Prolyl Endopeptidase Inhibitory Activity of Fourteen Kampo Formulas and Inhibitory Constituents of Tokaku-joki-to(桃核承気湯)
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概要
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Prolyl endopeptidase (PEP, EC 3.4.21.26) is an enzyme playing a role in the metabolism of proline-containing neuropeptides which have been suggested to be involved in learning and memory processes. In screening for PEP inhibitors from fourteen traditional Kampo formulas, we found that Tokaku-joki-to(桃核承気湯) shows a significant inhibitory activity. Examination of the constitutents of the Kampo formula resulted in the isolation of two new compounds, cis-3,5,4'-trihydroxystilbene 4'-O-β-D-(6-O-galloyl)glucopyranoside (10) and 4-(4-hydroxyphenyl)-2-butanone 4'-O-β-D-(6-O-galloyl-2-O-cinnamoyl)glucopyranoside (16), along with twenty-five known compounds, cinnamic acid (1), protocatechuic acid (2), gallic acid (3), torachrysone 8-O-β-D-glucoside (4), emodin (5), emodin 8-O-β-D-glucoside (6), 3,5,4'-trihydroxystilbene 4'-O-β-D-glucopyranoside (7), 3,5,4'-trihydroxystilbene 4'-O-β-D-(2-O-galloyl)glucopyranoside (8), 3,5,4'-trihydroxystilbene 4'-O-β-D-(6-O-galloyl)glucopyranoside (9), 4-(4-hydroxyphenyl)-2-butanone 4'-O-β-D-glucopyranoside (11), isolindleyin (12), lindleyin (13), 4-(4-hydroxyphenyl)-2-butanone 4'-O-β-D-(2,6-di-O-galloyl)glucopyranoside (14), 4-(4-hydroxyphenyl)-2-butanone 4'-O-β-D-(2-O-galloyl-6-O-cinnamoyl)glucopyranoside (15), 1-O-galloylglucose (17), 1,2,6-tri-O-galloylglucose (18), gallic acid 4-O-β-D-(6-O-galloyl)glucopyranoside (19), liquiritigenin (20), liquiritigenin 4'-O-β-D-glucoside (21), liquiritigenin 7,4'-diglucoside (22), liquiritigenin 4'-O-β-D-apiofuranosyl-(1→2)-β-D-glucopyranoside (23), licuroside (24), (-)-epicatechin (25), (-)-epicatechin 3-O-gallate (26) and (+)-catechin (27). Among these compounds, twelve (7-10,14-16,18,19,24-26) showed noncompetitive inhibtion with an IC_<50> of 22.9,3.0,14.9,2.8,10.5,0.69,8.2,0.44,9.39,26.5,28.1 and 0.052μM, respectively.
- 公益社団法人日本薬学会の論文
- 2000-07-01
著者
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KALAUNI Surya
Institute of Natural Medicine, University of Toyama
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Kadota S
Institute Of Natural Medicine University Of Toyama
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Tezuka Yasuhiro
Institute Of Natural Medicine Univeristy Of Toyama
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Fan Wenzhe
Institute Of National Medicine Toyama Medical And Pharmaceutical University
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Kadota Shigetoshi
Institute Of Natural Medicine Toyama Medical And Pharmaceutical University
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Kalauni S
Institute Of Natural Medicine University Of Toyama
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門田 重利
Institute of Natural Medicine, University of Toyama
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