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

Deadline for manuscript submissions: closed (30 August 2017) | Viewed by 82892

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Prof. Dr. Muraleedharan G. Nair

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Department of Horticulture, Michigan State University, Plant and Soil Sciences Building, 1066 Bogue Street, Room 420, East Lansing, MI 48824, USA
Interests: bioactive natural products; cancer; obesity; type-2 diabetes; inflammation; antioxidant; botanical drugs; phytomedicine; nutraceutical; functional food; herbal medicine; spices
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Dear Colleagues,

Intermediates and products of inflammatory pathways play a significant role in the onset of several illnesses, such as arthritis, cancer, obesity, type-2 diabetes, and Alzheimer’s disease. More than a decade has passed with little or no progress in developing new anti-inflammatory drugs. Several functional food agents and natural products have reported to possess anti-inflammatory activities. However, the mechanism of action and in vivo efficacy of these compounds were not studied enough to consider their potential use as therapeutic or functional food agents or use as anti-inflammatory agents. The time is upon us again, and the urgent need to focus on developing novel anti-inflammatory agents since it can mitigate pain and suffering for many. This Special Issue intends to provide a venue to share and discuss current state of the mechanistic approaches and discovery of next generation anti-inflammatory agents, both natural and synthetic.

Prof. Dr. Muraleedharan G. Nair
Guest Editor

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Keywords

Cyclooxygenase enzyme inhibitors
Inflammation signaling inhibitors
Prostaglandins
tumor necrosis factor-α (TNF-α)
G-protein coupled receptor kinases (GRKs)
Bioactive compounds
Botanical agents
Functional food agents
Alternative medicine

Published Papers (13 papers)

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Research

23 pages, 4417 KiB

Open AccessArticle

Design and Synthesis of New Benzophenone Derivatives with In Vivo Anti-Inflammatory Activity through Dual Inhibition of Edema and Neutrophil Recruitment

by Jaqueline P. Januario, Thiago B. De Souza, Stefânia N. Lavorato, Tatiane C. S. Maiolini, Olívia S. Domingos, João L. Baldim, Laís R. S. Folquitto, Marisi G. Soares, Daniela A. Chagas-Paula, Danielle F. Dias and Marcelo H. Dos Santos

Molecules 2018, 23(8), 1859; https://doi.org/10.3390/molecules23081859 - 26 Jul 2018

Cited by 9 | Viewed by 5615

Abstract

A series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to examine their effect on both prostaglandin (PG) production and neutrophils recruitment. The thiazole derivatives displayed a potent effect in terms of reducing ear edema. The analysis suggested that the presence of 4-phenyl-2-hydrazinothiazole and the absence of C4′-OCH₃ on the benzophenone derivative structure are strongly related to the inhibition of PG production. In addition, the derivatives 2e, 3a and 3c concomitantly inhibit PG production and neutrophil recruitment, which may be a mechanism of action better than of common NSAIDs due to their inability to inhibit the neutrophil recruitment. Thus, these compounds can be considered as potential lead compounds toward the development of new anti-inflammatory drugs with an innovating mechanism of action. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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1679 KiB

Open AccessArticle

Anti-Inflammatory Potential of 1-Nitro-2-Phenylethylene

by Michelle A. Sugimoto, Márcia De Jesus Amazonas da Silva, Larissa Froede Brito, Rosivaldo Dos Santos Borges, Flávio Almeida Amaral, Ana Paula De Araujo Boleti, Maritza Echevarria Ordoñez, Jose Carlos Tavares, Lirlandia Pires Sousa and Emerson Silva Lima

Molecules 2017, 22(11), 1977; https://doi.org/10.3390/molecules22111977 - 15 Nov 2017

