Advances in Natural Products and Their Derivatives for Metabolic and Chronic Inflammatory Disease Therapy—2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 20 July 2024 | Viewed by 2279

Special Issue Editors


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Guest Editor
LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: medicinal chemistry; drug discovery; inflammation; oxidative stress; diabetes; obesity; phenolic compounds
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: medicinal chemistry; inflammation; endocrine-disrupting chemicals; nanoparticles; oxidative stress; diabetes
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
LAQV, REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Interests: natural products; drug discovery; chronic inflammation; diabetes; obesity; osteoarthritis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The 21st century has seen a sharp increase in the incidence of metabolic and chronic diseases, including diabetes, obesity, dyslipidemia, cancer, and chronic inflammatory-related diseases (e.g., rheumatic diseases). Currently, there are several pharmacological approaches to treat these diseases. However, the available therapeutical options are not totally effective, frequently being associated with several adverse effects.

The pharmacological or biological activities of natural products have been intensively explored over the years, resulting in hundreds of molecules presently being used in clinics. Due to their structural diversity, natural products remain a major source and challenge for the identification of novel lead molecules with the potential to treat diseases, namely, metabolic and chronic diseases.

We are pleased to invite you to participate in this Special Issue on “Advances in Natural Products and Their Derivatives for Metabolic and Chronic Inflammatory Disease Therapy” by submitting a contribution in the form of an original research paper, short communication, and/or global or specialized critical review, according to your field of expertise.

This Special Issue aims to explore and describe biological activities, including antioxidant and anti-inflammatory properties, as well as antidiabetic, antiobesogenic, antirheumatic, and anticancer activities of natural products/substances and their derivatives, disclosing their role as possible therapeutic agents for metabolic and chronic inflammatory diseases.

Research in this area has significantly expanded to include the chemical identification of these compounds using advanced analytical techniques, determining their mechanism of action, allowing food fortification and supplement development, and enhancing their bioavailability and bioactivity using, for instance, nanotechnology.

Therefore, the main, but not exclusive, topics to be dealt with in the Special Issue “Advances in Natural Products and Their Derivatives for Metabolic and Chronic Inflammatory Disease Therapy” include the potential treatment of the following diseases, addressing whenever possible, the development of novel methodologies and the establishment of structure–activity relationships:

  • Diabetes;
  • Obesity;
  • Metabolic diseases;
  • Inflammation and oxidative-stress related diseases.

We look forward to receiving your contributions.

Dr. Eduarda Fernandes
Dr. Marisa Freitas
Dr. Ana Teresa Rufino
Guest Editors

Manuscript Submission Information

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Keywords

  • natural products
  • metabolic diseases
  • chronic inflammation
  • drug discovery
  • biological activity
  • diabetes
  • obesity
  • rheumatic diseases

Published Papers (2 papers)

