to β-glucans-based drugs and supplements and to elucidate future perspectives.

Dr. Diego Morales
Guest Editor

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Keywords

  • β-glucans
  • hypocholesterolemic
  • hypolipidemic
  • immune system
  • cancer
  • novel drugs
  • bioavailability
  • nutraceuticals
  • inflammation
  • microbiota

Published Papers (3 papers)

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Research

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24 pages, 5091 KiB  
Article
Antioxidant, Immunomodulatory and Potential Anticancer Capacity of Polysaccharides (Glucans) from Euglena gracilis G.A. Klebs
by Virginia Casas-Arrojo, María de los Ángeles Arrojo Agudo, Casimiro Cárdenas García, Paloma Carrillo, Claudia Pérez Manríquez, Eduardo Martínez-Manzanares and Roberto T. Abdala Díaz
Pharmaceuticals 2022, 15(11), 1379; https://doi.org/10.3390/ph15111379 - 10 Nov 2022
Cited by 4 | Viewed by 1905
Abstract
The present study was carried out to determine the bioactivity of polysaccharides extracted from Euglena gracilis (EgPs). These were characterized by FT-IR and GC-MS. Cytotoxicity analyses (MTT) were performed on healthy human gingival fibroblast cell lines (HGF-1), obtaining an IC50 of 228.66 [...] Read more.
The present study was carried out to determine the bioactivity of polysaccharides extracted from Euglena gracilis (EgPs). These were characterized by FT-IR and GC-MS. Cytotoxicity analyses (MTT) were performed on healthy human gingival fibroblast cell lines (HGF-1), obtaining an IC50 of 228.66 µg mL−1, and cell lines with anticancer activity for colon cancer (HCT-116), breast cancer (MCF-7), human leukemia (U-937, HL-60) and lung cancer (NCl-H460), showing that EgPs have anticancer activity, mainly in HTC-116 cells (IC50 = 26.1 µg mL−1). The immunological assay determined the immunomodulatory capacity of polysaccharides for the production of proinflammatory cytokines IL-6 and TNF-α in murine macrophages (RAW 264.7) and TNF-α in human monocytes (THP-1). It was observed that the EgPs had a stimulating capacity in the synthesis of these interleukins. The antioxidant capacity of polysaccharides and their biomass were analyzed using the ABTS method (18.30 ± 0.14% and (5.40 ± 0.56%, respectively, and the DPPH method for biomass (17.79 ± 0.57%). We quantitatively profiled HGF-1 proteins by liquid chromatography–tandem mass spectrometry analysis, coupled with 2-plex tandem mass tag labelling, in normal cells. In total, 1346 proteins were identified and quantified with high confidence, of which five were considered to be overexpressed. The data is available through ProteomeXchange, under identifier PXD029076. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery Based on β-Glucans)
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13 pages, 1805 KiB  
Article
Immunomodulatory Effect of Polysaccharides from the Mushroom-Forming Basidiomycete Gymnopilus imperialis (Agaricomycetes, Basidiomycota)
by Lhaís A. Caldas, Patricia D. Santos, Elaine R. Carbonero, Marisa Ionta, Marta Miyazawa, Ester S. Caixeta, Antonio M. Fregnan, Bianca Barros Nóbrega, Maria Carolina B. Di Medeiros, Nelson Menolli, Jr., Douglas M. M. Soares, Cassius V. Stevani and Patricia Sartorelli
Pharmaceuticals 2022, 15(10), 1179; https://doi.org/10.3390/ph15101179 - 23 Sep 2022
Cited by 1 | Viewed by 1932
Abstract
Gymnopilus consists of a widely distributed genus of basidiomycetes, especially in tropical regions of the world, such as Japan, Australia, Paraguay, and Brazil. This genus biosynthesizes interesting bioactive compounds, such as sesquiterpenoids, oligoisoprenoids, styrylpyrones, and lectins. In the present study, the aqueous extract [...] Read more.
Gymnopilus consists of a widely distributed genus of basidiomycetes, especially in tropical regions of the world, such as Japan, Australia, Paraguay, and Brazil. This genus biosynthesizes interesting bioactive compounds, such as sesquiterpenoids, oligoisoprenoids, styrylpyrones, and lectins. In the present study, the aqueous extract of the basidiomata of Gymnopilus imperialis (Basidiomycota, Agaricomycetes, Agaricales, Hymenogastraceae) was obtained by using the accelerated solvent extraction (ASE) technique, followed by the precipitation of polysaccharide fraction with ethanol. Further purification by freeze-thawing processes, Fehling solution precipitation, and membrane dialysis with different pore sizes yield three main polysaccharide fractions (Gi-MRSW, Gi-PFME, and Gi-SFME). According to monosaccharide composition and 13C-NMR data, the Gi-MRSW and Gi-SFME fractions showed to be composed mainly of β-glucans and Gi-PFME by a heterogalactan. Moreover, the immunomodulatory potential of Gi-MRSW was evaluated using RAW 264.7 murine macrophage as a study model. The nitric oxide production was significantly increased in treated samples, and the expression of inducible nitric oxide synthase (iNOS) showed that the fraction Gi-MRSW from G. imperialis induces the M1 polarization phenotype. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery Based on β-Glucans)
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Review

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12 pages, 342 KiB  
Review
Food By-Products and Agro-Industrial Wastes as a Source of β-Glucans for the Formulation of Novel Nutraceuticals
by Diego Morales
Pharmaceuticals 2023, 16(3), 460; https://doi.org/10.3390/ph16030460 - 20 Mar 2023
Cited by 1 | Viewed by 1620
Abstract
Food and agro-industrial by-products provoke a great environmental and economic impact that must be minimized by adding value to these wastes within the framework of circular economy. The relevance of β-glucans obtained from natural sources (cereals, mushrooms, yeasts, algae, etc.), in terms of [...] Read more.
Food and agro-industrial by-products provoke a great environmental and economic impact that must be minimized by adding value to these wastes within the framework of circular economy. The relevance of β-glucans obtained from natural sources (cereals, mushrooms, yeasts, algae, etc.), in terms of their interesting biological activities (hypocholesterolemic, hypoglycemic, immune-modulatory, antioxidant, etc.), has been validated by many scientific publications. Since most of these by-products contain high levels of these polysaccharides or can serve as a substrate of β-glucan-producing species, this work reviewed the scientific literature, searching for studies that utilized food and agro-industrial wastes to obtain β-glucan fractions, attending to the applied procedures for extraction and/or purification, the characterization of the glucans and the tested biological activities. Although the results related to β-glucan production or extraction using wastes are promising, it can be concluded that further research on the glucans’ characterization, and particularly on the biological activities in vitro and in vivo (apart from antioxidant capacity), is required to reach the final goal of formulating novel nutraceuticals based on these molecules and these raw materials. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery Based on β-Glucans)
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