scholarly journals Biseugenol Exhibited Anti-Inflammatory and Anti-Asthmatic Effects in an Asthma Mouse Model of Mixed-Granulocytic Asthma

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5384
Author(s):  
Vitor Ponci ◽  
Rafael C. Silva ◽  
Fernanda Paula R. Santana ◽  
Simone S. Grecco ◽  
Célia Regina M. Fortunato ◽  
...  
Keyword(s):  
Airway Hyperresponsiveness ◽  
Lavage Fluid ◽  
Similar Efficacy ◽  
Positive Control ◽  
In Silico Studies ◽  
Anti Inflammatory ◽  
Main Component ◽  
Higher Doses ◽  
Asthma Mouse Model

In the present work, the anti-inflammatory and antiasthmatic potential of biseugenol, isolated as the main component from n-hexane extract from leaves of Nectandra leucantha and chemically prepared using oxidative coupling from eugenol, was evaluated in an experimental model of mixed-granulocytic asthma. Initially, in silico studies of biseugenol showed good predictions for drug-likeness, with adherence to Lipinski’s rules of five (RO5), good Absorption, Distribution, Metabolism and Excretion (ADME) properties and no alerts for Pan-Assay Interference Compounds (PAINS), indicating adequate adherence to perform in vivo assays. Biseugenol (20 mg·kg−1) was thus administered intraperitoneally (four days of treatment) and resulted in a significant reduction in both eosinophils and neutrophils of bronchoalveolar lavage fluid in ovalbumin-sensitized mice with no statistical difference from dexamethasone (5 mg·kg−1). As for lung function parameters, biseugenol (20 mg·kg−1) significantly reduced airway and tissue damping in comparison to ovalbumin group, with similar efficacy to positive control dexamethasone. Airway hyperresponsiveness to intravenous methacholine was reduced with biseugenol but was inferior to dexamethasone in higher doses. In conclusion, biseugenol displayed antiasthmatic effects, as observed through the reduction of inflammation and airway hyperresponsiveness, with similar effects to dexamethasone, on mixed-granulocytic ovalbumin-sensitized mice.

scholarly journals Synthesis, Anti-Inflammatory Activity, and In Silico Study of Novel Diclofenac and Isatin Conjugates

2018 ◽  
Vol 2018 ◽  
pp. 1-11
Author(s):  
Musab Mohamed Ibrahim ◽  
Tilal Elsaman ◽  
Mosab Yahya Al-Nour
Keyword(s):  
Virtual Screening ◽  
Condensation Reaction ◽  
Docking Study ◽  
Positive Control ◽  
Inflammatory Activity ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Chemical Structures ◽  
Anti Inflammatory

The design, synthesis, and development of novel non-steroidal anti-inflammatory drugs (NSAIDs) with better activity and lower side effects are respectable area of research. Novel Diclofenac Schiff’s bases (M1, M2, M4, M7, and M8) were designed and synthesized, and their respective chemical structures were deduced using various spectral tools (IR, 1H NMR, 13C NMR, and MS). The compounds were synthesized via Schiff’s condensation reaction and their anti-inflammatory activity was investigated applying the Carrageenan-induced paw edema model against Diclofenac as positive control. Percentage inhibition of edema indicated that all compounds were exhibiting a comparable anti-inflammatory activity as Diclofenac. Moreover, the anti-inflammatory activity was supported via virtual screening using molecular docking study. Interestingly compound M2 showed the highest in vivo activity (61.32% inhibition) when compared to standard Diclofenac (51.36% inhibition) as well as the best binding energy score (-10.765) and the virtual screening docking score (-12.142).

Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents

2020 ◽  
Vol 186 ◽  
pp. 111863 ◽  
Author(s):  
Muhammad Saeed Jan ◽  
Sajjad Ahmad ◽  
Fida Hussain ◽  
Ashfaq Ahmad ◽  
Fawad Mahmood ◽  
...  
Keyword(s):  
In Silico ◽  
Design Synthesis ◽  
In Silico Studies ◽  
Anti Inflammatory

scholarly journals Antioxidant, analgesic and anti-inflammatory effects of lavender essential oil

2015 ◽  
Vol 87 (2 suppl) ◽  
pp. 1397-1408 ◽  
Author(s):  
GABRIELA L. DA SILVA ◽  
CAROLINA LUFT ◽  
ADROALDO LUNARDELLI ◽  
ROBSON H. AMARAL ◽  
DENIZAR A. DA SILVA MELO ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Essential Oil ◽  
Therapeutic Potential ◽  
Positive Control ◽  
Croton Oil ◽  
Antinociceptive Effects ◽  
Anti Inflammatory ◽  
Pre Treatment ◽  
Dose Dependent

