AETIQ: a novel synthetic compound with anti-inflammatory properties in activated microglia.

Abstract:

:Neuroinflammation is believed to be involved in the pathogenesis of neurodegenerative diseases. Our novel synthetic compound 2-acetyl-1-ethyl-7-hydroxy-6-methoxy-1, 2, 3, 4-tetrahydroisoquinoline (AETIQ) was tested for its anti-inflammatory properties in activated microglial BV-2 cells. AETIQ attenuated nitric oxide (NO) and reactive oxygen species generation. It also downregulated the production of the proinflammatory enzymes inducible NO synthase, cyclooxygenase-2, and matrix metalloproteinase-3 at both mRNA and protein levels. Furthermore, AETIQ suppressed generation of the proinflammatory cytokines IL-1β and TNF-α as determined by reverse transcriptase-polymerase chain reaction (RT-PCR) and ELISA assays. AETIQ attenuated NFκB signaling by downregulating NFκB nuclear translocation. The compound was stable against the liver enzymes in the microsomal and S9 fractions, indicative of good bioavailability. These results suggested that AETIQ might be utilized towards development of a therapy for neuroinflammation-related diseases.

journal_name

Inflammation

journal_title

Inflammation

authors

Son HJ,Shin N,Shin EJ,Chi DY,Seo JW,Lee CS,Hwang O

doi

10.1007/s10753-013-9795-8

subject

Has Abstract

pub_date

2014-06-01 00:00:00

pages

766-74

issue

3

eissn

0360-3997

issn

1573-2576

journal_volume

37

pub_type

杂志文章
  • Transient exposure of human bronchial epithelial cells to cytokines leads to persistent increased expression of ICAM-1.

    abstract::Effects of several cytokines on kinetics of Intercellular Adhesion Molecule-1 (ICAM-1) and Vascular Cell Adhesion Molecule-1 (VCAM-1) expression were studied on a bronchial epithelial cell line (BEAS-2B). VCAM-I was neither constitutively expressed on BEAS-2B cells nor induced by Interferon-gamma (IFN-gamma). Tumor Ne...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1023/a:1012850630351

    authors: Subauste MC,Choi DC,Proud D

    更新日期:2001-12-01 00:00:00

  • Partial Depletion of Regulatory T Cells Enhances Host Inflammatory Response Against Acute Pseudomonas aeruginosa Infection After Sepsis.

    abstract::Immune dysfunction contributes to secondary infection and worse outcomes in sepsis. Regulatory T cells (Tregs) have been implicated in sepsis-induced immunosuppression. Nevertheless, the role of Tregs in secondary infection after sepsis remains to be determined. In the present study, a two-hit model which mimics clini...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-018-0821-8

    authors: Hu ZQ,Yao YM,Chen W,Bian JL,Zhao LJ,Chen LW,Hong GL,Lu ZQ,Zhao GJ

    更新日期:2018-10-01 00:00:00

  • In Vitro Neutrophil Migration Requires Protein Kinase C-Delta (δ-PKC)-Mediated Myristoylated Alanine-Rich C-Kinase Substrate (MARCKS) Phosphorylation.

    abstract::Dysregulated release of neutrophil reactive oxygen species and proteolytic enzymes contributes to both acute and chronic inflammatory diseases. Therefore, molecular regulators of these processes are potential targets for new anti-inflammatory therapies. We have shown previously that myristoylated alanine-rich C-kinase...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-014-0078-9

    authors: Sheats MK,Sung EJ,Adler KB,Jones SL

    更新日期:2015-01-01 00:00:00

  • IFN-τ Alleviates Lipopolysaccharide-Induced Inflammation by Suppressing NF-κB and MAPKs Pathway Activation in Mice.

    abstract::IFN-τ, which is a type I interferon with low cytotoxicity, is defined as a pregnancy recognition signal in ruminants. Type I interferons have been used as anti-inflammatory agents, but their side effects limit their clinical application. The present study aimed to determine the anti-inflammatory effects of IFN-τ in a ...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-016-0348-9

    authors: Wu H,Zhao G,Jiang K,Chen X,Rui G,Qiu C,Guo M,Deng G

    更新日期:2016-06-01 00:00:00

  • Phagocytotic competence of differentiated U937 cells for colloidal drug delivery systems in immune cells.

    abstract::Drug delivery into immune cells has high potential for the treatment of all kinds of inflammation, allowing a target-oriented transport of active agents. The advantage of this local drug release is the prevention of negative effects of systemic applications and low-dose application. Thereby, the phagocytotic capabilit...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-010-9213-4

    authors: Lessig J,Neu B,Glander HJ,Arnhold J,Reibetanz U

    更新日期:2011-04-01 00:00:00

  • Lypopolysaccharide downregulates the expression of selected phospholipase C genes in cultured endothelial cells.

