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Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 July 2022) | Viewed by 28256

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Prof. Dr. Francesco Maione

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ImmunoPharmaLab, Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80138 Naples, Italy
Interests: inflammation; immuno-pharmacology; pharmacology of natural compounds and nutraceuticals
Special Issues, Collections and Topics in MDPI journals

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Dear Colleagues,

Inflammation is a complex biological response to injury as a result of different stimuli, such as pathogens, damaged cells, or irritants. Inflammatory injuries induce the release of a variety of systemic mediators, cytokines, and chemokines that orchestrate the cellular infiltration that consequentially brings about the resolution of inflammatory responses and the restoration of tissue integrity. However, persistent inflammatory stimuli or the dysregulation of mechanisms of the resolution phase can lead to chronic inflammation and inflammation-based diseases.

At present, commercially approved anti-inflammatory drugs are represented by nonsteroidal anti-inflammatory drugs (NSAIDs), glucocorticoids (SAIDs), and in some cases, immunosuppressant and/or biological drugs. These agents are effective for the relief of the main inflammatory symptoms. However, they induce severe side effects, and most of them are inadequate for chronic use.

Starting from these premises, the demand for new effective and safe anti-inflammatory drugs has furthered research into new therapeutic approaches. The recent and emerging scientific community approach is oriented towards natural products/compounds that could aid the discovery of new active molecules and the development of new drugs and potentially useful therapeutic agents in different inflammation-related diseases.

We hope that this Special Issue will stimulate the interest of the scientific community involved in studying the effects of natural and synthetic compounds in different fields of interest such as acute and chronic inflammation, inflammatory pain, inflammation-related diseases (e.g., autoimmune diseases), and others.

The papers published here will contribute to proposing new insights into the mechanisms of several conditions, in addition to suggesting new diagnostic alternatives and therapeutic targets in widespread pathologies.

Prof. Dr. Francesco Maione
Guest Editor

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Keywords

inflammation
inflammatory-based diseases
immunity
natural compounds
nutraceuticals

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Published Papers (10 papers)

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Research

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15 pages, 2543 KiB

Open AccessArticle

In Vitro Bioaccessibility and Anti-Inflammatory Activity of a Chemically Characterized Allium cepa L. Extract Rich in Quercetin Derivatives Optimized by the Design of Experiments

by Hammad Ullah, Alessandro Di Minno, Cristina Santarcangelo, Ariyawan Tantipongpiradet, Marco Dacrema, Rita di Matteo, Hesham R. El-Seedi, Shaden A. M. Khalifa, Alessandra Baldi, Antonietta Rossi and Maria Daglia

Molecules 2022, 27(24), 9065; https://doi.org/10.3390/molecules27249065 - 19 Dec 2022

Cited by 5 | Viewed by 2439

Abstract

Allium cepa L. is a highly consumed garden crop rich in biologically active phenolic and organosulfur compounds. This study aimed to assess the in vitro bioaccessibility and anti-inflammatory effect of a chemically characterized A. cepa extract rich in quercetin and its derivatives. Different varieties of A. cepa were studied; based on the highest total phenolic content, the “Golden” variety was selected. Its extracts, obtained from the tunicate bulb, tunic, and bulb, were subjected to determination of quercetin and its derivatives with LC-MS analysis and based on the highest total quercetin content, the tunic extract was utilized for further experiments. The extraction method was optimized through a design of experiment (DoE) method via full factorial design, which showed that 40% ethanol and 1 g tunic/20 mL solvent are the best extraction conditions. HPLC analysis of the optimized tunic extract identified 14 flavonols, including 10 quercetin derivatives. As far as in vitro bioaccessibility was concerned, the increases in some quercetin derivatives following the gastro-duodenal digestion process support the bioaccessibility of these bioactive compounds. Moreover, the extract significantly inhibited the production of PGE2 in stimulated J774 cell lines, while no effects of the tunic extract were observed against the release of IL-1β, TNF-α, and nitrites. The study provided insights into the optimized extraction conditions to obtain an A. cepa tunic extract rich in bioavailable quercetin derivatives with significant anti-inflammatory effects against PGE2. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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18 pages, 1627 KiB

