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目的研究小叶臭黄皮Clausena excavate根的化学成分及抗肿瘤活性。方法采用硅胶、RP-18和HPLC等色谱技术分离纯化,根据理化常数和波谱数据鉴定化合物的结构,采用SRB法测定化合物1、2、7、8、10的细胞毒活性。结果从小叶臭黄皮根的甲醇提取物中分离得到13个咔唑生物碱,分别鉴定为2,3-二甲氧基-3-羧基咔唑生物碱(1)、1-羟基-3-甲酸甲酯咔唑生物碱(2)、7-羟基-3-醛基咔唑生物碱(3)、2,7-二甲氧基-3-甲酸甲酯咔唑生物碱(4)、7-羟基-3-甲酸甲酯咔唑生物碱(5)、2-羟基-3-醛基咔唑生物碱(6)、1-羟基-3-醛基咔唑生物碱(7)、2,3-二羟基-3-醛基咔唑生物碱(8)、3-醛基咔唑生物碱(9)、6-甲氧基-3-醛基咔唑生物碱(10)、7-甲氧基-3-甲酸甲酯咔唑生物碱(11)、2-甲氧基-3-羧基咔唑生物碱(12)、1,6-二羟基-3-醛基咔唑生物碱(13)。结论化合物9、10、12为首次从该植物中分离得到。化合物1、2、7、8、10对3种人体肿瘤细胞(A549、He La和BGC-823)均有不同程度的杀伤作用,IC50为8.53~19.87μg/m L。
Objective To study the chemical constituents and anti-tumor activity of Clausena excavate roots. Methods The compounds were isolated and purified by chromatography on silica gel, RP-18 and HPLC. The structures of compounds were identified by physicochemical constants and spectral data. The cytotoxic activities of compounds 1, 2, 7, 8 and 10 were determined by SRB method. Results Thirteen carbazole alkaloids were isolated from the methanol extract of Radix Aconitum and identified as 2,3-dimethoxy-3-carboxycarbazole alkaloids (1), 1-hydroxy-3- Carbamate alkaloids (2), 7-hydroxy-3-carboxyalkylcarbazole alkaloids (3), methyl 2,7-dimethoxy- (5), 2-hydroxy-3-carboxyalkylcarbazole alkaloids (6), 1-hydroxy-3-carboxyalkylcarbazole alkaloids (7) 3-aldehyde carbazole alkaloids (8), 3-aldehyde carbazole alkaloids (9), 6-methoxy- Carboxymethyl carbazole alkaloids (11), 2-methoxy-3-carboxycarbazole alkaloids (12), 1,6-dihydroxy- ). Conclusion Compounds 9, 10 and 12 were isolated from this plant for the first time. Compounds 1, 2, 7, 8 and 10 had different degrees of cytotoxicity against three kinds of human tumor cells (A549, He La and BGC-823) with IC50 of 8.53-19.87 μg / m L.