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Identification of Neuroactive Constituents of the Ethyl Acetate Fraction from Cyperi Rhizoma Using Bioactivity-Guided Fractionation

  • Sim, Yeomoon (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Choi, Jin Gyu (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Gu, Pil Sung (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Ryu, Byeol (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Kim, Jeong Hee (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Kang, Insug (Department of Biochemistry and Molecular Biology, Medical Research Center for Bioreaction to Reactive Oxygen Species and Biomedical Science Institute, School of Medicine, Kyung Hee University) ;
  • Jang, Dae Sik (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University) ;
  • Oh, Myung Sook (Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University)
  • 투고 : 2016.04.29
  • 심사 : 2016.06.07
  • 발행 : 2016.07.01

초록

Cyperi Rhizoma (CR), the rhizome of Cyperus rotundus L., exhibits neuroprotective effects in in vitro and in vivo models of neuronal diseases. Nevertheless, no study has aimed at finding the neuroactive constituent(s) of CR. In this study, we identified active compounds in a CR extract (CRE) using bioactivity-guided fractionation. We first compared the anti-oxidative and neuroprotective activities of four fractions and the CRE total extract. Only the ethyl acetate (EA) fraction revealed strong activity, and further isolation from the bioactive EA fraction yielded nine constituents: scirpusin A (1), scirpusin B (2), luteolin (3), 6'-acetyl-3,6-diferuloylsucrose (4), 4',6' diacetyl-3,6-diferuloylsucrose (5), p-coumaric acid (6), ferulic acid (7), pinellic acid (8), and fulgidic acid (9). The activities of constituents 1-9 were assessed in terms of anti-oxidative, neuroprotective, anti-inflammatory, and anti-amyloid-${\beta}$ activities. Constituents 1, 2, and 3 exhibited strong activities; constituents 1 and 2 were characterized for the first time in this study. These results provide evidence for the value of CRE as a source of multi-functional neuroprotectants, and constituents 1 and 2 may represent new candidates for further development in therapeutic use against neurodegenerative diseases.

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