Cited by 6 | Viewed by 4272

Abstract

Inflammation is a reaction of the host to infectious or sterile stimuli and has the physiological purpose of restoring tissue homeostasis. However, uncontrolled or unresolved inflammation can lead to tissue damage, giving rise to a plethora of chronic inflammatory diseases, including metabolic syndrome and autoimmunity pathologies with eventual loss of organ function. Beta-nitrostyrene and its derivatives are known to have several biological activities, including anti-edema, vasorelaxant, antiplatelet, anti-inflammatory, and anticancer. However, few studies have been carried out regarding the anti-inflammatory effects of this class of compounds. Thereby, the aim of this study was to evaluate the anti-inflammatory activity of 1-nitro-2-phenylethene (NPe) using in vitro and in vivo assays. Firstly, the potential anti-inflammatory activity of NPe was evaluated by measuring TNF-α produced by human macrophages stimulated with lipopolysaccharide (LPS). NPe at non-toxic doses opposed the inflammatory effects induced by LPS stimulation, namely production of the inflammatory cytokine TNF-α and activation of NF-κB and ERK pathways (evaluated by phosphorylation of inhibitor of kappa B-alpha [IκB-α] and extracellular signal-regulated kinase 1/2 [ERK1/2], respectively). In a well-established model of acute pleurisy, pretreatment of LPS-challenged mice with NPe reduced neutrophil accumulation in the pleural cavity. This anti-inflammatory effect was associated with reduced activation of NF-κB and ERK1/2 pathways in NPe treated mice as compared to untreated animals. Notably, NPe was as effective as dexamethasone in both, reducing neutrophil accumulation and inhibiting ERK1/2 and IκB-α phosphorylation. Taken together, the results suggest a potential anti-inflammatory activity for NPe via inhibition of ERK1/2 and NF-κB pathways on leukocytes. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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1645 KiB

Open AccessArticle

Dimethyl Sulfoxide (DMSO) Decreases Cell Proliferation and TNF-α, IFN-γ, and IL-2 Cytokines Production in Cultures of Peripheral Blood Lymphocytes

by Lucas De Abreu Costa, Marcelo Henrique Fernandes Ottoni, Michaelle Geralda Dos Santos, Agnes Batista Meireles, Valéria Gomes de Almeida, Wagner De Fátima Pereira, Bethânia Alves de Avelar-Freitas and Gustavo Eustáquio Alvim Brito-Melo

Molecules 2017, 22(11), 1789; https://doi.org/10.3390/molecules22111789 - 10 Nov 2017

Cited by 105 | Viewed by 12340

Abstract

Dimethylsulfoxide (DMSO) is an amphipathic molecule composed of a polar domain characterized by the sulfinyl and two nonpolar methyl groups, for this reason it is able to solubilize polar and nonpolar substances and transpose hydrophobic barriers. DMSO is widely used to solubilize drugs of therapeutic applications and studies indicated that 10% v/v concentration did not modify culture viability when used to treat human peripheral blood mononuclear cells (PBMC). However, some DMSO concentrations could influence lymphocyte activation and present anti-inflammatory effects. Therefore, the objective of this study was to evaluate the effect of DMSO on lymphocyte activation parameters. Cell viability analysis, proliferation, and cytokine production were performed on PBMC from six healthy subjects by flow cytometry. The results indicated that 2.5% v/v DMSO concentrations did not modify lymphocytes viability. DMSO at 1% and 2% v/v concentrations reduced the relative proliferation index of lymphocytes and at 5% and 10% v/v concentrations reduced the percentage of total lymphocytes, cluster of differentiation 4⁺ (CD4⁺) T lymphocytes and CD8⁺ T lymphocytes interferon-γ (IFN-γ), tumor necrosis factor-α (TNF-α) and interleukin-2 (IL-2) producers. Thus, it was concluded that DMSO has an in vitro anti-inflammatory effect by reducing lymphocyte activation demonstrated with proliferation reduction and the decrease of cytokine production. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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5665 KiB

Open AccessArticle

N-(4-bromophenethyl) Caffeamide Protects Skin from UVB-Induced Inflammation Through MAPK/IL-6/NF-κB-Dependent Signaling in Human Skin Fibroblasts and Hairless Mouse Skin

by Yueh-Hsiung Kuo, Po-Yuan Wu, Chien-Wen Chen, Ping Lin, Kuo-Ching Wen, Chien-Yih Lin and Hsiu-Mei Chiang