Open AccessArticle

A Bio-Guided Screening for Antioxidant, Anti-Inflammatory and Hypolipidemic Potential Supported by Non-Targeted Metabolomic Analysis of Crepis spp.

by Christina Barda, Konstantina Anastasiou, Ariadni Tzara, Maria-Eleni Grafakou, Eleftherios Kalpoutzakis, Joerg Heilmann, Michael Rallis, Angeliki P. Kourounakis and Helen Skaltsa

Molecules 2022, 27(19), 6173; https://doi.org/10.3390/molecules27196173 - 20 Sep 2022

Cited by 2 | Viewed by 2081

Abstract

This study was designed to evaluate the chemical fingerprints and the antioxidant, anti-inflammatory and hypolipidemic activity of selected Crepis species collected in Greece, namely, C. commutata, C. dioscoridis, C. foetida, C. heldreichiana, C. incana, C. rubra, and Phitosia crocifolia (formerly known as Crepis crocifolia). For the phytochemical analyses, sample measurements were carried out by using nuclear magnetic resonance (NMR) spectroscopy and liquid chromatography coupled with mass spectrometry (LC-MS). Τhe extracts were evaluated both in vitro (radical scavenging activity: DPPH assay and total phenolic content: Folin–Ciocalteu) and in vivo (paw edema reduction and hypolipidemic activity: experimental mouse protocols). Among the tested extracts, C. incana presented the highest gallic acid equivalents (GAE) (0.0834 mg/mL) and the highest antioxidant activity (IC₅₀ = 0.07 mg/mL) in vitro, as well as the highest anti-inflammatory activity with 32% edema reduction in vivo. Moreover, in the hypolipidemic protocol, the same extract increased plasma total antioxidant capacity (TAC) by 48.7%, and decreased cholesterol (41.3%) as well as triglycerides (37.2%). According to fractionation of the extract and the phytochemical results, this biological effect may be associated with the rich phenolic composition; caffeoyl tartaric acid derivatives (cichoric and caftaric acid) are regarded as the most prominent bioactive specialized metabolites. The present study contributes to the knowledge regarding the phytochemical and pharmacological profile of Crepis spp. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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17 pages, 5664 KiB

Open AccessArticle

Protective Effect of Portulaca oleracea on Streptozotocin-Induced Type I Diabetes-Associated Reproductive System Dysfunction and Inflammation

by Hassan Rakhshandeh, Hamed Rajabi Khasevan, Anella Saviano, Mohammad Reza Mahdinezhad, Vafa Baradaran Rahimi, Sajjad Ehtiati, Leila Etemad, Alireza Ebrahimzadeh-bideskan, Francesco Maione and Vahid Reza Askari

Molecules 2022, 27(18), 6075; https://doi.org/10.3390/molecules27186075 - 17 Sep 2022

Cited by 24 | Viewed by 3078

Abstract

Background: Type-one diabetes (T1D), a chronic autoimmune disease with marked inflammatory responses, is associated with infertility complications and implications. Based on the anti-diabetic, antioxidant, and anti-hyperlipidemic potential of Portulaca oleracea (PO), this study aimed to evaluate the protective effect of this plant extract on streptozotocin-induced type-I-diabetes-associated reproductive system dysfunction and inflammation. Methods: Male rats were randomly divided into four experimental groups: control, diabetic, and treatment/s (PO extract at 100 or 300 mg/kg/daily). Then food and water consumption, body, testis and epididymis weights, histopathological evaluation, seminiferous tubules diameter, sperm count and motility, glucose levels, sex hormones, and inflammatory and oxidative stress markers were evaluated. Results: Our results showed that streptozotocin-induced diabetes significantly increased food and water consumption; increased glucose, MDA, TGF-β1, and TNF-α levels; and decreased the seminiferous tubules diameter, sperm count and motility, levels of LH, testosterone, total thiol, VEGF, and SOD activity. Interestingly, PO extract (phytochemically characterized by using liquid chromatography–mass spectrometry to detect bioactive molecules) significantly ameliorated these parameters and histopathological indexes’ damage in rats. Conclusion. Even if more preclinical assessments are needed to better characterize the mechanism/s of action, the results of this study will pave the way for the rational use of PO on diabetic-associated clinical complications and implications. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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16 pages, 3488 KiB

