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4. Beta-secretase (BACE1) inhibitors from Sanguisorbae Radix.

Author

Lee HJ, Seong YH, Bae KH, Kwon SH, Kwak HM, Nho SK, Kim KA, Hur JM, Lee KB, Kang YH, and Song KS

Subjects
Alzheimer Disease prevention & control, Amyloid Precursor Protein Secretases, Aspartic Acid Endopeptidases, Dose-Response Relationship, Drug, Gallic Acid isolation & purification, Gallic Acid pharmacology, Glucosides isolation & purification, Humans, Hydrolyzable Tannins isolation & purification, In Vitro Techniques, Inhibitory Concentration 50, Kinetics, Plant Extracts chemistry, Plant Extracts pharmacology, Protease Inhibitors isolation & purification, Endopeptidases metabolism, Gallic Acid analogs & derivatives, Glucosides pharmacology, Hydrolyzable Tannins pharmacology, Protease Inhibitors pharmacology, Sanguisorba chemistry
Abstract

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.

Published
2005
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