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KMID : 0043320080310020183
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Archives of Pharmacal Research
2008 Volume.31 No. 2 p.183 ~ p.187
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β-Secretase (BACE1) Inhibitors from Perilla frutescens var. acuta
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Choi Sun-Ha
Lee Kyung-Bok
Moon Eun-Ho
Song Kyung-Sik
Jun Mi-Ra
Yang Eun-Ju
Hur Jong-Moon
Park Hyo-Jun
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Abstract
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In the course of screening for anti-dementia agents from natural products, two β-Secretase (BACE1) inhibitors were isolated from the methanolic extract of Perilla frutescens var. acuta and identified as luteolin (1) and rosmarinic acid (2) IC50 with values of 5.0 M and M, respectively. They inhibited BACE1 in a non-competitive manner with a substrate in Dixon plots, suggesting that they might bind to either β-Secretase subsite or to another regulatory site. Ki values of 1 and 2 were M and M, respectively. They were less inhibitory against other enzymes such as β-Secretase (TACE), acetylcholine esterase (AchE), chymotrypsin, and elastase, indicating that they were relatively specific inhibitors of BACE1.
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KEYWORD
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Perilla frutescens var. acuta, β-Secretase (BACE1), Luteolin, Rosmarinic acid, Dementia, Alzheimer’s disease
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