Protoberberine alkaloids and their reversal activity of P-gp expressed multidrug resistance (MDR) from the rhizome of Coptis japonica Makino
Protoberberine alkaloids and their reversal activity of P-gp expressed multidrug resistance (MDR) from the rhizome of Coptis japonica Makino
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DOI：
10.1007/bf02974076
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发表时间：
2006-09-01
影响因子：
6.7
通讯作者：
Lee, Kang Ro
中科院分区：
文献类型：
--
作者：
Min, Yong Deuk;Yang, Min Cheol;Lee, Kang Ro
从毛茛科植物日本黄连（Coptis japonica Makino）根茎的氯仿层中分离得到6个原小檗碱类生物碱。经理化性质和波谱分析，确定其结构为6-（[1，3]二氧杂环戊烯[4，5-g]异喹啉-5-羰基）-2，3-二甲氧基苯甲酸甲酯（1）、氧化小檗碱（2）、8-氧代表小檗碱（3）、8-氧代黄连碱（4）、小檗碱（5）和巴马汀（6）。化合物3（8-oxo-epiberberine）首次从天然来源中分离得到。采用SRB法测定了化合物对5种肿瘤细胞的体外细胞毒活性，并测定了化合物的多药耐药逆转活性。化合物4具有显著的P-gp多药耐药抑制活性，其在MES-SA/DX 5细胞和HCT 15细胞中的ED 50值分别为0.018 μ g/mL和0.0005 μ g/mL。
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.