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Pharmaceuticals
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Polysaccharides as Drug Candidates
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Polysaccharides as Drug Candidates

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

Deadline for manuscript submissions: closed (25 March 2024) | Viewed by 9021

Special Issue Editor

Dr. Daniele Maria-Ferreira

E-Mail Website
Guest Editor
Programa de Pós-Graduação em Biotecnologia Aplicada à Saúde da Criança e do Adolescente, Faculdades Pequeno Príncipe, Curitiba, Brazil
Interests: natural products; natural polysaccharides; prebiotics; inflammatory bowel diseases; ulcerative colitis; intestinal chemotherapy mucositis

Special Issue Information

Dear Colleagues,

Polysaccharides are polymeric carbohydrates, which can be described as non-digestible fibers (or prebiotics), and in recent years, they have attracted attention because of their health benefits. These molecules are extracted from the most diverse sources (algae, bacteria, fruits, herbs, mushrooms, etc.), present a wide structural diversity, and can act by different mechanisms, providing several interesting activities. Notably, recent studies have shown that polysaccharides have, for instance, anti-inflammatory, immunomodulatory, antioxidant, antibacterial, anticarcinogenic, and anticoagulant activities, with high safety, and thus could be applied for the treatment of various pathologies. Therefore, polysaccharides have played a promising and fundamental role in the discovery of new drugs in various therapeutic areas, and comprehensive investigations are essential.

For the Special Issue on “Polysaccharides as Drug Candidates”, we welcome original research and review articles. Manuscripts must focus on any aspects of:

  • Advances and challenges in the application of polysaccharides or polysaccharides extracts;
  • Extraction/isolation and identification of bioactive polysaccharides or polysaccharides extracts (from herbs, fruits, mushrooms, etc.), with pharmacological applications;
  • Benefits and safety of bioactive polysaccharides or polysaccharides extracts;
  • Bioactivity of polysaccharides or polysaccharides extracts for the development of new drugs.

Dr. Daniele Maria-Ferreira
Guest Editor

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 submissions that pass pre-check are 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 monthly 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 2900 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

  • polysaccharides
  • polysaccharide extract
  • isolation/characterization of polysaccharides
  • biological activity screening of polysaccharides
  • bioactive polysaccharides
  • polysaccharides as drug candidates

Published Papers (6 papers)

