Natural Pharmaceuticals Focused on Anti-inflammatory Activities

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

Deadline for manuscript submissions: 20 May 2025 | Viewed by 4435

Special Issue Editors


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Guest Editor
Institute for the Application of Nuclear Energy INEP, University of Belgrade, Banatska 31b, 11080 Belgrade, Serbia
Interests: extraction of biologically active compounds from plants and fungi; encapsulation of biologically active compounds; biological activities of extracts and encapsulates; food and cosmetic safety

Special Issue Information

Dear Colleagues,

Plant and fungi kingdoms synthesize and store various bioactive compounds which are related to numerous health benefits in humans and animals. Additionally, many products from natural sources show significant anti-inflammatory effects. Since inflammation plays an important role in the development and progression of different illnesses, such as arthritis, asthma, cancer, cardiovascular, neurodegenerative, and autoimmune diseases, natural products possessing anti-inflammatory properties have attracted considerable scientific attention.

This Special Issue aims to present review papers and original articles focusing on current knowledge of bioactive natural products with anti-inflammatory properties. The results of anti-inflammatory activity studies documented in vitro and in vivo are appreciated. As for many natural products, there is a lack of data related to their bioactive compounds, and special emphasis is given to the submission of articles with biomolecular experiments. The identification and quantification of compounds with anti-inflammatory properties, their physicochemical characterization, mechanisms of biological activity, and relationships between structure and bioactivity (molecular docking) are welcome as well. Studies related to the complexes of natural products and carriers (as a system for controlled release) or natural products in the final formulation are also appreciated.

Research areas may include but are not limited to:

  • in vitro and in vivo study of anti-inflammatory activity of natural products
  • identification and quantification of compounds with anti-inflammatory properties and their physicochemical characterization
  • mechanisms of anti-inflammatory activity and structure-effect relationships
  • pharmaceutical formulations based on natural products with anti-inflammatory properties
  • delivery and controlled-release systems for natural products with anti-inflammatory properties
  • pharmaceutical process, engineering, biotechnology, and nanotechnology related to the production of natural anti-inflammatory agents
  • natural anti-inflammatory agent design and targeting
  • pharmacodynamics, pharmacokinetics (absorption, distribution, metabolism, and excretion), and toxicokinetics
  • physiological and biochemical effects of natural anti-inflammatory agents on the body

We look forward to receiving your contributions.

Dr. Katarina Šavikin
Dr. Aleksandra A. Jovanović
Guest Editors

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Keywords

  • anti-inflammatory properties
  • chemical identification of natural anti-inflammatory agents
  • delivery and controlled-release systems
  • natural extracts
  • mechanisms of natural anti-inflammatory agents
  • molecular docking
  • natural products
  • plants and fungi
  • structure–effect relationships

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Published Papers (5 papers)

