Korean Journal of Food Science and Technology (한국식품과학회지)

Korean Society of Food Science and Technology (한국식품과학회)
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The VHR Dual-Specificity Protein Tyrosine Phosphatase (DS-PTPase) Inhibitor Isolated from Gastrodia elata

천마(Gastrodia elata)로부터 분리한 VHR DS-PTPase 저해 물질

  • 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))
  • Published : 2002.06.01
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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).

천마의 methanol 추출물로부터 VHR DS-PTPase 저해 물질을 분리하여 이를 HREI-MS와 $^1H-NMR$, $^{13}C-NMR$, DEPT 등의 기기 분석 자료에 의하여 baicalein으로 구조를 동정 하였다. 이 물질은 VHR에 대하여 $2.4{\mu}M$의 $IC_{50}$값을 나타내었고 T-cell PTPase나 PPase 1과 같은 다른 단백질 탈인산화 효소에 대하여는 저해 활성을 나타내지 않았다. 또한 7종류의 인간 암세포주(흑색종 세포주인 LOX-IMVI, 폐암 세포주인 NCI H23과 A549, 대장암 세포주인 HCT 116와 SW 620, 전립선암 세포주인 PC-3와 백혈병 세포주인 MOLT 4F)에 대한 세포독성을 조사하여 본 결과 $5.26{\sim}12.93\;{\mu}g/mL$에서 $GI_{50}$값을 나타내었다.

Keywords

References

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