An Apoptosis Regulator isolated from Petasites japonicum

머위로부터 분리한 apoptosis 조절물질

  • Lee, Choong-Hwan (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Chung, Myung-Chul (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Lee, Ho-Jae (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology) ;
  • Kho, Yung-Hee (Enzyme Inhibition Research Unit, Korea Research Institute of Bioscience and Biotechnology)
  • 이충환 (생명공학연구소 효소저해연구실) ;
  • 정명철 (생명공학연구소 효소저해연구실) ;
  • 이호재 (생명공학연구소 효소저해연구실) ;
  • 고영희 (생명공학연구소 효소저해연구실)
  • Published : 2000.04.30

Abstract

During the screening of inhibitors of caspase-3 induction in U937 human monocytic leukemia cells from natural sources, Petasites japonicum, which showed a high level of inhibition was selected. The inhibiting compound was purified from the methanol extract by Sephadex LH-20 column chromatography and HPLC. The inhibitor was identified as [3-(3,4-dihydroxyphenyl)-2-oxopropyl]ester, petasiphenol, by spectroscopic methods of UV, EIMS, $^1H-NMR$, $^{13}C-NMR$ and HMBC. It showed a caspase-3 inducing inhibitory activity at $8\;{\mu}g/ml$ of $IC_{50}$ value with DNA fragmentation inhibition in U937 human leukemia cells. It also showed a free radical scavenging ability of 1,1-diphenyl-2-picrylhydrazyl.

천연물로부터 U937 세포주를 사용한 caspase-3 유도저해물질을 탐색한 결과 머위(Petasites japonicum)를 선발하였다. 머위의 메탄올 추출물로부터 Sephadex LH-20 column chromatography, HPLC 등을 사용하여 저해물질을 분리하였으며, UV, EIMS, 1H-NMR, $^{13}C-NMR$, HMBC등의 기기분석을 실시한 결과 [3-(3,4-dihydroxyphenyl)-2-oxopropyl] ester로 동정되었다. 이 물질은 $IC_{50}\;8\;{\mu}g/ml$의 농도로 U937 세포주의 etoposide에 의한 caspase 3 유도를 저해하였으며, DNA fragmentation도 저해하였다. 또한 1,1-diphenyl-2-picrylhydrazyl(DPPH) 라디칼 소거능을 나타내었다.

Keywords