| Autor: |
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 |
| Zdroj: |
Archives of Pharmacal Research; Jul2005, Vol. 28 Issue 7, p799-803, 5p |
| Abstrakt: |
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. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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