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、HeLa 和BGC-823)均有不同程度的杀伤作用,IC₅₀ 为8.53~19.87 μg/mL。

Objective To study the chemical constituents from the roots of Clausena excavata (Rutaceae). Methods The compounds were isolated and purified by means of column chromatographies including silica gel, RP-₁₈, and HPLC. Compound structures isolated were determined on the basis of spectroscopic data. Results Thirteen carbazole alkaloids clausine K (1), clausine E (2), 3-formyl-7-hydroxycarbazole (3), clausine H (4), clausine M (5), mukona (6), O-demethylmurrayanine (7), clausine O (8), 3-formylcarbazole (9), 3-formyl-6-methoxy carbazole alkaloid (10), clausine C (11), 2-methoxy-3-carboxylic acid-carbazole alkaloid (12), and clausine Z (13) were isolated from the roots of C. excavata. Conclusion Compounds 9, 10, and 12 are isolated from this plant for the first time. Compounds 1, 2, 7, 8, and 10 are tested for their cytotoxicities against A549, Hela, and BGC-823 cancer cell lines. The results show that they exhibit the cytotoxicity against A549, Hela, and BGC-823 with the IC₅₀ values of 8.53-19.87 μg/mL.

江西省博士后科研基金(06292023);江西农业大学博士科研启动基金项目(09004507)