Molecules 2017, 22(10), 1639; https://doi.org/10.3390/molecules22101639 - 29 Sep 2017

Cited by 9 | Viewed by 5018

Abstract

Long-term exposure to ultraviolet (UV) irradiation causes skin inflammation and aging. N-(4-bromophenethyl) caffeamide (K36H) possesses antioxidant and antimelanogenic properties. The present study investigated the effects of K36H on UVB-induced skin inflammation in human skin fibroblasts and hairless mice and evaluated the underlying mechanisms. The in vitro results indicated that K36H reduced UVB-induced mitogen-activated protein kinase (MAP kinase) expression. Furthermore, K36H treatment reduced cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) protein expression in UVB-irradiated fibroblasts by regulating IκB and nuclear factor-kappa B (NF-κB) expression. In the animal study, topically applied K36H markedly reduced inflammation and skin thickness and prevented photodamage to the skin of hairless mice. In addition, K36H inhibited the levels of UV-upregulated inflammation-related proteins levels such as IL-1, iNOS, and NF-κB in the dermis of hairless mice. Our findings demonstrated the antioxidant and anti-inflammatory properties of K36H in human skin fibroblasts and hairless mice. Therefore, K36H can be developed as an antiphotodamage and antiphotoinflammation agent. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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1461 KiB

Open AccessArticle

Acyclic Triterpenoids from Alpinia katsumadai Inhibit IL-6-Induced STAT3 Activation

by Hyun-Jae Jang, Seung-Jae Lee, Soyoung Lee, Kyungsook Jung, Seung Woong Lee and Mun-Chual Rho

Molecules 2017, 22(10), 1611; https://doi.org/10.3390/molecules22101611 - 25 Sep 2017

Cited by 9 | Viewed by 3998

Abstract

The seeds of Alpinia katsumadai yielded two new acyclic triterpenoids, 2,3,6,22,23-pentahydroxy-2,6,11,15,19,23-hexamethyl-tetracosa-7,10,14,18-tetraene (3) and 2,3,6,22,23-pentahydroxy-2,10,15,19,23-hexamethyl-7-methylenetetracosa-10,14,18-triene (4), as well as two known compounds, 2,3,22,23-tertrahydroxy-2,6,10,15,19,23-hexamethyl-tetracosa-6,10,14,18-tetraene (1) and 2,3,5,22,23-pentahydroxy-2,6,10,15,19,23-hexamethyl-tetracosa-6,10,14,18-tetraene (2). The absolute configurations of 2 and 3, which were determined by means of a modified Mosher’s method, are suggested as (3R; 5S; 22R) and (3R; 22R), respectively. Compounds 1–4 inhibited IL-6-induced JAK2/STAT3 activity in a dose-dependent fashion, with IC₅₀ values of 0.67, 0.71, 2.18, and 2.99 μM. Moreover, IL-6-stimulated phosphorylation of STAT3 was significantly suppressed in U266 cells by the administration of A. katsumadai EtOH extract and Compounds 1 and 2. These results suggest that major phytochemicals, Compounds 1 and 2, obtained from A. katsumadai may be useful candidates for designing new IL-6 inhibitors as anti-inflammatory agents. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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3761 KiB

Open AccessArticle

COX Inhibition Profile and Molecular Docking Studies of Some 2-(Trimethoxyphenyl)-Thiazoles

by Smaranda Dafina Oniga, Liliana Pacureanu, Cristina Ioana Stoica, Mariana Doina Palage, Alexandra Crăciun, Laurentiu Răzvan Rusu, Elena-Luminita Crisan and Cătălin Araniciu

Molecules 2017, 22(9), 1507; https://doi.org/10.3390/molecules22091507 - 09 Sep 2017

