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标题：Prolyl Endopeptidase Inhibitors from the Underground Part of Rhodiola sacra S. H. Fu
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作者：Wenzhe FAN ; Yasuhiro TEZUKA ; Katsuko KOMATSU 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1999
卷号：22
期号：2
页码：157-161
DOI：10.1248/bpb.22.157
出版社：The Pharmaceutical Society of Japan
摘要：Prolyl endopeptidase (PEP, EC 3.4.21.26) is an enzyme which plays a role in the metabolism of proline-containing neuropeptides, e.g., vasopressin, substance P and thyrotropin-releasing hormone (TRH), which have been suggested to be involved in learning and memory processes. In our systematic screening for PEP inhibitors from traditional Chinese medicines, we found that MeOH extract from the underground part of Rhodiola sacra S. H. Fu shows significant inhibitory activity against PEP from Flavobacterium meningosepticum. Examination of the constituents of the extract resulted in the isolation of nineteen known compounds, identified as hydroquinone (1), 4-hydroxybenzoic acid (2), caffeic acid (3), 4-hydroxycinnamic acid (4), suberic acid (5), protocatechuic acid (6), gallic acid (7), (-)-epigallocatechin 3-O-gallate (8), 2-phenylethyl β-D-glucopyranoside (9), 3-O-galloylepigallocatechin-(4β→8)-epigallocatechin 3-O-gallate (10), 2-phenylethyl α-L-grabinopyranosyl-(1→6)-β-D-glucopyranoside (11), sacranoside A (12), β-D-glucopyranosyl 4-hydroxybenzoate (13), rhodiocyanoside A (14), rhodiooctanoside (15), sarmentosin (16), heterodendrin (17), arbutin (18) and 4-O-(β-D-glucopyranosyl)-gallic acid (19). Among these, 1, 2, 5, 8-10, 13, 16, 18 and 19 have been isolated for the first time from R. sacra, among which 5, 9, 10, 13, 16, 18 and 19 have been isolated from Rhodiola plants for the first time. On the PEP inhibition, seven compounds (6-8, 10, 12, 18, 19) showed inhibition with an IC₅₀ of 27.8, 487, 1.47, 0.437, 348, 391 and 215 μM, respectively. The kinetic study of these inhibitors indicated that they are noncompetitive inhibitors, except for 6 which is a competitive inhibitor.
关键词：Prolyl endopeptidase (PEP) inhibitor;Rhodiola sacra;Crassulaceae;(-)-epigallocatechin 3-O-gallate;3-O-galloylepigallocatechin-(4β→8)-epigallocatechin 3-O-gallate;protocatechuic acid