| 16114494 |
Lee HJ, Seong YH, Bae KH, Kwon SH, Kwak HM, Nho SK, Kim KA, Hur JM, Lee KB, Kang YH, Song KS: Beta-secretase (BACE1) inhibitors from Sanguisorbae Radix. Arch Pharm Res. 2005 Jul;28(7):799-803.
In the course of screening anti-dementia agents from natural products, two beta-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-beta-D-glucopyranoside (Tellimagrandin II, 1) and 1,2,3,4,6-pentagalloyl-beta-D-glucopyranoside (2) and were shown to non-competitively inhibit beta-secretase (BACE1) with the IC50 values of 3.10x10 (-6) M and 3.76x10 (-6) M, respectively. The Ki values of 1 and 2 were 6.84x10 (-6) M and 5.13x10 (-6) M. They were less inhibitory to alphasecretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, suggesting that they were relatively specific inhibitors of BACE1. |
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