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Protoberberine alkaloids and their reversal activity of P-gp expressed multidrug resistance (MDR) from the rhizome ofCoptis japonica Makino


Six protoberberine alkaloids were isolated from the chloroform layer of the rhizome ofCoptis 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 compound3 (8-oxo-epiberberine) was first isolated from natural sources. The compounds were tested for cytotoxicity against five tumor cell linesin vitro by SRB method, and also tested for the MDR reversal activities. Compound4 was of significant P-gp MDR inhibition activity with ED50 value 0.018 μg/mL in MES-SA/DX5 cell and 0.0005 μg/mL in HCT15 cell, respectively.

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Correspondence to Kang Ro Lee.

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Min, Y.D., Yang, M.C., Lee, K.H. et al. Protoberberine alkaloids and their reversal activity of P-gp expressed multidrug resistance (MDR) from the rhizome ofCoptis japonica Makino. Arch Pharm Res 29, 757 (2006).

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Key words

  • Coptis japonica
  • Ranunculaceae
  • Protoberberine alkaloid
  • 8-Oxo-epiberberine
  • Multidrug resistance