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Pharmaceutics
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Advances in Natural Products and Their Derivatives for Metabolic and...
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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: closed (20 July 2024) | Viewed by 5150

Special Issue Editors

Dr. Eduarda Fernandes

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; drug discovery; inflammation; oxidative stress; diabetes; obesity; phenolic compounds
Special Issues, Collections and Topics in MDPI journals
Dr. Marisa Freitas

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
Dr. Ana Teresa Rufino

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.

You may choose our Joint Special Issue in Pharmaceuticals.

Dr. Eduarda Fernandes
Dr. Marisa Freitas
Dr. Ana Teresa Rufino
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 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. Pharmaceutics 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

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

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Published Papers (3 papers)

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Research

20 pages, 3319 KiB  
Article
Combinatory Effect of Pequi Oil (Caryocar brasiliense)-Based Nanoemulsions Associated to Docetaxel and Anacardic Acid (Anacardium occidentale) in Triple-Negative Breast Cancer Cells In Vitro
by Alicia Simalie Ombredane, Natália Ornelas Martins, Gabriela Mara Vieira de Souza, Victor Hugo Sousa Araujo, Ísis O. Szlachetka, Sebastião William da Silva, Márcia Cristina Oliveira da Rocha, Andressa Souza de Oliveira, Cleonice Andrade Holanda, Luiz Antonio Soares Romeiro, Elysa Beatriz de Oliveira Damas, Ricardo Bentes Azevedo and Graziella Anselmo Joanitti
Pharmaceutics 2024, 16(9), 1170; https://doi.org/10.3390/pharmaceutics16091170 - 5 Sep 2024
Cited by 1 | Viewed by 872
Abstract
Combination therapy integrated with nanotechnology offers a promising alternative for breast cancer treatment. The inclusion of pequi oil, anacardic acid (AA), and docetaxel (DTX) in a nanoemulsion can amplify the antitumor effects of each molecule while reducing adverse effects. Therefore, the study aims [...] Read more.
Combination therapy integrated with nanotechnology offers a promising alternative for breast cancer treatment. The inclusion of pequi oil, anacardic acid (AA), and docetaxel (DTX) in a nanoemulsion can amplify the antitumor effects of each molecule while reducing adverse effects. Therefore, the study aims to develop pequi oil-based nanoemulsions (PeNE) containing DTX (PDTX) or AA (PAA) and to evaluate their cytotoxicity against triple-negative breast cancer cells (4T1) in vitro. The PeNE without and with AA (PAA) and DTX (PDTX) were prepared by sonication and characterized by ZetaSizer® and electronic transmission microscopy. Viability testing and combination index (CI) were determined by MTT and Chou-Talalay methods, respectively. Flow cytometry was employed to investigate the effects of the formulations on cell structures. PeNE, PDTX, and PAA showed hydrodynamic diameter < 200 nm and a polydispersity index (PdI) of 0.3. The association PDTX + PAA induced a greater decrease in cell viability (~70%, p < 0.0001) and additive effect (CI < 1). In parallel, an association of the DTX + AA molecules led to antagonism (CI > 1). Additionally, PDTX + PAA induced an expressive morphological change, a major change in lysosome membrane permeation and mitochondria membrane permeation, cell cycle blockage in G2/M, and phosphatidylserine exposure. The study highlights the successful use of pequi oil nanoemulsions as delivery systems for DTX and AA, which enhances their antitumor effects against breast cancer cells. This nanotechnological approach shows significant potential for the treatment of triple-negative breast cancer. Full article
(This article belongs to the Special Issue Advances in Natural Products and Their Derivatives for Metabolic and Chronic Inflammatory Disease Therapy, 2nd Edition)
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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 - 5 Mar 2024
Viewed by 1409
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
(This article belongs to the Special Issue Advances in Natural Products and Their Derivatives for Metabolic and Chronic Inflammatory Disease Therapy, 2nd Edition)
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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 - 9 Feb 2024
Viewed by 1964
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
(This article belongs to the Special Issue Advances in Natural Products and Their Derivatives for Metabolic and Chronic Inflammatory Disease Therapy, 2nd Edition)
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