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Research

18 pages, 13610 KiB  
Article
An Inulin-Type Fructan CP-A from Codonopsis pilosula Alleviated 5-Fluorouracil-Induced Intestinal Mucositis via the ERK/MLCK/MLC2 Pathway and Regulation of Gut Microbiota
by Jiangtao Zhou, Deyun Li, Jiajing Wang, Zhuoyang Cheng, Changjian Wang, Xuepeng Zhang, Xiexin Xu and Jianping Gao
Pharmaceuticals 2024, 17(3), 297; https://doi.org/10.3390/ph17030297 - 26 Feb 2024
Viewed by 749
Abstract
Intestinal mucositis (IM) is a common adverse effect of chemotherapy, limiting its clinical application. Codonopsis pilosula-derived CP-A (an inulin-type fructan) is an edible Chinese medicine with anti-inflammatory and gastrointestinal protective effects, which may be useful for treating IM. Here, we explored CP-A’s [...] Read more.
Intestinal mucositis (IM) is a common adverse effect of chemotherapy, limiting its clinical application. Codonopsis pilosula-derived CP-A (an inulin-type fructan) is an edible Chinese medicine with anti-inflammatory and gastrointestinal protective effects, which may be useful for treating IM. Here, we explored CP-A’s role in ameliorating IM induced by 5-fluorouracil (5-FU) and investigated the underlying mechanism using in vitro experiments and rat models. Western blotting, immunohistochemistry (IHC), and real-time PCR (RT-PCR) analyses were used to assess protein expression related to the extracellular-regulated protein kinases (ERK)/myosin light chain kinase (MLCK)/myosin light chain 2 (MLC2) signaling pathway and tight junction proteins. Inflammatory factors were quantified using enzyme-linked immunosorbent assays (ELISAs), and 16S rRNA amplicon sequencing was employed for cecum content analysis. The results indicated that CP-A restored body weight and food intake and reversed histopathological changes in IM rats. Further, abnormal MLCK activation induced by 5-FU was attenuated by CP-A via the ERK/MLCK/MLC2 pathway. CP-A treatment improved tight junction protein levels and reduced inflammatory factor expression. Moreover, CP-A intervention regulated the intestinal microbiota community structure, increasing the abundance of Lactobacillus and decreasing the abundance of Shigella. In conclusion, CP-A mitigates 5-FU-induced IM by inhibiting the ERK/MLCK/MLC2 pathway, reducing the expression of inflammatory factors, improving the intestinal mucosal barrier, and regulating the intestinal microbial community. This study highlights CP-A’s therapeutic potential in IM treatment and provides insights for future research. Full article
(This article belongs to the Special Issue Polysaccharides as Drug Candidates)
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13 pages, 3108 KiB  
Article
Combined Lycium barbarum Polysaccharides with Plasmon-Activated Water Affect IFN-γ/TNF-α Induced Inflammation in Caco-2 Cells
by Yu Zhi Lian, Yu-Chuan Liu, Chun-Chao Chang, Tomonori Nochi and Jane C.-J. Chao
Pharmaceuticals 2023, 16(10), 1455; https://doi.org/10.3390/ph16101455 - 13 Oct 2023
Viewed by 1062
Abstract
The effects of Lycium barbarum polysaccharides (LBP) and plasmon-activated water (PAW) against IFN-γ/TNF-α induced inflammation in human colon Caco-2 cells were investigated. Cells were divided into the control, induction, LBP treatment (100–500 μg/mL), and combination groups with PAW. Inflammation was induced 24 h [...] Read more.
The effects of Lycium barbarum polysaccharides (LBP) and plasmon-activated water (PAW) against IFN-γ/TNF-α induced inflammation in human colon Caco-2 cells were investigated. Cells were divided into the control, induction, LBP treatment (100–500 μg/mL), and combination groups with PAW. Inflammation was induced 24 h with 10 ng/mL IFN-γ when cell confluency reached >90%, and various doses of LBP with or without PAW were treated for 3 h, and subsequently 50 ng/mL TNF-α was added for another 24 h to provoke inflammation. Combination of LBP with PAW significantly decreased the secretion of IL-6 and IL-8. Cyclooxygenase-2 and inducible NO synthase expression was attenuated in all LBP-treated groups with or without PAW. NLRP3 inflammasome and related protein PYCARD expression were inhibited by LBP at the highest dose (500 μg/mL). All doses of LBP alone significantly decreased p-ERK expression, but combination with PAW increased p-ERK expression compared to those without PAW. Additionally, 250 and 500 μg/mL of LBP with or without PAW inhibited procaspase-3/caspase-3 expression. Therefore, LBP possesses anti-inflammation and anti-apoptosis by inhibiting the secretion of inflammatory cytokines and the expression of NLRP3 inflammasome-related protein. The combination with PAW exerts additive or synergistic effect on anti-inflammation. Full article
(This article belongs to the Special Issue Polysaccharides as Drug Candidates)