    abstract::The signaling system of phosphoinositides (PI) is involved in a variety of cell and tissue functions, including membrane trafficking, ion channel activity, cell cycle, apoptosis, differentiation, and cell and tissue polarity. Recently, PI and related molecules, such as the phosphoinositide-specific phospholipases C (P...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-013-9613-3

    authors: Lo Vasco VR,Leopizzi M,Chiappetta C,Puggioni C,Della Rocca C,Polonia P,Businaro R

    更新日期:2013-08-01 00:00:00

  • Synergism between interleukin-1 beta and tumor necrosis factor-alpha in production by 3T3 cells of a chemotactic factor for rat polymorphonuclear leukocytes.

    abstract::Recombinant human interleukin-1 beta (IL-1) and tumor necrosis factor-alpha (TNF) synergistically stimulated BALB/c 3T3 cells to produce a chemotactic factor for rat polymorphonuclear leukocytes (PMNs), whereas an addition of 10(-11)-10(-8) M IL-1 or TNF alone to the cell culture resulted in a slight increase in the p...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00916761

    authors: Nakagawa H,Miyai H,Hirata M,Watanabe K,Onuma I

    更新日期:1989-10-01 00:00:00

  • Inflammatory mediators as biomarkers in brain disorders.

    abstract::Neurodegenerative diseases such as Alzheimer, Parkinson, amyotrophic lateral sclerosis, and Huntington are incurable and debilitating conditions that result in progressive death of the neurons. The definite diagnosis of a neurodegenerative disorder is disadvantaged by the difficulty in obtaining biopsies and thereby t...

    journal_title:Inflammation

    pub_type: 杂志文章,评审

    doi:10.1007/s10753-013-9780-2

    authors: Nuzzo D,Picone P,Caruana L,Vasto S,Barera A,Caruso C,Di Carlo M

    更新日期:2014-06-01 00:00:00

  • Macrophage-Microglia Networks Drive M1 Microglia Polarization After Mycobacterium Infection.

    abstract::Central nervous system tuberculosis (CNS-TB) is caused by infection with Mycobacterium tuberculosis (Mtb). The inflammatory response following CNS-TB involves the activation of resident microglia and the infiltration of macrophages. However, it has not been clarified whether microglia can be polarized into the classic...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-015-0136-y

    authors: Qin Y,Sun X,Shao X,Cheng C,Feng J,Sun W,Gu D,Liu W,Xu F,Duan Y

    更新日期:2015-08-01 00:00:00

  • The effect of cortisone on the accumulation, activation, and necrosis of macrophages in tuberculous lesions.

    abstract::Rabbits were injected intramuscularly with cortisone acetate (2 mg/kg) on alternate days. Six days after the first injection these rabbits and controls were injected intradermally in multiple sites with BCG (the vaccine strain of tubercle bacillus). Periodically, over the next 2 months, the resulting lesions were meas...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00910737

    authors: McCue RE,Dannenberg AM Jr,Higuchi S,Sugimoto M

    更新日期:1978-06-01 00:00:00

  • Characterization of a 130,000-dalton glycoprotein isolated from pulmonary secretions of patients with alveolar proteinosis.

    abstract::A new glycoprotein with an apparent molecular weight of 130,000 was isolated, purified, and partially characterized from the pulmonary secretions which accumulate so massively in the lungs of patients suffering from pulmonary alveolar proteinosis. The amino acid analysis of the glycoprotein showed the presence of rela...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00913501

    authors: Sahu S,Lynn WS

    更新日期:1979-09-01 00:00:00

  • Lack of association between TESPA1 gene polymorphisms (rs1801876, rs2171497, rs4758994, and rs997173) and ankylosing spondylitis in a Chinese population.

    abstract::We investigated whether TESPA1 gene polymorphisms were associated with increased risk of developing ankylosing spondylitis (AS). We also studied whether TESPA1 gene interacts with environmental factors. A total of 494 patients with AS and 478 matched healthy controls were genotyped for four SNPs (rs1801876, rs2171497,...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-014-9936-8

    authors: Liu S,Liu L,Wu S,Yang T,Pan F,Laslett L,Xia G,Hu Y,Fan D,Ding N,Xu S,Cai G,Wang L,Xin L

    更新日期:2014-12-01 00:00:00

  • Neutrophil-mediated proteolysis. Differential roles for cathepsin G and elastase.

    abstract::In this study, we assessed the underlying mechanisms by which proteinases released from activated neutrophils mediate fibronectin degradation. Purified human neutrophils (1 x 10(6)) were incubated for 1 hr with 1 microM PMA in the absence or presence of different proteinase inhibitors in 96-well microtiter plates that...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00918993

    authors: Kubes P,Smith R,Grisham MD,Granger DN

    更新日期:1993-06-01 00:00:00

  • Experimental Study of the Protective Effect of Simvastatin on Lung Injury in Rats with Sepsis.