Cited by 46 | Viewed by 7393

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used therapeutic agents that exhibit frequent and sometimes severe adverse effects, including gastrointestinal ulcerations and cardiovascular disorders. In an effort to obtain safer NSAIDs, we assessed the direct cyclooxygenase (COX) inhibition activity and we investigated the potential COX binding mode of some previously reported 2-(trimethoxyphenyl)-thiazoles. The in vitro COX inhibition assays were performed against ovine COX-1 and human recombinant COX-2. Molecular docking studies were performed to explain the possible interactions between the inhibitors and both COX isoforms binding pockets. Four of the tested compounds proved to be good inhibitors of both COX isoforms, but only compound A3 showed a good COX-2 selectivity index, similar to meloxicam. The plausible binding mode of compound A3 revealed hydrogen bond interactions with binding site key residues including Arg120, Tyr355, Ser530, Met522 and Trp387, whereas hydrophobic contacts were detected with Leu352, Val349, Leu359, Phe518, Gly526, and Ala527. Computationally predicted pharmacokinetic profile revealed A3 as lead candidate. The present data prove that the investigated compounds inhibit COX and thus confirm the previously reported in vivo anti-inflammatory screening results suggesting that A3 is a suitable candidate for further development as a NSAID. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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1224 KiB

Open AccessArticle

Targeting PDE10A GAF Domain with Small Molecules: A Way for Allosteric Modulation with Anti-Inflammatory Effects

by Ana M. García, José Brea, Alejandro González-García, Concepción Pérez, María Isabel Cadavid, María Isabel Loza, Ana Martinez and Carmen Gil

Molecules 2017, 22(9), 1472; https://doi.org/10.3390/molecules22091472 - 04 Sep 2017

Cited by 5 | Viewed by 3667

Abstract

Phosphodiesterase (PDE) enzymes regulate the levels of cyclic nucleotides, cAMP, and/or cGMP, being attractive therapeutic targets. In order to modulate PDE activity in a selective way, we focused our efforts on the search of allosteric modulators. Based on the crystal structure of the PDE10A GAF-B domain, a virtual screening study allowed the discovery of new hits that were also tested experimentally, showing inhibitory activities in the micromolar range. Moreover, these new PDE10A inhibitors were able to decrease the nitrite production in LPS-stimulated cells, thus demonstrating their potential as anti-inflammatory agents. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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4699 KiB

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Chemical Composition of Pinus roxburghii Bark Volatile Oil and Validation of Its Anti-Inflammatory Activity Using Molecular Modelling and Bleomycin-Induced Inflammation in Albino Mice

by Rola M. Labib, Fadia S. Youssef, Mohamed L. Ashour, Mohamed M. Abdel-Daim and Samir A. Ross

Molecules 2017, 22(9), 1384; https://doi.org/10.3390/molecules22091384 - 29 Aug 2017

Cited by 54 | Viewed by 6937

Abstract

The chemical composition of Pinus roxburghii bark essential oil (PRO) was qualitatively and quantitatively determined using GC/FID and GC/MS. The anti-inflammatory activity was assessed in vitro by evaluating the binding percentages on the cannabinoids and opioids receptors. Bleomycin (BLM)-induced pulmonary inflammation in albino mice was adopted to assess PRO anti-inflammatory efficacy in vivo. In silico molecular modelling of its major components was performed on human glucocorticoids receptor (GR). Seventy-five components were identified in which longifolene (33.13%) and palmitic acid (9.34%) constituted the predominant components. No binding was observed on cannabinoid receptor type 1 (CB1), whereas mild binding was observed on cannabinoid receptor type 2 (CB2), delta, kappa, and mu receptors accounting for 2.9%, 6.9%, 10.9% and 22% binding. A significant in vivo activity was evidenced by reduction of the elevated malondialdehyde (MDA), nitric oxide (NO), myeloperoxidase (MPO), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) levels by 55.56%, 55.66%, 64.64%, 58.85% and 77.78% with concomitant elevation of superoxide dismutase (SOD) and catalase (CAT) activities comparable to BLM-treated group at 100 mg/kg body weight. In silico studies showed that palmitic acid exerted the fittest binding. PRO could serve as a potent anti-inflammatory natural candidate that should be supported by further clinical trials. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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956 KiB