Several studies have investigated the antinociceptive, immunomodulatory and anti-inflammatory properties of compounds found in the lavender essential oil (LEO), however to date, there is still lack of substantial data. The objective of this study was to assess the antioxidant, anti-inflammatory and antinociceptive effects of lavender essential oil. The 1,1-diphenyl-2-picrylhydrazyl radical decolorization assay was used for antioxidant activity evaluation. The anti-inflammatory activity was tested using two models of acute inflammation: carrageenan-induced pleurisy and croton oil-induced ear edema. The antinociceptive activity was tested using the pain model induced by formalin. LEO has antioxidant activity, which is dose-dependent response. The inflammatory response evoked by carrageenan and by croton oil was reduced through the pre-treatment of animals with LEO. In the pleurisy model, the drug used as positive control, dexamethasone, was more efficacious. However, in the ear swelling, the antiedematogenic effect of the oil was similar to that observed for dexamethasone. In the formalin test, LEO consistently inhibited spontaneous nociception and presented a similar effect to that of tramadol. The results of this study reveal (in vivo) the analgesic and anti-inflammatory activities of LEO and demonstrates its important therapeutic potential.

Regulation of LPS-mediated inflammation in vivo and in vitro by the thiol antioxidant Nacystelyn

2004 ◽  
Vol 286 (6) ◽  
pp. L1319-L1327 ◽  
Author(s):  
Frank Antonicelli ◽  
David Brown ◽  
Maryline Parmentier ◽  
Ellen M. Drost ◽  
Nik Hirani ◽  
...  
Keyword(s):  
Dna Binding ◽  
Transforming Growth Factor ◽  
Lavage Fluid ◽  
Human Macrophage ◽  
Antioxidant Agents ◽  
Thiol Antioxidant ◽  
Anti Inflammatory ◽  
Tgf Β1

Increased levels of proinflammatory cytokines are present in bronchoalveolar lavage fluid in various lung diseases. Redox-sensitive transcription factors such as NF-κB regulate gene transcription for these cytokines. We therefore studied the effect of a new thiol antioxidant compound, Nacystelyn (NAL), on IL-8 regulation in a human macrophage-derived cell line (THP-1). LPS (10 μg/ml) increased IL-8 release compared with control levels. This LPS activation was inhibited by coincubation with NAL (1 and 5 mM). Pretreatment with cycloheximide or okadaic acid, protein synthesis, and serine/threonine phosphatase inhibitors, respectively, did not modify inhibition of IL-8 release caused by NAL. NF-κB and C/EBP DNA binding were increased after LPS treatment compared with control, an effect inhibited by cotreatment with NAL. Activator protein (AP)-1 DNA binding was unaffected. The enhanced neutrophil chemotaxis produced by conditioned media from LPS-treated cells was inhibited when cells were cotreated with NAL. The selectivity of NAL inhibition upon IL-8 expression was studied. LPS-treated THP-1 cells also had higher levels of TNF-α, transforming growth factor (TGF)-β1 and -3, MIP-1α and -β, and RANTES gene expression. However, only LPS-induced IL-8 and TGF-β1 expressions were inhibited by NAL. An anti-inflammatory effect of NAL was confirmed in vivo as shown by a reduction in LPS-induced neutrophil recruitment to the lungs following instillation of NAL into the lungs. Our studies demonstrate that NAL has anti-inflammatory properties in vitro and in vivo, may therefore have a therapeutic role in lung inflammation, and has the advantage over other antioxidant agents in that it may be administrated by inhalation.

scholarly journals Anti-Inflammatory Effects of Ellagic Acid on Acute Lung Injury Induced by Acid in Mice

2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
Daniely Cornélio Favarin ◽  
Maxelle Martins Teixeira ◽  
Ednéia Lemos de Andrade ◽  
Claudiney de Freitas Alves ◽  
Javier Emilio Lazo Chica ◽  
...  
Keyword(s):  
Acute Lung Injury ◽  
Lung Injury ◽  
Ellagic Acid ◽  
Neutrophil Migration ◽  
Lavage Fluid ◽  
Positive Control ◽  
Oral Route ◽  
Dexamethasone Treatment ◽  
Acid Aspiration ◽  
Anti Inflammatory

Acute lung injury (ALI) is characterized by alveolar edema and uncontrolled neutrophil migration to the lung, and no specific therapy is still available. Ellagic acid, a compound present in several fruits and medicinal plants, has shown anti-inflammatory activity in several experimental disease models. We used the nonlethal acid aspiration model of ALI in mice to determine whether preventive or therapeutic administration of ellagic acid (10 mg/kg; oral route) could interfere with the development or establishment of ALI inflammation. Dexamethasone (1 mg/kg; subcutaneous route) was used as a positive control. In both preventive and therapeutic treatments, ellagic acid reduced the vascular permeability changes and neutrophil recruitment to the bronchoalveolar lavage fluid (BALF) and to lung compared to the vehicle. In addition, the ellagic acid accelerated the resolution for lung neutrophilia. Moreover, ellagic acid reduced the COX-2-induced exacerbation of inflammation. These results were similar to the dexamethasone. However, while the anti-inflammatory effects of dexamethasone treatment were due to the reduced activation of NF-κB and AP-1, the ellagic acid treatment led to reduced BALF levels of IL-6 and increased levels of IL-10. In addition, dexamethasone treatment reduced IL-1β. Together, these findings identify ellagic acid as a potential therapeutic agent for ALI-associated inflammation.

