@article{oai:tohoku-mpu.repo.nii.ac.jp:00000588, author = {千田, 一慶 and Chida, Kazunori and 齊藤, 亮 and Saito, Ryo and 山﨑, 寛之 and Yamazaki, Hiroyuki and 菅野, 秀一 and Kanno, Syu-ichi and 石川, 正明 and Ishikawa, Masaaki and 浪越, 通夫 and Namikoshi, Michio}, issue = {61}, journal = {東北薬科大学研究誌, Journal of Tohoku Pharmaceutical University}, month = {Dec}, note = {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.}, pages = {35--39}, title = {青森県で採集した水圏由来糸状菌からの protein tyrosine phosphatase 1B 阻害剤の探索}, year = {2014}, yomi = {チダ, カズノリ and サイトウ, リョウ and ヤマザキ, ヒロユキ and カンノ, シュウイチ and イシカワ, マサアキ and ナミコシ, ミチオ} }