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26 pages, 7556 KiB  
Article
Polysaccharides from Passion Fruit Peels: From an Agroindustrial By-Product to a Viable Option for 5-FU-Induced Intestinal Damage
by Karien Sauruk da Silva, Kahlile Youssef Abboud, Carolina Silva Schiebel, Natalia Mulinari Turin de Oliveira, Laryssa Regis Bueno, Lara Luisa Valerio de Mello Braga, Bruna Carla da Silveira, Isabella Wzorek França dos Santos, Everton dos Santos Gomes, Marcelo Biondaro Gois, Lucimara Mach Côrtes Cordeiro and Daniele Maria Ferreira
Pharmaceuticals 2023, 16(7), 912; https://doi.org/10.3390/ph16070912 - 21 Jun 2023
Cited by 1 | Viewed by 1483
Abstract
Gastrointestinal mucositis is a serious and dose-limiting toxic side effect of oncologic treatment. Interruption of cancer treatment due to gastrointestinal mucositis leads to a significant decrease in cure rates and consequently to the deterioration of a patient’s quality of life. Natural polysaccharides show [...] Read more.
Gastrointestinal mucositis is a serious and dose-limiting toxic side effect of oncologic treatment. Interruption of cancer treatment due to gastrointestinal mucositis leads to a significant decrease in cure rates and consequently to the deterioration of a patient’s quality of life. Natural polysaccharides show a variety of beneficial effects, including a gastroprotective effect. Treatment with soluble dietary fiber (SDF) from yellow passion fruit (Passiflora edulis) biomass residues protected the gastric and intestinal mucosa in models of gastrointestinal injury. In this study, we investigated the protective therapeutic effect of SDF on 5-FU-induced mucositis in male and female mice. Oral treatment of the animals with SDF did not prevent weight loss but reduced the disease activity index and preserved normal intestinal function by alleviating diarrhea and altered gastrointestinal transit. SDF preserved the length of the colon and histological damage caused by 5-FU. SDF significantly restored the oxidative stress and inflammation in the intestine and the enlargement and swelling of the spleen induced by 5-FU. In conclusion, SDF may be a promising adjuvant strategy for the prevention and treatment of intestinal mucositis induced by 5-FU. Full article
(This article belongs to the Special Issue Polysaccharides as Drug Candidates)
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21 pages, 4047 KiB  
Article
Isolation, Purification, and Structural Characterization of Polysaccharides from Codonopsis pilosula and Their Anti-Tumor Bioactivity by Immunomodulation
by Nan Li, Ying-Xia Xiong, Fan Ye, Bing Jin, Jin-Jia Wu, Miao-Miao Han, Tian Liu, Yi-Kai Fan, Cun-Yu Li, Jiu-Shi Liu, Ying-Hua Zhang, Gui-Bo Sun, Yun Zhang and Zheng-Qi Dong
Pharmaceuticals 2023, 16(6), 895; https://doi.org/10.3390/ph16060895 - 19 Jun 2023
Cited by 3 | Viewed by 1613
Abstract
The activity of polysaccharides is usually related to molecular weight. The molecular weight of polysaccharides is critical to their immunological effect in cancer therapy. Herein, the Codonopsis polysaccharides of different molecular weights were isolated using ultrafiltration membranes of 60- and 100-wDa molecular weight [...] Read more.
The activity of polysaccharides is usually related to molecular weight. The molecular weight of polysaccharides is critical to their immunological effect in cancer therapy. Herein, the Codonopsis polysaccharides of different molecular weights were isolated using ultrafiltration membranes of 60- and 100-wDa molecular weight cut-off to determine the relationship between molecular weight and antitumor activities. First, three water-soluble polysaccharides CPPS-I (<60 wDa), CPPS-II (60–100 wDa), and CPPS-III (>100 wDa) from Codonopsis were isolated and purified using a combination of macroporous adsorption resin chromatography and ultrafiltration. Their structural characteristics were determined through chemical derivatization, GPC, HPLC, FT–IR, and NMR techniques. In vitro experiments indicated that all Codonopsis polysaccharides exhibited significant antitumor activities, with the tumor inhibition rate in the following order: CPPS-II > CPPS-I > CPPS-III. The treatment of CPPS-II exhibited the highest inhibition rate at a high concentration among all groups, which was almost as efficient as that of the DOX·HCL (10 μg/mL) group at 125 μg/mL concentration. Notably, CPPS-II demonstrated the ability to enhance NO secretion and the antitumor ability of macrophages relative to the other two groups of polysaccharides. Finally, in vivo experiments revealed that CPPS-II increased the M1/M2 ratio in immune system regulation and that the tumor inhibition effect of CPPS-II + DOX was superior to that of DOX monotherapy, implying that CPPS-II + DOX played a synergistic role in regulating the immune system function and the direct tumor-killing ability of DOX. Therefore, CPPS-II is expected to be applied as an effective cancer treatment or adjuvant therapy. Full article