scholarly journals Apigenin Acts as Anti-inflammatory Compound through Reducing IL-1β, IL-6 and TNF-α in LPS-induced Inflammation; in-vivo Study

2021 ◽  
Author(s):  
Sanaz Jamshidi ◽  
Mohammad Sofiabadi ◽  
Mina Eslami ◽  
Farshad Foroughi
Keyword(s):  
Positive Control ◽  
Enzyme Linked Immunosorbent Assay ◽  
Tnf Α ◽  
Male Wistar Rats ◽  
Steroid Drug ◽  
Spss Software ◽  
Anti Inflammatory ◽  
Α Level ◽  
Control Sham

Abstract Background: Consumption of herbal flavonoids instead of chemical drugs has increased in recent years due to fewer side effects and affordability. In this study, the effect of apigenin was investigated on inflammation induced by lipopolysaccharide in male rat's serum by measuring the pro-inflammatory cytokines, i.e., IL-1β, IL-6, and TNF-α.Methods: 90 male Wistar rats weighing 200 ±2 grams were used and divided into control, sham (solvent), and positive control (dexamethasone 15 mg/kg. ip), and 3 experimental groups which received 5, 15 or 30 mg/kg of apigenin, intraperitoneally. In 30 minutes after interventions, lipopolysaccharide (LPS) [30 μg/kg. ip] was injected. Then, at 4, 12- and 24-hour intervals, rats were anesthetized, and blood samples were prepared intracardially. Samples were centrifuged, and serums were separated and stored at -80 ° C. Measurement of IL-1β, IL-6, and TNF-α were conducted by the enzyme-linked immunosorbent assay (ELISA) method. Data were analyzed using the SPSS software version 19.Results: Pre-injection of apigenin at 5 mg/kg dosage were reduced TNF-α and IL-1β levels at 24-hours after LPS injection, compared to control (for both P <0.05). Pre-injection of 15 mg/kg of apigenin was reduced IL-6 level at 24-hours after LPS injection (P <0.05). Pre-injection of 30 mg/kg of apigenin were reduced TNF-α level at 4- (P <0.05), 12- (P <0.01) and 24- (P <0.01) hours, IL-1β level at 24-hours (P <0.01), and IL-6 level at 4- (P <0.05) and 24- (P <0.01) hours after LPS injection.Conclusions: Apigenin reduces proinflammatory cytokines in serum in acute inflammation induction. This impact is close to the dexamethasone effect as an anti-inflammatory steroid drug.

In vivo anti-inflammatory action of eugenol on lipopolysaccharide-induced lung injury

2010 ◽  
Vol 108 (4) ◽  
pp. 845-851 ◽  
Author(s):  
Clarissa B. Magalhães ◽  
Douglas R. Riva ◽  
Leonardo J. DePaula ◽  
Aline Brando-Lima ◽  
Vera Lúcia G. Koatz ◽  
...  
Keyword(s):  
Lung Injury ◽  
Lavage Fluid ◽  
Nuclear Factor Κb ◽  
Tissue Expression ◽  
The Other ◽  
Alveolar Collapse ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Inflammatory Action

Eugenol, a methoxyphenol component of clove oil, suppresses cyclooxygenase-2 expression, while eugenol dimers prevent nuclear factor-κB (NF-κB) activation and inflammatory cytokine expression in lipopolysaccharide-stimulated macrophages. Our aim was to examine the in vivo anti-inflammatory effects of eugenol. BALB/c mice were divided into four groups. Mice received saline [0.05 ml intratracheally (it), control (Ctrl) and eugenol (Eug) groups] or Escherichia coli LPS (10 μg it, LPS and LPSEug groups). After 6 h, mice received saline (0.2 ml ip, Ctrl and LPS groups) or eugenol (160 mg/kg ip, Eug and LPSEug groups). Twenty-four hours after LPS injection, pulmonary resistive (ΔP1) and viscoelastic (ΔP2) pressures, static elastance (Est), and viscoelastic component of elastance (ΔE) were measured. Lungs were prepared for histology. In parallel mice, bronchoalveolar lavage fluid was collected 24 h after LPS injection. TNF-α was determined by ELISA. Lung tissue expression of NF-κB was determined by EMSA. ΔP1, ΔP2, Est, and ΔE were significantly higher in the LPS group than in the other groups. LPS mice also showed significantly more alveolar collapse, collagen fibers, and neutrophil influx and higher TNF-α levels and NF-κB expression than the other groups. Eugenol treatment reduced LPS-induced lung inflammation, improving lung function. Our results suggest that eugenol exhibits in vivo anti-inflammatory action in LPS-induced lung injury.

