KMID : 0043320060290090757
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Archives of Pharmacal Research 2006 Volume.29 No. 9 p.757 ~ p.761
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Protoberberine Alkaloids and their Reversal Activity of P-gp Expressed Multidrug Resistance (MDR) from the Rhizome of Coptis japonica Makino
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Min Yong-Deuk
Yang Min-Cheol Lee Kyu-Ha Kim Kyung-Ran Choi Sang-Un Lee Kang-Ro
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Abstract
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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 ¥ìg/mL in MES-SA/DX5 cell and 0.0005 ¥ìg/mL in HCT15 cell, respectively.
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KEYWORD
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Coptis japonica, Ranunculaceae, Protoberberine alkaloid, 8-Oxo-epiberberine, Multidrug resistance
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