    abstract::Simvastatin, which is primarily prescribed to lower cholesterol, may also mitigate lung injury caused by sepsis, although the mechanisms remain elusive. This study aimed to evaluate the protective effect of simvastatin on acute lung injury in rats with sepsis and to investigate possible mechanisms. Male Wistar rats we...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-017-0668-4

    authors: Wang Y,Yang W,Zhao X,Zhang R

    更新日期:2018-02-01 00:00:00

  • Effects of Paeonol and Gastroretention Tablets of Paeonol on Experimental Gastric Ulcers and Intestinal Flora in Rats.

    abstract::Paeonol, a major ingredient isolated from Moutan Cort, has various pharmacological effects. Our previous studies have shown that paeonol can exert antioxidant and anti-inflammatory therapeutic effects on ethanol-induced experimental gastric ulcer (GU). Therefore, in this study, we designed two GU models in rats induce...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-020-01285-y

    authors: Guo Y,Du Y,Xie L,Pu Y,Yuan J,Wang Z,Zhang T,Wang B

    更新日期:2020-12-01 00:00:00

  • Effect of the PAF-receptor antagonist SM-12502 on human platelets.

    abstract::We analyzed the effect of the PAF receptor antagonist (+)-cis-3,5-dimethyl-2-(3-pyridyl)thiazolidin-4-one hydrochloride (SM-12502) on human platelet aggregation as well as mediator release. After incubation of human platelet with different concentrations of SM-12502 the cells were subsequently stimulated with either t...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF01487746

    authors: Köller M,Hilger RA,König W

    更新日期:1996-02-01 00:00:00

  • Oroxylin A Inhibits Allergic Airway Inflammation in Ovalbumin (OVA)-Induced Asthma Murine Model.

    abstract::Oroxylin A, a natural flavonoid isolated from the medicinal herb Scutellaria baicalensis Georgi, has been reported to have anti-inflammatory property. In this study, we aimed to investigate the protective effects and mechanism of oroxylin A on allergic inflammation in OVA-induced asthma murine model. BABL/c mice were ...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-016-0317-3

    authors: Zhou DG,Diao BZ,Zhou W,Feng JL

    更新日期:2016-04-01 00:00:00

  • CPEB1 Expression Correlates with Severity of Posttraumatic Ankle Osteoarthritis and Aggravates Catabolic Effect of IL-1β on Chondrocytes.

    abstract::Most cases of posttraumatic ankle osteoarthritis (PTAOA) represent a sequela of ankle fractures. The cytoplasmic polyadenylation element-binding protein 1 (CPEB1) is an RNA binding protein that controls protein expression. Here, we report the previously unappreciated association of CPEB1 with PTAOA. We found that CPEB...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-018-0920-6

    authors: Li L,Lan J,Ye Y,Yang B,Yang X,Cai Z

    更新日期:2019-04-01 00:00:00

  • Analysis of the PKC-gamma-related immunocrossreactive region of a novel leukocyte protein gamma-rp.

    abstract::The newly discovered gamma-PKC-related-protein of human leukocytes (gamma-rp) crossreacts with a polyclonal antibody preparation originally designed to be specific for PKC-gamma (gammaMb-Ab). As this antibody is currently the only suitable probe for gamma-rp, we sought to characterize the binding of the two proteins. ...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1023/a:1020265701407

    authors: Smallwood JI,Malawista SE

    更新日期:1999-08-01 00:00:00

  • Lipid composition of sputum from patients with asthma and patients with cystic fibrosis.

    abstract::Lipids from the sputum of patients with asthma and with cystic fibrosis were isolated and characterized. In both cases, lipids constituted approximately 30% of the dry material. Phosphatidlycholine was the most abundant lipid, Significant amounts of phosphatidylethanolamine and phosphatidylglycerol were present. Hexos...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00917319

    authors: Sahu S,Lynn WS

    更新日期:1978-03-01 00:00:00

  • The anti-inflammatory mechanism of heme oxygenase-1 induced by hemin in primary rat alveolar macrophages.

    abstract::Alveolar macrophages (AMs) can initiate lung inflammation by producing pro-inflammatory cytokines and chemokines, but they participate actively in the prevention of inflammation during acute lung injury (ALI). Heme oxygenase-1 (HO-1) is mainly expressed in AMs and has anti-inflammatory properties in ALI, but the anti-...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-011-9415-4

    authors: Hualin C,Wenli X,Dapeng L,Xijing L,Xiuhua P,Qingfeng P

    更新日期:2012-06-01 00:00:00

  • An interaction between genetic factors and gender determines the magnitude of the inflammatory response in the mouse air pouch model of acute inflammation.

