Abstract:
:Neuroinflammation has recently been implicated as an important mechanism responsible for the progression of neurodegenerative diseases. Activated microglia produce various proinflammatory cytokines and nitric oxide (NO) that are toxic to neurons. Thus, inhibition of microglial activation may alleviate neuroinflammatory and neurodegenerative processes. Among several fluorovinyloxyacetamide derivatives that were screened by microglia cell-based assay, a novel synthetic compound KT-15073 was identified to strongly attenuate the microglial production of NO and tumor necrosis factor-alpha (TNF-alpha). This compound also suppressed the gene expression of interleukin-1beta, inducible nitric oxide synthase, and TNF-alpha. KT-15073 inhibited the nuclear translocation and DNA binding of nuclear factor-kappaB as well as phosphorylation of p38 mitogen-activated protein kinase. In addition, KT-15073 reduced the cytotoxicity of lipopolysaccharide (LPS)-stimulated microglia toward B35 neuroblastoma cells in the microglia/neuroblastoma coculture, suggesting that the compound might exhibit the neuroprotective activity. Thus, KT-15073 has an anti-inflammatory activity in microglia, and may have a therapeutic potential for the treatment of neuroinflammatory or neurodegenerative diseases.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Ock J,Hong SH,Suk Kdoi
10.1248/bpb.33.461subject
Has Abstractpub_date
2010-01-01 00:00:00pages
461-7issue
3eissn
0918-6158issn
1347-5215pii
JST.JSTAGE/bpb/33.461journal_volume
33pub_type
杂志文章abstract::The tumor microenvironment is one of the key factors contributing to the efficiency of drug delivery to a tumor. It has been reported that lymphangiogenesis is induced in certain tumors. Because the lymphatic system functions as a drainage one, it is possible that tumor lymphatic vessels alter not only the tumor micro...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b17-00730
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.21.1
更新日期:1998-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2010-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2020-09-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b12-00133
更新日期:2012-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.257
更新日期:1999-03-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2010-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2012-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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doi:10.1248/bpb.b16-00915
更新日期:2017-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:1993-08-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2017-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2005-10-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2011-01-01 00:00:00
abstract::To determine the mechanism involved, the incorporation rate (ICR) of drugs into hair was compared to melanin affinity, lipophilicity and membrane permeability. The following 20 drugs were tested; amphetamine, methamphetamine, p-hydroxyamphetamine, p-hydroxymethamphetamine, cocaine, benzoylecgonine, ecgonine methyl est...
journal_title:Biological & pharmaceutical bulletin
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更新日期:1995-09-01 00:00:00
abstract::Potent ligands of peroxisome proliferator-activated receptor γ (PPARγ) such as thiazolidinediones (pioglitazone, troglitazone, etc.) improve insulin sensitivity by increasing the levels of adiponectin, an important adipocytokine associated with insulin sensitivity in adipose tissue. Several constituents from medicinal...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
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更新日期:2014-01-01 00:00:00
abstract::We compared effects of the antiarrhythmic drug bepridil on the electrophysiological parameters in the isolated pulmonary vein preparation from guinea pigs with those in the left atrium. Three pairs of bipolar electrodes were attached to the left atrium, pulmonary vein and junctional region of left atrium and pulmonary...
journal_title:Biological & pharmaceutical bulletin
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更新日期:2013-01-01 00:00:00
abstract::The possibility of pharmacokinetic interactions between Sho-saiko-to extract powder (TJ-9), the most widely used traditional Chinese herbal (Kampo) medicine in Japan, and carbamazepine (CBZ), an important anti-epileptic drug, was examined in rats. There was no significant difference in the protein binding of CBZ in se...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.1461
更新日期:2002-11-01 00:00:00
abstract::Nitrogen oxide, which is produced by activated macrophages, has been demonstrated to possess anti-tumor activity. We report herein the synergistic effect of sodium nitrite (NO2-) and/or sodium nitroprusside (SNP) on lysophospholipid (LysoPL)-mediated cytolysis. The incubation of 51Cr-labeled mouse melanoma (B16) cells...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1994-01-01 00:00:00
abstract::It is known that the onset of major depressive disorder (MDD) would be associated with genetic factors. To investigate the susceptibility to psychiatric disorders, e.g. MDD, schizophrenia etc., it is necessary to compare the genetic differences of objective polymorphisms between in patients and in relative contol subj...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.35.265
更新日期:2012-01-01 00:00:00