Lee M K, Kim H S
College of Pharmacy, Chungbuk National University, Cheongju, South Korea.
Planta Med. 1996 Feb;62(1):31-4. doi: 10.1055/s-2006-957791.
The effects of protoberberine alkaloids from Coptis japonica Makino (COPT) on catecholamine content and tyrosine hydroxylase (TH) activity in PC12 cells were investigated. The butanol (BuOH) fraction from COPT at a concentration of 40 micrograms/ml medium inhibited catecholamine biosynthesis. The BuOH fraction was further fractionated into separate bioactive fractions (Fr. I-IV) by silica gel column chromatography, and Fr. II and III, which contain protoberberine alkaloids such as berberine and palmatine, were isolated. Fr. III at 40 micrograms/ml medium showed 77% inhibition on dopamine content in PC12 cells (IC50; 19.5 micrograms/ml medium). TH activity was reduced by the treatment of Fr. III. Berberine and palmatine also showed an inhibitory activity on dopamine biosynthesis in PC12 cells. The IC50 values of berberine and palmatine were 9.5 and 7.7 micrograms/ml medium, respectively. This suggests that the protoberberine alkaloids from COPT have an inhibitory effect on catecholamine biosynthesis by reducing TH activity in PC12 cells.
研究了来自日本黄连（COPT）的原小檗碱生物碱对PC12细胞中儿茶酚胺含量和酪氨酸羟化酶（TH）活性的影响。COPT的正丁醇（BuOH）馏分在浓度为40微克/毫升培养基时抑制儿茶酚胺生物合成。通过硅胶柱色谱将BuOH馏分进一步分离为单独的生物活性馏分（馏分I-IV），并分离出含有小檗碱和巴马汀等原小檗碱生物碱的馏分II和III。馏分III在40微克/毫升培养基时对PC12细胞中的多巴胺含量显示出77%的抑制作用（IC50；19.5微克/毫升培养基）。通过馏分III处理可降低TH活性。小檗碱和巴马汀对PC12细胞中的多巴胺生物合成也显示出抑制活性。小檗碱和巴马汀的IC50值分别为9.5和7.7微克/毫升培养基。这表明来自COPT的原小檗碱生物碱通过降低PC12细胞中的TH活性对儿茶酚胺生物合成具有抑制作用。
