콘텐츠 본문
논문 국내 국내전문학술지(KCI급) SELECTIVE BUTYRYLCHOLINESTERASE INHIBITORS USING POLYPHENOL-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)
Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybridmolecules between the free or acetyl protected poly phenol compounds were synthesized and their in vitro antioxidantactivity (DPPH assay) and cholinesterase [a cetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl prote cted hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetylprotected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than fre e phenolic hybrid compounds (6 and 8).Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE (IC50 = 2.3 ± 0.3 μM) and also had a great selectivity for BuChE over AChE (more than 170 fold). Inhibition kinetic studies with acetyl protected compounds (5, 7, 9, and 10) indicated that 5, 7 and 10 are a h yperbolic mixed-type inhibition and 10 is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is 2.32 ± 0.15 μM.