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Research

14 pages, 3243 KiB  
Article
Anti-Inflammatory Effects of Chamaecyparis obtusa (Siebold & Zucc.) Endl. Leaf Extract Fermented by Ganoderma applanatum Mycelia
by Chae-Hyun Kim, Yong-Jin Kwon and Young-Ah Jang
Pharmaceutics 2024, 16(3), 365; https://doi.org/10.3390/pharmaceutics16030365 - 05 Mar 2024
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Abstract
Corticosteroids are commonly used anti-inflammatory agents. However, their prolonged use can lead to side effects. Therefore, the development of natural compounds with minimal side effects is necessary. This study was performed to investigate the anti-inflammatory effects and mechanisms of action of Chamaecyparis obtusa [...] Read more.
Corticosteroids are commonly used anti-inflammatory agents. However, their prolonged use can lead to side effects. Therefore, the development of natural compounds with minimal side effects is necessary. This study was performed to investigate the anti-inflammatory effects and mechanisms of action of Chamaecyparis obtusa (Siebold & Zucc.) Endl. leaf (COL), bioconverted using Ganoderma applanatum (G. applanatum) in lipopolysaccharide (LPS)-induced RAW264.7 cells. The COL 70% EtOH extract fermented by G. applanatum (70COLGA) improved the high cytotoxicity of 70% EtOH extracts (70COL). When RAW264.7 cells were pre-treated with 100 and 200 μg/mL of 70COLGA for 2 h and then treated with LPS for 16 h, LPS induced the production of nitric oxide (NO), and the expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2) were significantly inhibited. When RAW264.7 cells were pre-treated with 100 and 200 μg/mL of 70COLGA for 2 h and then treated with LPS for 4 h, the phosphorylation of signal transducers and activators of transcription (STAT) was markedly decreased. In addition, 70COLGA markedly suppressed the production of the inflammatory cytokines interleukin (IL)-1β and IL-6 in LPS-induced RAW264.7 cells. Analysis of pro-inflammatory molecules using cytokine arrays showed that macrophage inflammatory protein (MIP)-2, granulocyte–macrophage colony-stimulating factor (GM-CSF), granulocyte colony-stimulating factor (G-CSF) and IL-27 expressions were also suppressed by 200 μg/mL of 70COLGA in LPS-induced RAW264.7 cells. These results demonstrate that 70COLGA significantly prevented inflammatory responses by inhibiting the secretion of pro-inflammatory molecules in LPS-induced RAW264.7 cells. When RAW264.7 cells were pre-treated with 100 and 200 μg/mL of 70COLGA for 2 h and then treated with LPS-conditioned medium (LPS-CM) for 30 min, 70COLGA directly inhibited STAT activation. In summary, our findings suggest that 70COLGA has therapeutic potential for the treatment of inflammatory diseases. Full article
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18 pages, 3717 KiB  
Article
Melanoxetin: A Hydroxylated Flavonoid Attenuates Oxidative Stress and Modulates Insulin Resistance and Glycation Pathways in an Animal Model of Type 2 Diabetes Mellitus
by Sónia Rocha, Andreia Amaro, Marcos D. Ferreira-Junior, Carina Proença, Artur M. S. Silva, Vera M. Costa, Sara Oliveira, Diogo A. Fonseca, Sónia Silva, Maria Luísa Corvo, Marisa Freitas, Paulo Matafome and Eduarda Fernandes
Pharmaceutics 2024, 16(2), 261; https://doi.org/10.3390/pharmaceutics16020261 - 09 Feb 2024
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Abstract
Type 2 diabetes mellitus (DM) continues to escalate, necessitating innovative therapeutic approaches that target distinct pathways and address DM complications. Flavonoids have been shown to possess several pharmacological activities that are important for DM. This study aimed to evaluate the in vivo effects [...] Read more.
Type 2 diabetes mellitus (DM) continues to escalate, necessitating innovative therapeutic approaches that target distinct pathways and address DM complications. Flavonoids have been shown to possess several pharmacological activities that are important for DM. This study aimed to evaluate the in vivo effects of the flavonoid melanoxetin using Goto-Kakizaki rats. Over a period of 14 days, melanoxetin was administered subcutaneously to investigate its antioxidant, anti-inflammatory, and antidiabetic properties. The results show that melanoxetin reduced insulin resistance in adipose tissue by targeting protein tyrosine phosphatase 1B. Additionally, melanoxetin counteracted oxidative stress by reducing nitrotyrosine levels and modulating superoxide dismutase 1 and hemeoxygenase in adipose tissue and decreasing methylglyoxal-derived hydroimidazolone (MG-H1), a key advanced glycation end product (AGE) implicated in DM-related complications. Moreover, the glyoxalase 1 expression decreased in both the liver and the heart, correlating with reduced AGE levels, particularly MG-H1 in the heart. Melanoxetin also demonstrated anti-inflammatory effects by reducing serum prostaglandin E2 levels, and increasing the antioxidant status of the aorta wall through enhanced acetylcholine-dependent relaxation in the presence of ascorbic acid. These findings provide valuable insights into melanoxetin’s therapeutic potential in targeting multiple pathways involved in type 2 DM, particularly in mitigating oxidative stress and glycation. Full article
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