書誌事項
- タイトル別名
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- Quest of protein tyrosine phosphatase 1B inhibitors from aquatic fungi collected in Aomori
- アオモリケン デ サイシュウ シタ スイケン ユライ シジョウキン カラ ノ protein tyrosine phosphatase 1B ソガイザイ ノ タンサク
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抄録
In the course of our studies on the bioactive metabolites of aquatic fungi, we have tested the inhibitory activity on the culture broths of 21 fungal strains isolated from marine and freshwater(lake)environments against protein tyrosine phosphatase(PTP)1B, an important target enzyme for the treatment of typeⅡ diabetes and obesity. The ethyl acetate extracts from the culture broths of five fungal strains inhibited the PTP1B activity. Bioassayguided isolation from the extract of a marine-derived Trichoderma sp. strain TPU1239 yielded two knownα-pyrone derivatives, 6[-(E)-hept-1-enyl]-α-pyrone(1)and 6-n-pentyl-α-pyrone(2)as PTP1B inhibitors. The structures of 1 and 2 were identified on the basis of their spectroscopic data. Compound 1 showed an inhibitory activity against PTP1B with an iC50 value of 32.4μm. This is the first time to report the PTP1B inhibitory activity for compounds 1 and 2. moreover, compound 1 did not inhibit the cell proliferation of the human hepatoma huh-7 cells. a hepatocyte is one of the locations of PTP1B, and huh-7 cells are used for the study on the mechanism of action for PTP1B inhibitors.
収録刊行物
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- 東北薬科大学研究誌
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東北薬科大学研究誌 (61), 35-39, 2014-12
東北薬科大学
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詳細情報 詳細情報について
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- CRID
- 1050845762534075776
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- NII論文ID
- 110009900748
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- NII書誌ID
- AA1149311X
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- NDL書誌ID
- 026705402
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- ISSN
- 1345157X
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- 本文言語コード
- ja
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- 資料種別
- departmental bulletin paper
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- データソース種別
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- IRDB
- NDL
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