(This article belongs to the Special Issue Polysaccharides as Drug Candidates)
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20 pages, 1574 KiB  
Article
Characterization, In Vitro Biological Activity and In Vivo Cardioprotective Properties of Trametes versicolor (L.:Fr.) Quél. Heteropolysaccharides in a Rat Model of Metabolic Syndrome
by Marina Nikolic, Nevena Lazarevic, Jovana Novakovic, Nevena Jeremic, Vladimir Jakovljevic, Vladimir Zivkovic, Jovana Bradic, Danijela Pecarski, Gülsen Tel-Çayan, Jasmina Glamocija, Marina Sokovic, Andrej Gregori and Jovana Petrovic
Pharmaceuticals 2023, 16(6), 787; https://doi.org/10.3390/ph16060787 - 25 May 2023
Cited by 3 | Viewed by 1762
Abstract
The present study aimed to examine the biological activity and cardioprotective potential of Trametes versicolor heteropolysaccharides (TVH) in a rat model of metabolic syndrome (MetS). This study included 40 Wistar rats divided into 5 groups: CTRL—healthy non-treated rats; MetS—non-treated rats; and H-TV, M-TV [...] Read more.
The present study aimed to examine the biological activity and cardioprotective potential of Trametes versicolor heteropolysaccharides (TVH) in a rat model of metabolic syndrome (MetS). This study included 40 Wistar rats divided into 5 groups: CTRL—healthy non-treated rats; MetS—non-treated rats; and H-TV, M-TV and L-TV-rats with MetS treated with either 300, 200 or 100 mg/kg TVH per os for 4 weeks. After finishing the treatment, we conducted an oral glucose tolerance test (OGTT), hemodynamic measurements and the animals were sacrificed, hearts isolated and subjected to the Langendorff technique. Blood samples were used for the determination of oxidative stress parameters, lipid status and insulin levels. We showed that α-amylase inhibition was not the mode of TVH antidiabetic action, while TVH showed a moderate inhibition of pathogenic microorganisms’ growth (MIC 8.00 mg·mL−1; MBC/MFC 16.00 mg·mL−1). H-TV and M-TV significantly reduced the level of prooxidants (O2−, H2O2, TBARS; p < 0.05), increased antioxidants activity (SOD, CAT, GSH; p < 0.05), reduced blood pressure (p < 0.05), improved glucose homeostasis in the OGTT test (p < 0.05), and ejection fraction (p < 0.05) and cardiac contractility (p < 0.05) compared to MetS (p < 0.05). Moreover, TVH treatment normalized the lipid status and decreased insulin levels compared to MetS rats (p < 0.05). The obtained results demonstrated that the TVH may be considered a useful agent for cardioprotection in MetS conditions. Full article
(This article belongs to the Special Issue Polysaccharides as Drug Candidates)
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13 pages, 2657 KiB  
Article
Analysis of Structure and Antioxidant Activity of Polysaccharides from Aralia continentalis
by Yan-bo Hu, Hui-li Hong, Li-yang Liu, Jia-ning Zhou, Yue Wang, Yi-ming Li, Li-yuan Zhai, Zeng-hui Shi, Jun Zhao and Duo Liu
Pharmaceuticals 2022, 15(12), 1545; https://doi.org/10.3390/ph15121545 - 13 Dec 2022
Cited by 3 | Viewed by 1325
Abstract
We extracted, purified, and characterized three neutral and three acidic polysaccharides from the roots, stems, and leaves of Aralia continentalis Kitigawa. The results of the analysis of monosaccharide composition indicated that the polysaccharides from the roots and stems were more similar to each [...] Read more.
We extracted, purified, and characterized three neutral and three acidic polysaccharides from the roots, stems, and leaves of Aralia continentalis Kitigawa. The results of the analysis of monosaccharide composition indicated that the polysaccharides from the roots and stems were more similar to each other than they were to the polysaccharides from the leaves. The in vitro antioxidant results demonstrated that the acidic polysaccharides had stronger antioxidant activity than the neutral fractions. Therefore, we investigated the primary purified acidic polysaccharide fractions (WACP(R)-A-c, WACP(S)-A-c, and WACP(L)-A-d) by NMR and enzymatic analysis. The structural analytical results indicated that WACP(R)-A-c contained homogalacturonan (HG); WACP(S)-A-c contained HG and rhamnogalacturonan II (RG-II), and WACP(L)-A-d contained HG, RG-II, and rhamnogalacturonan I (RG-I) domains. Our findings offer insights into the screening of natural polysaccharide-based antioxidants and provide a theoretical basis for the application of A. continentalis. Full article
(This article belongs to the Special Issue Polysaccharides as Drug Candidates)
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