红厚壳枝条中的细胞毒活性成分研究

Study on the cytotoxic chemical constituents from the twigs of Calophyllum inophyllum

目的研究红厚壳(Calophyllum inophyllum Linn.)枝条的化学成分。方法采用硅胶柱色谱、凝胶柱色谱等方法进行分离纯化,根据理化常数和波谱数据鉴定结构。结果从红厚壳枝条中提取分离得到5个化合物,分别鉴定为:1,2,3-三羟基-5-甲氧基口山酮(1)、3,5-二羟基-1-甲氧基口山酮(2)、1,7-二羟基-3-甲氧基口山酮(3)、3-羟基-4-甲氧基口山酮(4)和12-甲氧基红厚壳素P(5)。结论以上5个化合物均为首次从该种植物中分离得到。采用MTT法对以上化合物进行了体外肿瘤细胞毒活性测试,实验结果表明,化合物1和5均显示了肿瘤细胞毒活性。

Calophyllum inophyllum Linn, which belongs to the family of Clusiaceae, is an evergreen shrub wildly distributed in tropical areas. It is used in traditional Chinese folk medicine for the treatment of eye diseases, wounds, rheumatism and inflammations. Previous studies on chemical constituents and their activities from this plant led to the isolation of several classes of compounds including pyranocoumarins, xanthones, triterpenes and flavonoids, which possessed various bioactivities such as anti-HIV-1, anti-microbial, and cyto- toxic activities. During our continuous investigation on C. inophyllum, five compounds were separated and purified from the ethanolic extract of the twigs of C. inophyllum by means of chromatographic technology.Their structures were identified as 1,2,3-trihydroxy-5-methoxyxanthone （ 1 ）, 3,5-dihydroxy-1 -methoxyxan- thone （ 2 ）, 1,7-dihydroxy-3 -methoxyxanthone （ 3 ）, 3 -hydroxy-4-methoxyxanthone （ 4 ） and 12-methoxy ino- phyllum P（5 ） on the basis of spectral data. All the compounds were isolated from C. inophyllum for the first time. Compound 1 exhibited cytotoxicity against human hepatoma （SMMC-7721） cell line with IC50 of 16.5 μg·mL-1. Compound 5 exhibited cytotoxicity against human hepatoma cell line, human gastric cancer cell line（ SGC-7901 ） and myelogenous leukemia cell line（ K562 ） with IC50 of 25.5,30. 7 and 44.2 μg·mL - 1, respectively.