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Research

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17 pages, 1529 KiB  
Article
Apodanthera glaziovii (Cucurbitaceae) Shows Strong Anti-Inflammatory Activity in Murine Models of Acute Inflammation
by Maria Lorena de Oliveira Andrade, Pedro Artur Ferreira Marinho, Alisson Macário de Oliveira, Thalisson Amorim de Souza, Samuel Paulo Cibulski and Harley da Silva Alves
Pharmaceutics 2024, 16(10), 1298; https://doi.org/10.3390/pharmaceutics16101298 - 4 Oct 2024
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Abstract
Background/objectives: Apodanthera glaziovii is an endemic species from the semi-arid Brazilian, which has limited toxicological and pharmacological studies. This species belongs to a well-studied family known for its bioactive compounds used in treating inflammatory. This study aimed to identify secondary metabolites in [...] Read more.
Background/objectives: Apodanthera glaziovii is an endemic species from the semi-arid Brazilian, which has limited toxicological and pharmacological studies. This species belongs to a well-studied family known for its bioactive compounds used in treating inflammatory. This study aimed to identify secondary metabolites in the stems from A. glaziovii, evaluate toxicity, and investigate the anti-inflammatory potential of the stem hydroalcoholic extract (SHE-Ag). Methods: qualitative and quantitative assays were employed to identify secondary metabolites, along with chromatographic analyses and 1H and 13C NMR. Toxicity was assessed through in vitro hemolytic toxicity, in vivo genotoxicity, and oral acute toxicity tests before the pharmacological assays were conducted. Results: phytochemical screening, HPLC and NMR analyses suggested the presence of saponins of the norcucurbitacin class. The SHE-Ag exhibited no hemolytic activity and no mutagenic potential. However, in vivo toxicity at a dose of 2000 mg/kg revealed hematological and biochemical alterations, while the 500 mg/kg dose was safe. In the anti-inflammatory assays, SHE-Ag at 100 mg/kg reduced paw edema by 55.8%, and leukocyte and neutrophil migration by 62% and 68% in the peritonitis model, respectively; inflammatory cell migration by 70% in the air pouch model, outperforming indomethacin, which showed a 54% reduction. Conclusions: these findings indicate that SHE-Ag is rich in saponins, confirmed through HPLC and 1H and 13C NMR analyses. The SHE-Ag also demonstrated low toxicity. The inflammation models used showed a reduction in inflammation, pro-inflammatory cells, and edema, highlighting the significant anti-inflammatory activity of hydroethanolic extract A. glaziovii stems. Full article
(This article belongs to the Special Issue Natural Pharmaceuticals Focused on Anti-inflammatory Activities)
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22 pages, 5463 KiB  
Article
Newly Developed Semi-Solid Formulations Containing Mellilotus officinalis Extract: Characterization, Assessment of Stability, Safety, and Anti-Inflammatory Activity
by Jovana Bradic, Anica Petrovic, Milos Nikolic, Nikola Nedeljkovic, Marijana Andjic, Nebojsa Kladar, Stefani Bolevich, Vladimir Jakovljevic and Aleksandar Kocovic
Pharmaceutics 2024, 16(8), 1003; https://doi.org/10.3390/pharmaceutics16081003 - 29 Jul 2024
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Abstract
Melilotus officinalis has been traditionally used as an anti-inflammatory agent; nevertheless, a comprehensive evaluation of its efficacy and safety and comparison with standard drugs are lacking. Taking into consideration concerns with current therapies, like efficacy limitations, side effects, and resistance, we aimed to [...] Read more.
Melilotus officinalis has been traditionally used as an anti-inflammatory agent; nevertheless, a comprehensive evaluation of its efficacy and safety and comparison with standard drugs are lacking. Taking into consideration concerns with current therapies, like efficacy limitations, side effects, and resistance, we aimed to develop a natural gel and cream based on Melilotus officinalis extract and explore their anti-inflammatory potential. After the chemical analysis of the extract confirmed the presence of coumarin, p-coumaric acid, gallic acid, and quercetin, formulations were prepared and subjected to physical and chemical stability evaluations over 6 months. The safety potential was tested in rats, while the anti-inflammatory activity was assessed both via in silico tests and in a rat model of inflammation. The examined formulations showed stable physical characteristics at the defined storage conditions and did not exert any sign of adverse skin reaction. The gel formulation exhibited a remarkable effect in inflammation reduction comparable with hydrocortisone. The in silico results suggest that coumarin, p-coumaric, and gallic acid bind to COX-1 and COX-2 with a lower affinity compared to diclofenac. On the other hand, quercetin demonstrated comparable inhibitory activity and stronger interaction compared to the control drug. Our results indicate that the examined formulations are stable and safe and may be promising dermal products for the alleviation of inflammatory skin conditions. Full article
(This article belongs to the Special Issue Natural Pharmaceuticals Focused on Anti-inflammatory Activities)
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21 pages, 23648 KiB  
Article
Liposome Encapsulation Enhances the Antidiabetic Efficacy of Silibinin
by Svetlana Dinić, Jelena Arambašić Jovanović, Aleksandra Uskoković, Aleksandra Jovanović, Nevena Grdović, Jovana Rajić, Marija Đorđević, Ana Sarić, Branko Bugarski, Melita Vidaković and Mirjana Mihailović
Pharmaceutics 2024, 16(6), 801; https://doi.org/10.3390/pharmaceutics16060801 - 13 Jun 2024
Cited by 1 | Viewed by 971
Abstract
Silibinin has considerable therapeutic potential for the treatment of diabetes through anti-inflammatory, antioxidant, and immunomodulatory properties. However, the therapeutic application of silibinin is quite limited due to its poor bioavailability. In the present study, an attempt was made to improve the antidiabetic efficacy [...] Read more.
Silibinin has considerable therapeutic potential for the treatment of diabetes through anti-inflammatory, antioxidant, and immunomodulatory properties. However, the therapeutic application of silibinin is quite limited due to its poor bioavailability. In the present study, an attempt was made to improve the antidiabetic efficacy of silibinin by its encapsulation in liposomal vesicles. The liposomes with a high encapsulation efficiency of silibinin (96%) and a zeta potential of −26.2 ± 0.6 mV were developed and studied using nicotinamide/streptozotocin-induced diabetic rats. Administration of silibinin-loaded liposomes to diabetic rats lowered glucose levels, increased insulin levels, and improved pancreatic islet architecture. The anti-inflammatory effect of silibinin-loaded liposomes was demonstrated by a decrease in serum C-reactive protein (CRP) levels and a reduced deposition of collagen fibers in the islets of diabetic rats. Furthermore, silibinin-loaded liposomes were more efficient in lowering glucose, alanine transaminase, triglyceride, and creatinine levels in diabetic rats than pure silibinin. In addition, silibinin-loaded liposomes had a significantly better effect on beta-cell mass and Glut2 glucose receptor distribution in diabetic islets than pure silibinin. The present results clearly show that liposome encapsulation of silibinin enhances its antidiabetic efficacy, which may contribute to the therapeutic benefit of silibinin in the treatment of diabetes and its complications. Full article
(This article belongs to the Special Issue Natural Pharmaceuticals Focused on Anti-inflammatory Activities)
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41 pages, 2188 KiB  
Article
Vaccinium myrtillus L. Leaf Waste as a Source of Biologically Potent Compounds: Optimization of Polyphenol Extractions, Chemical Profile, and Biological Properties of the Extracts
by Muna Rajab Elferjane, Violeta Milutinović, Milica Jovanović Krivokuća, Mohammad J. Taherzadeh, Witold Pietrzak, Aleksandar Marinković and Aleksandra A. Jovanović
Pharmaceutics 2024, 16(6), 740; https://doi.org/10.3390/pharmaceutics16060740 - 30 May 2024
Cited by 1 | Viewed by 1102
Abstract
The aims of the present research include (1) optimization of extraction from Vaccinium myrtillus leaf waste via investigation of plant material:medium ratio, extraction medium, and extraction period, employing extractions at room and high temperatures, or using ultrasound and microwaves (M, HAE, UAE, and [...] Read more.
The aims of the present research include (1) optimization of extraction from Vaccinium myrtillus leaf waste via investigation of plant material:medium ratio, extraction medium, and extraction period, employing extractions at room and high temperatures, or using ultrasound and microwaves (M, HAE, UAE, and MAE, respectively), (2) physicochemical characterization, and (3) investigation of extract biological potential. The statistical analysis revealed that optimal levels of parameters for the greatest polyphenolic yield were a proportion of 1:30 g/mL, ethyl alcohol 50% (v/v) during 2 min of microwave irradiation. By LC-MS analysis, 29 phenolic components were detected; HAE showed the highest richness of almost all determined polyphenols, while chlorogenic acid and quercetin 3-O-glucuronide were dominant. All extracts showed a high inhibition of Staphylococcus aureus growth. The effect of different parameters on extracts’ antioxidant capacity depended on the used tests. The extracts also showed a stimulative influence on keratinocyte viability and anti-inflammatory activity (proven in cell-based ELISA and erythrocyte stabilization assays). The extraction procedure significantly affected the extraction yield (MAE ≥ maceration ≥ UAE ≥ HAE), whereas conductivity, density, surface tension, and viscosity varied in a narrow range. The presented research provides evidence on the optimal extraction conditions and technique, chemical composition, and antioxidant, antimicrobial, anti-inflammatory, and keratinocyte viability properties of bilberry extracts for potential applications in pharmacy and cosmetics. Full article
(This article belongs to the Special Issue Natural Pharmaceuticals Focused on Anti-inflammatory Activities)
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Review

