scholarly journals Virtual prediction of purple rice ferulic acid as anti-inflammatory of TNF-α signaling

2021 ◽  
Vol 27 (2) ◽  
pp. 59-66
Author(s):  
Ernanin Dyah Wijayanti ◽  
Anna Safitri ◽  
Dian Siswanto ◽  
Fatchiyah Fatchiyah
Keyword(s):  
Biological Activity ◽  
Ferulic Acid ◽  
Inhibition Mechanism ◽  
Drug Candidate ◽  
Inflammatory Drug ◽  
Lipinski’S Rule ◽  
Discovery Studio ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Docking Energy

Purple rice is one of the main sources of ferulic acid (FA). Some studies reported anti-inflammatory properties of FA, but the interaction of FA with TNF-α signaling has not been elucidated. TNF-α is a target for anti-inflammatory drug research due to its major role in the inflammatory process. This study aims to investigate the interaction of FA with TNF-α and TNF-α receptor (TNFR) through in silico study and evaluate the drug-like properties and biological activity of FA. The interactions among FA (CID 445858), TNF-α (2AZ5), and TNFR (1NCF) were docked by Hex 8.0.0 Cuda, then visualized by Discovery Studio 2020 and LigPlot V.1.4.5. Apigenin-7-glucuronide (AG, CID 5319484) was used as the positive control. The drug-like properties were predicted by Lipinski’s rule of five and the biological activity was analyzed by PASS online. FA showed good properties as a drug-like molecule and biological activity as an anti-inflammatory. FA also showed good interaction with TNF-α and TNFR. FA bound to TNF-α at Asn92(B), Val91(B), Leu93(B), Phe124(B), Phe124(D), and Leu93(D) residues with docking energy of -214.6 kJ/mol, and bound to TNFR at Pro16(A), Glu56(B), Cys55(B), Glu54(B) residues with docking energy of -191.1 kJ/mol. FA could inhibit TNF-α – TNFR interaction by binding to TNFR at Glu54 residue, the same inhibition mechanism to AG which bind to TNFR at Glu54 and Val90. The current study shows that FA has the potential as an anti-inflammatory of TNF-α signaling and can be developed as an oral anti-inflammatory drug candidate.

scholarly journals Inhibitory Effect of Ferulic Acid and Isoferulic Acid on the Production of Macrophage Inflammatory Protein-2 in Response to Respiratory Syncytial Virus Infection in RAW264.7 Cells

1999 ◽  
Vol 8 (3) ◽  
pp. 173-175 ◽  
Author(s):  
S. Sakai ◽  
H. Kawamata ◽  
T. Kogure ◽  
N. Mantani ◽  
K. Terasawa ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Ferulic Acid ◽  
Dependent Manner ◽  
Inflammatory Drug ◽  
Inflammatory Protein ◽  
Isoferulic Acid ◽  
Infected Cells ◽  
Anti Inflammatory ◽  
Syncytial Virus ◽  
Macrophage Inflammatory Protein

We investigated the effect of ferulic acid (FA) and isoferulic acid (IFA), which are the main active components of the rhizoma ofCimicifuga heracleifolia(CH), an anti-inflammatory drug used frequently in Japanese traditional medicine, on the production of macrophage inflammatory protein-2 (MIR-2) in a murine macrophage cell line, RAW264.7, in response to respiratory syncytial virus (RSV) infection. Following the exposure of cells to RSV for 20 h, the MIP-2 level in condition medium was increased to about 20 ng/ml, although this level in mock-infected cells was negligible. In the presence of either FA or IFA, RSV-infected cells reduced MIP-2 production in a dose-dependent manner. These data suggest that FA and IFA might be responsible, at least in part, for the anti-inflammatory drug effect of CH extract through the inhibition of MIP-2 production.

