Anti-Inflammatory Effects from Natural Bioactive Compounds—from Bench to Bedside, 3rd Edition

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

Deadline for manuscript submissions: 30 November 2025 | Viewed by 559

Special Issue Editor


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Guest Editor
Department of Structural and Functional Biology, Institute of Biosciences, São Paulo State University (Unesp), Botucatu 18618-689, Brazil
Interests: biopharmaceutics; inflammation; morphophysiology; drug design; natural products; antioxidants; gastrointestinal diseases; diabetes; wound healing
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Special Issue Information

Dear Colleagues,

Inflammation is a response of organisms to the breakdown of tissue homeostasis. Infection, injury, autoimmune diseases, and chemicals can cause inflammation. The acute inflammatory response begins with increased vascular permeability and leukocyte migration, which will try to eliminate pathogenic organisms through the release of reactive oxygen species, reactive nitrogen species, and proteases. Additionally, neutrophils release inflammatory mediators, including chemokines, attracting macrophages to the site of inflammation and increasing the inflammatory response. These macrophages produce a whole cascade of inflammatory mediators, such as prostaglandins, leukotrienes, and cytokines. The chronic inflammatory response starts with the persistence of the inflammatory agent in a process that could be harmful not only to the inflammatory agent, but also to healthy tissues.

Although conventional anti-inflammatory treatments demonstrate effectiveness in treating inflammation, their use could trigger low, mild, and severe adverse effects. The use of biopharmaceutics and natural products of animal or vegetal origin to treat inflammation is increasing worldwide and encouraging researchers to investigate the anti-inflammatory mechanisms of isolated compounds from natural sources.

Thus, this Special Issue will highlight current research exploring the anti-inflammatory mechanisms of bioproducts of natural origin (including but not limited to vegetal and animal sources), which could be investigated in several diseases using in vivo models or described using in vitro assays. Clinical assays are also welcome.

Prof. Dr. Ariane Leite Rozza
Guest Editor

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Keywords

  • inflammation
  • bioproducts
  • isolated compounds
  • cytokines
  • macrophages
  • autoimmune diseases
  • in vivo assay
  • in vitro assay

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23 pages, 1706 KB  
Article
Polyphenol-Rich Citrullus lanatus Rind Extract Mitigates Doxorubicin-Induced Cardiotoxicity: HPLC Profiling and In Vivo Evaluation
by Bader Alsuwayt
Pharmaceutics 2025, 17(11), 1469; https://doi.org/10.3390/pharmaceutics17111469 - 14 Nov 2025
Viewed by 328
Abstract
Background/Objectives: Cardiovascular diseases (CVDs) remain a major cause of mortality globally, driven in part by oxidative stress and inflammation. The present study investigated the polyphenolic composition and cardioprotective potential of polyphenol-rich Citrullus lanatus (PRCL) rind extract against doxorubicin-induced cardiotoxicity in rats; Methods: [...] Read more.
Background/Objectives: Cardiovascular diseases (CVDs) remain a major cause of mortality globally, driven in part by oxidative stress and inflammation. The present study investigated the polyphenolic composition and cardioprotective potential of polyphenol-rich Citrullus lanatus (PRCL) rind extract against doxorubicin-induced cardiotoxicity in rats; Methods: High-performance liquid chromatography (HPLC) was employed to identify and quantify the major bioactive compounds present in the extract. Total 30 healthy male Wistar Kyoto rats were recruited and divided into 6 groups and various cardiovascular markers and antioxidant were measured in vivo and in vitro methods; Results: Ethanolic extraction of Citrullus lanatus rind yielded 19.58 g extract per 100 g of dry plant material. HPLC analysis identified five phenolic acids, i.e., gallic acid, p-hydroxybenzoic acid (PHBA), chlorogenic acid, caffeic acid, and vanillic acid, and two flavonoids, i.e., catechin and hesperetin, with PHBA (163.66 mg/g of extract) being the most abundant. Total phenolic and flavonoid content was determined to be 35.6 mg GAE/g and 12.8 mg CE/g, respectively. In vitro antioxidant assays showed moderate free radical scavenging, reducing power, and 86.9% inhibition of linoleic acid peroxidation. In vivo, Wistar rats were treated with doxorubicin (10 mg/kg) to induce cardiotoxicity, followed by PRCL extract administration (21 days at 250 and 500 mg/kg/day). The extract significantly improved body weight, serum lipid profile, and reduced cardiovascular risk indices. Antioxidant biomarkers (SOD, CAT, GPx, GSH) were restored, while lipid peroxidation (MDA) and inflammatory cytokines (TNF-α, IL-6) were significantly reduced in treated groups. The 500 mg/kg dose demonstrated superior efficacy, comparable to the standard quercetin group. Histopathological examination revealed notable protection of cardiac tissue architecture in the high-dose PRCL-500 group; Conclusions: These findings suggest that PRCL rind extract contains potent compounds having antioxidant and cardioprotective properties and may be used as a natural therapeutic agent against cardiotoxicity. Full article
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