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15 pages, 1954 KiB  
Review
Hydroxytyrosol: A Promising Therapeutic Agent for Mitigating Inflammation and Apoptosis
by Wafa Ali Batarfi, Mohd Heikal Mohd Yunus, Adila A. Hamid, Yi Ting Lee and Manira Maarof
Pharmaceutics 2024, 16(12), 1504; https://doi.org/10.3390/pharmaceutics16121504 - 22 Nov 2024
Abstract
Inflammation and apoptosis are interrelated biological processes that have a significant impact on the advancement and growth of certain chronic diseases, such as cardiovascular problems, neurological conditions, and osteoarthritis. Recent research has emphasized that focusing on these mechanisms could result in novel therapeutic [...] Read more.
Inflammation and apoptosis are interrelated biological processes that have a significant impact on the advancement and growth of certain chronic diseases, such as cardiovascular problems, neurological conditions, and osteoarthritis. Recent research has emphasized that focusing on these mechanisms could result in novel therapeutic approaches that aim to decrease the severity of diseases and enhance patient outcomes. Hydroxytyrosol (HT), which is well-known for its ability to prevent oxidation, has been identified as a possible candidate for regulating both inflammation and apoptosis. In this review, we will highlight the multifaceted benefits of HT as a therapeutic agent in mitigating inflammation, apoptosis, and associated conditions. This review provides a comprehensive overview of the latest in vitro and in vivo research on the anti-inflammatory and antiapoptotic effects of HT and the mechanisms by which it works. Based on these studies, it is strongly advised to use HT as a bioactive ingredient in pharmaceutical products intended for mitigating inflammation, as well as those with apoptosis applications. Full article
(This article belongs to the Special Issue Natural Pharmaceuticals Focused on Anti-inflammatory Activities)
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