β-secretase (BACE1)-inhibiting stilbenoids from Smilax Rhizoma
| Autor: | Y.-Y. Lee, S.-Y. Jeon, J.-M. Hur, Yeon Hee Seong, KiHwan Bae, Kyung-Sik Song, D.-Y. Suh, S.-H. Kwon |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Stereochemistry
Ethyl acetate Pharmaceutical Science Serine chemistry.chemical_compound Stilbenes Drug Discovery medicine Pharmacology Chymotrypsin Dose-Response Relationship Drug Molecular Structure biology Elastase Smilax china Smilax Trypsin biology.organism_classification Oxyresveratrol Complementary and alternative medicine chemistry biology.protein Molecular Medicine Amyloid Precursor Protein Secretases Rhizome medicine.drug |
| Zdroj: | Phytomedicine. 14:403-408 |
| ISSN: | 0944-7113 |
| DOI: | 10.1016/j.phymed.2006.09.003 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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