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Isolation and Purification of Three Ecdysteroids from the Stems of Diploclisia glaucescens by High-Speed Countercurrent Chromatography and Their Anti-Inflammatory Activities In Vitro

by Lei Fang, Jialian Li, Jie Zhou, Xiao Wang and Lanping Guo

Molecules 2017, 22(8), 1310; https://doi.org/10.3390/molecules22081310 - 07 Aug 2017

Cited by 12 | Viewed by 4069

Abstract

High-speed counter-current chromatography was used to separate and purify ecdysteroids for the first time from the stems of Diploclisia glaucescens using a two-phase solvent system composed of ethyl acetate–n-butanol–ethanol–water (3:0.2:0.8:3, v/v). Three ecdysteroids were obtained from 260 mg of ethyl acetate extract of the residue obtained after evaporation of the crude ethanolicextractof D. glaucescens in one-step separation, which were identified as paristerone (I, 30.5 mg), ecdysterone (II, 7.2 mg), and capitasterone (III, 8.1 mg) by electrospray ionization mass spectrometry (ESI-MS) and nuclear magnetic resonance (NMR). Their anti-inflammatory activities were evaluated by measuring the inhibitory ratios of β-glucuronidase release in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor. Compounds I–III showed significant anti-inflammatory activities with IC₅₀-values ranging from 1.51 to 11.68 μM, respectively. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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2853 KiB

Open AccessArticle

Study of the Interactions of Bovine Serum Albumin with the New Anti-Inflammatory Agent 4-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(4-ethoxy-phenyl)methylidene]benzohydrazide Using a Multi-Spectroscopic Approach and Molecular Docking

by Tanveer A. Wani, Ahmed H. Bakheit, Abdul-Rahman A. Al-Majed, Mashooq A. Bhat and Seema Zargar

Molecules 2017, 22(8), 1258; https://doi.org/10.3390/molecules22081258 - 27 Jul 2017

Cited by 51 | Viewed by 7282

Abstract

The lipophilic derivative of thalidomide (4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(4-ethoxyphenyl)methylidene]benzohydrazide, 6P) was synthesized to enhance its characteristics and efficacy. Earlier studies have proved the immunomodulatory and anti-inflammatory effects of 6P. In this study the interaction between bovine serum albumin (BSA) and 6P was studied using a multi-spectroscopic approach which included UV spectrophotometry, spectrofluorimetry and three dimensional spectrofluorometric and molecular docking studies. Static quenching was involved in quenching the fluorescence of BSA by 6P, because a complex formation occurred between the 6P and BSA. The binding constant decreased with higher temperature and was in the range of 2.5 × 10⁵–4.8 × 10³ L mol⁻¹ suggesting an unstable complex at higher temperatures. A single binding site was observed and the the site probe experiments showed site II (sub-domain IIIA) of BSA as the binding site for 6P. The negative values of ∆G⁰, ∆H⁰ and ∆S⁰ at (298/303/308 K) indicated spontaneous binding between 6P and BSA as well as the interaction was enthalpy driven and van der Waals forces and hydrogen bonding were involved in the interaction. The docking results and the results from the experimental studies are complimentary to each other and confirm that 6P binds at site II (sub-domain IIIA) of BSA. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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Synthesis and Identification of Novel Berberine Derivatives as Potent Inhibitors against TNF-α-Induced NF-κB Activation

by Yan-Xiang Wang, Lu Liu, Qing-Xuan Zeng, Tian-Yun Fan, Jian-Dong Jiang, Hong-Bin Deng and Dan-Qing Song

Molecules 2017, 22(8), 1257; https://doi.org/10.3390/molecules22081257 - 27 Jul 2017

