Jeon S-Y, Kwon S-H, Seong Y-H, Bae K, Hur J-M, Lee Y-Y, Suh D-Y, Song K-S
Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, 1370 Sankyuk-Dong, Daegu 702-701, Republic of Korea.
Phytomedicine. 2007 Jun;14(6):403-8. doi: 10.1016/j.phymed.2006.09.003. Epub 2006 Nov 3.
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.
在从天然产物中寻找β-分泌酶1（BACE1）抑制剂的过程中，菝葜（中国菝葜干燥根茎）的乙酸乙酯可溶部分显示出强效抑制活性。活性化合物被鉴定为反式/顺式白藜芦醇混合物、氧化白藜芦醇、藜芦酚和顺式水麦冬素A。它们被证明以非竞争性方式抑制BACE1，其抑制常数（Ki）值分别为5.4×10⁻⁶、5.4×10⁻⁶、3.4×10⁻⁶和5.4×10⁻⁶M，半数抑制浓度（IC₅₀）值分别为1.5×10⁻⁵、7.6×10⁻⁶、4.2×10⁻⁶和1.0×10⁻⁵M。这些活性化合物对α-分泌酶（TACE）和其他丝氨酸蛋白酶如胰凝乳蛋白酶、胰蛋白酶和弹性蛋白酶的抑制作用较小，表明它们是相对特异性的BACE1抑制剂。
