Melanin-concentrating Hormone-1 Receptor (MCH-1) Antagonism of the Leaves Extract from Morus alba

  • Oh, Byung-Koo (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Oh, Kwang-Seok (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Lee, Sung-Hou (Department of Biotechnology and Informatics, College of Engineering, Sangmyung University) ;
  • Seo, Ho-Won (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Choi, Yeon-Hee (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Choi, Jae-Seok (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Kim, Young-Sup (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Lee, Byung-Ho (Bio-Organic Science Division, Korea Research Institute of Chemical Technology) ;
  • Kwon, Kwang-Il (College of Pharmacy, Chungnam National University) ;
  • Ryu, Shi-Yong (Bio-Organic Science Division, Korea Research Institute of Chemical Technology)
  • Published : 2009.03.31

Abstract

The present study was performed to investigate the binding affinity of the ethanol extract from the leaves of Morus alba (EMA) and some EMA related plant materials (EMA-D, EMA-DM) for melanin-concentrating hormone-1 receptor (MCH-1) and also to examine the antagonistic effect of them for the recombinant MCH-1 receptor expressed in CHO cells. EMA, dichloromethane fraction (EMA-D) and EMA-DM exhibited high affinity for mammalian MCH receptor in receptor binding assays ($IC_{50}$ value: 2.3, 1.6 and $1.0{\mu}g/ml$, respectively). Other plant materials (MMA-D, MMA-DM) obtained from methanol extracts from the leaves of Morus alba (MMA) also exhibited high affinity for mammalian MCH receptor, even though the $IC_{50}$ values of them were lower than those of EMA-D and EMA-DM. In Chinese hamster ovary (CHO) cells expressing human MCH-1, EMA-DM and EMA-D significantly inhibited MCH-induced intracellular $Ca^{2+}$ increase ($IC_{50}$ values: 16.5 and $22.7{\mu}g/ml$, respectively). These results clearly indicate that the ethanol extract from the leaves of Morus alba (EMA) and some EMA related plant materials (EMA-D, EMA-DM) are novel selective MCH-1 receptor antagonist, respectively.

Keywords

References

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