Open AccessArticle

Ameliorative Effect of Citropten Isolated from Citrusaurantifolia Peel Extract as a Modulator of T Cell and Intestinal Epithelial Cell Activity in DSS-Induced Colitis

by Hyun-Su Lee, Eun-Nam Kim and Gil-Saeng Jeong

Molecules 2022, 27(14), 4633; https://doi.org/10.3390/molecules27144633 - 20 Jul 2022

Cited by 8 | Viewed by 2111

Abstract

Citropten is a coumarin that is mainly found in fruits of Rutaceae trees, but its anti-inflammatory activities in colitis is still unknown. In this study, we investigated its attenuating effect of citropten isolated from Citrus aurantifolia extract on DSS-induced colitis through the modulation of the activity of T cells and intestinal epithelial cells. We found that pre-treatment with citropten downregulates the activity of T cells and intestinal epithelial cells without a negative effect on the viability of Jurkat and HT-29 cells. The results from the Western blot analysis revealed that pre-treatment with citropten reduces the NFκB and MAPK signaling pathway in activated T cells and intestinal epithelial cells. We elucidated that the oral administration of citropten alleviates the colonic inflammation and activity of effector T cells in DSS-induced colitis by measuring changes in body weight, histological scoring from H&E-stained sections, mRNA levels of pro-inflammatory cytokines and the phosphorylation level of the MAPK signaling pathway. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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11 pages, 1767 KiB

Open AccessArticle

Calceolarioside A, a Phenylpropanoid Glycoside from Calceolaria spp., Displays Antinociceptive and Anti-Inflammatory Properties

by Stefano Pieretti, Anella Saviano, Adriano Mollica, Azzurra Stefanucci, Anna Maria Aloisi and Marcello Nicoletti

Molecules 2022, 27(7), 2183; https://doi.org/10.3390/molecules27072183 - 28 Mar 2022

Cited by 11 | Viewed by 2142

Abstract

Phenylpropanoid glycosides are a class of natural substances of plant origin with interesting biological activities and pharmacological properties. This study reports the antinociceptive and anti-inflammatory effects of calceolarioside A, a phenylpropanoid glycoside previously isolated from various Calceolaria species. In models of acute nociception induced by thermal stimuli, such as the hot plate and tail flick test, calceolarioside administered at doses of 1, 5, and 10 μg in the left cerebral ventricles did not modify the behavioral response of mice. In an inflammatory based persistent pain model as the formalin test, calceolarioside A at the high dose tested (100 μg/paw) reduced the licking activity induced by formalin by 35% in the first phase and by 75% in the second phase of the test. In carrageenan-induced thermal hyperalgesia, calceolarioside A (50 and 100 μg/paw) was able to significantly reverse thermal hyperalgesia induced by carrageenan. The anti-inflammatory activity of calceolarioside A was then assessed using the zymosan-induced paw edema model. Calceolarioside A (50 and 100 μg/paw) induced a significant reduction in the edema from 1 to 4 h after zymosan administration. Measuring IL-6, TNFα, and IL-1β pro-inflammatory cytokines released from LPS-stimulated THP-1 cells, calceolarioside A in a concentration-dependent manner reduced the release of these cytokines from THP-1 cells. Taken together, our results highlight, for the first time, the potential and selective anti-inflammatory properties of this natural-derived compound, prompting its rationale use for further investigations. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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15 pages, 10107 KiB

Open AccessArticle

Protective Effects of Baicalin on Peritoneal Tight Junctions in Piglets Challenged with Glaesserella parasuis

by Jiacheng Zhang, Zhaoran Zhang, Jianfeng Xu, Chun Ye, Shulin Fu, Chien-An Andy Hu, Yinsheng Qiu and Yu Liu

Molecules 2021, 26(5), 1268; https://doi.org/10.3390/molecules26051268 - 26 Feb 2021