scholarly journals Spearmint (Mentha spicata L.) essential oil from tipaza (Algeria): in vivo anti-inflammatory and analgesic activities in experimental animal models

2020 ◽  
Vol 90 (1) ◽  
pp. 15-26
Author(s):  
Sarah Kehili ◽  
Mohamed Amine Boukhatem ◽  
Asma Belkadi ◽  
Faiza Boulaghmen ◽  
Mohamed Amine Ferhat ◽  
...  
Keyword(s):  
Essential Oil ◽  
Acute Inflammation ◽  
Kidney Injury ◽  
Topical Administration ◽  
Positive Control ◽  
Control Group ◽  
Mentha Spicata ◽  
Ear Edema ◽  
Anti Inflammatory

Introduction Although analgesic and nonsteroidal anti-inflammatory drugs (NSAIDs) are usually used to treat a diversity of illnesses, their administration is linked with acute kidney injury and gastrointestinal side effects. The research of new biomolecules and natural products is still needed such as medicinal plants. Aims The present research was aimed to investigate, for the first time, the anti-inflammatory and anti-nociceptive effects of spearmint essential oil (SEO) in mouse models of acute inflammation and pain. Materials and Method Chemical analysis of SEO was done by gas chromatography. The anti-inflammatory activity was tested using two models of acute inflammation namely carrageenan-induced paw edema and xylene-induced ear edema. Histological examination of both non-inflamed and inflamed tissues was evaluated. The anti-nociceptive activity was tested using the pain model induced by acetic acid. Results The main constituent of the SEO was found to be carvone (52.60%). The SEO exhibited a promising anti-inflammatory effect as demonstrated by statistically significant (p<0.05) inhibition of paw volume by 77.24% at the dose of 20 µL/kg and 65.87% at the dose of 200 µL/kg. Furthermore, topical administration of the SEO inhibited xylene-induced ear edema in comparison with the control group (p<0.05). The higher dose (200 µL /kg) significantly (p<0.001) reduced xylene-induced ear edema which was similar to that observed with positive control (ketoprofen). The pathological analysis of the paws and ears revealed that SEO was capable of reducing cellular infiltration and subcutaneous edema. Else, the SEO produced significant anti-nociceptive activity (p<0.001) at higher dose by inhibiting spontaneous nociception. Conclusion These results support the use of SEO in the development of pharmaceuticals for the management of inflammation and pain.

Structure Modifications of Pinostrobin from Temu Kunci (Boesenbergia pandurata ROXB. SCHLECHT) and Their Analgesic Activity Based on in Silico Studies

2021 ◽  
pp. 2089-2094
Author(s):  
Andy Suryadi ◽  
Siswandono Siswodihardjo ◽  
Tri Widiandani ◽  
Retno Widyowati
Keyword(s):  
Analgesic Activity ◽  
In Silico ◽  
Spectrophotometric Analysis ◽  
Acyl Chloride ◽  
In Silico Studies ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Derivatives Of

Temu kunci (Boesenbergia pandurata ROXB. SCHLECHT) is one of Indonesia medicinal plants which contains essential oils and flavonoids and it has interesting pharmacological activities, such as antifungal, antibacterial, antioxidant, anti-inflammatory and anti-cancer. It also contains pinostrobin which potent as anti-inflammatory and analgesic activities through inhibition of COX-2 enzymes. This research was to obtain pinostrobin derivatives of acylation reactions between pinostrobin and acyl chloride derivatives. The structure modifications of pinostrobin were obtained by Schotten-Baumann method through nucleophilic substitution reactions between pinostrobin and acyl chloride derivatives. Their structure had analyzed using the spectrophotometric analysis (NMR, IR, and GC/MS). The investigation of structure modifications of pinostrobin (1) from this plant has demonstrated the presence of pinostrobin acetate (2) and new pinostrobin propionate (3). The 2 and 3 are derivatives of pinostrobin that can be synthesized using the Schotten-Baumann method to yield 84.3% and 73.9%, respectively. The results of in silico study between pinostrobin and pinostrobin acyl derivatives on the COX-2 receptor with a PDB code: 1PXX showed that pinostrobin RS value was -87.18kcal/mol, while pinostrobin propionate had a RS value of -98.61 kcal/mol. It can be predicted that the pinostrobin acyl derivative has greater analgesic activity than pinostrobin, so it is feasible to be developed and carried out research on its analgesic activity in vivo.

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