Preparation and characterization of antibacterial and anti-inflammatory hyaluronic acid-chitosan-dexamethasone hydrogels for peri-implantitis repair

2021 ◽  
pp. 088532822110479
Author(s):  
Zhen Zhou ◽  
Qiang Zhang ◽  
Yamin Wang
Keyword(s):  
Hyaluronic Acid ◽  
Physicochemical Characterization ◽  
Inflammatory Drug ◽  
Composite Hydrogels ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Nih 3T3

Numerous treatment methods for peri-implantitis have been widely used including oral cleaning, traditional metal scraping means, or local antibiotic application. However, to continuously release antibacterial and anti-inflammatory drug in location in situ for effective peri-implantitis repair is still challenging. Herein, an anti-inflammatory drug dexamethasone (DE)–incorporated hyaluronic acid (HA)-chitosan (CT) composite hydrogels system was developed to repair peri-implantitis. The physicochemical characterization and biocompatibility of the hydrogel were evaluated in vitro. The in vivo hydrogels degradation and peri-implantitis repair were assessed in mice. The results showed that the prepared multifunctional hydrogels achieved sustained release, with an equilibrium swelling of 18, and promoted the growth against NIH-3T3 fibroblast cells. The in vitro antibacterial tests showed HA-CT-DE hydrogels can inhibit methicillin-resistant Staphylococcus aureus and Escherichia coli. It down-regulated the expression levels of inflammation factor IL-1β, IL-6 and, TNF-α in peri-implantitis. The prepared HA-CT-DE composite hydrogels with integrated function is promising for the treatment of peri-implantitis.

scholarly journals Ferulic Acid Improves Depressive-Like Behavior in Prenatally-Stressed Offspring Rats via Anti-Inflammatory Activity and HPA Axis

2019 ◽  
Vol 20 (3) ◽  
pp. 493 ◽  
Author(s):  
Xingxing Zheng ◽  
Ying Cheng ◽  
Yiwei Chen ◽  
Yisong Yue ◽  
Yingchun Li ◽  
...  
Keyword(s):  
Protein Expression ◽  
Ferulic Acid ◽  
Hpa Axis ◽  
Glucocorticoid Receptors ◽  
Metabolic Diseases ◽  
Inflammatory Activity ◽  
Tnf Α ◽  
Immobility Time ◽  
Prenatally Stressed ◽  
Anti Inflammatory

Prenatal stress (PS) can increase the risk of nervous, endocrine and metabolic diseases, and immune dysfunction. Ferulic acid (FA) is a dietary phenolic acid that has pharmacological properties, including potent anti-inflammatory action. We used male, prenatally-stressed offspring rats to investigate the anti-depressive-like effects and possible anti-inflammatory mechanism of FA. We determined the animal behaviors, and the mRNA expression and concentration of inflammatory cytokines, and HPA axis. In addition, we assessed the modulation of hippocampal nuclear factor-κB (NF-κB) activation, neuronal nitric oxide synthase (nNOS) and glucocorticoid receptors (GR) expression via western blotting and immunohistochemistry. Administration of FA (12.5, 25, and 50 mg/kg/day, i.g.) for 28 days markedly increased sucrose intake, and decreased immobility time and total number of crossings, center crossings, rearing, and grooming in the male PS offspring. FA significantly reduced IL-6, IL-1β, and TNF-α concentration and increased IL-10 concentration in male, prenatally-stressed offspring, stimulated by the NF-κB pathway. In addition, FA inhibited interleukin-6 (IL-6), interleukin-1β (IL-1β), and tumor necrosis factor-α (TNF-α), and increased interleukin-10 (IL-10) mRNA and protein expression. Furthermore, FA markedly decreased the serum adrenocorticotropin (ACTH) and corticosterone concentration by the increase of GR protein expression. Taken together, this study revealed that FA has anti-depressive-like effects in male, prenatally-stressed offspring, partially due to its anti-inflammatory activity and hypothalamic-pituitary-adrenal (HPA) axis.

scholarly journals Anti-Neuroinflammatory Property of Phlorotannins from Ecklonia cava on Aβ25-35-Induced Damage in PC12 Cells