Cited by 9 | Viewed by 2466

Abstract

Glaesserella parasuis (G. parasuis) causes inflammation and damage to piglets. Whether polyserositis caused by G. parasuis is due to tight junctions damage and the protective effect of baicalin on it have not been examined. Therefore, this study aims to investigate the effects of baicalin on peritoneal tight junctions of piglets challenged with G. parasuis and its underlying molecular mechanisms. Piglets were challenged with G. parasuis and treated with or without baicalin. RT-PCR was performed to examine the expression of peritoneal tight junctions genes. Immunofluorescence was carried out to detect the distribution patterns of tight junctions proteins. Western blot assays were carried out to determine the involved signaling pathways. Our data showed that G. parasuis infection can down-regulate the tight junctions expression and disrupt the distribution of tight junctions proteins. Baicalin can alleviate the down-regulation of tight junctions mRNA in peritoneum, prevent the abnormalities and maintain the continuous organization of tight junctions. Our results provide novel evidence to support that baicalin has the capacity to protect peritoneal tight junctions from G. parasuis-induced inflammation. The protective mechanisms of baicalin could be associated with inhibition of the activation of PKC and MLCK/MLC signaling pathway. Taken together, these data demonstrated that baicalin is a promising natural agent for the prevention and treatment of G. parasuis infection. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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16 pages, 9194 KiB

Open AccessArticle

Sulforaphane Inhibits Osteoclastogenesis via Suppression of the Autophagic Pathway

by Tingting Luo, Xiazhou Fu, Yaoli Liu, Yaoting Ji and Zhengjun Shang

Molecules 2021, 26(2), 347; https://doi.org/10.3390/molecules26020347 - 12 Jan 2021

Cited by 19 | Viewed by 3109

Abstract

Previous studies have demonstrated that sulforaphane (SFN) is a promising agent against osteoclastic bone destruction. However, the mechanism underlying its anti-osteoclastogenic activity is still unclear. Herein, for the first time, we explored the potential role of autophagy in SFN-mediated anti-osteoclastogenesis in vitro and in vivo. We established an osteoclastogenesis model using receptor activator of nuclear factor kappa-β ligand (RANKL)-induced RAW264.7 cells and bone marrow macrophages (BMMs). Tartrate-resistant acid phosphatase (TRAP) staining showed the formation of osteoclasts. We observed autophagosomes by transmission electron microscopy (TEM). In vitro, we found that SFN inhibited osteoclastogenesis (number of osteoclasts: 22.67 ± 0.88 in the SFN (0) group vs. 20.33 ± 1.45 in the SFN (1 μM) group vs. 13.00 ± 1.00 in the SFN (2.5 μM) group vs. 6.66 ± 1.20 in the SFN (2.5 μM) group), decreased the number of autophagosomes, and suppressed the accumulation of several autophagic proteins in osteoclast precursors. The activation of autophagy by rapamycin (RAP) almost reversed the SFN-elicited anti-osteoclastogenesis (number of osteoclasts: 22.67 ± 0.88 in the control group vs. 13.00 ± 1.00 in the SFN group vs. 17.33 ± 0.33 in the SFN+RAP group). Furthermore, Western blot (WB) analysis revealed that SFN inhibited the phosphorylation of c-Jun N-terminal kinase (JNK). The JNK activator anisomycin significantly promoted autophagy, whereas the inhibitor SP600125 markedly suppressed autophagic activation in pre-osteoclasts. Microcomputed tomography (CT), immunohistochemistry (IHC), and immunofluorescence (IF) were used to analyze the results in vivo. Consistent with the in vitro results, we found that the administration of SFN could decrease the number of osteoclasts and the expression of autophagic light chain 3 (LC3) and protect against lipopolysaccharide (LPS)-induced calvarial erosion. Our findings highlight autophagy as a crucial mechanism of SFN-mediated anti-osteoclastogenesis and show that the JNK signaling pathway participates in this process. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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14 pages, 2520 KiB

