A Caspase Inducing Inhibitor Isolated from Forsythiae fructus

연교(Forsythiae fructus)로부터 분리한 caspase 유도 저해물질

  • Kim, Jin-Hee (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) ;
  • Kim, Hyun-A (Korea Research Institute of Bioscience and Biotechnology) ;
  • Lee, Sang-Myung (Korea Research Institute of Bioscience and Biotechnology) ;
  • Lee, Choong-Hwan (Korea Research Institute of Bioscience and Biotechnology)
  • Published : 2002.02.01

Abstract

During the screening of inhibitors of caspase-3 induction in U937 human monocytic leukemia cells from natural sources, Forsythiae fructus, which showed a high level of inhibition, was selected. And then, the compound was purified from the methanol extract using silica gel column chromatography and HPLC. The inhibitor was identified as rengyolone, by spectroscophic methods of ESI-MS, $^1H-NMR$, $^{13}C-NMR$, DEPT, and HMBC. Rengyolone showed inhibitory activity of caspase-3 induction, a major protease of apoptosis cascade, with an $IC_{50}$ value of $6.25\;{\mu}g/mL$ after 7 h of treatment in U937 cells. It also showed inhibitory activity of caspace-1 induction, with an $IC_{50}$ value of $7.50\;{\mu}g/mL$ after 40 h of treatment in D10S cells. In addition, it showed protective effect against cell death with an $IC_{50}$ value of $11\;{\mu}g/mL$ on U937 cells induced by etoposide after 24 h of treatment, but did not show any cytotoxicity at the same condition without etoposide, a caspase 3 inducing agent.

Keywords

apoptosis;rengyolone;etoposide;U937;D10S

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