논문 국내 국내전문학술지(KCI급) SELECTIVE BUTYRYLCHOLINESTERASE INHIBITORS USING POLYPHENOL-POLYPHENOL HYBRID MOLECULES
- 학술지 구분 국내전문학술지(KCI급)
- 게재년월 2011-08
- 저자명 Go Heum Yeun,박정호,원무호,김상헌,Yeun Ji Woo,Bo Hyun Lee,이봉호공동(참여),Hyun Ju Kim
- 학술지명 Bulletin of the Korean Chemical Society
- 발행처명 대한화학회
- 발행국가 국내
- 논문언어 한국어
홈페이지논문 초록 (Abstract)
Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybrid molecules between the free or acetyl protected polyphenol compounds were synthesized and their in vitro antioxidant activity (DPPH assay) and cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl protected hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetyl protected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than free phenolic hybrid compounds (6 and 8). Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE (IC_50 = 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 hyperbolic mixed-type inhibition and 10is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is 2.32 ± 0.15 μM.