Prolyl Endopeptidase Inhibitors from the Roots of Lindera strychnifolia F. VILL
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概要
- 論文の詳細を見る
Prolyl endopeptidase (PEP, EC 3.4.21.26) has been proposed to play a role in degradation of proline-contaming neuropeptides involved in the processes of learning and memory, e.g., vasopressin, substance P, and thyrotropin-releasing hormone (TRH). In the course of our search for bioactive constituents in medicinal plants, we studied the PEP inhibitory constituents of the roots of Lindera strychnifolia F. VILL and isolated two known tannins, epicatechin (1) and aesculitannin B (2), and four known sesquiterpenes, linderene (3), linderene acetate (4), linderalactone (5) and isolinderalactone (6) as inhibitors. On the inhibitory activities of six compounds against PEP from Flavobacterium meningosepticum and that from rat brain supernatant, compounds 1, 2 and 4 inhibited the enzyme from Flavobacterium more strongly than that from rat brain supernatant. However, compounds 3, 5 and 6 inhibited the enzymes from both origins to the same extent and furthermore, compound 6 was the strongest natural inhibitor against PEP from rat brain supernatant. The kinetic study of these inhibitors indicated that compounds 1, 2 are noncompetitive inhibitors and compounds 3-6 are competitive inhibitors. This is the first example of non-phenolic constituents showing significant competitive inhibitory activity being isolated from natural medicines.
- 公益社団法人日本薬学会の論文
- 2002-08-01
著者
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UMEHARA Kaoru
School of Pharmaceutical Sciences, University of Shizuoka
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三浦 進司
School of Pharmaceutical Sciences University of Shizuoka
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WARASHINA Tsutomu
Institute for Environmental Sciences, University of Shizuoka
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MIYASE Toshio
School of Pharmaceutical Sciences, University of Shizuoka
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Miyase T
School Of Pharmaceutical Sciences University Of Shizuoka
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Miyase Toshio
School Of Pharmaceutical Science University Of Shizuoka
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梅原 薫
School of Pharmaceutical Sciences, University of Shizuoka
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Noguchi Hiroshi
School of Pharmaceutical Sciences and the COE 21 Program, University of Shizuoka
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SANO Mitsuaki
School of Pharmaceutical Sciences, University of Shizuoka
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Umehara K
School Of Pharmaceutical Sciences University Of Shizuoka
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Sano Mitsuaki
School Of Pharmaceutical Sciences University Of Shizuoka
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梅原 薫
School Of Pharmaceutical Sciences University Of Shizuoka
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Umehara Kaoru
School Of Pharmaceutical Sciences University Of Shizuoka
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KOBAYASHI Wataru
School of Pharmaceutical Sciences, University of Shizuoka
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Warashina T
Institute For Environmental Sciences University Of Shizuoka
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Warashina Tsutomu
Institute For Environmental Sciences University Of Shizuoka
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Noguchi H
Department Of Biology Faculty Of Science Chiba University
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Kobayashi Wataru
School Of Pharmaceutical Sciences University Of Shizuoka
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Noguchi Hiroshi
School Of Pharmaceutical Sciences And The Coe 21 Program University Of Shizuoka
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SANO Mitsuaki
School of Pharmaceutical Science, University of Shizuoka
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