| Literature DB >> 17084604 |
S-Y Jeon1, S-H Kwon, Y-H Seong, K Bae, J-M Hur, Y-Y Lee, D-Y Suh, K-S Song.
Abstract
In the course of searching for BACE1 (beta-secretase) inhibitors from natural products, the ethyl acetate soluble fraction of Smilax Rhizoma (the dried rhizomes of Smilax china L.) showed potent inhibitory activity. The active compounds were identified as a trans/cis-resveratrol mixture, oxyresveratrol, veraphenol, and cis-scirpusin A. They were shown to non-competitively inhibit BACE1 with the Ki values of 5.4 x 10(-6), 5.4 x 10(-6), 3.4 x 10(-6), and 5.4 x 10(-6)M and IC(50) values of 1.5 x 10(-5), 7.6 x 10(-6), 4.2 x 10(-6), and 1.0 x 10(-5)M, respectively. The active compounds were less inhibitory to alpha-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific inhibitors of BACE1.Entities:
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Year: 2006 PMID： 17084604 DOI： 10.1016/j.phymed.2006.09.003
Source DB: PubMed Journal: Phytomedicine ISSN： 0944-7113 Impact factor: 5.340