    abstract::The widely used mouse air pouch model of acute inflammation is inducible in a variety of inbred strains, but the potential influence of genetic background and gender on inflammation severity has never been examined. We directly compared the degree of inflammation induced in the air pouch model across four commonly uti...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-006-8962-6

    authors: Delano DL,Montesinos MC,D'Eustachio P,Wiltshire T,Cronstein BN

    更新日期:2005-02-01 00:00:00

  • Serum Cystatin C as an Inflammatory Marker in Exacerbated and Convalescent COPD Patients.

    abstract::Chronic obstructive pulmonary disease (COPD) is a common chronic inflammatory disease with high morbidity and mortality rates. Cystatin C (Cys C) is a sensitive indicator for various chronic inflammatory diseases. In this study, we aimed to evaluate the role of Cys C in COPD patients comparing with the other well-know...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-015-0287-x

    authors: Zhang M,Li Y,Yang X,Shan H,Zhang Q,Ming Z,Xie Y,Chen H,Liu Y,Zhang J

    更新日期:2016-04-01 00:00:00

  • Correction to: Immunomodulatory Effects of CP-25 on Splenic T Cells of Rats with Adjuvant Arthritis.

    abstract::The original version of this article contained mistakes, and the authors would like to correct them. ...

    journal_title:Inflammation

    pub_type: 杂志文章,已发布勘误

    doi:10.1007/s10753-018-0770-2

    authors: Wang Y,Han CC,Cui D,Luo TT,Li Y,Zhang Y,Ma Y,Wei W

    更新日期:2018-06-01 00:00:00

  • Effects of Naringenin on inflammation in complete freund's adjuvant-induced arthritis by regulating Bax/Bcl-2 balance.

    abstract::Naringin (COG) is a flavanone with various bioactivities including an expectorant effect, antitussive effect, and inhibitory effect on asthma and acute lung injury. The aims of the present study were to investigate the antiarthritis activities of COG and elucidate the underlying mechanisms with regard to its molecular...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-014-0027-7

    authors: Zhu L,Wang J,Wei T,Gao J,He H,Chang X,Yan T

    更新日期:2015-02-01 00:00:00

  • Protective Effects of Isoliquiritigenin on LPS-Induced Acute Lung Injury by Activating PPAR-γ.

    abstract::Isoliquiritigenin (ILG), a major ingredient of licorice, has been reported to have anti-oxidative and anti-inflammatory effects. The aim of this study was to investigate the protective effects of ILG on lung injury using an animal model of lipopolysaccharide (LPS)-induced acute lung injury (ALI). Male BALB/c mice were...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-018-0777-8

    authors: Zhang W,Wang G,Zhou S

    更新日期:2018-08-01 00:00:00

  • Properties of lymphocyte chemotactic factor (lymphotactin) in thymus.

    abstract::Aqueous extracts of calf thymus from immunologically stimulated animals contain trypsin- and neuraminidase-labile macromolecules with molecular weights of less than 30,000 daltons which will specifically attract chemotactically lymphocytes. This activity we ascribe to "lymphotactin." ...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00917531

    authors: Houck JC,Chang CM

    更新日期:1976-03-01 00:00:00

  • Chemokine CXCL13 activates p38 MAPK in the trigeminal ganglion after infraorbital nerve injury.

    abstract::Recent data demonstrated that chemokine CXCL13 mediates neuroinflammation and contributes to the maintenance of neuropathic pain after nerve injury in the spinal cord. Pro-nociceptive chemokines activate mitogen-activated protein kinases (MAPKs) which are potential signaling pathways contributing to the nociceptive be...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/s10753-017-0520-x

    authors: Zhang Q,Zhu MD,Cao DL,Bai XQ,Gao YJ,Wu XB

    更新日期:2017-06-01 00:00:00

  • Exogenous nitric oxide increases neutrophil adhesion to cultured human endothelial monolayers through a protein kinase G dependent mechanism.

    abstract::Endothelial-neutrophil adhesion is a critical step in acute inflammatory diseases, which is mediated in part by P-selectin and platelet-activating factor (PAF). Nitric oxide (NO) is well known as an endogenous second messenger derived from endothelial cells, and regulates many important physiological events, however, ...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1023/a:1020287516911

    authors: Okayama N,Coe L,Itoh M,Alexander JS

    更新日期:1999-02-01 00:00:00

  • Clostridial collagenase. A chemoattractant for human neutrophils.

    abstract::Leukocyte chemoattractants markedly alter the morphology and membrane functions of leukocytes. Bacterial collagenase causes a change in cell shape similar to that seen with the leukocyte chemoattractant, f-Met-Leu-Phe, and also promotes capping of concanavalin A. Human neutrophils in suspension or adherent to cover gl...

    journal_title:Inflammation

    pub_type: 杂志文章

    doi:10.1007/BF00915819

    authors: Walter RJ

    更新日期:1986-12-01 00:00:00