β-secretase (BACE1) inhibitors from sanguisorbae radix

Hee Ju Lee; Yeon Hee Seong; Ki Hwan Bae; Soon Ho Kwon; Hye Min Kwak; Si Kab Nho; Kyung A. Kim; Jong Moon Hur; Bok Lee Kyung; Young Hwa Kang; Kyung Sik Song

doi:10.1007/BF02977345

β-secretase (BACE1) inhibitors from sanguisorbae radix

Hee Ju Lee, Yeon Hee Seong, Ki Hwan Bae, Soon Ho Kwon, Hye Min Kwak, Si Kab Nho, Kyung A. Kim, Jong Moon Hur, Bok Lee Kyung, Young Hwa Kang, Kyung Sik Song

Department of Horticultural Science

Research output: Contribution to journal › Article › peer-review

38 Scopus citations

Abstract

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 IC ₅₀ 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.

Original language	English
Pages (from-to)	799-803
Number of pages	5
Journal	Archives of Pharmacal Research
Volume	28
Issue number	7
DOIs	https://doi.org/10.1007/BF02977345
State	Published - 31 Jul 2005

Keywords

1,2,3,4,6-Pentagalloyl-β-D glucopyranoside
Alzheimer's disease
Inhibitor
Sanguisorbae radix
Tellimagrandin II
β-secretase (BACE1)

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title = "β-secretase (BACE1) inhibitors from sanguisorbae radix",

abstract = "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 IC 50 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.",

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author = "Lee, {Hee Ju} and Seong, {Yeon Hee} and Bae, {Ki Hwan} and Kwon, {Soon Ho} and Kwak, {Hye Min} and Nho, {Si Kab} and Kim, {Kyung A.} and Hur, {Jong Moon} and Kyung, {Bok Lee} and Kang, {Young Hwa} and Song, {Kyung Sik}",

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AU - Lee, Hee Ju

AU - Seong, Yeon Hee

AU - Bae, Ki Hwan

AU - Kwon, Soon Ho

AU - Kwak, Hye Min

AU - Nho, Si Kab

AU - Kim, Kyung A.

AU - Hur, Jong Moon

AU - Kyung, Bok Lee

AU - Kang, Young Hwa

AU - Song, Kyung Sik

PY - 2005/7/31

Y1 - 2005/7/31

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AB - 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 IC 50 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.

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KW - Alzheimer's disease

KW - Inhibitor

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β-secretase (BACE1) inhibitors from sanguisorbae radix

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