|
KMID : 0370220050490010103
|
|
Yakhak Hoeji
2005 Volume.49 No. 1 p.103 ~ p.108
|
|
|
Inhibitory Effects of of Tacrine Derivatives on Activity of Prostanoids Biosynthesis Prostaglandin Biosynthesis: A Potential Use for Degenerative Brain Disease Treatment
|
|
신혜순/Shin HS
|
|
|
Abstract
|
|
|
|
Tacrine analogues for degenerative brain disease treatments have been designed. A series of diazaanthrine derivatives as novel analogues of tacrine has been prepared through the alkyl substitution and the ring expansion. They were expected to retain anti-inflammatory activity by inhibition of prostaglandin production with reduction of side effect as the selective prostaglandin synthase inhibitor. Prostaglandin synthase expression is associated with the deposition of beta-amyloid protein in neuritic plaques in brain inflammation. Therefore selective prostaglandin synthase blockade is important for the prevention and treatment of alzheimer’s disease. To evaluate inhibitory effect of prostaglandin synthase, synthetic tacrine derivatives were screened with accumulation of prostaglandin biosynthesis by lipopolysaccharide in aspirin-treated murine macrophage cell. Most of synthetic compounds have shown significant prostaglandin synthase activities in vitro screening with 84.3～33.6% inhibition of the prostaglandin E₂ production at 10 ㎍/ml.
|
|
|
KEYWORD
|
|
|
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|