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- Title
β-Secretase (BACE1) inhibitors from Sanguisorbae Radix.
- Authors
Lee, Hee-Ju; Seong, Yeon-Hee; Bae, Ki-Hwan; Kwon, Soon-Ho; Kwak, Hye-Min; Nho, Si-Kab; Kim, Kyung-A; Hur, Jong-Moon; Lee, Kyung; Kang, Young-Hwa; Song, Kyung-Sik
- Abstract
In the course of screening anti-dementia agents from natural products, two β-secretase (BACE1) inhibitors were isolated from the ethyl acetate soluble fraction of Sanguisorbae Radix by the activity-guided purification using silica gel, Sephadex LH-20, and RP-HPLC. They were identified as 1,2,3-trigalloyl-4,6-hexahydroxydiphenoyl-β- d-glucopyranoside (Tellimagrandin II, 1) and 1,2,3,4,6-pentagalloyl-β- d-glucopyranoside ( 2) and were shown to non-competitively inhibit β-secretase (BACE1) with the IC50 values of 3.10×10−6 M and 3.76×10−6 M, respectively. The Ki values of 1 and 2 were 6.84×10−6 M and 5.13×10−6 M. They were less inhibitory to α-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific inhibitors of BACE1.
- Publication
Archives of Pharmacal Research, 2005, Vol 28, Issue 7, p799
- ISSN
0253-6269
- Publication type
Article
- DOI
10.1007/BF02977345