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New protein tyrosine phosphatase inhibitors from fungus Aspergillus gorakhpurensis F07ZB1707

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机构: [1]Hebei Med Univ, Sch Pharmaceut Sci, Shijiazhuang 050017, Hebei, Peoples R China [2]Hebei Ind Microbial Metab Engn & Technol Res Ctr, Natl Microbial Med Engn & Res Ctr, Key Lab New Drug Screening Technol Shijiazhuang C, North China Pharmaceut Grp Corp,New Drug Res & De, Shijiazhuang 050015, Hebei, Peoples R China [3]Hebei Med Univ, Collaborat Innovat Ctr Forens Med Mol Identi cati, Hebei Key Lab Forens Med, Shijiazhuang 050017, Hebei, Peoples R China [4]Queens Univ, Dept Chem, Kingston, ON K7L 3N6, Canada [5]Syngenta Jealotts Hill Int Res Ctr, Bracknell RG42 6EY, Berks, England [6]Hebei Univ, Sch Basic Med Sci, Affiliated Hosp, Baoding 071000, Peoples R China
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Twelve new compounds, aspergorakhins A-L (1-12) coupled with one known xanthone leptosphaerin D (13), were isolated from the extract of soil-derived fungus Aspergillus gorakhpurensis F07ZB1707. Their structures were elucidated by spectroscopic data analysis including UV, IR, NMR, and HRESIMS. The absolute configurations of 5 and 8-11 were identified using ECD and OR calculations. All compounds were tested by enzyme inhibitory activity assay in vitro. Aspergorakhin A (1) showed selective activities against PTP1B and SHP1 over TCPTP with IC50 values 0.57, 1.19, and 22.97 mu M, respectively. Compounds 1 and 2 exhibited modest cytotoxicity against tumor cell lines A549, HeLa, Bel-7402, and SMMC-7721 with IC50 values in the range of 6.75-83.4 mu M.

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出版当年[2022]版:
大类 | 3 区 化学
小类 | 3 区 化学:综合
最新[2025]版:
大类 | 3 区 化学
小类 | 3 区 化学:综合
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出版当年[2021]版:
Q2 CHEMISTRY, MULTIDISCIPLINARY
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Q2 CHEMISTRY, MULTIDISCIPLINARY

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第一作者机构: [1]Hebei Med Univ, Sch Pharmaceut Sci, Shijiazhuang 050017, Hebei, Peoples R China
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通讯机构: [1]Hebei Med Univ, Sch Pharmaceut Sci, Shijiazhuang 050017, Hebei, Peoples R China [3]Hebei Med Univ, Collaborat Innovat Ctr Forens Med Mol Identi cati, Hebei Key Lab Forens Med, Shijiazhuang 050017, Hebei, Peoples R China
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