Open AccessArticle

Alginic Acid from Padina boryana Abate Particulate Matter-Induced Inflammatory Responses in Keratinocytes and Dermal Fibroblasts

by Thilina U. Jayawardena, K. K. Asanka Sanjeewa, Lei Wang, Won-Suk Kim, Tae-Ki Lee, Yong-Tae Kim and You-Jin Jeon

Molecules 2020, 25(23), 5746; https://doi.org/10.3390/molecules25235746 - 5 Dec 2020

Cited by 12 | Viewed by 2797

Abstract

Particulate matter (PM) is a significant participant in air pollution and is hence an inducer of serious health issues. This study aimed to evaluate the dust protective effects of alginate from Padina boryana (PBA) via inflammatory-associated pathways to develop anti-fine dust skincare products. In between the external and internal environments, the skin is considered to be more than a physical barrier. It was observed that PM stimulates inflammation in the skin via activating NF-κB and MAPK pathways. The potential of PBA to inhibit the studied pathways were evident. The metal ion content of PM was considerably reduced by PBA and thus attributed to its chelation ability. Current research demonstrated the potential of P. boryana alginates to be implemented as a protective barrier against inflammation imposed with heavy metal and bacterial-derived endotoxin bound to the surface of the PM. Concisely, the results suggest that the bioactive components derived from the brown algae Padina boryana increased the cellular resistance to PM-stimulated inflammation-driven skin damage. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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Review

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14 pages, 2913 KiB

Open AccessReview

A Selective Review and Virtual Screening Analysis of Natural Product Inhibitors of the NLRP3 Inflammasome

by Sherihan El-Sayed, Sally Freeman and Richard A. Bryce

Molecules 2022, 27(19), 6213; https://doi.org/10.3390/molecules27196213 - 21 Sep 2022

Cited by 10 | Viewed by 3532

Abstract

The NLRP3 inflammasome is currently an exciting target for drug discovery due to its role in various inflammatory diseases; however, to date, no NLRP3 inhibitors have reached the clinic. Several studies have used natural products as hit compounds to facilitate the design of novel selective NLRP3 inhibitors. Here, we review selected natural products reported in the literature as NLRP3 inhibitors, with a particular focus on those targeting gout. To complement this survey, we also report a virtual screen of the ZINC20 natural product database, predicting favored chemical features that can aid in the design of novel small molecule NLRP3 inhibitors. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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Other

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14 pages, 1402 KiB

Open AccessOpinion

Present Status and Future Trends of Natural-Derived Compounds Targeting T Helper (Th) 17 and Microsomal Prostaglandin E Synthase-1 (mPGES-1) as Alternative Therapies for Autoimmune and Inflammatory-Based Diseases

by Anella Saviano, Federica Raucci, Gian Marco Casillo, Chiara Indolfi, Alessia Pernice, Carmen Foreste, Asif Jilani Iqbal, Nicola Mascolo and Francesco Maione

Molecules 2020, 25(24), 6016; https://doi.org/10.3390/molecules25246016 - 18 Dec 2020

Cited by 4 | Viewed by 2923

Abstract

Several natural-based compounds and products are reported to possess anti-inflammatory and immunomodulatory activity both in vitro and in vivo. The primary target for these activities is the inhibition of eicosanoid-generating enzymes, including phospholipase A2, cyclooxygenases (COXs), and lipoxygenases, leading to reduced prostanoids and leukotrienes. Other mechanisms include modulation of protein kinases and activation of transcriptases. However, only a limited number of studies and reviews highlight the potential modulation of the coupling enzymatic pathway COX-2/mPGES-1 and Th17/Treg circulating cells. Here, we provide a brief overview of natural products/compounds, currently included in the Italian list of botanicals and the BELFRIT, in different fields of interest such as inflammation and immunity. In this context, we focus our opinion on novel therapeutic targets such as COX-2/mPGES-1 coupling enzymes and Th17/Treg circulating repertoire. This paper is dedicated to the scientific career of Professor Nicola Mascolo for his profound dedication to the study of natural compounds. Full article

(This article belongs to the Special Issue Targeting Inflammation and Inflammatory-Related Diseases with Natural Bioactives)

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