퇴행성 뇌질환 치료제 Tacrine 유도체의 프로스타글란딘 생합성 억제효과

• 영문명: Inhibitory Effects of of Tacrine Derivatives on Activity of Prostanoids Biosynthesis Prostaglandin Biosynthesis: A Potential Use for Degenerative Brain Disease Treatment
• 발행기관: 대한약학회
• 저자명: 신혜순(Hea Soon Shin)
• 간행물 정보: 『약학회지』제49권 제1호 (2005년), 103~108쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2005.02.28

영문 초록

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.

키워드

tacrine derivatives prostaglandin synthase inhibitor