A Caspase Inducing Inhibitor Isolated from Caesalpinia sappan

소목(Caesalpinia sappan)으로부터 분리한 caspase 유도 저해 물질

  • Son, Eun-Jung (Korea Research Institute of Bioscience and Biotechnology) ;
  • Kim, Jin-Hee (Korea Research Institute of Bioscience and Biotechnology) ;
  • Kim, Hyun-A (Korea Research Institute of Bioscience and Biotechnology) ;
  • Baek, Seung-Hwa (Korea Research Institute of Bioscience and Biotechnology) ;
  • Kho, Yung-Hee (Korea Research Institute of Bioscience and Biotechnology) ;
  • Kim, Mee-Ree (Department of Food and nutrition, Chungnam National University) ;
  • Lee, Choong-Hwan (Korea Research Institute of Bioscience and Biotechnology)
  • Published : 2003.08.01

Abstract

Through the screening of caspase-3 inducing inhibitors in U937 human monocytic leukemia cell from natural sources, Caesalpiniae sappan, which showed a high level of inhibition, was selected. The inhibition compound was purified from methanol extract by silica gel column chromatography and HPLC. The inhibitor was identified as brazilin by spectroscopic methods of ESI-MS, $^1H-NMR$, and $^{13}C-NMR$. Brazilin showed inhibitory activity of caspase-3 induction, a major protease of apoptosis cascade, with $IC_{50}$ value of $4.5\;{\mu}g/mL$ after 7 hr of treatment in U937 cells.

한약재로부터 U937 세포주를 사용한 caspase-3 유도저해물질을 탐색한 결과 소목(Caesalpiniae sappan)을 선발하였다. 소목의 메탄올 추출물로부터 silica gel column chromatography, HPLC 등을 사용하여 저해물질을 분리하였으며, ESI-MS, $^1H-NMR,\;^{13}C-NMR$ 등의 기기분석을 실시하여 brazilin이 동정되었다. 이 물질은 $IC_{50}\;4.5\;{\mu}g/mL$의 농도로 U937세포주의 etoposide에 의한 caspase-3 유도를 저해하였으며, DPPH 라디칼 소거능도 나타내었다.

Keywords

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