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The VHR Dual-Specificity Protein Tyrosine Phosphatase (DS-PTPase) Inhibitor Isolated from Gastrodia elata  

Lee, Myung-Sun (Korea Research Institute of Bioscience and Biotechnology (KRIBB))
Oh, Won-Keun (Korea Research Institute of Bioscience and Biotechnology (KRIBB))
Bae, Eun-Young (Korea Research Institute of Bioscience and Biotechnology (KRIBB))
Ahn, Soon-Cheol (Korea Research Institute of Bioscience and Biotechnology (KRIBB))
Sohn, Cheon-Bae (Department of Food and Nutrition, Chungnam National University)
Osada, Hiroyuki (The Institute of Physical and Chemical Research (RIKEN))
Ahn, Jong-Seog (Korea Research Institute of Bioscience and Biotechnology (KRIBB))
Publication Information
Korean Journal of Food Science and Technology / v.34, no.3, 2002 , pp. 505-509 More about this Journal
Abstract
In the course of screening program for VHR DS-PTPase (dual-specificity protein tyrosine phosphatase) from natural sources, Gastrodia elata was selected. One compound showing potent inhibitory activity was isolated by the solvent extraction and column chromatography including silica gel, ODS RP-18, Sephades LH-20, and HPLC. This compound was identified as baicalein by several NMR techniques such as $^1H-NMR$, $^{13}C-NMR$, and DEPT. Baicalein showed selective inhibitory activity against VHR DS-PTPase with $IC_{50}=2.4\;{\mu}M$, and showed cytotoxicity against several human cancer cell lines with an $GI_{50}$ of $5.26{\sim}12.93\;{\mu}g/mL$ range, including, melanoma (LOX-IMVI), lung cancer (NCI H23 and A549), colon cancer (HCT 116 and SW 620), prostate cancer (PC-3), and leukemia (MOLT 4F).
Keywords
Gastrodia elata; VHR DS-PTPase; baicalein; cytotoxicity;
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