콘텐츠 본문
논문 국내 국내전문학술지(KCI급) DEVELOPMENT OF SELECTIVE BUTYRYLCHOLINESTERASE INHIBITORS USING (R)-LIPOIC ACID-POLYPHENOL HYBRID MOLECULES
- 학술지 구분 국내전문학술지(KCI급)
- 게재년월 2011-08
- 저자명 박정호
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 대한화학회
- 발행국가 국내
- 논문언어 외국어
- 전체저자수 8
논문 초록 (Abstract)
A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholineste rase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The IC50 values of all hybr id molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA -acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE (IC50 = 0. 5 ± 0.2 μM) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity (Ki) value to BuChE is 1.52 ± 0.18 μM.