Marine Drugs ◽  
2018 ◽  
Vol 17 (1) ◽  
pp. 7 ◽  
Author(s):  
Seungeun Lee ◽  
Kumju Youn ◽  
Dong Kim ◽  
Mok-Ryeon Ahn ◽  
Eunju Yoon ◽  
...  
Keyword(s):  
Pc12 Cells ◽  
Neurodegenerative Disorder ◽  
Brown Seaweed ◽  
Ecklonia Cava ◽  
Drug Candidate ◽  
Protein Levels ◽  
Tnf Α ◽  
Caspase Family ◽  
Anti Inflammatory ◽  
New Generation

Alzheimer disease (AD) is a neurodegenerative disorder characterized by excessive accumulation of amyloid-beta peptide (Aβ) and progressive loss of neurons. Therefore, the inhibition of Aβ-induced neurotoxicity is a potential therapeutic approach for the treatment of AD. Ecklonia cava is an edible brown seaweed, which has been recognized as a rich source of bioactive derivatives, mainly phlorotannins. In this study, phlorotannins including eckol, dieckol, 8,8′-bieckol were used as potential neuroprotective candidates for their anti-apoptotic and anti-inflammatory effects against Aβ25-35-induced damage in PC12 cells. Among the tested compounds, dieckol showed the highest effect in both suppressing intracellular oxidative stress and mitochondrial dysfunction and activation of caspase family. Three phlorotannins were found to inhibit TNF-α, IL-1β and PGE2 production at the protein levels. These result showed that the anti-inflammatory properties of our compounds are related to the down-regulation of proinflammatory enzymes, iNOS and COX-2, through the negative regulation of the NF-κB pathway in Aβ25-35-stimulated PC12 cells. Especially, dieckol showed the strong anti-inflammatory effects via suppression of p38, ERK and JNK. However, 8,8′-bieckol markedly decreased the phosphorylation of p38 and JNK and eckol suppressed the activation of p38. Therefore, the results of this study indicated that dieckol from E. cava might be applied as a drug candidate for the development of new generation therapeutic agents against AD.

scholarly journals Anti-Inflammatory Effects of the Fraction from the Leaves of Pyrus pyrifolia on LPS-Stimulated THP-1 Cells

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Gilhye Lee ◽  
Jung-Hee Kim ◽  
Hyun-Jae Jang ◽  
Ji-Won Park ◽  
Jae-Won Lee ◽  
...  
Keyword(s):  
East Asia ◽  
Biological Activities ◽  
Pyrus Pyrifolia ◽  
Rna Expression ◽  
Inflammatory Drug ◽  
Pyrus Pyrifolia Nakai ◽  
Tnf Α ◽  
Bioactive Fraction ◽  
Anti Inflammatory ◽  
Inflammatory Molecules

Pyrus pyrifolia Nakai (P. pyrifolia) has been traditionally used in East Asia to treat diseases such as phlegm, cough, hangover, and fever. However, there is no investigation that evaluates the biological activities of the leaves of P. pyrifolia. This study aims at describing the anti-inflammatory effects of PP, a bioactive fraction from the leaves of P. pyrifolia, in lipopolysaccharide (LPS)-stimulated THP-1 cells. Initially, PP decreased the protein and RNA expression of TNF-α, MCP-1, IL-8, and IL-6 induced by LPS. Moreover, PP attenuated the phosphorylation of p38, JNK, and ERK. In addition, after stimulation with LPS, the degradation of IκB-α was suppressed by PP, and the phosphorylation of IκB-α and p65 was suppressed by PP. Additionally, PP increased HO-1, which controls the production of inflammatory molecules, by activating Nrf2. These results indicated that PP could be used as an anti-inflammatory drug to promote wellness.

scholarly journals Polymorphic characterization and implications on biopharmaceutics properties of potential anti‐inflammatory drug candidate eremantholide C from Lychnophora trichocarpha (Brazilian Arnica)

2019 ◽  
Vol 71 (6) ◽  
pp. 910-919
Author(s):  
Tamires G. Caldeira ◽  
Dênia A. Saúde‐Guimarães ◽  
Dâmaris L. R. De Lacerda ◽  
Wagner Da Nova Mussel ◽  
Maria Irene Yoshida ◽  
...  
Keyword(s):  
Drug Candidate ◽  
Inflammatory Drug ◽  
Anti Inflammatory
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