Cited by 35 | Viewed by 6420

Abstract

Twenty-three new berberine (BBR) analogues defined on substituents of ring D were synthesized and evaluated for their activity for suppression of tumor necrosis factor (TNF)-α-induced nuclear factor (NF)-κB activation. Structure–activity relationship (SAR) analysis indicated that suitable tertiary/quaternary carbon substitutions at the 9-position or rigid fragment at position 10 might be beneficial for enhancing their anti-inflammatory potency. Among them, compounds 2d, 2e, 2i and 2j exhibited satisfactory inhibitory potency against NF-κB activation, with an inhibitory rate of around 90% (5 μM), much better than BBR. A preliminary mechanism study revealed that all of them could inhibit TNF-α-induced NF-κB activation via impairing IκB kinase (IKK) phosphorylation as well as cytokines interleukin (IL)-6 and IL-8 induced by TNF-α. Therefore, the results provided powerful information on further structural modifications and development of BBR derivatives into a new class of anti-inflammatory candidates for the treatment of inflammatory diseases. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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Combined Treatment with Hyaluronic Acid and Mesalamine Protects Rats from Inflammatory Bowel Disease Induced by Intracolonic Administration of Trinitrobenzenesulfonic Acid

by Chih-Tung Chiu, Sheng-Nan Kuo, Shao-Wen Hung and Cheng-Yao Yang

Molecules 2017, 22(6), 904; https://doi.org/10.3390/molecules22060904 - 30 May 2017

Cited by 16 | Viewed by 7203

Abstract

Drugs such as mesalamine (5-ASA) are currently recommended for the treatment of inflammatory bowel disease (IBD). To reduce the frequency of their administration and improve their therapeutic effect, this study investigated the adhesion efficacy, wound healing promotion, and decrease in inflammation in ulcers in the colonic tissue of rats with colitis after combined treatment with hyaluronic acid (HA) and 5-ASA (IBD98-M). HA-fluoresceinamine (FL) conjugates successfully adhered to the mucosal layer and were conjugated in the vascular tissue. In addition, macroscopic and microscopic observations indicated that colonic injuries reduced significantly after treatment with IBD98-M. Compared with PBS and 5-ASA treatment alone, treatment with IBD98-M more effectively reduced bowel inflammation and promoted colonic mucosal healing in TNBS-induced colitis. IBD98-M treatment also reduced myeloperoxidase activity and the expression levels of cyclooxygenase 2 and tumor necrosis factor-αin the colitis tissue. In conclusion, IBD98-M treatment strongly promoted wound healing in colonic injuries and significantly inhibited MPO activity in the inflamed colon tissue of rats. Combined treatment with HA and 5-ASA can accelerate wound healing and reduce inflammatory reaction in rat colitis. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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Synthesis of Gallic Acid Analogs as Histamine and Pro-Inflammatory Cytokine Inhibitors for Treatment of Mast Cell-Mediated Allergic Inflammation

by Xiang Fei, In-Gyu Je, Tae-Yong Shin, Sang-Hyun Kim and Seung-Yong Seo

Molecules 2017, 22(6), 898; https://doi.org/10.3390/molecules22060898 - 29 May 2017

Cited by 15 | Viewed by 7888

Abstract

Gallic acid (3,4,5-trihydroxybenzoic acid), is a natural product found in various foods and herbs that are well known as powerful antioxidants. Our previous report demonstrated that it inhibits mast cell-derived inflammatory allergic reactions by blocking histamine release and pro-inflammatory cytokine expression. In this report, various amide analogs of gallic acid have been synthesized by introducing different amines through carbodiimide-mediated amide coupling and Pd/C-catalyzed hydrogenation. These compounds showed a modest to high inhibitory effect on histamine release and pro-inflammatory cytokine expression. Among them, the amide bearing (S)-phenylglycine methyl ester 3d was found to be more active than natural gallic acid. Further optimization yielded several (S)- and (R)-phenylglycine analogs that inhibited histamine release in vitro. Our findings suggest that some gallamides could be used as a treatment for allergic inflammatory diseases. Full article

(This article belongs to the Special Issue Anti-inflammatory Agents)

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