Protoberberine Alkaloids and their Reversal Activity of P-gp Expressed Multidrug Resistance (MDR) from the Rhizome of Coptis japonica Makino

  • Min, Yong-Deuk (Natural Products Laboratory, College of Pharmacy, Sungkyunkwan University) ;
  • Yang, Min-Cheol (Natural Products Laboratory, College of Pharmacy, Sungkyunkwan University) ;
  • Lee, Kyu-Ha (Natural Products Laboratory, College of Pharmacy, Sungkyunkwan University) ;
  • Kim, Kyung-Ran (Natural Products Laboratory, College of Pharmacy, Sungkyunkwan University) ;
  • Choi, Sang-Un (Korea Research Institute of Chemical Technology) ;
  • Lee, Kang-Ro (Natural Products Laboratory, College of Pharmacy, Sungkyunkwan University)
  • Published : 2006.09.01

Abstract

Six protoberberine alkaloids were isolated from the chloroform layer of the rhizome of Coptis japonica Makino (Ranunculaceae). The structures of the isolated compounds were determined to be 6-([1,3]dioxolo[4,5-g]isoquinoline-5-carbonyl)-2,3-dimethoxy-benzoic acid methyl ester (1), oxyberberine (2), 8-oxo-epiberberine (3), 8-oxocoptisine (4), berberine (5) and palmatine (6) by physicochemical and spectroscopic methods. The compound 3 (8-oxo-epiberberine) was first isolated from natural sources. The compounds were tested for cytotoxicity against five tumor cell lines in vitro by SRB method, and also tested for the MDR reversal activities. Compound 4 was of significant P-gp MDR inhibition activity with ED50 value $0.018\;{\mu}g/mL$ in MES-SA/DX5 cell and $0.0005\;{\mu}g/mL$ in HCT15 cell, respectively.

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References

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